1. Determining the Influence of Breadfruit Mucilage on the Disintegration and Dissolution of Losartan Fast-Dissolving Tablets
Nina Varghese, M. Komala
Nina Varghese, M. Komala
Abstract
This study investigated breadfruit starch as a potential excipient for immediate-release losartan tablets. The solubility, pH, organoleptic characteristics, hydration, swelling capacity, and pasting temperature of breadfruit starch were determined. It was found that breadfruit starch exhibited partial solubility in warm water, a pH of 5.8, and good hydration and swelling capacities. Furthermore, a compatibility test using differential scanning calorimetry confirmed the compatibility of losartan and breadfruit starch. It was determined that the formulated losartan tablets were satisfactory in terms of flow properties as well as consistent drug content both before and after compression. Dissolution studies in-vitro showed improved drug release profiles than those of losartan tablets marketed on the market. According to stability studies, the physical appearance and color of the drug did not change over 3 months, but there was a slight decrease in the amount of the drug and the rate of drug release during that period. Overall, breadfruit starch showed promise as an excipient for losartan tablets, offering potential benefits in terms of enhanced drug release characteristics. Further investigations are necessary to optimize the formulation and evaluate its clinical efficacy and safety
2. Iraqi Hyacinthus orientalis L. Flowers as the Source of Bioactive Compounds Especially Stigmasterol: Identification, Isolation and Characterization
Noor M. Shareef, Thukaa Z. Abdul-Jalil
Noor M. Shareef, Thukaa Z. Abdul-Jalil
Abstract
This research concentrated on the isolation and identification of stigmasterol from cultivated Iraqi Hyacinthus orientalis flowers part, as there are few studies that deal with these plant-specific flowers as e-research shows. Extraction were done for the flowers part of plant, by the soxhlet apparatus using 85% ethanol, followed by fractionation with petroleum ether to obtain the target of this study. Phytochemical screening was done by gas chromatography mass spectrometry (GC-MS) for petroleum ether fraction qualitative and quantitative estimation and isolation of stigmasterol by reverse phase high-performance liquid chromatography (RP-HPLC), identification of isolated stigmasterol by Fourier transforms infrared (FTIR) spectroscopy, ultraviolet spectroscopy and liquid chromatography/Mass spectroscopy (LC/MS). Announcing that the study considered the first to isolate stigmasterol from flowers part of Iraqi Hyacinthus orientalis.
3. Association of Extracelluar Matrix Protien 1 with Semen Parameters and Testosterone Concentration in Male Infertility
Mohammed A. Assi, Sajjad S. Hameed
Mohammed A. Assi, Sajjad S. Hameed
Abstract
Background: Extracellular matrix protein 1 (ECM1) is a glycoprotein that interacts with extracellular proteins into semen predominantly by epididymis, supports considering the role of the epididymis in sperm maturation. Testosterone is a steroid hormone from the androgen group is primarily secreted in the testes.
Objectives: The aim of this study is to assess the concentration of ECM1 and serum by (ELISA) kit with semen parameters in fertile and infertile men in Najaf City, Iraq.
Material and Methods: A total of 90 participants (45 infertile and 45 fertile men) were mean age (40.02) control fertility male, while the mean age as infertile (40.22) years included in the current study. The patients were sub-grouped into: 45 infertile with semen abnormal oligozoospermia, azoospermia, asthenozoospermia and teratozoospermia patients, it used for measuring the concentration and parameters ECM1and serum testosterone by Elisa kit.
Results: Statistical analysis showed highly significant differences between the two groups show (p-value <0.05). The level of ECM in the infertile group was lower in concentration than the control group with statistically significant differences (p-value<0.0001*). The difference between the totals was highly significant by a criterion (p-value<0.0001*) 45 in all group that studied a positive person correlation highly significant between serum testosterone (IU/mL) and seminal ECM1, (pg/mL) in all age groups of 45 male infertility at a (p-value of <0.001*).
Conclusion: The decrease in serum testosterone levels with the decrease in the level of seminal plasma ECM1 in infertile men provide evidence that levels can be used as reliable markers in the diagnostic criteria of male infertility. This study’s results suggest that concentration ECM1.
Objectives: The aim of this study is to assess the concentration of ECM1 and serum by (ELISA) kit with semen parameters in fertile and infertile men in Najaf City, Iraq.
Material and Methods: A total of 90 participants (45 infertile and 45 fertile men) were mean age (40.02) control fertility male, while the mean age as infertile (40.22) years included in the current study. The patients were sub-grouped into: 45 infertile with semen abnormal oligozoospermia, azoospermia, asthenozoospermia and teratozoospermia patients, it used for measuring the concentration and parameters ECM1and serum testosterone by Elisa kit.
Results: Statistical analysis showed highly significant differences between the two groups show (p-value <0.05). The level of ECM in the infertile group was lower in concentration than the control group with statistically significant differences (p-value<0.0001*). The difference between the totals was highly significant by a criterion (p-value<0.0001*) 45 in all group that studied a positive person correlation highly significant between serum testosterone (IU/mL) and seminal ECM1, (pg/mL) in all age groups of 45 male infertility at a (p-value of <0.001*).
Conclusion: The decrease in serum testosterone levels with the decrease in the level of seminal plasma ECM1 in infertile men provide evidence that levels can be used as reliable markers in the diagnostic criteria of male infertility. This study’s results suggest that concentration ECM1.
4. Design and Development of Novel Mini Tablet Cap Technology for the Treatment of Cardiovascular Diseases
Anil K. Adimulapu, Lalchand D. Devhare, Anasuya Patil, Nilesh O. Chachda, G. Dharmamoorthy
Anil K. Adimulapu, Lalchand D. Devhare, Anasuya Patil, Nilesh O. Chachda, G. Dharmamoorthy
Abstract
Objectives: The purpose of the investigation was to extend and evaluate the novel mini tablet cap for treating cardiovascular disease at a desired combinational therapeutic activity and to improve patient compliance. A cheap four-in-one pill can guard against heart attacks and stroke.
Methods and Materials: The drug product was manufactured by Mini Tablet Cap technology. The technology was designed to initially use hydrochlorothiazide, simvastatin immediate release, metoprolol succinate, and asprin sustained release to reach the therapeutic levels at prolonged therapy. The two mini-bilayer tablets were prepared by wet granulation method and compression coated with a hydrophobic and hydrophilic polymer like ethyl cellulose and super disintegrating agents to release simvastatin and hydrochlorothiazide immediately.
Results: Fourier transformer infrared spectroscopy (FTIR) studied the interaction studies of four chosen drugs. The mini tablet cap technology was designed as two mini bi-layer tablets in a capsule. The quantitative detection of four individual drugs was determined by using the RP-HPLC method. It was found that RP-HPLC is sensitive, reproducible, and valid for determining the mini tablet cap. The in-vitro drug release studies found that simvastatin and hydrochlorothiazide release 90% immediately within 20 minutes. Metoprolol and aspirin controlled the release for up to 24 hours, and drug release kinetics found that the drug release behavior of the optimized formulation followed first-order kinetics.
Conclusion: The mini tablet cap is one of the best dosage forms to treat cardiovascular diseases. Because it was reported, the combination of these four drugs reduces mortality by 83% in high-risk patients with heart diseases, hypertension, diabetes, and obesity. The novel mini tablet cap approach data revealed a promising formula for improved relief of patient complaints during treatment or prevention of cardiovascular diseases.
Methods and Materials: The drug product was manufactured by Mini Tablet Cap technology. The technology was designed to initially use hydrochlorothiazide, simvastatin immediate release, metoprolol succinate, and asprin sustained release to reach the therapeutic levels at prolonged therapy. The two mini-bilayer tablets were prepared by wet granulation method and compression coated with a hydrophobic and hydrophilic polymer like ethyl cellulose and super disintegrating agents to release simvastatin and hydrochlorothiazide immediately.
Results: Fourier transformer infrared spectroscopy (FTIR) studied the interaction studies of four chosen drugs. The mini tablet cap technology was designed as two mini bi-layer tablets in a capsule. The quantitative detection of four individual drugs was determined by using the RP-HPLC method. It was found that RP-HPLC is sensitive, reproducible, and valid for determining the mini tablet cap. The in-vitro drug release studies found that simvastatin and hydrochlorothiazide release 90% immediately within 20 minutes. Metoprolol and aspirin controlled the release for up to 24 hours, and drug release kinetics found that the drug release behavior of the optimized formulation followed first-order kinetics.
Conclusion: The mini tablet cap is one of the best dosage forms to treat cardiovascular diseases. Because it was reported, the combination of these four drugs reduces mortality by 83% in high-risk patients with heart diseases, hypertension, diabetes, and obesity. The novel mini tablet cap approach data revealed a promising formula for improved relief of patient complaints during treatment or prevention of cardiovascular diseases.
5. Evaluation of A Newly Formulated Anti-Inflammatory Ointment From Ficus religiosa Root Bark
Jyothisree G, S. Umadevi
Jyothisree G, S. Umadevi
Abstract
The basis of the medical system is medicinal herbs. Herbal combinations for therapeutic alignment often include botanical components. This work aims to make an anti-inflammatory ointment from the Ficus religiosa root bark and test the medicine using a novel HPTLC technique. The flavonoid component from the hydroalcoholic extract was separated by column chromatography. The mobile phase used was a mixture of toluene, ethyl acetate, and methanol in the ratio 04:04:02. By using the fusion method to create a straightforward ointment from this separation, it was discovered that the formulation’s physicochemical properties were all within acceptable bounds. The mobile phase for the HPTLC study included toluene, ethyl acetate, formic acid, and methanol (3:3:0.8:0.2), and the wavelength was 280 nm. Using albino mice and the Carrageenan-induced paw edema method, the anti-inflammatory effect was assessed. Rf value is discovered to be 0.86, 0.88, and 0.89 for simple ointment, fractionate, and standard quercetin, respectively. According to ICH criteria, the HPTLC method was validated, and all parameters were within acceptable ranges. The created ointment can be used in a straightforward manner to alleviate inflammation. In comparison to NSAIDS, the topical formulation showed good anti-inflammatory action in carrageenan-induced paw edema.
6. Solubility Enhancement of Itraconazole by Centrifugal Melt Spinning Technique
Rodge PJ, Shirolkar SV
Rodge PJ, Shirolkar SV
Abstract
Itraconazole is an antifungal drug with poor water solubility and limited bioavailability, presenting difficulties in achieving effective therapeutic applications. This study aimed to employ centrifugal melt spinning, an innovative method, to improve the solubility of itraconazole. In this process, itraconazole was subjected to centrifugal forces while melting, forming amorphous solid dispersions. Microfibers loaded with 10% w/w itraconazole were prepared through centrifugal melt spinning, employing sucrose as a carrier. ITZ-sucrose microfibers with uniform morphology and an average diameter of 14.27 ± 2.90 μm were successfully fabricated, as evidenced by the scanning electron microscopy results. XRD and DSC measurements confirmed the amorphous nature of the spun microfibers. The solubility of Itraconazole sucrose microfibers was significantly enhanced by 17-fold compared to plain itraconazole. The dissolution experiments demonstrated that sucrose microfibers loaded with ITZ achieved a significant release of 94.96 ± 1.47% within 10 minutes, representing a substantial enhancement compared to plain drugs. The study indicated that utilizing the centrifugal melt spinning technique successfully generated amorphous solid dispersions of itraconazole, leading to a considerable improvement in the drug’s solubility.
7. Formulation and Evaluation of Moxifloxacin Dry Powder Inhaler Combined with Mucolytic Agent for Pulmonary Diseases
Ratnaparkhi M.P, Kamble O. V., Salvankar S. S., Shinde S. R., Kulkarni G. M., Shewale A. B., Kadam D. D., Shaikh A. J.
Ratnaparkhi M.P, Kamble O. V., Salvankar S. S., Shinde S. R., Kulkarni G. M., Shewale A. B., Kadam D. D., Shaikh A. J.
Abstract
The DPI is the device that administers the drug through the dry powder to the lungs. People with Multi-drug resistant tuberculosis or other lung diseases frequently use such devices to take their prescribed medicines. Numerous approaches have been used to formulate dry powder inhalation formulation and enhance the delivery performance of dry powder inhaler preparation. In the case of multi-drug resistance tuberculosis, a high dose of combination therapy was delivered, resulting in resistance to the anti-TB medications in the majority of patients. Moxifloxacin and levofloxacin are being used to minimize the need for a high-dose treatment regimen. This study aimed to achieve local lung administration of tumor-targeting Moxifloxacin, by administering microspheres that can be inhaled as a dry powder inhaler for targeting Phagocytes of alveoli via pulmonary passage. Spray drying had been used to formulate MXN-DPI formulations, afterward optimized with the 23-factorial design model. Two different amounts of lactose, leucine, and medication were used to make the eight batches. The developed formulation was studied for physicochemical properties like morphology and particle size. The particle dimensions of the MXN-DPI compositions have been confirmed to be in the range of 1.4 to 4.1 μm. The prepared formulations effectively showed drug release up to 93% in 5 hours, which was observed through in-vitro diffusion studies.
8. A Relationship of Dickkopf-1 with Glutathione in Iraqi Patients with Unstable Angina as a Model of Pharmaceutical Compounds
Mohanad S. B. Musleh, Khalid F. A. Alrawi, Hazim I. Ghazzay
Mohanad S. B. Musleh, Khalid F. A. Alrawi, Hazim I. Ghazzay
Abstract
Background: The importance of inflammation in coronary artery disease and the inflammatory biomarkers linked to adverse outcomes have recently been the subject of numerous investigations. In addition to examining the relationship between dickkopf-1 and high mobility group box-1 with other biochemical markers, this study seeks to ascertain the relationship between dickkopf-1 and high mobility group box-1 in patients whose angina pectoris is not stable.
Methods: The work includes 50 patients (20 female and 30 male) and 40, 20 female and 20 males as controls who attended Al Ramadi Teaching Hospital between November 2021 and April. The sample age ranged between 52.16 ± 8.423 years in comparison to 49.58 ± 8.098 for the controls.
Results: The serum DKK-1 levels (ng/mL) rose in unstable angina (UA) patients (135.527.13 for UA patients vs. 36.614.07 for the control group), so UA patients had higher DKK-1 release during platelet aggregation because DKK1 is involved in platelet-induced endothelial cell activation, so DKK1 causes inflammation. Additionally, the GSH was significantly lower in those having UA than in controls.
Conclusion: Serum DKK-1 levels was significantly higher for those with UA compared to the healthy and there is a significant drop in GSH levels in people with UA than in controls.
Methods: The work includes 50 patients (20 female and 30 male) and 40, 20 female and 20 males as controls who attended Al Ramadi Teaching Hospital between November 2021 and April. The sample age ranged between 52.16 ± 8.423 years in comparison to 49.58 ± 8.098 for the controls.
Results: The serum DKK-1 levels (ng/mL) rose in unstable angina (UA) patients (135.527.13 for UA patients vs. 36.614.07 for the control group), so UA patients had higher DKK-1 release during platelet aggregation because DKK1 is involved in platelet-induced endothelial cell activation, so DKK1 causes inflammation. Additionally, the GSH was significantly lower in those having UA than in controls.
Conclusion: Serum DKK-1 levels was significantly higher for those with UA compared to the healthy and there is a significant drop in GSH levels in people with UA than in controls.
9. Formulation Development and Evaluation of Herbal Tablet of Diplocyclos palmatus (L.) Jeffry.
Sumeet Dwivedi, Devendra S. Lodhi, Deepak Kumawat, Pradeep Golani, Anup K. Chakraborty, Rekha Bisht
Sumeet Dwivedi, Devendra S. Lodhi, Deepak Kumawat, Pradeep Golani, Anup K. Chakraborty, Rekha Bisht
Abstract
Diplocyclos palmatus (L.) Jeffry. (Shivlingi), is a plant in the Cucurbitaceae family that has been utilized extensively in indigenous medicine due to its purported biological properties. The goal of the current study was to formulate herbal tablets for the treatment of inflammation that contained a hydro-alcoholic extract of D. palmatus (L.) Jeffry. The formulated herbal tablet underwent IP evaluation, and all the results were found satisfactory.
10. Fabrication, Optimization and Evaluation of Escin Enriched Emulgel System for Treatment of Varicose Veins
Chougule PN, Koumaravelou K, Chougule NB
Chougule PN, Koumaravelou K, Chougule NB
Abstract
Varicose veins, a widespread chronic venous ailment in lower limbs, impact many individuals, causing considerable physical, financial, and social burdens. While surgery is the most effective treatment, its cost hinders personalized care. In the quest for venous-specific therapies, herbal remedies, particularly horse chestnut extract containing escin, are being explored. Escin, a key component, offers anti-inflammatory, anti-edematous, and antioxidant effects. The saponin escin has two forms, α and β, with distinct actions via oral and topical routes. A gel system with permeability enhancers was developed to enhance topical escin’s effectiveness following meticulous pre-formulation and optimization studies. The physiochemical characteristics of emulsion and emulgel system, assay of escin, in-vitro permeation, emulgel studies such as pH, viscosity, spreadability and stability studies are all included in the evaluation part. The 2% escin in the light beige-colored emulgel system was significantly improved permeability when soy lecithin was added. The investigation on permeation enhancement shows that there is 1.5 times more activity than there would be with standard preparation. Escin’s concentration was measured using a UV spectrophotometer and was found to be between 98 and 102%. Studies such as pH, viscosity and spreadability are within the predefined limits. Overall, the developed escin-based emulgel system shows promising results for the management of varicose veins.
11. Effect of Some Psychotic Drug Quetiapine on Reproductive System Activity in Male Rats
Mohammed A. Assi, Makarim H. Mohammed
Mohammed A. Assi, Makarim H. Mohammed
Abstract
Aim of study: To investigate the effects of antipsychotic medications utilized to treat schizophrenic patients and its effects on the reproductive system.
Introduction: Antipsychotics, anticonvulsants, and other all psychotropic drugs have negative effects on the quality of sperm and sexual activity. These negative side effects differ amongst males and its less severe for some drugs, enabling some degree of control over their effects. Sperm can suffer oxidative damage from spending too much time in the male reproductive system. One of the antipsychotics most frequently administered to treat schizophrenia in adults is quetiapine. In this work, the effects of repeated rats’ healthy production of sperm in response to therapeutic doses of quetiapine was studied. Rats were also used to assess quetiapine’s effects on hormonal balance and oxidative state.
Methodology: The experiment employed male wistar rats weighing 300 to 350 g at 10 to 12 weeks of age. The experiment employed male wistar rats weighing 300 to 350 g at 10 to 12 weeks of age. Rats received oral dosages of quetiapine for 30 days. At this time’s conclusion, the body’s weights and the organs were analyzed, additionally to sperm concentration, motility, shape, and degree of sperm damage. The levels of testosterone, LH, and other male hormones related to reproduction were measured in the serum. Malondialdehyde and glutathione levels were measured to assess the oxidative state of testicular tissues.
Results: The results of this investigation demonstrated that in rats receiving quetiapine, aberrant sperm morphology increased while relative epididymis weights and sperm concentration dropped. Rats receiving quetiapine experienced a drop in serum LH and testosterone levels. Rats receiving quetiapine also had lower amounts of malondialdehyde, which was assessed.
Conclusion: Quetiapine therapy this negative effect may be attributed to lower sperm quality, changed hormone levels, and enhanced oxidative stress.
Introduction: Antipsychotics, anticonvulsants, and other all psychotropic drugs have negative effects on the quality of sperm and sexual activity. These negative side effects differ amongst males and its less severe for some drugs, enabling some degree of control over their effects. Sperm can suffer oxidative damage from spending too much time in the male reproductive system. One of the antipsychotics most frequently administered to treat schizophrenia in adults is quetiapine. In this work, the effects of repeated rats’ healthy production of sperm in response to therapeutic doses of quetiapine was studied. Rats were also used to assess quetiapine’s effects on hormonal balance and oxidative state.
Methodology: The experiment employed male wistar rats weighing 300 to 350 g at 10 to 12 weeks of age. The experiment employed male wistar rats weighing 300 to 350 g at 10 to 12 weeks of age. Rats received oral dosages of quetiapine for 30 days. At this time’s conclusion, the body’s weights and the organs were analyzed, additionally to sperm concentration, motility, shape, and degree of sperm damage. The levels of testosterone, LH, and other male hormones related to reproduction were measured in the serum. Malondialdehyde and glutathione levels were measured to assess the oxidative state of testicular tissues.
Results: The results of this investigation demonstrated that in rats receiving quetiapine, aberrant sperm morphology increased while relative epididymis weights and sperm concentration dropped. Rats receiving quetiapine experienced a drop in serum LH and testosterone levels. Rats receiving quetiapine also had lower amounts of malondialdehyde, which was assessed.
Conclusion: Quetiapine therapy this negative effect may be attributed to lower sperm quality, changed hormone levels, and enhanced oxidative stress.
12. Fexofenadine Hydrochloride Dispersible Tablets: A Taste Masking Strategy using Ion Exchange Resin
Kajal Barge, Shivali Tank, Bhagyashri Parab, Mangal Nagarsenkar, Supriya Shidhaye
Kajal Barge, Shivali Tank, Bhagyashri Parab, Mangal Nagarsenkar, Supriya Shidhaye
Abstract
The pediatric population is more sensitive to allergies. Fexofenadine hydrochloride (FXD-HCL), a non-sedative antihistaminic drug, was chosen to create taste-masked patient-compliant pediatric dispersible tablets. Due to its bitter taste, fexofenadine hydrochloride is unsuitable for the formulation of dispersible tablets; therefore, Kyron T-134®, cation exchange resin was used to form a taste-masked complex with the drug to overcome its bitterness. The FXD HCL-resin complex was prepared using a kneading method and the complexation was confirmed by differential scanning calorimetry and FTIR studies. The FXD HCL-resin complex was evaluated for flow properties, degree of bitterness, assay and release study. Dispersible tablets were formulated by using a co-processed excipient, Granfiller-D211® containing croscarmellose sodium and crosspovidone, microcrystalline cellulose and mannitol. 22 factorial designs with two replicates optimized the dispersible tablets. The tablets, prepared using the direct compression technique on a single-stroke tablet compression machine, were elegant in appearance. Various pre and post-compression tests were conducted on all formulations. The tablets of hardness 3.5 kg/cm2 showed friability, disintegration time, assay within the compendial limit and showed immediate release of a drug (NLT 60% in 10 min and NLT 80% in 30 minutes) in 0.001 N HCl (pH 3). The DSC thermogram indicated partial amorphization of the FXD HCL. Dispersible tablets of fexofenadine hydrochloride and Granfiller-D®211 at 1:4 proportion was stable for one month at ambient and accelerated storage conditions.
13. Comparative Study of Isomalt and Co-processed Isomalt
Sandhan S B, Wagh M P
Sandhan S B, Wagh M P
Abstract
Objective: The study aims to compare the tableting qualities of isomalt and co-processed isomalt.
Methodology: Co-processed isomalt prepared by melt granulation method evaluated for flow property, dilution potential, Kawakita plot, consolidation index, tabletability, Heckel plot and elastic recovery and compared with isomalt.
Result and Discussion: The co-processed isomalt demonstrated superior packing ability compared to isomalt and got rearranged in the early compression stage, as per modified Kawakita equation. Co-processed isomalt had 40% dilution potential for paracetamol as compared with 20% for isomalt. Co-processed isomalt showed 40% dilution potential for ascorbic acid, and nimesulide, whereas mefenamic acid and aspirin showed 30% dilution potential. Co-processed isomalt overcomes the lamination and sticking problem of isomalt which has better tabletability.
Methodology: Co-processed isomalt prepared by melt granulation method evaluated for flow property, dilution potential, Kawakita plot, consolidation index, tabletability, Heckel plot and elastic recovery and compared with isomalt.
Result and Discussion: The co-processed isomalt demonstrated superior packing ability compared to isomalt and got rearranged in the early compression stage, as per modified Kawakita equation. Co-processed isomalt had 40% dilution potential for paracetamol as compared with 20% for isomalt. Co-processed isomalt showed 40% dilution potential for ascorbic acid, and nimesulide, whereas mefenamic acid and aspirin showed 30% dilution potential. Co-processed isomalt overcomes the lamination and sticking problem of isomalt which has better tabletability.
14. Organic Extraction, Purification and Evaluation of Long Chain Fatty Alcohol from Saccharum officinarum of Sugar Refinery Waste for Human Wellness
Singh A. K, Kharb R, Kandpal J.B
Singh A. K, Kharb R, Kandpal J.B
Abstract
The current study has explored an extraction and purification method for 1-octacosanol from sugarcane waste, commonly known as press mud, through the application of SCFE by the unique concept of solid-solid and liquid-liquid extraction which increases content and decreases impurity which is an extra advantage at purification stage by help of green solvent instead any carcinogenic solvent, which reduce process time, increase content and environment friendly. The isolated compounds were characterized by gas chromatography-flame ionization detection, which shows 50% content of octacosanol in the final product. Novel refinement technique through hot ethanolic reflux method has substantially increased the octacosanol assay to ≥ 50% with more than 67% purity from the crude wax assay of 26% obtained by the current method of extraction. The identity of said compound was further authenticated by X-ray diffraction (XRD), Diffraction scanning calorimetry (DSC) and FTIR studies. The purity of the octacosanol obtained was ≤70% and the conversion recovery of octacosanol was 80.04% by the reflux method, thereby representing the simplicity of the above process for industrial feasibility. The current process represents a value addition liquid-liquid supercritical extraction with a time-saving, cost-effective, reproducible, newer, green, safe, and sustainable technology valorizing sugarcane waste for a high-end nutraceutical.
15. In-silico Assessment of Potent Immunomodulators from Pimpinella anisum and its Antioxidant Potential
Snehal Kashid, Ashish Suttee, Prasad Kadam, Ramesh Kasarla
Snehal Kashid, Ashish Suttee, Prasad Kadam, Ramesh Kasarla
Abstract
New targets, effective substances, and safety in pharmacological models are highlighted by recent drug development. The study’s primary goal is to use an in-silico technique to determine the immunomodulatory potential of phytoconstituents from Pimpinella anisum. Several computer aided tool were utilized for in-silico. autodock vina is major free tool utilized to examine a drug discovery strategy based on the atomic-level screening of small compounds and proteins and protein-ligand interactions. Basic docking phases include ligand position, orientation, and binding affinities. The current methodology includes ligand choice, protein prep, target, ligand optimisation, target active binding site analysis, and binding affinity. SwissADME was used to assess the pharmacokinetic parameters, and Lipinski’s “rules” were used to assess drug similarity. In the current research paper six ligands such as P-anisaldehyde, trans-anethole, cis-anethole, estragole, and linalool were dock against two proteins 1M48 and 1P9M. Molecular docking studies suggest strong binding affinity between -6.9 to -4.2 in case on 1M48 and -6.2 to -4.7 in case of 1P9M. Further antioxidant potential of P. anisum using several solvents was determined. In-vitro antioxidant study and in-silico screening suggested that P. anisum ethanolic extract can be contributed in immunomodulation.
16. Isolation and Characterization of Phytoconstituents from the Plant Excoecaria agallocha Linn
Maruti K. Shelar, Manohar J. Patil, Santosh S. Patil
Maruti K. Shelar, Manohar J. Patil, Santosh S. Patil
Abstract
Background: Marine resources are currently widely studied because academic and industrial researchers are striving to extract lead molecules from the interior of oceans. Marine resources are increasingly the subject of significant research. Excoecaria agallocha Linn., one of the plants with several pharmacological effects such as anti-inflammatory, analgesic, antiulcer, anticancer, etc., is one of the phytoconstituents in mangroves that have been widely used in folk medicine to treat disorders.
Objective: The objective of present study to perform a comprehensive phytochemical investigation of milky mangrove. The plant E. agallocha were collected, extracted, isolated, and analyzed in an attempt to better comprehend the various phytochemical aspects of the plant.
Material and method: The isolated product was analyzed by different spectroscopic method.
Results: The isolated product is characterized as steroidal moiety containing two double bond at 6 and 22-position and alcoholic group at 3-position of cyclopentanoperhydrophenanthrene in to the isolation of (1,2,3,4,5,10,11,12,14,15,17-dodecahydro-3-hydroxy-4,4,10,13,14-pentamethyl17-(( E )- 5,6-dimethylhept-3-en- 2- yl-)9-H-cyclopenta[a]phenanthren-6,16-dione.
Conclusion: The compound’s actual structure is made known using all of the UV, IR, NMR, and mass spectrometry evidence.
Objective: The objective of present study to perform a comprehensive phytochemical investigation of milky mangrove. The plant E. agallocha were collected, extracted, isolated, and analyzed in an attempt to better comprehend the various phytochemical aspects of the plant.
Material and method: The isolated product was analyzed by different spectroscopic method.
Results: The isolated product is characterized as steroidal moiety containing two double bond at 6 and 22-position and alcoholic group at 3-position of cyclopentanoperhydrophenanthrene in to the isolation of (1,2,3,4,5,10,11,12,14,15,17-dodecahydro-3-hydroxy-4,4,10,13,14-pentamethyl17-(( E )- 5,6-dimethylhept-3-en- 2- yl-)9-H-cyclopenta[a]phenanthren-6,16-dione.
Conclusion: The compound’s actual structure is made known using all of the UV, IR, NMR, and mass spectrometry evidence.
17. Development and Validation of a Stability-Indicating RP-HPLC Method for Estimation of Glibenclamidei Bulk and Pharmaceutical Formulation
Jirvankar Pranita, Rishabh Agrawal, Nikhita Chambhare, Sahare A.Y.
Jirvankar Pranita, Rishabh Agrawal, Nikhita Chambhare, Sahare A.Y.
Abstract
Glibenclamide is the choice of medicine for diabetes type II. There are numerous methods for estimation; however the methods are either not suitable or expensive. A simple, cheap, precise, and accurate stability-indicating HPLC method was developed and further validated.
The wavelength of 229 nm with a constant flow rate of (Methanol: Mixed Phosphate Buffer, 70:30% v/v (pH 7.3)) 1 mL/min was used during the experimentation. The run time was (run time). The internal standard used was (Internal standard). The sample eluted and showed a sharp peak at 2.1 minutes. It was discovered that calibration curve experiments had a5–50 ppm linearity. The precision of the developed method was lower than 2% RSD. Recovery studies showed that the method’s accuracy and precision ranged from 99.25 to 101.81%. Stress testing was used to determine specificity. The developed method was capable of separating the drug peak from any probable degradation products. There was no evidence of recipient or impurity interference. The method can be used to anticipate how long glibenclamide will be stable. The method was feasible and appropriate for analyzing the presence of glibenclamide in a drug substance as well as a drug product.
The wavelength of 229 nm with a constant flow rate of (Methanol: Mixed Phosphate Buffer, 70:30% v/v (pH 7.3)) 1 mL/min was used during the experimentation. The run time was (run time). The internal standard used was (Internal standard). The sample eluted and showed a sharp peak at 2.1 minutes. It was discovered that calibration curve experiments had a5–50 ppm linearity. The precision of the developed method was lower than 2% RSD. Recovery studies showed that the method’s accuracy and precision ranged from 99.25 to 101.81%. Stress testing was used to determine specificity. The developed method was capable of separating the drug peak from any probable degradation products. There was no evidence of recipient or impurity interference. The method can be used to anticipate how long glibenclamide will be stable. The method was feasible and appropriate for analyzing the presence of glibenclamide in a drug substance as well as a drug product.
18. Phytochemical Screening, GC-MS Analysis and Total Phenolic Content Determination of Bioactive Compound of Propolis
Meenu, Tarun Virmani, Lubhan Singh, Rahul Kaushik
Meenu, Tarun Virmani, Lubhan Singh, Rahul Kaushik
Abstract
India is a hub for a large variety of natural products that have proven their therapeutic efficacy in various ailments and disorders. Despite it, a lot of natural products are yet to be explored, and Indian propolis is one of them. Indian propolis is a waxy natural product obtained from beehives. In this research, phytochemical constituents present in Indian propolis were qualitatively analyzed using phytochemical screening, gas chromatography-mass spectroscopy (GC-MS), and quantitatively using total phenolic content. Phytochemical screening results revealed the presence of total phenolic content, saponins, glycosides, alkaloids, terpenoids, proteins, steroids, flavonoids, oils & resins supported by GC-MS results. The GC-MS analysis revealed the presence of 17 different constituents having higher peak areas. Amongst these 17 bioactive compounds, oxirane, phenyl ethyl alcohol, caffeine, chrysene, riboflavin and 2-aminophenol were found to have higher peak areas of 5.78, 4.58, 4.46, 3.11, 2.65 and 2.56%, respectively. The results of total phenolic contents revealed the presence of 23 different constituents in different concentrations amongst ellagic acid, kaempferol, epicatechin, galangin, and quercetin were present in rich amounts 538.73, 402.34, 234.85, 121.95 and 95.3 μg/kg, respectively. These constituents are well known for their therapeutic efficacy, which is an indication for the exploration of the therapeutic efficacy of Indian propolis in the future.
19. A Study of Hepcidin Levels and Other Biochemical Parameters in Women with Osteoarthritis: As a Pharmaceutical Control
Shuaib Y. Ahmed, Noorhan K. Shafeeq
Shuaib Y. Ahmed, Noorhan K. Shafeeq
Abstract
Background: Hepcidin, one of the peptide hormones generated from the liver, can be defined as an important regulator regarding systemic iron homeostasis, while its lopsided production plays a role in the pathogenesis of a variety of iron diseases. Osteoarthritis (OA) frequently coexists with a number of diseases, including hemochromatosis, ß-thalassemia, cell disease, sickle cell disease, and hemosiderosis caused by iron overload. Evidence suggests that iron deficiency and iron overload negatively impact the bone, which acts immediately on the bone’s cells. The present work aims to determine whether a direct correlation exists between female patient’s OA and levels of hepcidin, DHVD3, and other indicators.
Methods: A total of 60 participants were split into two groups for this work: 30 healthy controls and 30 female OA patients. This work was carried out from Nov. 2021 to the end of June. 2021. The ages ranged from (40 to 55). In Al-Mahmudiya Hospital and in Al-Yarmok Teaching Hospital, an endocrinologist assessed each one of the patients. We measured Hb, BMI, ferritin, hepcidin, DHVD3, iron, Ca, and PO4.
Results: Hepcidin levels significantly increased, whereas ferritin, BMI, iron, vitamin D, calcium, and PO4 levels significantly decreased compared with the control group. However, alterations in lipid profile and glycemic profile were not statistically significant.
Conclusion: By connecting low levels of iron, ferritin, calcium, vitamin D3, and PO4 with high levels of hepcidin in women with OA, it may be concluded that vitamin D3 insufficiency is associated with hepcidin malfunction as a factor affecting women with OA.
Methods: A total of 60 participants were split into two groups for this work: 30 healthy controls and 30 female OA patients. This work was carried out from Nov. 2021 to the end of June. 2021. The ages ranged from (40 to 55). In Al-Mahmudiya Hospital and in Al-Yarmok Teaching Hospital, an endocrinologist assessed each one of the patients. We measured Hb, BMI, ferritin, hepcidin, DHVD3, iron, Ca, and PO4.
Results: Hepcidin levels significantly increased, whereas ferritin, BMI, iron, vitamin D, calcium, and PO4 levels significantly decreased compared with the control group. However, alterations in lipid profile and glycemic profile were not statistically significant.
Conclusion: By connecting low levels of iron, ferritin, calcium, vitamin D3, and PO4 with high levels of hepcidin in women with OA, it may be concluded that vitamin D3 insufficiency is associated with hepcidin malfunction as a factor affecting women with OA.
20. Computational Exploration of Anti-Alzheimer Potential of Flavonoids against Inducible Nitric Oxide Synthetase: An In-silico Molecular Docking and ADMET Analysis Approach
Mahesh Nemade, Khushabu Patil, Anjali Bedse, Piyush Chandra, Rakesh Ranjan, Harshal Tare, Samir Patil
Mahesh Nemade, Khushabu Patil, Anjali Bedse, Piyush Chandra, Rakesh Ranjan, Harshal Tare, Samir Patil
Abstract
Alzheimer’s disease (AD) is a formidable challenge in neurodegenerative disorders, marked by relentless cognitive decline, memory impairment, and a pervasive neuroinflammatory milieu. Recent scientific inquiries have unveiled a compelling link between the rampant overexpression of inducible nitric oxide synthetase (iNOS) and the intricate pathogenesis of AD. Within this context, flavonoids, a diverse class of polyphenolic compounds widely distributed in fruits & vegetables, have garnered substantial interest due to their recognized antioxidant and anti-inflammatory attributes. This research endeavor harnessed the power of cutting edge in-silico molecular docking techniques to embark on a compelling exploration. Specifically, we aimed to unravel the therapeutic potential of various flavonoids as putative inhibitors of iNOS, with the ultimate objective of combatting the insidious progression of AD. Our investigative odyssey unveiled promising outcomes. Molecular docking simulations illuminated the binding interactions between diverse flavonoids and the iNOS enzyme, offering insights into their potential inhibitory prowess. Among these flavonoids, a notable contender emerged, denoted as CHEMBL490697, which exhibited a remarkable negative binding affinity of -8.3 kcal/mol, demonstrating its strong attraction to the targeted protein. Furthermore, CHEMBL490697, admirably traversed the rigorous terrain of drug likeness parameters, underscoring its potential as a viable therapeutic candidate. In summation, this comprehensive investigation has illuminated the potential of CHEMBL490697 as a promising therapeutic agent with drug like properties, exemplified by its robust, stable, and tight binding to the iNOS enzyme. These findings present a compelling avenue for further research and development in the pursuit of best managements for AD.
21. In-silico Exploration for Novel CDK8 Inhibitors: A Virtual Study by Pharmacophore Screening
Khushabu Patil, Mahesh Nemade, Anjali Bedse, Piyush Chandra, Rakesh Ranjan,Harshal Tare, Samir Patil
Khushabu Patil, Mahesh Nemade, Anjali Bedse, Piyush Chandra, Rakesh Ranjan,Harshal Tare, Samir Patil
Abstract
The primary goal of this research is to identify potent and safe CDK8 inhibitors from the ChEMBL (kinases) database. The study employs a multi-faceted computational approach to achieve its objectives. Structure-based pharmacophore modeling is used for the initial screening of potential CDK8 inhibitors. Subsequent molecular docking studies are conducted to assess the binding affinities of the screened molecules. Finally, toxicity profiling is carried out to ensure the safety of the potential inhibitors. A total of 150 molecules were identified that passed the initial pharmacophore screening. Among these, molecule CHEMBL404766 was found to have the highest binding affinity in molecular docking studies. Furthermore CHEMBL404766 was found to be the safest candidate, exhibiting a negligible toxic dose in toxicity profiling. The study suggests the potential use of computational approaches for the identification and design of potent and safe CDK8 inhibitors. These findings have significant implications for the development of targeted therapies in diseases where CDK8 plays a crucial role.
22. Exploring Film Forming Ability of Newly Synthesized Rosin Esters
Pramod Burakale, Suresh Sudke, Manish Bhise, Harshal Tare, Ramanlal Kachave
Pramod Burakale, Suresh Sudke, Manish Bhise, Harshal Tare, Ramanlal Kachave
Abstract
The present investigation was planned to confirm the film-forming potential of synthesized rosin esters. The free films of rosin esters were prepared by solvent evaporation and characterized for the physicochemical and mechanical attributes. Suitable concentrations of rosin esters were used for coating tablets, and coated tablets were evaluated for official and unofficial quality control tests. The free films had low tensile strength, higher percent elongation value, and smooth surfaces. Therefore, the plasticizer was used to provide tensile strength to the films. The tablets were coated rapidly without agglomeration, confirming the suitability of rosin esters as a coating agent. The drug release from tablets was delayed up to 6 to 8 hours because of10% w/w coating of rosin ester, and regioselectivity was achieved by coating with hydroxypropyl methylcellulose with sodium bicarbonate. The pH-dependent solubility of rosin esters produces chrono-triggered drug release from coated tablets. The present investigation confirms the suitability of newly synthesized rosin esters in in designing a region selective chrono- triggered drug delivery system.
23. Development and Evaluation of Herbal Shampoo as an Antifungal Formulation
Milind Dyagatwar, Bhushan Pimple, Mohini Kuchekar, Suvarna Vadje, Siddhant Gaikwad,Vanita Bhurkunde, Harshal Tare, Deshraj Chumbhale
Milind Dyagatwar, Bhushan Pimple, Mohini Kuchekar, Suvarna Vadje, Siddhant Gaikwad,Vanita Bhurkunde, Harshal Tare, Deshraj Chumbhale
Abstract
The herbal shampoo is a normal hair care solution used to clear out grease, debris and dandruff, stimulating hair growth and strength. It also gives the hair a glossy appearance and smoothness, reducing tenderness. This research aims to develop an herbal shampoo and assess its physical and chemical properties with an eye toward ensuring its safety and effectiveness. Moreover, it also aims to replace hazardous synthetic chemicals and with safe natural ones. Herbal shampoo was formulated using plants viz Tea, ashwagandha, sandalwood and Nagarmotha which compared with the marketed formulation. Various physicochemical tests were carried out, like visual inspection, pH, detergency, dirt dispersion, determination of foam, viscosity and stability evaluation, and antimicrobial activity. It was observed that prepared herbal shampoo had good cleansing properties and was very efficient in controlling the growth of Candida and Malassezia fungi.
24. Preparation and Evaluation of Primidone Solid Lipid Nanoparticle for Alleviating Seizure Activity in Wistar Rats
Pooja Agarwal, B. Vasudha
Pooja Agarwal, B. Vasudha
Abstract
In order to increase primidone’s anticonvulsant action, the study set out to manufacture it in solid lipid nanoparticle form (PRI-SLN).
Method: Microemulsification and ultrasonication procedures were used to create 17 PRI-SLN formulations.
Results: The PRI-SLN displayed a high entrapment efficiency (46.37 ± 2.42% to 81.82 ± 1.21%), as well as small particle size (149.9 ± 6.72 to 188.8 ± 5.25 nm). According to the in-vitro release study, PRI from SLNs releases more slowly than PRI by itself. The thermal analysis showed the drug’s compatibility with other substances and its presence in the more soluble amorphous state. Following a lethal and chronic dosage of picrotoxin, the PRI-SLN exhibited a higher anticonvulsant efficacy, according to in-vivo research on rats (p< 0.05).
Conclusion: SLN with stronger anticonvulsant action can be made from PRI.
Method: Microemulsification and ultrasonication procedures were used to create 17 PRI-SLN formulations.
Results: The PRI-SLN displayed a high entrapment efficiency (46.37 ± 2.42% to 81.82 ± 1.21%), as well as small particle size (149.9 ± 6.72 to 188.8 ± 5.25 nm). According to the in-vitro release study, PRI from SLNs releases more slowly than PRI by itself. The thermal analysis showed the drug’s compatibility with other substances and its presence in the more soluble amorphous state. Following a lethal and chronic dosage of picrotoxin, the PRI-SLN exhibited a higher anticonvulsant efficacy, according to in-vivo research on rats (p< 0.05).
Conclusion: SLN with stronger anticonvulsant action can be made from PRI.
25. Synthesis and Characterization of Colloidally Stable Self-crosslinking Water-based Anticorrosive Polymer at Room Temperature
Khalida A. Omran
Khalida A. Omran
Abstract
The emulsion polymerization of butyl acrylate (BuA), styrene (St), and 3-isopropenyl-α,α-dimethylbenzyl isocyanate (IPMBI) is presented in this work. Obtain colloidally stable latexes for the poly (BuA/St/IPMBI) system during polymerization and storage for use in a water-based coating formulation. A series of semicontinuous polymerizations were also performed to investigate the effect of comonomer composition (w/w) in the feed (BuA/St) on conversion. The particle diameter (Dp), particle number (Np), hydrolysis of the IPMBI’s isocyanate groups, stability and storage properties. Films were created in which the effect of comonomer composition was also investigated, the glass transition temperature (Tg) was determined, the gel content was selected, and the mechanical properties and capacity as a barrier to water vapour and oxygen were assessed. Another series of reactions, on the other hand, was carried out in which the effect of the IPMBI content (1.5, 3.5, and 5.5%) was studied using a constant composition BuA/St=60/40. The studies conducted are the same as those mentioned for the effect of comonomer composition in feed. With increasing IPMBI percentage, slight differences in conversion, Dp, and Np were observed; the latices undergo hydrolysis during polymerization and storage. Colloidal stability, on the other hand, was preserved. The mechanical properties of the films improved as the percentage of IPMBI increased, while the boundary characteristics to moisture and oxygen improved when compared to the white film (0% of IPMBI). Finally, the formulation of a self-crosslinking water-based coating at room temperature using the previously obtained latex as a binder is reported; the coating demonstrated excellent adhesion, scratch hardness, and gloss regardless of the type of latex used.
26. Novel Synthesis, Physicochemical Characterization of 1,3,4-Oxadiazinoindole Derivatives for the Purpose of Antidepressant Activity
Mahadev Agarwal, Neelam Singla, S. K. Singh
Mahadev Agarwal, Neelam Singla, S. K. Singh
Abstract
The present study synthesized a series of 1,3,4-oxadiazinoindole moiety-containing compounds by combining MAOI’s hydrazide moiety and tricyclic moiety having antidepressant activity. The formation of amino acid chloride from amino acids started the synthesis. Further, they were converted into amino acid hydrazide, and then amino acid hydrazones were prepared by reaction of amino acid hydrazide with isatin. Finally, cyclization was acted on hydrazone-containing compounds in the presence of cold H2SO4. Synthesized compounds are characterized and confirmed via mass spectroscopy, 1H-nuclear magnetic resonance strategies, fourier transform infrared spectroscopy, thin layer chromatography, and melting point. The compounds were evaluated for antidepressant activity.
27. Evaluation of Lipid Profile and Sexual Hormones in Women with Polycystic Ovarian Syndrome at Al-Najaf Province
Abdul-Samad U. Hassan, Ameer N. Adnan
Abdul-Samad U. Hassan, Ameer N. Adnan
Abstract
Background: A multiple-factorial condition influencing females’ reproductive years is polycystic ovarian syndrome (PCOS). This study aims to investigate lipid profiles and sex hormones, and DHEA hormones related to patients suffering from PCOS. Method: In this investigation, the sex hormones, lipid profile and DHEA hormone of 45 females in their reproductive years who were suffering from PCOS were compared to those of 45 women who were healthy and of a similar age. Results: Our results showed that the mean ± standard deviation of triglyceride parameter is higher than others parameters in both women patients with polycystic syndrome (73.2 ± 147.3 mg/dl) and control (57.9 ± 123.7 mg/dl) groups with highly significant difference (p-value < 0.001). While, mean ± standard deviation of other parameters, including cholesterol, HDL, LDL and VLDL, was higher in women with polycystic syndrome than in the control groupe. Conclusion: The more active fertile age group, 21 to 30 years old are more susceptible to the incidence of PCOS. Our data shows a significant correlation between DHEA and cholesterol, HDL, VLDL in the patient group. There is a positive statistical correlation between DHEA and LDL and between DHEA and LH, prolactin, and testosterone. The correlation between DHEA and FSH showed a passive association (statistically significant).
28. Phenol Glucosides as Potential Inhibitors of SGLT1 for Enhanced Diabetes Mellitus Treatment in Patients with Declining Renal Function
Mahesh Nemade, Khushabu Patil, Anjali Bedse, Piyush Chandra, Rakesh Ranjan, Harshal Tare, Manish Bhise
Mahesh Nemade, Khushabu Patil, Anjali Bedse, Piyush Chandra, Rakesh Ranjan, Harshal Tare, Manish Bhise
Abstract
Diabetes mellitus poses a significant global health challenge, necessitating the continual search for innovative therapeutic strategies. While sodium-glucose cotransporter 2 (SGLT2) inhibitors have shown promise in diabetes management, their efficacy diminishes in patients with declining renal function.
This study aims to evaluate the potential of phenol glucosides as inhibitors for the sodium-glucose transport protein 1 (SGLT1), a key player in glucose uptake. We identified phlorizin as a representative phenol glucoside for experimental validation. The SGLT1 protein structure (PDB ID 7wmv) was analyzed through Ramachandran plot, ERRAT score, and ProSAweb Z-score, confirming its high-quality 3D conformation. A ligand-based virtual screening approach yielded 400 compounds that matched well with our pharmacophore models, including 10 compounds from virtual libraries. Notably, two compounds stood out for their high matching scores. Molecular docking simulations revealed strong binding affinities with SGLT1, especially for the compound CHEMBL2303983 with a binding energy of -11.2 kcal/mol.
ADMET analysis was conducted to evaluate the drug-likeness & safety profile of such high-affinity compounds. The compounds exhibited variable water solubility and moderate lipophilicity but were generally compliant with most drug-likeness rules. However, certain challenges such as low GI absorption and inability to cross the blood-brain barrier were identified. No PAINS or Brenk alerts were raised, suggesting a low likelihood of assay interference or toxicity.
In conclusion, our in-silico approach has identified promising candidates among phenol glucosides for inhibition of SGLT1, albeit with challenges in solubility and pharmacokinetics that require further optimization. The study opens new avenues for the synthesis and experimental verification of novel SGLT1 inhibitors.
This study aims to evaluate the potential of phenol glucosides as inhibitors for the sodium-glucose transport protein 1 (SGLT1), a key player in glucose uptake. We identified phlorizin as a representative phenol glucoside for experimental validation. The SGLT1 protein structure (PDB ID 7wmv) was analyzed through Ramachandran plot, ERRAT score, and ProSAweb Z-score, confirming its high-quality 3D conformation. A ligand-based virtual screening approach yielded 400 compounds that matched well with our pharmacophore models, including 10 compounds from virtual libraries. Notably, two compounds stood out for their high matching scores. Molecular docking simulations revealed strong binding affinities with SGLT1, especially for the compound CHEMBL2303983 with a binding energy of -11.2 kcal/mol.
ADMET analysis was conducted to evaluate the drug-likeness & safety profile of such high-affinity compounds. The compounds exhibited variable water solubility and moderate lipophilicity but were generally compliant with most drug-likeness rules. However, certain challenges such as low GI absorption and inability to cross the blood-brain barrier were identified. No PAINS or Brenk alerts were raised, suggesting a low likelihood of assay interference or toxicity.
In conclusion, our in-silico approach has identified promising candidates among phenol glucosides for inhibition of SGLT1, albeit with challenges in solubility and pharmacokinetics that require further optimization. The study opens new avenues for the synthesis and experimental verification of novel SGLT1 inhibitors.
29. Some Immunological and Physiological Parameters Levels in Iraq Children with Autism Spectrum Disorders
Rusul A. A. Alshammary, Jamela Jouda, Adil A. S. Al-Salihy
Rusul A. A. Alshammary, Jamela Jouda, Adil A. S. Al-Salihy
Abstract
Some studies suggested that dysfunction of immune and endocrine systems could link with neurodevelopment disorder and immunopathogenesis of ASD. Therefore, the goal of this research is to examine the level of some immunological and physiological indicators in an effort to identify a new biomarker for ASD. In the current study, there were 72 Iraqi kids (both boys and girls), 50 kids with ASD who attended different autism centers in Iraq, and 22 kids without ASD. They were between the ages of 6 and 12. These children’s peripheral venous blood was drawn in order to measure the concentrations of several cytokines, such as (TNF-α and IL-6), cortisol, and WBCs indices and platelets/lymphocytes ratio. The study’s findings revealed: 1) a significantly higher level of TNF- α but not IL-6 in ASD patients when compared to control; 2) a significantly higher level of cortisol in ASD patients compared to controls; and 3) a significantly higher level of lymphocytes and total WBCs but not neutrophils and monocytes. 4) A significant increase in the platelets/lymphocytes ratio. Furthermore, there were no differences in these parameters based on the gender and severity of the autism. As a result, our findings revealed that cytokine level alterations may be crucial in the development of neurological diseases like autism since microglia release large amounts of TNF-α, which plays a significant role in the so-called neuroinflammatory response. An abnormal HPA axis with high or low concentration of cortisol in more than 22% of the ASD was found in our results, which could explain the different reactions of autistic children when exposed to the same situation. So we thought that cytokines, especially TNF-α, and cortisol, may represent a serological marker for autism.
30. One Pot Synthesis of 1-(phenyl)-1H Indoles, their Biological Screening and ADME Studies
Tirth Thaker, Dipen Panchani, Vaishali Bhuva
Tirth Thaker, Dipen Panchani, Vaishali Bhuva
Abstract
This research aims to develop a novel way for synthesizing indole derivatives. 1-(phenyl)-1H-indole analogues were synthesized by cyclization of 1-phenyl-2-(phenyl amino)-ethane-1-one. Biological evaluation of title compounds and absorption, distribution, metabolism and excretion (ADME) studies were performed and title compounds had a higher affinity and created ample interactions with different proteins.
31. Virtual Screening, Molecular Docking, and ADMET Analysis of Flavonoids as a Potential Pi3k Inhibitor for Cancer Treatment
Khushabu Patil, Mahesh Nemade, Anjali Bedse, Piyush Chandra, Rakesh Ranjan,Harshal Tare, Manish Bhise
Khushabu Patil, Mahesh Nemade, Anjali Bedse, Piyush Chandra, Rakesh Ranjan,Harshal Tare, Manish Bhise
Abstract
Cancer continues to be a global health burden, necessitating the exploration of innovative anti-cancer therapeutics. This study leverages computational biology tools such as molecular docking, ligand-based virtual screening, and ADMET to evaluate quercetin flavonoids as potential PI3K inhibitors for cancer treatment. Using Swiss Similarity and CB-Dock tools, 51 compounds were identified that showed promising interactions with PI3K. DB01645 exhibited the highest binding affinity among these, with a Vina score of -8.6. ADMET analysis revealed that this compound has favorable physicochemical properties, moderate lipophilicity, and good water solubility. The study adds to the growing evidence that Quercetin flavonoids have significant potential as next-generation anti-cancer agents targeting the PI3K pathway.
32. Pharmaceutical Interventions in the Management of Oral Mucositis in Cancer Patients Undergoing Dental Treatments: A Randomized Controlled Trial
Dushyantsinh Vala, Neha Gupta, Prajna P Nayak, Dhaval Niranjan Mehta, Md Waquar Alam, Santosh Kumar
Dushyantsinh Vala, Neha Gupta, Prajna P Nayak, Dhaval Niranjan Mehta, Md Waquar Alam, Santosh Kumar
Abstract
Benzydamine hydrochloride, chlorhexidine as mouthwash, amifostine, palifermin, and a placebo were the five treatments that were investigated in this study. Oral mucositis is a common adverse effect of cancer treatment, and this study aimed to analyse and compare the effectiveness of these treatments. For the purpose of evaluating the treatments, we used descriptive statistics, analysis of variance (ANOVA), and rigorous tests to determine whether or not the means were equal. We took into account standard scores, deviations from the mean, and statistically significant differences. The data showed significant differences in the mean scores of each treatment group (p 0.001), indicating that different treatments had different levels of effectiveness in treating oral mucositis. Benzydamine hydrochloride consistently had superior mean scores and lower standard deviations compared to chlorine dioxide mouthwash, amifostine, palifermin, and the placebo. Oral mucositis may be treated with a variety of different medications, however the research suggests that benzydamine hydrochloride in is the most successful option. These results have significant ramifications for the decisions that should be made for therapy based on evidence, and they highlight the need to compare the relative efficacy of the many drugs used to treat oral mucositis. Additional research is required to examine the underlying mechanisms and unique treatment responses, which will pave the way for more individualised and effective treatment approaches.
33. Chemometric Assisted UV-Spectrophotometric Quantification of Tigecycline in Parenteral Dosage Form
Kirtimaya Mishra, A Dash, A Jabeen, S Vegesna, SK Sahoo, V Gupta, D Jena
Kirtimaya Mishra, A Dash, A Jabeen, S Vegesna, SK Sahoo, V Gupta, D Jena
Abstract
Relating to the current study, the quality by design (QbD) concept is used for creating and validating an unique, resilient, accurate, and reliable spectrophotometric approach to quantify Tigecycline (TIG) in injections. Fractional factorial design (FFD) was a design implemented to screen the initial parameters. Moreover, the variables went through the central composite design (CCD) to assess the dependency and optimize the design. Several measures were analyzed statistically to determine the appropriateness of the data obtained from the experiments. At 250 nm, by the use of ethanol, TIG displays an absorption maximum. Variables like screening, slit-width, and sampling interval were recognized as critical method and again, evaluation was done by a CCD. A good linearity was produced for TIG within a range of 2 to 12 μg/mL, with R2 less than 0.999. The process was determined to be perfect, having a good average percent recovery (greater than 100%). According to ICH guidelines, validation of the developed method was performed. By the implementation of QbD principles, spectrophotometric techniques were created and planned to, integrate the qualities into the methods. These processes were manifested for being flexible and pertinent for identifying TIG in pharmaceutical dose regimens.
34. Synergistic Effect of L-cycloserine and Capecitabine on Human Colon Cancer Cell Line
Zena H. Sahib, Seher A. R. Almedeny
Zena H. Sahib, Seher A. R. Almedeny
Abstract
Introduction: Colon cancer comes in second place in the list of cancers in developed countries. Drug resistance is one of the causes of colorectal cancer therapeutic failure that usually occurs in most patients in advanced stage of colon cancer. This study investigates the effect of adding L-cycloserine to capecitabine in the HCT-116 colon cancer cell line.
Materials and methods: We compared the combined L-cycloserine-capecitabine effect with each of the two drugs alone on the HCT-116 colon cancer cell line as a positive control group. The growth rate inhibition was examined by crystal violet assay.
Results: The growth inhibition effect of L-cycloserine-capecitabine, L-cycloserine and capecitabine on HCT-116 cells was assessed with crystal violet assay, different concentrations including 3.12, 6.25, 12.5, 25, 50, and 100 μg/mL were used for L-cycloserine-capecitabine combination, and for both L-cycloserine and capecitabine. After incubation for 24 hours, results appeared that the combination of L-cycloserine and capecitabine increased the effect of both drugs alone as seen by a significant increase (p < 0.05) of the growth inhibition percentages in the L-cycloserine-capecitabine combination as compared with the positive control groups.
Conclusion: From the result, we can conclude that the L-cycloserine combination with capecitabine has a synergistic effect for colon cancer treatment that could be a more effective regimen.
Materials and methods: We compared the combined L-cycloserine-capecitabine effect with each of the two drugs alone on the HCT-116 colon cancer cell line as a positive control group. The growth rate inhibition was examined by crystal violet assay.
Results: The growth inhibition effect of L-cycloserine-capecitabine, L-cycloserine and capecitabine on HCT-116 cells was assessed with crystal violet assay, different concentrations including 3.12, 6.25, 12.5, 25, 50, and 100 μg/mL were used for L-cycloserine-capecitabine combination, and for both L-cycloserine and capecitabine. After incubation for 24 hours, results appeared that the combination of L-cycloserine and capecitabine increased the effect of both drugs alone as seen by a significant increase (p < 0.05) of the growth inhibition percentages in the L-cycloserine-capecitabine combination as compared with the positive control groups.
Conclusion: From the result, we can conclude that the L-cycloserine combination with capecitabine has a synergistic effect for colon cancer treatment that could be a more effective regimen.
35. Design of Mouth Dissolving Polyherbal Films for Dental Caries
Sushma M, Ashoka Babu VL, Sharon C. Furtado, Aishwarya R, Jyothi Lakshmi N
Sushma M, Ashoka Babu VL, Sharon C. Furtado, Aishwarya R, Jyothi Lakshmi N
Abstract
Oral disease is still a major public health problem across the globe in developed countries as well as developing countries. Dental caries is one of humans’ oldest and most prevalent diseases or conditions of factor situations. The present study was designed to evaluate the antimicrobial potential of polyherbal film containing extracts of Annona squamosa L, Mentha piperita and Acalypha indica leaves against Streptococcus mutans. The mouth-dissolving poly herbal films were formulated with 1% (OF1), 2% (OF2) and 3% (OF3) extract concentrations. OF3 produced better results than OF1 and OF2 in folding endurance, disintegration time and dissolution time. The antimicrobial properties of the polyherbal films and standard marketed formulations S1 and S2 mouthwash were evaluated against the dental pathogen, S. mutans. OF3 produced a zone of inhibition 18.3 ± 0.21 mm compared to S2 which produced an inhibition zone of 27.0 ± 0.24 mm, whereas S1 has not shown any zone of inhibition. These results indicated that the mouth dissolving poly herbal films could be effective in the treatment of dental caries and gingivitis.
36. Preparation of Bentonite Clay/TiO2 Nanocomposites Surface as Drug Carrier: In-vitro Release Study of Chloramphenicol Drug
Mohammed K. Al-Hussainawy, Aseel M. Aljeboree, Mohammed A. Jawad, Fatime S. Sheri, Ayad F. Alkaim
Mohammed K. Al-Hussainawy, Aseel M. Aljeboree, Mohammed A. Jawad, Fatime S. Sheri, Ayad F. Alkaim
Abstract
The delivery of pharmaceuticals via nanocomposites has become a fascinating area of study in recent years, with applications in the development of tools and the treatment of infections and cancer. The porous properties of titanium dioxide and clay nanocomposites play a key role in the targeted delivery system. So, the large surface area and porous volume have more interest in the delivery of drugs and their loading. In this study, bentonite clay and titanium dioxide (TiO2) nanocomposites were synthesized by a hydrothermal method to guide infections and drugs. The composites of nanocomposites were used by the adsorption technique as loading drugs and studied for their ability to deliver drugs. It was confirmed that titanium oxide was added to the bentonite clay through the EDX and XRD. Sharp diffraction values were observed by the X-ray spectrum for clay and titanium oxide and less intensity for the superimposed (TiO2/bentonite), While it was found that EDX spreads the titanium and other ions. The thermal stability of the composite (TiO2/bentonite) was increased after adding titanium dioxide nanoparticles. The removal rate of chloramphenicol was higher in the base media, reaching 98% for both bentonite and TiO2/bentonite. An examination of the release rate of the drug was carried out by bentonite clay and TiO2/bentonite in the stomach and blood media, and the percentage of release was 26.6 and 5% in pH 1.2 and 7.5 for bentonite and 54.6 and 23.6% in pH 1.2 and 7.5, respectively, for TiO2/bentonite.
37. Synthesis and Characterization of Co3O4 Spinel Nanoparticles with Antibacterial Activity
Mustafa Hammadi, Rulla Sabah, Esam H. Hummadi
Mustafa Hammadi, Rulla Sabah, Esam H. Hummadi
Abstract
Nanoparticles are abundant and usable in the medical field as an antibiotic. It has been found that metal oxide nanoparticles, such as Co3O4, are efficient against bacteria that are resistant to antibiotics. Escherichia and Staphylococcus bring on enteric sickness and other illnesses. This study used co-precipitation to create Co3O4 nanoparticles. SEM, X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy were used to analyze these oxide nanoparticles. The XRD pattern validated the Co3O4 crystalline match. SEM also showed the morphology of Co3O4 nanoparticles. As determined by X-rays, Co3O4 has an average diameter of around 37.08 nm. The Co3O4 nanoparticles were highly pure, showed by an energy-dispersive EDX pattern. Both on their own and in conjunction with cephalexin, these metal oxide nanoparticles demonstrated antibacterial efficacy against S. aureus and E. coli. These Co3O4 nanoparticles showed high growth inhibition compared with using cephalexin individually. These conclusions found that the presence of cephalexin with Co3O4 showed high growth inhibition. The antibacterial activity of Co3O4 nanoparticles should be subjected for further studies.
38. Antioxidant Role of Methionine: As an Essential Sulfur-containing Amino Acids
Samera M. Alkatib, Ahmed M. Zaki, May Kh. Ismail, Raghad Kh. Alsarraf
Samera M. Alkatib, Ahmed M. Zaki, May Kh. Ismail, Raghad Kh. Alsarraf
Abstract
Methionine is one of the essential sulfur-containing amino acids that are used in building proteins. In the body, methionine condenses with ATP to form S-adenosylmethionine (SAM), which acts as a methylation donor in various biological pathways. Methionine is characterized by its antioxidant activity and its ability to modify tissue sensitivity against oxidizing agents. Therefore, this study’s aim included using hydrogen peroxide 0.5% in drinking water to induce oxidative stress in the male rats and testing the ability of different concentrations of methionine for protection or prevention the oxidative stress during 10, 20 and 30 days.
Forty male rats with the age of 3-4 months and of weights ranging between 300 to 400 gm were divided into 4 groups: Group (1): control group received drinking tap water, group (2): treated with H2O2 0.5% in drinking water, group (3): treated with H2O2 and methionine 0.3%, group (4): treated with H2O2 and methionine 0.6%. The following parameters in the serum were measured: Vit. C, Vit. E, peroxynitrite, albumin, selenium, zinc, and copper.
Treatment with 0.3% methionine produced clear effects on the vit C, peroxynitrite, Zn and Cu levels in the serum, while the treatment with 0.6% methionine produced clear effects on the serum vit E, albumin, and Se levels.
Forty male rats with the age of 3-4 months and of weights ranging between 300 to 400 gm were divided into 4 groups: Group (1): control group received drinking tap water, group (2): treated with H2O2 0.5% in drinking water, group (3): treated with H2O2 and methionine 0.3%, group (4): treated with H2O2 and methionine 0.6%. The following parameters in the serum were measured: Vit. C, Vit. E, peroxynitrite, albumin, selenium, zinc, and copper.
Treatment with 0.3% methionine produced clear effects on the vit C, peroxynitrite, Zn and Cu levels in the serum, while the treatment with 0.6% methionine produced clear effects on the serum vit E, albumin, and Se levels.
39. Synthesis and Molecular Docking Studies of New Pyrimidinone ring Containing 1,2,3-Triazole Derivatives
Ahmed A. Kozan, Riyadh J. Nahi
Ahmed A. Kozan, Riyadh J. Nahi
Abstract
The current work describes the design, synthesis and molecular mocking studies of a series of new 1,4-disubstituted-1,2,3-triazole linked 2-pyrimidinone derivatives. Firstly, 4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)benzene sulfonic acid 1 was synthesized as a key starting material. This compound was reacted with a series of aromatic aldehydes under-investigated conditions to give a new series of chalcones 2a-f. Reaction of compounds 2a-f with urea in the presence of an aqueous solution of sodium hydroxide led to the construct 2-pyrimidinone ring system to obtain a series of new compounds containing 1,2,3-triaozle ring and pyrimidinone ring 3a-f. The newly synthesized compounds 2a-f and 3a-f were characterized by FT-IR, 1H-NMR and 13C-NMR spectra. In-silico molecular docking simulations, compounds 3a-f and their precursors 2a-f were conducted on two selected proteins: 7dpp and 8cx9. The results revealed that all of the newly synthesized compounds 2a-f and 3a-f displayed have a good binding affinity with the target proteins and higher than values recorded for the selected three standard antiviral drugs.
40. Evaluation of Anti-aging Effects of Gemfibrozil on D-galactose induced Aging Mouse Model
Rana J. H. AL-Bairmani, Haitham M. Kadhim
Rana J. H. AL-Bairmani, Haitham M. Kadhim
Abstract
Background: Aging is the sequential or progressive changes in the organisms that is associated with increasing susceptibility to disease and death. Advanced age is associated with increased incidence of a variety of chronic disease states that share oxidative stress and inflammation as causative role players. Accumulating evidence in published literature showed that the use of antioxidant and anti-inflammatory agents is an effective approach to alleviate or reverse aging-related changes with consequent reduction of the aging rate and related disease. Gemfibrozil, as a peroxisome proliferator-activated alpha receptor ligand (PPARα), is reported to have antioxidant and inflammatory activity.
Aim of the study: Evaluate the anti-aging effect of gemfibrozil on many parameters associated with the aging process on the D-galactose induced aging mice model.
Method: The current work was an experimental randomized controlled study in which 60 albino male mice weighing between 25 to 40 gm were randomly divided into 6 groups (10 mice each group). group1 apparently healthy group, receive normal saline orally. Group 2 (age induction group receive D-galactose 500 mg/kg) orally only for 6 weeks, group 3 (+D-galactose 500 mg/kg + vitc 100 mg/kg orally for 6 weeks) group 4 (D-galactose 500 mg/kg for 6 weeks then vitc 100 mg/kg for another 6 consecutive weeks group 5 (D-galactose 500 mg/kg + gemfibrozil 7.5 mg/kg concomitantly for 6 weeks) group 6 (D-galactose 500 mg/kg for 6 weeks then gemfibrozil 7.5 mg/kg for another 6 consecutive weeks. Then animals were sacrificed, liver and kidney were weighed for organ index measurement and tissue sections and heart homogenate were prepared for ELISA assay (measurement of TN alpha, IL1beta, SOD, GPX) and histopathological analysis of myocardial tissue.
Results: results showed a significant rise in liver and kidney indices in animals that received gemfibrozil orally administered (during and after induction) compared to aged group, with a dramatic decrease in inflammatory and oxidative stress mediator level and a marked reversal effect on myocardial hypertrophy induced by D-galactose.
Conclusion: Gemfibrozil oral administration alleviates aging-associated atrophic changes in liver and kidney, oxidative stress and inflammatory state in myocardial tissue and reverses aging-related myocardial hypertrophic changes.
Aim of the study: Evaluate the anti-aging effect of gemfibrozil on many parameters associated with the aging process on the D-galactose induced aging mice model.
Method: The current work was an experimental randomized controlled study in which 60 albino male mice weighing between 25 to 40 gm were randomly divided into 6 groups (10 mice each group). group1 apparently healthy group, receive normal saline orally. Group 2 (age induction group receive D-galactose 500 mg/kg) orally only for 6 weeks, group 3 (+D-galactose 500 mg/kg + vitc 100 mg/kg orally for 6 weeks) group 4 (D-galactose 500 mg/kg for 6 weeks then vitc 100 mg/kg for another 6 consecutive weeks group 5 (D-galactose 500 mg/kg + gemfibrozil 7.5 mg/kg concomitantly for 6 weeks) group 6 (D-galactose 500 mg/kg for 6 weeks then gemfibrozil 7.5 mg/kg for another 6 consecutive weeks. Then animals were sacrificed, liver and kidney were weighed for organ index measurement and tissue sections and heart homogenate were prepared for ELISA assay (measurement of TN alpha, IL1beta, SOD, GPX) and histopathological analysis of myocardial tissue.
Results: results showed a significant rise in liver and kidney indices in animals that received gemfibrozil orally administered (during and after induction) compared to aged group, with a dramatic decrease in inflammatory and oxidative stress mediator level and a marked reversal effect on myocardial hypertrophy induced by D-galactose.
Conclusion: Gemfibrozil oral administration alleviates aging-associated atrophic changes in liver and kidney, oxidative stress and inflammatory state in myocardial tissue and reverses aging-related myocardial hypertrophic changes.
41. The Impact of Carvedilol on Organ Index, Inflammatory Mediators, Oxidative Stress Parameters and Skin Markers in D-Galactose-Induced Aging Mice
Elaf M. Shihab, Haitham M. Kadhim
Elaf M. Shihab, Haitham M. Kadhim
Abstract
Background: Aging processes are defined as those that increase the susceptibility of individuals, as they grow older, to the factors that eventually lead to death. It is a complex multi-factorial process where several factors may interact simultaneously and may operate at many levels of functional organization.. Accumulating evidence has suggested that active ingredients that possess antioxidative and anti-inflammatory proprties could decrease the incidence and development of aging-related diseases and promote longevity. Carvedilol is a non-selective third generation β-blocker/α1-blocker with antioxidant and inflammatory activity to evaluate its antiaging effect and to investigate if it is better to given carvedilol with aging induction or after aging induction is established.
Aim: To evaluate the effect of carvedilol on organ index, inflammatory mediators, oxidative stress parameters and skin markers in d-galactose-induced aging mice.
Method: Male (swiss albino mice) weighing 20 to 30 g and aged 3 to 6 months was randomly divided into six groups , each consisting of 10 animals (60 mice in total). Group I was given normal saline orally only for six weeks, group II was given d-galactose 500 mg/kg orally only for six weeks, group III was given d-galactose 500 mg/kg orally and vitamin C 100 mg/kg orally concomitantly for six weeks, group IV given d-galactose 500 mg/kg orally only for six weeks, then directly next day after ending of aging induction, vitamin c 100 mg/kg started for another six weeks, group V given d-galactose 500 mg/kg orally and carvedilol 10 mg/kg orally concomitantly for six weeks, group VI given d-galactose 500 mg/kg orally only for six weeks, then directly next day after ending of aging induction, carvedilol 10 mg/kg started for another six weeks. After that, animals were weighed, euthanized, and dissected, the heart was removed and the organ index was calculated. Also the heart tissue is divided in to two parts, one homogenated to measure interleukin-Iβ, tumor necrosis factor-alpha, glutathione peroxidase and malondialdehyde, while the other piece for histopathological analysis to determine the presence of hypertrophy. Skin tissue was taken and homogenated for ELISA assay (measurement of collagen I and III levels ).
Results: Results showed a significant decrease in heart organ index in animals that received carvedilol orally administered compared to aged group, with a substantial decrease in inflammatory mediators, malondialdehyde level and a marked increase in glutathione peroxidase level, collagen I and collagen III levels. Furthermore, carvedilol reverses the myocardial hypertrophy induced by D-galactose.
Conclusion: The present study suggests that carvedilol has a positive antiaging benefit in reducing oxidative stress, decreasing inflammatory and skin aging markers and improving hypertrophic cardiac cells. Regarding the timing of drug administration, although carvedilol shows a benficial continuing impact when given with and after the initiation of aging. It’s better to give at starting of the aging process to control the aging series as soon as possible.
Aim: To evaluate the effect of carvedilol on organ index, inflammatory mediators, oxidative stress parameters and skin markers in d-galactose-induced aging mice.
Method: Male (swiss albino mice) weighing 20 to 30 g and aged 3 to 6 months was randomly divided into six groups , each consisting of 10 animals (60 mice in total). Group I was given normal saline orally only for six weeks, group II was given d-galactose 500 mg/kg orally only for six weeks, group III was given d-galactose 500 mg/kg orally and vitamin C 100 mg/kg orally concomitantly for six weeks, group IV given d-galactose 500 mg/kg orally only for six weeks, then directly next day after ending of aging induction, vitamin c 100 mg/kg started for another six weeks, group V given d-galactose 500 mg/kg orally and carvedilol 10 mg/kg orally concomitantly for six weeks, group VI given d-galactose 500 mg/kg orally only for six weeks, then directly next day after ending of aging induction, carvedilol 10 mg/kg started for another six weeks. After that, animals were weighed, euthanized, and dissected, the heart was removed and the organ index was calculated. Also the heart tissue is divided in to two parts, one homogenated to measure interleukin-Iβ, tumor necrosis factor-alpha, glutathione peroxidase and malondialdehyde, while the other piece for histopathological analysis to determine the presence of hypertrophy. Skin tissue was taken and homogenated for ELISA assay (measurement of collagen I and III levels ).
Results: Results showed a significant decrease in heart organ index in animals that received carvedilol orally administered compared to aged group, with a substantial decrease in inflammatory mediators, malondialdehyde level and a marked increase in glutathione peroxidase level, collagen I and collagen III levels. Furthermore, carvedilol reverses the myocardial hypertrophy induced by D-galactose.
Conclusion: The present study suggests that carvedilol has a positive antiaging benefit in reducing oxidative stress, decreasing inflammatory and skin aging markers and improving hypertrophic cardiac cells. Regarding the timing of drug administration, although carvedilol shows a benficial continuing impact when given with and after the initiation of aging. It’s better to give at starting of the aging process to control the aging series as soon as possible.
42. Synthesis, Characterization, Biological Activity and Thermal Study of New Complexes [Ni II, Hg II and La III] from Mixed Ligands(Curcumin and Azo compounds type N2O2)
Muna A. Shakir, Wurood A. Jaafar, Malath K. Rasheed
Muna A. Shakir, Wurood A. Jaafar, Malath K. Rasheed
Abstract
The compound [L] was produced in the current study through the reaction of 4-aminoacetophenon with 4-methoxyaniline in the cold, concentrated HCl with 10% NaNO2. Curcumin, several transition metal complexes (Ni (II), La (III), and Hg (II)), and compound [L] were combined in EtOH to create new complexes. UV-vis spectroscopy, FTIR, AA, TGA-DSC, conductivity, chloride content, and elemental analysis (CHNS) were used to describe the structure of produced complexes. Biological activities against fungi, S. aureus (G+), Pseudomonas (G-), E. coli (G-), and Proteus (G-) were demonstrated using complexes. Depending on the outcomes of the aforementioned methods, octahedral formulas were given as the geometrical structures for each created complex.
43. Neuroprotective Effect of Chlorogenic Acid against Pentylenetetrazol Induced Kindled Epilepsy in Mice
Akansha Singh, Lubhan Singh, Rupesh Pandey, Prabhat Singh, Moazzam Ali, Rahul Kaushik, Priyadarshini Soni
Akansha Singh, Lubhan Singh, Rupesh Pandey, Prabhat Singh, Moazzam Ali, Rahul Kaushik, Priyadarshini Soni
Abstract
Background: Epilepsy is a group of chronic neurological disorders characterized by seizures. Kindling, a chronic epileptic mouse model that was used to explore the epileptogenic mechanism and seeking new anti-epileptics. In kindling, sub-convulsive (chemical/ electrical) stimuli are delivered repeatedly and erratically, eventually causes massive convulsions. The aim of this study was to investigate the neuroprotective effects of chlorogenic acid, a phenolic acid derived from coffee, on seizure severity and kindling progression. Memory impairment inflammation due to oxidative stress by pentylenetetrazol (PTZ).
Objective: This study was used to investigate the neuroprotective effect of chlorogenic acid against pentylenetetrazol induced kindled epilepsy in mice.
Methods: Kindling was provoked by subsequent (one-day-gap) injections of PTZ (subconvulsive; 35 mg/kg; s.c.) for 29 days in mice. The experimental protocol included six groups (n=6) receiving proconvulsant doses of PTZ (35 mg/kg i.p.) every other day for 31 days. Alternating subcutaneous injections of PTZ induced priming with 15 injections of PTZ. Compared with the PTZ group, pre-treatment with chlorogenic acid (5 and 10 mg/kg) 1 h before PTZ administration reduced seizure score, reduced metastasis latency due to increased normal maze, and decreased metastasis latency extension at FST. PTZ-induced biochemical changes were enhanced in chlorogenic acid-treated animals, as indicated by decreased lipid peroxidation (MDA), nitric oxide and AChE levels, and increased SOD, GSH, catalase level. Following PTZ injection, convulsive behaviours were noted for 30 minutes. Open-field-test (locomotor activity), force swimming test (depressive behaviors), elevated plus-maze and passive avoidance tests were employed to evaluate cognition. Brain homogenate was used to estimate oxidative stress (glutathione,superoxide-dismutase, lipid-peroxidation), and acetylcholinesterase activity.
Results: This result suggest the neuroprotective potential of chlorogenic acid. This may be correlated with its ability to inhibit oxidative damage and reduce the occurrence of seizures and other related damage. It may be a promising candidate for mitigating the consequences of events.
Conclusion: Our findings suggest effect of chlorogenic acid against pentylenetetrazol-induced kindled epilepsy in mice which were established by behavioral and biochemical paradigms.
Objective: This study was used to investigate the neuroprotective effect of chlorogenic acid against pentylenetetrazol induced kindled epilepsy in mice.
Methods: Kindling was provoked by subsequent (one-day-gap) injections of PTZ (subconvulsive; 35 mg/kg; s.c.) for 29 days in mice. The experimental protocol included six groups (n=6) receiving proconvulsant doses of PTZ (35 mg/kg i.p.) every other day for 31 days. Alternating subcutaneous injections of PTZ induced priming with 15 injections of PTZ. Compared with the PTZ group, pre-treatment with chlorogenic acid (5 and 10 mg/kg) 1 h before PTZ administration reduced seizure score, reduced metastasis latency due to increased normal maze, and decreased metastasis latency extension at FST. PTZ-induced biochemical changes were enhanced in chlorogenic acid-treated animals, as indicated by decreased lipid peroxidation (MDA), nitric oxide and AChE levels, and increased SOD, GSH, catalase level. Following PTZ injection, convulsive behaviours were noted for 30 minutes. Open-field-test (locomotor activity), force swimming test (depressive behaviors), elevated plus-maze and passive avoidance tests were employed to evaluate cognition. Brain homogenate was used to estimate oxidative stress (glutathione,superoxide-dismutase, lipid-peroxidation), and acetylcholinesterase activity.
Results: This result suggest the neuroprotective potential of chlorogenic acid. This may be correlated with its ability to inhibit oxidative damage and reduce the occurrence of seizures and other related damage. It may be a promising candidate for mitigating the consequences of events.
Conclusion: Our findings suggest effect of chlorogenic acid against pentylenetetrazol-induced kindled epilepsy in mice which were established by behavioral and biochemical paradigms.
44. Polymeric Fluoroquinolone Microparticles for Pulmonary Drug Delivery: A Review on Characteristics, Drug Release Profile, and Antibacterial Study
Deliaz, M.F, Hendradi, E., Hariyadi, D.M
Deliaz, M.F, Hendradi, E., Hariyadi, D.M
Abstract
Polymeric microparticles have recently gained significant attention as promising carriers for antibiotic administration to the pulmonary route, especially the antibiotics from the fluoroquinolone class. The versatility and efficiency of fluoroquinolones, combined with the stability, biocompatibility, and tunable protection provided by polymeric encapsulation in microparticles, contribute to the effectiveness of fluoroquinolone microparticles in achieving desirable characteristics, particularly precise and controlled drug release in the lungs. Such characteristics, drug release profile, and antibacterial activities are mainly influenced by the physics and chemistry of the fluoroquinolones-polymer system as a whole, formulation parameters, and solvent usage. Therefore, this review provides a comprehensive summary of studies and research conducted between 2012 and the present, focusing on the characteristics, drug release profile, and antibacterial investigation of fluoroquinolone microparticles that utilize polymeric formulations for the purpose of delivering drugs to the lungs.
45. A Bird Eye View on Effervescent Drug Delivery System
Sanjali Jadhav, Avinash Gangurde
Sanjali Jadhav, Avinash Gangurde
Abstract
Effervescent drug delivery systems (EDDS) have gained significant attention in the pharmaceutical industry due to their unique characteristics and potential advantages over conventional dosage forms. This comprehensive review aims to provide an in-depth understanding of EDDS, including their formulation strategies, underlying mechanisms, and diverse applications in drug delivery. EDDS are effervescent dosage forms that release drugs upon water dissolution, leading toward carbon dioxide gas generation. The effervescence, resulting from the reaction between an acid and a base, facilitates rapid drug dissolution and enhances drug bioavailability. The primary components of an EDDS include an active pharmaceutical ingredient (API), effervescent agents (e.g., organic acids and bases), binders, disintegrants, and other excipients. Effervescent tablets, granules, powders, and effervescent-coated dosage forms are commonly employed formulations. Several factors, such as pH, temperature, solubility, and particle size, influence the drug’s effervescence process and subsequent release kinetics. The drug release mechanisms from EDDS can be attributed to various phenomena, including effervescence-driven disintegration, gas evolution, and solubilization. The effervescence-induced carbon dioxide bubbles mechanically disrupt the dosage form, leading to enhanced drug dissolution and subsequent release. Additionally, the carbon dioxide gas acts as a propellant, providing rapid drug delivery and potentially improving patient compliance. EDDS find applications in diverse therapeutic areas, including analgesics, antacids, dietary supplements, and antiviral agents. They offer several advantages, such as improved drug stability, enhanced bioavailability, increased patient convenience, and ease of administration, particularly for populations with swallowing difficulties.
Furthermore, EDDS can be tailored to achieve controlled release, targeted drug delivery, and taste masking through appropriate formulation modifications. However, challenges associated with EDDS include their sensitivity to environmental conditions, potential drug degradation during effervescence, and the need for specialized packaging to maintain stability. The selection of suitable effervescent agents, excipients, and manufacturing processes is crucial to overcome these limitations and ensure consistent product performance. In conclusion, effervescent drug delivery methods offer an auspicious approach instead of enhancing drug delivery and patient compliance. Their formulation versatility, rapid drug release, and potential for controlled release make them an attractive option for various therapeutic applications.
Furthermore, EDDS can be tailored to achieve controlled release, targeted drug delivery, and taste masking through appropriate formulation modifications. However, challenges associated with EDDS include their sensitivity to environmental conditions, potential drug degradation during effervescence, and the need for specialized packaging to maintain stability. The selection of suitable effervescent agents, excipients, and manufacturing processes is crucial to overcome these limitations and ensure consistent product performance. In conclusion, effervescent drug delivery methods offer an auspicious approach instead of enhancing drug delivery and patient compliance. Their formulation versatility, rapid drug release, and potential for controlled release make them an attractive option for various therapeutic applications.
46. Solid Lipid Nanoparticles: Drug Delivery Systems for Enhancing the Bioavailability of Antihypertensives
Neeraj K. Chauhan, Anuj Malik, Paramjeet K. Ratiyen
Neeraj K. Chauhan, Anuj Malik, Paramjeet K. Ratiyen
Abstract
The pharmaceutical industry focuses the SLNs as promising drug deliverance methods for improving bioavailability. SLNs are a swiftly budding field of nanotechnology amid plentiful budding applications in medicine and research. Lipid-based nanoparticles possess unique properties due to their small size, allowing novel therapeutics to be developed. The encapsulation of drugs within nano-carriers presents a new paradigm in drug delivery, enabling enhanced targeting at secondary and tertiary levels. Consequently, SLNs have garnered significant attention from researchers for their site-specific drug delivery. This review enlightens on the responsibilities of SLN for improving the pharmacokinetics of poorly soluble antihypertensive drugs. Profound investigations confirmed SLNs have latent to transfigure antihypertensives through enhanced oral delivery.
47. Vitamin-E TPGS Based Microemulsion: An Approach for Solubility Enhancement of Poorly Water-Soluble Drugs
Vallabh Deulkar, Sunitha Sampathi
Vallabh Deulkar, Sunitha Sampathi
Abstract
Poor aqueous solubility is the primary concern for dissolving new drug substances during early development. Several novel solubility enhancement techniques such as particle size reduction, salt formation, making solid dispersion, complex formation, use of cosolvent techniques, use of surfactants, physical and chemical modification, and PH adjustment using buffering agents have been explored extensively to resolve the issue of poor aqueous solubility of drug substances. Drug delivery in micro and nano-sized formulations is one of the ways to improve the solubility of these drug candidates over the physiological pH range. In recent years, combination methods have also been considered an interesting approach where more than one solubility enhancement technique is used. The present review focuses on the feasible approach for improving the solubility by forming Vitamin E TPGS-based suspension in micro or nano form by particle size reduction. Further, by granulation or spray drying techniques, these suspensions converted to a solid dosage form for oral drug delivery for patient compliance are being explored.
48. Beyond Syringes and Pills: Advances in Drug Delivery Systems for Diabetes
Muggu S. Bhavani, Ravindran Saravanan
Muggu S. Bhavani, Ravindran Saravanan
Abstract
Diabetes is a chronic disease that affects millions of people worldwide, and its prevalence is increasing. The two primary subtypes, type 1 and 2, have different causes and mechanisms, but both result in abnormal glucose metabolism. The standard of care for diabetes includes insulin therapy, oral anti-diabetic medications, diet, exercise, weight loss, and frequent self-monitoring of blood glucose levels. However, these treatments have limitations that can lead to poor patient compliance and suboptimal outcomes. Alternative insulin delivery systems such as inhalers, patches, and oral sprays offer potential benefits such as increased convenience, reduced pain, and improved adherence. Non-insulin injectables, long-acting basal insulins, and GLP-1 agonists have also shown promise in improving glycemic control and reducing the risk of complications. Nanoparticle-based systems like SLNs are a novel approach that offers several advantages for diabetic management. They allow for targeted drug delivery, controlled release, and improved biocompatibility, enhancing drug efficacy and reducing side effects. SLNs have shown potential in animal models for reducing extracellular matrix degradation, inhibiting carbohydrate digestive enzymes, and enhancing the regeneration of insulin-producing beta cells. More studies are needed to validate their safety and efficacy in humans, but the potential benefits of SLNs make them a promising option for diabetes management.
49. An Overview of Arachidonic Acid Metabolic Pathway and Recent Updates on a Few Heterocyclic Derivatives showing COX-2 Inhibition
Swagatam Sahoo, Ragghee Bhattacharya, Manish Yadav, Debasis Sai Panda, Tunul Guria, Kirtimaya Mishra
Swagatam Sahoo, Ragghee Bhattacharya, Manish Yadav, Debasis Sai Panda, Tunul Guria, Kirtimaya Mishra
Abstract
Inflammation crucial part of the immune response associated with a broad range of immunological diseases. The arachidonic acid (AA) pathway, which is an essential inflammatory mediator present at the internal surface of the cellular matrix, is hydrolyzed by phospholipase A2, which leads to the development of metabolites such as cytochrome P450 (CYP), lipoxygenases (LOXs), cyclooxygenases (Coxs) and enzymes which further develops into bioactive mediators such as prostanoids, leukotrienes (LTs) and more. Cyclooxygenases produce prostaglandins, available as 2 isomorphs, COX-1(constitutive) & COX-2(inducible), targeted by NSAIDs used to treat inflammation. Yet, they have a number of negative effects that lead to market withdrawal. Research has been done to look at novel COX-2 inhibitors and safety precautions. By structural alteration at COX-2 strong receiving site, structural along with functional research on a number of selective COX-2 blockers results in the creation of novel structures that are more potent and selective against inflammation while having a very low risk of side effects. This is made possible by computer-assisted medication design. This review gives an explanation regarding the biological functionalization of several COX-2 derivatives obtained by the help of in vitro, in vivo & molecular docking for better understanding of the structures and bonding accountable for an action.
50. Assessment of Blood Lipids in People with Chronic Hypertensive
Methaq N. Mahmoo, Noor S. Hasan, Sabreen H. Majeed
Methaq N. Mahmoo, Noor S. Hasan, Sabreen H. Majeed
Abstract
High blood pressure remains one of the world’s leading health problems. High blood pressure is already manageable, and early detection can prevent complications by using therapy or changing lifestyle to healthy habits. High blood pressure and dyslipidemia are two of the main hazard factors for cardiovascular disease. The current study was conducted on 60 male and female samples aged 35 to 70 years, which divided the samples into three groups each group including 20 samples. The first group are healthy people who don’t have high blood pressure or chronic diseases (control group), the second group of patients with chronic hypertension without treatment but follow lifestyle modification, and the third group of patients with chronic hypertension with treatment the active substance hydrochlorothiazide and Losartan potassium, The regulated questionnaire information was recorded for all members of the sample and was measured the lipid profile test of triglycerides, cholesterol, lipoprotein (HDL, VLDL, LDL) in serum, atherogenic index plasma, body mass index (BMI), waistline. Levels of triglycerides and cholesterol were a non-significant increase in group of patients hypertensive without treatment and a significant increase in group of patients hypertensive with treatment than the control group. The results of lipoproteins showed non-significant differences than the control group while there was a significant increase in the VLDL level of group patients hypertensive with treatment than the control group. The results also indicated non-significant differences in the groups of atherogenic index plasma, body mass index and waistline measurement except for group of patients hypertensive without treatment that showed a significant increase in BMI than control group.
51. Evaluation of Few Immunological Parameters in Patients with Chronic Renal Failure in Najaf
Buthaina Abd E. Naser, Zainab S. Mahdi
Buthaina Abd E. Naser, Zainab S. Mahdi
Abstract
Kidney failure is a chronic disease currently spreading worldwide, and one of its most important complications. Many indicators can be used to detect kidney disease early, which, if not treated, will eventually lead to failure. Kidney disease often leads to death. The study aimed to find a relationship between chronic renal failure and some immunological parameters and its relationship to the mechanism of dialysis, if it was hemorrhagic or peritoneal This study was conducted at the Kidney Center in Al-Sadr Teaching Hospital, Al-Najaf, and lasted from September 2022 to May 2023, including 57 males with chronic renal failure and 33 males. Listening male subjects who were considered as a control group. It was divided into age groups from 20 to 70, the duration of infection from 1 to 4 years, 5 to 7 and 8 to 15 years, and the body mass index included normal, excess, and obesity for patients with hemodialysis, peritoneal dialysis, and patients who did not reach the stage hemodialysis. The study concluded significant differences in the immunological indicators MCP-1 NTN-1, IL-1, α-TNF in the renal failure serum compared with healthy subjects. There was a positive relationship in the MCP-1, NTNT-1,IL-1, α TNF level. The results showed that there are significant differences p < 0.05 in age groups and body mass index in patients with renal failure compared with healthy subjects. There are no significant differences p > 0.05 with the duration of infection in patients with chronic renal failure compared with healthy controls. The presence of significant differences predicted kidney failure, p < 0.05, in the MCP-1 immunological indicators NTN-1, IL-1, α-TNF –TNF, The approved ROC table in patients with renal failure showed that the highest area of the biomarker NTN-1 and the lowest area is the biomarker α- TNF and immunological indicators are considered as predictors of early diagnosis of chronic renal failure.
52. Cervicovaginal Fetal Fibronectin Levels in Preterm Labor: Just Association or Reliable Screening Biomarker
Mazenah H. J. Al-Hachami, Bushra J. U. Alrubayae
Mazenah H. J. Al-Hachami, Bushra J. U. Alrubayae
Abstract
Background: Preterm birth (PTB) is a chief reason for neonatal illness and death. Prediction of PTB can prevent complications. The cervico-vaginal fetal fibronectin (fFN) test is a good predictor for preterm labor (PTL) within 7 to 14 days from testing. The levels of fFN are high during the first 16 to 22 weeks of gestation in normal pregnancy before it drops to very low values and rises over again as the gestation reaches term. The current work aimed to assess the association and reliability of cervicovaginal fFN in predicting PTL.
Patient and method: The study was cross-sectional that included hundred pregnant (aging from 20–34 years), gestational age ranging (from 24–34 weeks), and presented with abdominal pain. All applicants’ Detailed medical history regarding age, gravidity, and parity were taken from all applicants. Gestational age was calculated through general examination and abdominal and vaginal examination. During speculum vaginal examination, fFN samples were taken from the cervix and were examined for fFN using the quick check for assay. Statistical scrutiny was carried out by SPSS version 17. A p ≤ 0.05 was measured as significant.
Result: The mean age was (27.53 ± 4.23), range (of 20–34). Positive fFN results were detected in only (22%) of patients. Around two-thirds of the women end their pregnancy by normal vaginal delivery. Less than half (45.5%) of the included women delivered within one week after presentation, around 1/3rd (31.8%) delivered after the second week, and only 22.2% delivered during the first day of presentation. There was a significant association between pregnancy outcome and fFN results. A majority (90.9%) of patients end with preterm labor during 2 weeks of follow-up were presented with positive fetal fibronectin. The majority (90.9%) of patients end with preterm labor during 2 weeks of follow-up were presented with positive fFN results. There were non-significant variations between means of gestational ages, parity, and gestational age/weeks between those with positive and negative fFN results.
Conclusion: Among pregnant women with uterine contraction before advanced cervical dilatation, the presence of cervicovaginal fFN is an associated and reliable screening test in predicting the risk of PTL.
Patient and method: The study was cross-sectional that included hundred pregnant (aging from 20–34 years), gestational age ranging (from 24–34 weeks), and presented with abdominal pain. All applicants’ Detailed medical history regarding age, gravidity, and parity were taken from all applicants. Gestational age was calculated through general examination and abdominal and vaginal examination. During speculum vaginal examination, fFN samples were taken from the cervix and were examined for fFN using the quick check for assay. Statistical scrutiny was carried out by SPSS version 17. A p ≤ 0.05 was measured as significant.
Result: The mean age was (27.53 ± 4.23), range (of 20–34). Positive fFN results were detected in only (22%) of patients. Around two-thirds of the women end their pregnancy by normal vaginal delivery. Less than half (45.5%) of the included women delivered within one week after presentation, around 1/3rd (31.8%) delivered after the second week, and only 22.2% delivered during the first day of presentation. There was a significant association between pregnancy outcome and fFN results. A majority (90.9%) of patients end with preterm labor during 2 weeks of follow-up were presented with positive fetal fibronectin. The majority (90.9%) of patients end with preterm labor during 2 weeks of follow-up were presented with positive fFN results. There were non-significant variations between means of gestational ages, parity, and gestational age/weeks between those with positive and negative fFN results.
Conclusion: Among pregnant women with uterine contraction before advanced cervical dilatation, the presence of cervicovaginal fFN is an associated and reliable screening test in predicting the risk of PTL.
53. Clopidogrel Responsiveness in Patients Undergoing Percutaneous Coronary Intervention using Multiplate Analyzer: Frequency and Outcomes
Murad A. Khadim, Hasan A. Farhan, Muthanna, Muthanna H. Al-Quraishi
Murad A. Khadim, Hasan A. Farhan, Muthanna, Muthanna H. Al-Quraishi
Abstract
Objectives: Over and under response to dual antiplatelet therapy (DAPT) can lead to bleeding and thrombotic events in patients undergoing coronary stent placement. The present study aimed to assess the platelet response to clopidogrel in patient undergoing percutaneous coronary intervention (PCI) using Multiplate Analyzer. The primary outcome in the present study was the short-term incidence of stent thrombosis and bleeding events.
Background: Multiple electrode aggregometry is a rapid and standardized tool to for diagnosis of platelet defects and monitoring response to DAPT.
Methods: A hospital-based, prospective study was conducted on 431 patients who underwent PCI from September 2016 to November 2017 and received clopidogrel therapy. The platelet aggregometry was done using a Multiplate analyzer (Dynabyte, Munich, Germany). Patients were followed for 30 days to assess the incidence of stent thrombosis and bleeding.
Results: The patients’ mean age was 58 ± 6.7 years. A total of 40% of the patients were diabetic and 7.7% had chronic renal failure. The rate of clopidogrel non-responders was 10.7%, while clopidogrel over-responders were 18.3%. Patients with diabetes and chronic renal failure had significantly lower platelet responsiveness (40.1% with p < 0.05 and 7.7% with p <0.005, respectively). Smoking was significantly associated with platelet over-responsiveness (39.4%, p < 0.001). Patients with low platelet responsiveness to clopidogrel were associated with an increased risk of definite stent thrombosis (p < 0.005), while increasing bleeding risk was significantly associated with over-responsiveness to patients to clopidogrel (p <0.001).
Conclusions: Antiplatelet responsiveness showing individual variability with increased risk of stent thrombosis among the cases with no response to the effect of clopidogrel and high risk of bleeding with the over-responsiveness group.
Background: Multiple electrode aggregometry is a rapid and standardized tool to for diagnosis of platelet defects and monitoring response to DAPT.
Methods: A hospital-based, prospective study was conducted on 431 patients who underwent PCI from September 2016 to November 2017 and received clopidogrel therapy. The platelet aggregometry was done using a Multiplate analyzer (Dynabyte, Munich, Germany). Patients were followed for 30 days to assess the incidence of stent thrombosis and bleeding.
Results: The patients’ mean age was 58 ± 6.7 years. A total of 40% of the patients were diabetic and 7.7% had chronic renal failure. The rate of clopidogrel non-responders was 10.7%, while clopidogrel over-responders were 18.3%. Patients with diabetes and chronic renal failure had significantly lower platelet responsiveness (40.1% with p < 0.05 and 7.7% with p <0.005, respectively). Smoking was significantly associated with platelet over-responsiveness (39.4%, p < 0.001). Patients with low platelet responsiveness to clopidogrel were associated with an increased risk of definite stent thrombosis (p < 0.005), while increasing bleeding risk was significantly associated with over-responsiveness to patients to clopidogrel (p <0.001).
Conclusions: Antiplatelet responsiveness showing individual variability with increased risk of stent thrombosis among the cases with no response to the effect of clopidogrel and high risk of bleeding with the over-responsiveness group.
54. Effect of Adding Taurine to Gabapentin on Toronto Clinical Neuropathy Score in Patient with Diabetic Neuropathy
Haider R. Mohammad, Mohammed M. Mohammed, Ahmed A. Hlail
Haider R. Mohammad, Mohammed M. Mohammed, Ahmed A. Hlail
Abstract
Diabetic neuropathy is a type of nerve damage that can occur in patients with diabetes mellitus. High blood glucose can injure nerves throughout the body. Diabetic neuropathy most often damages nerves in the legs and feet causing symptoms like pain and numbness. Taurine has been widely investigated regarding to its properties as a neuroprotective agent, antioxidant, anti-inflammatory in several neurodegenerative diseases. A sample consist of 40 participants enrolled randomly into two groups; group A, 20 patients treated with gabapentin capsules 300 mg once daily at night for 3 consecutive months, and group B, 20 patients treated with gabapentin capsules 300 mg once daily at night plus taurine 1 g thrice daily for 3 consecutive months. Adding taurine in combination with gabapentin significantly improves numbness, tingling, and temperature when compared with gabapentin alone. As well as, has a highly significant improving on ataxia. Taurine is better in improving insulin sensitivity due to lowering HbA1c level significantly, beside a medium degree in increasing insulin secretion; as evidenced by decreased fasting serum glucose, decreased HbA1c significantly, increased insulin level significantly, and increased C-peptide level. The conclusion of this study, adding taurine to patients with diabetic neuropathy has a significant improving effect on Toronto clinical neuropathy score by alleviating signs and symptoms, and improving insulin sensitivity.
55. Depression and Associated Factors among Type 2 Diabetics in Karbala City, Iraq: As a Model of Anti-depressant Drugs
Sammar J. Mahan, Mohammed M. Mahammad
Sammar J. Mahan, Mohammed M. Mahammad
Abstract
Background: Diabetes mellitus is in the 21st century, it is a very common disease that affects a lot of people. DM and depression symptoms are well-known co-occurring diseases. A person’s ability to do everyday things can be affected by depressed symptoms and DM.
Objectives: To find the level of depression symptoms among type 2 diabetics, observe the socio-demographic & disease-related agents that cause depression.
Methods: A cross-sectional study design was used to assess depression in 200 people suffering from type 2 diabetes and 120 healthy participants as a control group. Patients scoring 5 or more were termed depressed. Each participant’s verbal informed consent was obtained before the interview. On the questionnaires, no names were written. Depression was correlated with demographic and patient-related disease characteristics using Spearman’s rho correlation.
Results: The severe, moderate, and mild depression rates were 7.5, 56, and 29%, respectively and 92.5% of diabetics had depressed symptoms. Among the control group, absences of depressed symptoms and mild depressed symptoms were more common. Diabetics had moderate, moderately severe, and severe depression are all more common than mild depression symptoms. Diabetic patients’ median PHQ-9 score (10) was significantly higher than the control group’s 8.
Conclusion: Depression is common among diabetes mellitus type 2 patients. Glycemic control is poor & obesity have an impact on it. Endocrinologists should be aware of the elevated risk of depression in this patient population.
Objectives: To find the level of depression symptoms among type 2 diabetics, observe the socio-demographic & disease-related agents that cause depression.
Methods: A cross-sectional study design was used to assess depression in 200 people suffering from type 2 diabetes and 120 healthy participants as a control group. Patients scoring 5 or more were termed depressed. Each participant’s verbal informed consent was obtained before the interview. On the questionnaires, no names were written. Depression was correlated with demographic and patient-related disease characteristics using Spearman’s rho correlation.
Results: The severe, moderate, and mild depression rates were 7.5, 56, and 29%, respectively and 92.5% of diabetics had depressed symptoms. Among the control group, absences of depressed symptoms and mild depressed symptoms were more common. Diabetics had moderate, moderately severe, and severe depression are all more common than mild depression symptoms. Diabetic patients’ median PHQ-9 score (10) was significantly higher than the control group’s 8.
Conclusion: Depression is common among diabetes mellitus type 2 patients. Glycemic control is poor & obesity have an impact on it. Endocrinologists should be aware of the elevated risk of depression in this patient population.