The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by co-processing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon^® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon^® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon^® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon^® K 30 could be one of the filler-binder alternatives for direct compression process.

In this research work, prodrugs of norfloxacin with various benzothiazoles were synthesized and studied for hydrolytic studies at various physiological pH. The results indicated that all of the prodrugs exhibited more and faster hydrolysis mainly in phosphate buffer (pH 7.4) rather than in HCl buffer (pH 1.2). These prodrugs were characterized by FTIR, ¹H NMR, mass spectroscopy and physical analysis. The synthesized prodrugs showed better partition coefficient as compared to parent compound, norfloxacin. All of the prodrugs were tested for antimicrobial activity against selected microbial strains. Among the synthesized prodrugs, M1 was found to exhibit significant antibacterial efficacy having MIC 6.25 µg/ml against S. aureus MTCC 96 and prodrug M6 depicted good antibacterial activity (MIC 6.25 µg/ml) against E. coli MTCC 443 when compared with norfloxacin (MIC 10 µg/ml). Prodrugs M2 and M4 showed comparable activity against E. coli MTCC 443 and P. aeruginosa MTCC 1688 respectively to standard drug norfloxacin. The antibacterial activity of prodrug M4 (MIC 25 µg/ml) was found to be better than ciprofloxacin (MIC 50 µg/ml) against S. pyogenus MTCC 442. Moreover, prodrugs M4 and M6 possessed better antifungal activities (MIC 250, 75 µg/ml respectively) against C. albicans MTCC 227 while M2 showed significant potency against A. niger MTCC 282 and A. clavatus MTCC 1323 (MIC 50 µg/ml) compared to standard drug nystatin (MIC 100 µg/ml).

Matrix tablets of Lovastatin were fabricated using Ae (okra) gum and guar gum, alone or on combination with other excipients. The tablets were evaluated for physical characteristics like hardness, weight variation, friability, swelling index and drug content. In this study Ae(okra ) gum was extracted and purified by the researcher. In vitro release of drug was performed in 0.1NHCl (pH 1.2) (without enzymes) for up to 2 h and the rest of dissolution in citric acid-phosphate buffer (pH 6.0) and phosphate buffer (pH 7.4) up to 3 h. All the physical characteristics of the fabricated tablets were within accepted limit. The tablets with Ae gum gave better release properties. The level of matrix affects drug release. The Ae gum showed better sustained release properties compared to guar gum. Okra gum also served as colon targeted matrix forming material in tablet form using Lovastatin as model drug. Chemical compounds studied In this article: Lovastatin [PubChem CID: 53232]

The present research article represents the formulation and evaluation of buccoadhessive film of ropinirole hydrochloride. This drug is an oral non-ergoline dopamine agonist with the greater affinity at D3 receptor. This drug having low molecular weight (296.84 g/mol), and short biological half-life (4-6 hrs) which necessitates for multiple dosing for maintaining therapeutic effect throughout the day. Moreover, drug is metabolized in liver forming several inactive metabolites which decrease it oral bioavailability upto 50% making it a suitable candidate for administration of drug through buccal mucosa. Buccal films of ropinirole hydrochloride were prepared using various polymers (HPMC, EC, PVA and Carbopol) by solvent casting method using propylene glycol as plasticizer. These films were evaluated for various parameter such as appearance, surface texture, weight uniformity, thickness, folding endurance, surface pH, drug content and swelling index. All the formulations were subjected to in vitro drug release study which were carried out using egg membrane as semi permeable membrane.