Taguchi Design for Development of Lipid-Polymer Effervescent Floating Tablets for Metformin Prolonged Release
García-Guzmán P*, Schifter-Aceves L, Ortega-Almanza L, Romero-Canto P
Department of Biological Systems, Metropolitan Autonomous University, Campus Xochimilco, México City, México.
Received: 10th November, 2023; Revised: 21st January, 2024; Accepted: 14th February, 2024; Available Online: 25th March, 2024
ABSTRACT
Floating drug delivery systems (FDDS) formulated with hydrophilic polymers and effervescent agents are a promising gastro retentive tool for prolonged drug release, especially with drug with low bioavailability and low solubility. Lately, it has been reported that the combination of lipids with hydrophilic polymers in the development of blends or composite hybrid materials may bring together the properties of individual components. This study proposed four formulations of effervescent lipid-polymer FDDS through a Taguchi experimental design for metformin’s prolonged release. Tablets were obtained by wet granulation, and the effect of HPMC, Compritol®, and sodium bicarbonate was studied. All formulations were evaluated with pharmacotechnical and biopharmaceutical properties such as in-vitro drug delivery, flotation, swelling, erosion and release kinetics. Effervescent lipid-polymer FDDS were obtained with prologued release until 24 hours. Formulation F1 meets the acceptance criteria of USP extended delivery. Compritol®, combined with HPMC and sodium bicarbonate, impacted release behavior and buoyancy properties. Formulations with high amounts of HPMC and Compritol® were found to have the lowest release rates and followed the Peppas-Sahlin kinetic model. Successful preparation of effervescent lipid-polymer was achieved and evaluated through a Taguchi experimental design, expected to result in prologued release and better therapeutic behavior.
Keywords: Lipid-polymer, Floating tablet, Taguchi, Metformin, Diabetes, Kinetic release.
International Journal of Drug Delivery Technology (2024); DOI: 10.25258/ijddt.14.1.07
How to cite this article: García-Guzmán P, Schifter-Aceves L, Ortega-Almanza L, Romero-Canto P. Taguchi Design for Development of Lipid-Polymer Effervescent Floating Tablets for Metformin Prolonged Release. International Journal of Drug Delivery Technology. 2024;14(1):38-44.
REFERENCES
- Reed J, Bain S, Kanamarlapudi V. A review of current trends with type 2 diabetes epidemiology, aetiology, pathogenesis, treatments and future Diabetes, Metab Syndr Obes Targets Ther. 2021;14:3567-3602. doi:10.2147/DMSO.S319895
- Fadheel Prevalence of diabetes mellitus and it’s complications in iraq. Int J Pharm Qual Assur. 2018;9(2):109-116. doi:10.25258/ ijpqa.v9i2.13631
- Zhao R, Lu Z, Yang J, Zhang L, Li Y, Zhang X. Drug Delivery System in the Treatment of Diabetes Mellitus. Front Bioeng Biotechnol. 2020;8(July):1-16. doi:10.3389/fbioe.2020.00880
- Bhavani MS, Saravanan Beyond Syringes and Pills: Advances in Drug Delivery Systems for Diabetes. Int J Drug Deliv Technol. 2023;13(3):1069-1077. doi:10.25258/ijddt.13.3.48
- Rajora A, Nagpal A Critical Review on Floating Tablets as a Tool for Achieving Better Gastric Retention. Crit Rev Ther Drug Carrier Syst. 2022;39(1):65-102. doi:10.1615/ CritRevTherDrugCarrierSyst.2021038568
- Basim P, Gorityala S, Kurakula Advances in Functionalized Hybrid Biopolymer Augmented Lipid-based Systems: A Spotlight on Their Role in Design of Gastro Retentive Delivery Systems. Arch Gastroenterol Res. 2021;2(1):35-47. doi:10.33696/ gastroenterology.2.025
- Kaushik A, Tiwari A, Gaur Role of excipients and polymeric advancements in preparation of floating drug delivery systems. Int J Pharm Investig. 2015;5(1):1. doi:10.4103/2230-973x.147219
- Chaudhury A, Duvoor C, Reddy Dendi VS, et Clinical Review of Antidiabetic Drugs: Implications for Type 2 Diabetes Mellitus Management. Front Endocrinol (Lausanne). 2017;8(January). doi:10.3389/fendo.2017.00006
- Waje MK, Barge VU, Talole BB. Development and validation of stability indicating assay method for simultaneous estimation of Glibenclamide and Metformin. Int J Pharm Qual Assur. 2017;8(3):111-118. doi:10.25258/ijpqa.v8i03.9572
- Djebbar M, Chaffai N, Bouchal F, Aouf Effervescent floating tablets of metformin HCl developed by melt granulation. Part I: Effect of hydrophilic polymer on biopharmaceutical properties. GSC Biol Pharm Sci. 2019;6(2):052-067. doi:10.30574/ gscbps.2019.6.2.0014
- Lamoudi L, Chaumeil JC, Daoud Swelling, erosion and drug release characteristics of Sodium Diclofenac from heterogeneous matrix tablets. J Drug Deliv Sci Technol. 2016;31:93-100. doi:10.1016/j.jddst.2015.12.005
- Wook Huh H, Na YG, Kang HC, et al. Novel self-floating tablet for enhanced oral bioavailability of metformin based on Int J Pharm. 2021;592(July 2020):120113. doi:10.1016/j. ijpharm.2020.120113
- Gambhire MN, Ambade KW, Kurmi SD, Kadam VJ, Jadhav KR. Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride. AAPS PharmSciTech. 2007;8(3). doi:10.1208/pt0803051
- Thapa P, Jeong Effects of formulation and process variables on gastroretentive floating tablets with a high-dose soluble drug and experimental design approach. Pharmaceutics. 2018;10(3):9-doi:10.3390/pharmaceutics10030161
- Gong L, Sun Y, Yu M, Gao Y, Zou M, Cheng G. Development and Evaluation of Compression Coating Gastro-Floating Tablet of Alfuzosin Hydrochloride for Zero-Order Controlled AAPS PharmSciTech. 2018;19(7):3277-3286. doi:10.1208/s12249- 018-1168-z
- Senjoti FG, Mahmood S, Jaffri JM, Mandal UK. Design and In-vitro evaluation of sustained release f loating tablets of metformin HCl based on effervescence and swelling. Iran J Pharm Res. 2016;15(1):53-70.
- El Nabarawi MA, Teaima MH, El-Monem RAA, El Nabarawy NA, Gaber DA. Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl. Drug Des Devel Ther. 2017;11:1081-1093. doi:10.2147/DDDT.S131936
- Patel MB, Shaikh F, Patel V, Surti NI. Application of simplex centroid design in formulation and optimization of floating matrix tablets of J Appl Pharm Sci. 2017;7(4):23-30. doi:10.7324/JAPS.2017.70403
- Teaima M, Hamid MMA, Shoman NA, Jasti BR, El-Nabarawi Promising swellable floating bupropion tablets: Formulation, in vitro/in vivo evaluation and comparative pharmacokinetic study in human volunteers. Drug Des Devel Ther. 2020;14:2741- 2757. doi:10.2147/DDDT.S258571
- El Nabarawi MA, Teaima MH, El-Monem RAA, El Nabarawy NA, Gaber DA. Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl. Drug Des Devel Ther. 2017;11:1081-1093. doi:10.2147/DDDT.S131936
- Aburahma MH, Badr-Eldin SM. Compritol 888 ATO: A multifunctional lipid excipient in drug delivery systems and Expert Opin Drug Deliv. 2014;11(12):1865- 1883. doi:10.1517/17425247.2014.935335
- Rosiaux Y, Girard JM, Desvignes F, Miolane C, Marchaud Optimizing a wet granulation process to obtain high-dose sustained-release tablets with Compritol 888 ATO. Drug Dev Ind Pharm. 2015;41(10):1738-1744. doi:10.3109/03639045.2014.1002410
- Jagdale SC, Patil SA, Kuchekar BS, Chabukswar Preparation and characterization of metformin hydrochloride-compritol 888 ATO solid dispersion. J Young Pharm. 2011;3(3):197-204. doi:10.4103/0975-1483.83758
- Patere SN, Kapadia CJ, Nagarsenker Inf luence of formulation factors and compression force on release profile of sustained release metoprolol tablets using compritol® 888ato as lipid excipient. Indian J Pharm Sci. 2015;77(5):620-625. doi:10.4103/0250-474X.169030
- Djebbar M, Chaffai N, Bouchal F. Development of floating tablets of metformin HCl by thermoplastic part II: In vitro evaluation of the combined effect of acacia Gum/ HPMC on biopharmaceutical performances. Adv Pharm Bull. 2020;10(3):399-407. doi:10.34172/apb.2020.048
- Kim B, Byun Y, Lee EH. Doe-based design of a simple but efficient preparation method for a non-effervescent gastro- retentive floating tablet containing metformin Pharmaceutics. 2021;13(8). doi:10.3390/pharmaceutics13081225
- Jain DD, Tambe SM, Amin PD. Formulation performance window for manufacturing cellulose-based sustained-release mini-matrices of highly water-soluble drug via hot-melt extrusion Cellulose. 2022;29(6):3323-3350. doi:10.1007/s10570- 022-04458-0
- Jadi RK, Bomma R, Sellappan V. Development of a new single unit dosage form of propranolol HCl extended release non-effervescent floating matrix tablets: In vitro and in vivo evaluation. J Appl Pharm Sci. 2016;6(5):112-118. doi:10.7324/ 2016.60517
- Jadhav S, Gangurde A. A Bird Eye View on Effervescent Drug Delivery Int J Drug Deliv Technol. 2023;13(3):1046-1058. doi:10.25258/ijddt.13.3.45
- Hasçiçek C, Yüksel-Tilkan G, Türkmen B, Özdemir N. Effect of formulation parameters on the drug release and floating properties of gastric floating two-layer tablets with acetylsalicylic acid. Acta Pharm. 2011;61(3):303-312. doi:10.2478/v10007-011- 0028-0
- Santamaría López KJ. Formulación y Caracterización De un Sistema de Liberación Gastroflotante de Tabletas Clorhidrato de Metformina basado en efervescencia e hinchamiento. Univ Autónoma Nuevo León Fac Ciencias Químicas. Published online 2018:106-128.
- Tadros Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: Development, optimization and in vitro-in vivo evaluation in healthy human volunteers. Eur J Pharm Biopharm. 2010;74(2):332-339. doi:10.1016/j. ejpb.2009.11.010
- Rahamathulla M, Alsahhrani SM, Al Saqr A, Alshetaili A, Shakeel F. Effervescent floating matrix tablets of a novel anti- cancer drug neratinib for breast cancer J Drug Deliv Sci Technol. 2021;66(August):102788. doi:10.1016/j. jddst.2021.102788