Taguchi Design for Development of Lipid-Polymer Effervescent Floating Tablets for Metformin Prolonged Release

Abstract

TFloating 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