FORMULATION AND EVALUATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEM OF ANTIDIABETIC DRUGS

Abstract

quotThe current research was aimed to formulate, evaluate and optimize gastroretentive formulations for antidiabetic drugs. The drugs chosen for the study were metformin (MH), glipizide (GLP) and mitiglinide (MTG), which are benefited by preparing stomach specific drug delivery systems in the form of floating matrix tablet and floating microsponges. newlineIdentification of drugs was done by physical characterization and FTIR scan. The analytical methods on UV spectrophotometer and HPLC were developed for the in vitro analysis of drug. The bioanalytical methods were developed for MTG and GLP for evaluating pharmacokinetic parameter of the drug in vivo wistar rats. newlineThe floating matrix tablet was prepared for MH using HPMC K15M, as release retarding polymer along with other ionic and anionic polymeric substances. Final formulations were prepared using HPMC K15M and kappa carrageenan as the release retarding polymers. The optimization of metformin floating matrix tablet was done by simplex centroid design using HPMC K4 M (X1), kappa-Carrageenan (X2), gas-generating agent, sodium bicarbonate (X3), as independent variable. The floating lag time (Flag), drug released after 1 hour and time required for 90% drug release, were taken as dependent variables. All the tablets showed acceptable physicochemical properties. Formulation prepared with 150mg of X1, 75mg of X2 and 150mg of X3 was found to be the optimum having good floating lag time and also matching the desirability criteria for drug release. newlineAnother antidiabetic drug, for which the gastroretentive formulations were developed, was MTG. The floating matrix tablet of MTG was prepared using the combination of release controlling polymer HPMC K15M and sodium alginate. The final optimization was done by applying 32 full factorial design, taking floating lag time (Flag), time to release 50% of drug (t50) and time to release 90% of drug (t90) as dependent factors. All the formulations were evaluated and results showed that M-3 formulation containing maximum amount of both variabl