FORMULATION AND EVALUATION OF GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF SITAGLIPTIN

Abstract

This study aimed to develop a novel gastro-retentive drug delivery system in the form of floating tablets containing the antidiabetic medication sitagliptin. Sitagliptin acts by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), which helps break down hormones released by the gut in response to food intake, including glucagon-like peptide-1 (GLP-1).The tablets contains Pectin and HPMC K as binders, with lactose monohydrate serving as a diluent. The effervescent agent, utilizing Citric acid as a gas-generating agent, was the basis for causing the tablet to float. Magnesium stearate and  talc are used in this tablet to increase the flow properties of the powder thus it helps in punching of the tablet. The direct compression method facilitated the production of six distinct formulations. Evaluation of these formulations focused on pre compression studies and post compression studies of the tablet. Consistency was observed across all formulations, indicated by minimal weight variation and good in vitro dissolution profiles. Among these formulations, M5 distinguished itself as the most promising. It was composed of 3mg Pectin and 7mg HPMC K, achieving an extended floating duration of 12 hours coupled with an efficient drug release profile over 8 hours. This formulation’s performance suggests its potential as an effective gastro retentive delivery system for Sitagliptin, offering a controlled release that could enhance patient compliance and therapeutic efficacy.