Gastroretgentive floating matrix tablets of mitiglinide

Abstract

Gastroretentive drug delivery systems (GRDDS) are designed to prolong gastric residence time and enhance the bioavailability of drugs with a narrow absorption window. Floating drug delivery systems remain buoyant in gastric fluid by forming low-density matrices or through gas-generating mechanisms, allowing prolonged gastric retention. Mitiglinide, a short-acting insulin secretagogue used in the management of Type-2 diabetes mellitus, exhibits low oral bioavailability, a short biological half-life, and requires frequent dosing. The present study aimed to develop and evaluate gastroretentive floating matrix tablets of Mitiglinide to achieve sustained drug release and improved glycemic control. Floating tablets were prepared by the direct compression method using hydrophilic polymers such as HPMC (K4M and K15M), Carbopol 934P, and sodium alginate, along with sodium bicarbonate and citric acid as gas-generating agents. Nine formulations were developed by varying polymer concentrations and evaluated for pre-compression flow properties and post-compression quality parameters. Floating lag time, total floating time, and in-vitro drug release studies were conducted. The results demonstrated satisfactory flow properties, acceptable tablet characteristics, rapid buoyancy, prolonged floating time, and sustained drug release up to several hours. Drug release followed Higuchi diffusion kinetics, with increased polymer concentration resulting in slower release. The study concludes that gastroretentive floating matrix tablets of Mitiglinide are a promising approach for enhancing bioavailability and reducing dosing frequency in Type-2 diabetes management.