Enhancement of Dissolution Properties of Glibenclamide by using Liquisolid Compact Technique

Abstract

Glibenclamide, a sulfonylurea derivative is widely used as hypoglycaemic agent. Glibenclamide is a highly permeable class II drug. Hence, rate of oral absorption is often controlled by the dissolution rate in the gastrointestinal(GI)tract. Therefore, the Liquisolid compact of Glibenclamide has been prepared for the enhancement of dissolution of Glibenclamide. Neusilin US2 was selected as carrier material and Aerosil 200 was selected as coating material. A Central composite factorial design was applied to optimize the drug release profile systematically. The amounts of drug (%) in PEG 400 (X1) and Excipient ratio, R (X2) were selected as independent variables. Angle of repose (Y1), Hardness (Y2) and CPR at 10 min (Y3) were selected as dependent variables. All the batches of Liquisolid compacts showed significance improvement in dissolution of Glibenclamide. Various dissolution parameters like DP10min, %DE10min and MDT of optimized batch and direct conventional tablet were compared. DSC and XRD analysis of pure Glibenclamide, physical mixture and final formulation indicated that the drug was solubilized in non-volatile vehicle and solubilization of Glibenclamide was the main cause of enhancement of solubility of Glibenclamide. Storage of the prepared formulations at 45°C for one month showed no any chemical incompatibility. It was concluded that, Liquisolid compact technique can be a simple and effective to enhance the dissolution of poorly water soluble drug.