In-vitro and in-vivo Consideration of Repaglinide Immediate-release Tablet: Assessment of Porous Aceto-starch as a Promising Carrier for Dissolution Rate Enhancement

Abstract

In the present investigation, porous aceto-starch has been prepared for the first time using aqua-gel to an aceto-gel method to facilitate solubility and dissolution rate of Repaglinide (RPGD) to enhance oral bioavailability. The RPGD was selected as a model drug due to its low aqueous solubility and dissolution rate in GI fluid. Fabricated aceto-starch was characterized using FT-IR, DSC, XRPD, BET and FESEM studies followed by in-vitro drug release rate. It showed outstanding features like high surface area, good drug loading and significant improvement in drug dissolution rate, making it a potential drug carrier. Consequently, repaglinide loaded aceto-starch (R-aceto-starch) immediate-release tablets were prepared by direct compression method. Pre and post-compression parameters for blend and tablets were studied and found within pharmacopoeial acceptable limits. R-aceto-starch and immediate-release tablets demonstrated improved dissolution rate compared with pure crystalline RPGD, physical mixture and marketed tablets. The in-vivo assessment of tablet indicated efficient control of blood glucose levels than pure RPGD and showed good in-vitro and in-vivo correlation. The results of stability studies revealed that there were no significant differences in physico–chemical parameters and dissolution rate between the initial and stored R-acetostarch immediate-release tablets. In a nutshell, it can be concluded that encapsulating poorly soluble drugs in porous aceto-starch would be an innovative strategy for dissolution rate enhancement of BCS II drug, when administered orally.