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

Acetostarch was prepared using aqua-gel to an aceto-gel method and used as carrier to improved 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. In present research work, acetostarch was prepared by solvent exchange method and characterized by using FT-IR, DSC, XRPD, BET and FESEM studies followed by in-vitro drug release rate. In order to study drug interaction, compatibility, surface area, structural and morphological characteristics. Repaglinide loaded acetostarch (R-acetostarch) showed significant improvement in drug dissolution rate. Consequently, R-acetostarch 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-acetostarch and immediate-release tablets demonstrated improved dissolution rate, when compared with pure crystalline RPGD, physical mixture and marketed tablets. The in-vivo assessment of R-acetostarch and immediate-release tablets were study by using oral glucose tolerance test and its 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 acetostarch would be an innovative strategy for dissolution rate enhancement of BCS II drugs, when administered orally.