Development and in vivo evaluation of mucoadhesive tablets of Rebapimide

Abstract

The aim of the present work was in vitro and in vivo evaluation of mucoadhesive tablets of rebapimide to prolong the gastric residence time after oral administration. The solubility of rebapimide was enhanced by kneading technique with that mixture formulations were prepared by using 3 3 full factorial designs to explore the effects of gum Kondagogu, gum Olibanum and Guar gum (as independent variables) on mucoadhesive strength, drug release and Ex vivo residence time (as dependent variables) was studied and published in the earlier research paper.In this investigation the formulated mucoadhesive tablets which was optimized through in vitro studies was selected and performed the in vivo studies on human volunteers. The drug-polymer interaction was also studied by conducting FTIR and DSC tests. The in vitro release kinetics studies reveal that all formulations fits well with zero order, followed by Korsmeyer-Peppas, Higuchi and the mechanism of drug release is erosion. After analysis of different evaluation parameters and drug release kinetics, formulation code F13 was selected as a promising formulation for delivery of rebapimide as a mucoadhesive gastroretentive tablet with best mucoadhesive strength and 99.34% drug release at 12 th hour. Radiological evidences suggest that, a formulated tablet was well adhered for >10 h in human stomach. The bioavailability studies of F13 containing rebapimide was carried out which exhibited increased pharmacokinetic parameters of Cmax (427.01±73), Tmax (4.00±1.23 h) and AUC 0-t (2242±18.24) as compared to marketed formulations which indicates improved bioavailability of formulations.