Utilization of Superdisintegrants in the Design, Evaluation and Optimization of Orodispersible Tablets containing Simvastatin-Cyclodextrin Inclusion Complexes

Abstract

A B S T R A C T Simvastatin is a BCS class II drug, having low aqueous solubility [1.45μg/ml] and therefore low oral bioavailability [5%]. In present study attempt has been made to prepare orodispers in cyclodextrin complexes. For enhancing solubility of drug, inclusion complexes of drug were prepared using hydroxy propyl β-cyclodextrin. The inclusion coplexes prepared by solvent evaporation method exhibited highest enhancement in solubility (520μg/ml) and also showed fastest dissolution profile (99.30% of drug release in 120 min) in comparison of pure drug and other formulations. These copmlexes were characterized by solubility study, differential scanning calorimetry, and X-ray diffractometry. So, this complex was worked further for formulation of simvastatin orodispersible tablets. To aid in faster disintegration of tablets, superdisintegrants in 2 different proportions were used and their effect on 2 2 disintegration was studied. The formulation was optimized using 3 factorial design. In 3 factorial design, amount of superdisintegrant (X1) and amount of effervescing agent (X2) were selected as independent variables. The time of disintegration (Y1) and percentage of friability (Y2) were selected as dependent variables. The data clearly indicated that the disintegration time and percentage friability values strongly depend on the selected independent variables. Hence, use of hydroxyl propyl β-cyclodextrin and addition of superdisitigrants is useful technique in enhancement of dissolution rate of simvastatin. ible tablets of simvastat