Effect of Polar Protic Solvents on the Physicochemical Properties and Dissolution of Soluplus Based Solid Dispersions of Rosuvastatin Calcium

Abstract

Solid dispersions (SD) is a promising technology for improving dissolution and thereby bioavailability of poorly soluble drugs. This study aimed to prepare SD of rosuvastatin calcium, a BCS class II
drug, through solvent evaporation method using variable ratios of soluplus to achieve the objective of boosted solubility. Moreover, impact of polar protic solvents (acetone, MeOH and AC:MeOH) was also investigated to foresee the transformation of physicochemical properties. The prepared formulations were assessed for
saturation solubility, in-vitro drug release, FTIR, XRD, DSC and SEM analysis. The results revealed that all
SDs profoundly increased solubility as well as drug release. Among the optimized SD formulations, RSEB-10
with a remarkable increase of 34.95 fold in solubility presented 81.67% of drug release within 5 min in contrast to only 25% release of pure RoCa. Importantly, the role of solvent, though present in minute amounts
after evaporation, could not be underrated and the combination of polar solvents noticeably influenced in
potentiating the solubility of RoCa.