Title: Effect of polar protic solvents on the physicochemical properties and dissolution of soluplus based solid dispersions of Rosuvastatin calcium
Summary
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
minutes 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.