TY - JOUR
T1 - Effect of Polar Protic Solvents on the Physicochemical Properties and Dissolution of Soluplus Based Solid Dispersions of Rosuvastatin Calcium
AU - Inam, Sana
AU - Irfan, Muhammad
AU - Iqbal, Muhammad Shahid
AU - Syed, Haroon Khalid
AU - Islam, Nayyer
N1 - Publisher Copyright:
© 2022, Colegio de Farmaceuticos de la Provincia de Buenos Aires. All rights reserved.
PY - 2022
Y1 - 2022
N2 - Solid dispersions (SD) is a promising technology for improving dissolution and thereby bio-availability 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 boost-ed 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 con-trast 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.
AB - Solid dispersions (SD) is a promising technology for improving dissolution and thereby bio-availability 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 boost-ed 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 con-trast 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.
KW - increased solubility
KW - rosuvastatin calcium
KW - solid dispersion
KW - solpuplus
KW - solvent evaporation
UR - http://www.scopus.com/inward/record.url?scp=85139404217&partnerID=8YFLogxK
M3 - Article
AN - SCOPUS:85139404217
SN - 0326-2383
VL - 41
SP - 455
EP - 462
JO - Latin American Journal of Pharmacy
JF - Latin American Journal of Pharmacy
IS - 2
ER -