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Preparation and Evaluation of Solid Dispersion of Atorvastatin Calcium with Soluplus® by Spray Drying Technique

Authors :
Eun Sol Ha
In-hwan Baek
Wonkyung Cho
Sung Joo Hwang
Min-Soo Kim
Source :
Chemical and Pharmaceutical Bulletin. 62:545-551
Publication Year :
2014
Publisher :
Pharmaceutical Society of Japan, 2014.

Abstract

The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.

Details

ISSN :
13475223 and 00092363
Volume :
62
Database :
OpenAIRE
Journal :
Chemical and Pharmaceutical Bulletin
Accession number :
edsair.doi.dedup.....518bbf92573a00fd3b090a752b1ea62e
Full Text :
https://doi.org/10.1248/cpb.c14-00030