Preparation and evaluation of solid dispersion of atorvastatin calcium with Soluplus® by spray drying technique.

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.

authors

Ha ES,Baek IH,Cho W,Hwang SJ,Kim MS

doi

10.1248/cpb.c14-00030

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

545-51

issue

6

eissn

0009-2363

issn

1347-5223

pii

DN/JST.JSTAGE/cpb/c14-00030

journal_volume

62

pub_type

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