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

Eun Sol Ha, In Hwan Baek, Wonkyung Cho, Sung Joo Hwang, Min Soo Kim

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39 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)545-551
Number of pages7
JournalChemical and Pharmaceutical Bulletin
Volume62
Issue number6
DOIs
Publication statusPublished - 2014 Jun

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All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Drug Discovery

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