Solubility enhancement of atorvastatin calcium and ethanol-mediated transition with some surfactants

ABSTRACT

Atorvastatin calcium (ATC) is a class II BCS blockbuster synthetic cholesterol-lowering drug. The aim of this work is to examine the solubility of ATC in ethanol and water mixtures at room temperature and to study the effect of various concentrations of Tween 80 and benzalkonium chloride (BAC) on drug solubility in aqueous mixtures of ethanol. ATC shows maximum solubility in ethanol + water mixtures at a ratio of w₁ = 0.7 ethanol. The addition of a surfactant changed the drug solubility profile relative to the surfactant type and its concentration. XRD and DSC results indicate that a high concentration of BAC may induce the formation of ATC solvate which influenced the melting point and solubility of the drug. Surfactant type and concentration influence the morphology, nucleation, and growth of drug crystals. A high concentration of BAC accelerates crystal habits and its relative growth rate while Tween 80 slows its growth rate.

KEYWORDS:

• Atorvastatin calcium
• ethanol
• crystalline
• solvate
• Tween 80
• benzalkonium chloride

Acknowledgments

This work is partial fulfilment for a Pharm. D degree submitted by Hadi Foroughi in Urmia University of Medical Sciences (Grant No.1399-10460).

Disclosure statement

No potential conflict of interest was reported by the authors.

Correction Statement

This article has been republished with minor changes. These changes do not impact the academic content of the article.