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

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 w(1) = 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.

Automated summary

This study examines the solubility of atorvastatin calcium (ATC) in ethanol and water mixtures, and studies the impact of different concentrations of Tween 80 and benzalkonium chloride (BAC) on the drug's solubility in aqueous ethanol mixtures. ATC has the highest solubility in ethanol + water mixtures with a ratio of w(1) = 0.7 ethanol. The addition of a surfactant alters the drug's solubility profile based on the type and concentration of the surfactant. XRD and DSC results indicate that a high concentration of BAC may lead to the formation of ATC solvate, affecting the drug's melting point and solubility. The type and concentration of surfactant 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 down the growth rate.