Solubility and solution thermodynamics of raloxifene hydrochloride in various (DMSO + water) compositions

Abstract

The solubility of the poorly soluble drug raloxifene hydrochloride (3) in binary {dimethyl sulfoxide (DMSO) (1) + water (2)} mixtures have been recorded at several temperatures under atmospheric pressure. Four different computational models were applied to model the experimental solubility values of studied drug. Raloxifene hydrochloride mole fraction solubility was improved with higher temperature and DMSO mass fraction in {(DMSO) (1) + water (2)} compositions. Pure DMSO had the maximum mole fraction solubility of raloxifene hydrochloride (5.05 × 10–2 at 323.2 K), while pure water had the lowest (1.051 × 10–5 at 298.2 K). The “van't Hoff, Yalkowsky-Roseman, Jouyban-Acree, and Jouyban-Acree-van't Hoff models” had mean percent deviations of 5.13%, 11.96%, 1.14%, and 1.37%, showing excellent correlations. According to the results of apparent thermodynamic analyses, the dissolution of studied drug was “endothermic and entropy-driven” in all {(DMSO) (1) + water (2)} mixtures studied. The main mechanism for raloxifene hydrochloride solvation in {(DMSO) (1) + water (2)} mixtures was uncovered as an enthalpy-driven process. In comparison to raloxifene hydrochloride-water, raloxifene hydrochloride-DMSO produced the most molecular interactions. Finally, these results showed that DMSO has a lot of potential for solubilizing a poorly soluble raloxifene hydrochloride in water.

Keywords

• Correlation
• {DMSO (1) + water (2)} mixtures
• Molecular interactions
• Raloxifene hydrochloride
• Solubility
• Thermodynamics