Cosolvent effect on solubility of aripiprazole in mixed solvents and apparent thermodynamic analysis of dissolution process. (August 2019)

• Record Type: Journal Article
• Authors: Wu, Yüfang; Cheng, Long; Wu, Jiaqin; Zhai, Mingyue; Cai, Liner
• Is Part Of: Journal of chemical thermodynamics. Volume 135(2019)
• Page Start: 330
• Page End: 335
• Publication Date: 2019-08
• Subjects: Aripiprazole -- Dissolution behavior -- Cosolvent effect -- Thermodynamic analysis; Thermodynamics -- Periodicals; Thermochemistry -- Periodicals; Thermodynamique -- Périodiques; Thermochimie -- Périodiques; Thermochemistry; Thermodynamics; Periodicals; 541.369
• DOI: 10.1016/j.jct.2019.03.021
• Languages: English
• ISSNs: 0021-9614

Abstract

Graphical abstract: Highlights: Research on the solid-liquid phase of aripiprazole in mixed solvents. The solubility data were correlated by some thermodynamic models. Some thermodynamic properties of dissolution process are evaluated. Abstract: Due to different polymorphs demonstrate significant variations in the drug properties such as solubility, stability and dissolution rate. In this work, we study the shape of the solubility profile of form X 0 (the thermodynamically stable form at room temperature) in two mixtures of ( n -propanol + acetone) and ( iso propanol + acetone) at T = 278.15–318.15 K. The solubility value is a function of temperature and solvent composition. It increases at first and then decreases with the increasing concentration of acetone in mass fraction, and the composition dependence of the solubility has a maximum around mass fraction of acetone w = 0.6 at all investigated temperatures. The Jouyban-Acree model and CNIBS/R-K model are applied to correlate the solubility, and CNIBS/R-K model is more suitable. The values of dissolution standard Gibbs energy ( Δ G sol o ) and dissolution standard entropy ( Δ S sol o ) are all positive which indicate that the dissolution is not only endothermic but also entropy-driving.