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Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility by Nikita A. Vasilev; Artem O. Surov; Alexander P. Voronin; Ksenia V. Drozd; German L. Perlovich is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.
What is Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility about?
In this work, the cocrystallization approach was applied to itraconazole (ITR), a very slightly soluble triazole antifungal drug, which led to the formation of two new solid forms of ITR with 4-aminobenzoic acid (4AmBA) and 4-hydroxybenzamide (4OHBZA). A thermodynamic analysis of the solid-liquid binary phase diagrams for the (ITR + 4AmBA) and (ITR + 4OHBZA) systems provided conclusive evidence of the cocrystal stoichiometry: 1:1 for the cocrystal with 4-aminobenzoic acid, and 1:2 for the cocrystal with 4-hydroxybenzamide. Powder X-Ray diffraction analysis confirmed the formation of two different polymorphic forms of the [ITR + 4OHBZA] (1:2) cocrystal obtained either through solution or melt crystallization. Cocrystal formation and polymorphic transition processes were investigated in detail by the DSC and HSM methods. The thermodynamic functions of cocrystal formation were estimated from the solubility of the cocrystals and the corresponding solubility of the pure compounds at different temperatures. The combination of ITR and 4OHBZA was found to be more favorable than the reaction between ITR and 4AmBA in terms of both Gibbs energy and enthalpy. The pH-solubility behavior of the
Who reads Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility?
It is typically read by researchers, students, and practitioners in Pharmacology, Toxicology and Pharmaceutics.
- Author
- Nikita A. Vasilev; Artem O. Surov; Alexander P. Voronin; Ksenia V. Drozd; German L. Perlovich
- Publisher
- Elsevier BV
- Published
- 2021
- Language
- EN
- Field
- Pharmacology, Toxicology and Pharmaceutics (Life Sciences)