Most drugs are delivered as crystalline solids, but some widely used pharmaceutical ingredients cannot be crystallized at ambient conditions: propofol, one of the most widely used anesthetic agents in the world is a liquid. Here we stabilize propofol in a crystalline phase by cocrystallization, and we thoroughly characterize the structural and thermodynamic properties of the new materials. Ternary solubility diagrams of a liquid pharmaceutical ingredient cocrystallized with a solid coformer are presented and analyzed for the first time. It is shown that, when equilibrated with the solid cocrsytal, the concentration of propofol in water is kept constant in a wide range of starting compositions.

Turning Liquid Propofol into Solid (without Freezing It): Thermodynamic Characterization of Pharmaceutical Cocrystals Built with a Liquid Drug / Alessia Bacchi, *; Davide Capucci, †; Marco Giannetto, †; Monica Mattarozzi, †; Paolo Pelagatti, †; Nair Rodriguez-Hornedo, †; Katia Rubini, ‡; Andrea, Sala. - In: CRYSTAL GROWTH & DESIGN. - ISSN 1528-7483. - 16:11(2016), pp. 6547-6555. [10.1021/acs.cgd.6b01241]

Turning Liquid Propofol into Solid (without Freezing It): Thermodynamic Characterization of Pharmaceutical Cocrystals Built with a Liquid Drug

BACCHI, Alessia;CAPUCCI, Davide;GIANNETTO, Marco;MATTAROZZI, Monica;PELAGATTI, Paolo;
2016

Abstract

Most drugs are delivered as crystalline solids, but some widely used pharmaceutical ingredients cannot be crystallized at ambient conditions: propofol, one of the most widely used anesthetic agents in the world is a liquid. Here we stabilize propofol in a crystalline phase by cocrystallization, and we thoroughly characterize the structural and thermodynamic properties of the new materials. Ternary solubility diagrams of a liquid pharmaceutical ingredient cocrystallized with a solid coformer are presented and analyzed for the first time. It is shown that, when equilibrated with the solid cocrsytal, the concentration of propofol in water is kept constant in a wide range of starting compositions.
Turning Liquid Propofol into Solid (without Freezing It): Thermodynamic Characterization of Pharmaceutical Cocrystals Built with a Liquid Drug / Alessia Bacchi, *; Davide Capucci, †; Marco Giannetto, †; Monica Mattarozzi, †; Paolo Pelagatti, †; Nair Rodriguez-Hornedo, †; Katia Rubini, ‡; Andrea, Sala. - In: CRYSTAL GROWTH & DESIGN. - ISSN 1528-7483. - 16:11(2016), pp. 6547-6555. [10.1021/acs.cgd.6b01241]
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11381/2817274
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