title: Lidocaine/L-menthol binary system: cocrystallization versus solid-state immiscibility.
abstract: We present the synthesis, structure determination, and thermodynamic properties of a never reported cocrystal prepared with lidocaine and L-menthol. The temperature-composition phase diagram of the lidocaine/L-menthol binary system was achieved using differential scanning calorimetry and X-ray diffraction experiments. The present study demonstrates that the only way to perform a phase equilibrium survey of the lidocaine/L-menthol system is to prepare the binary mixtures from the cocrystal, an equimolar stoichiometric compound of L-menthol and lidocaine. We describe a process that is crucial to elaborate pharmaceutical agents that remain in their thermodynamical stable state throughout their preparation, manufacture, and storage for effective use.
authors.affiliation: Laboratoire Physico-Chimie Industrielle du Médicament, EA 4066, Faculté des Sciences Pharmaceutiques et Biologiques, Université Paris Descartes, 4 Avenue de l'Observatoire, 75 270 Paris Cedex 06, France. yohann.corvis@parisdescartes.fr
authors.forename: Yohann
authors.initials: Y
authors.lastname: Corvis
authors.forename: Philippe
authors.initials: P
authors.lastname: Négrier
authors.forename: Mathieu
authors.initials: M
authors.lastname: Lazerges
authors.forename: Stéphane
authors.initials: S
authors.lastname: Massip
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Léger
authors.forename: Philippe
authors.initials: P
authors.lastname: Espeau
mesh_terms: D018360:Crystallography, X-Ray; D008012:Lidocaine / Q000737:chemistry*; D008610:Menthol / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D013237:Stereoisomerism; D013696:Temperature; D013816:Thermodynamics
chemical_list: D008610:Menthol; D008012:Lidocaine