Lidocaine/L-menthol binary system: cocrystallization versus solid-state immiscibility.
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.
Corvis
Yohann
Y
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
Négrier
Philippe
P
Lazerges
Mathieu
M
Massip
Stéphane
S
Léger
Jean-Michel
JM
Espeau
Philippe
P
D018360:Crystallography, X-Ray; D008012:Lidocaine / Q000737:chemistry*; D008610:Menthol / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D013237:Stereoisomerism; D013696:Temperature; D013816:Thermodynamics
D008610:Menthol; D008012:Lidocaine