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From Molecules to Materials: Engineering New Ionic Liquid Crystals Through Halogen Bonding

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Lidocaine/L-menthol binary system: cocrystallization versus solid-state immiscibility.

Yohann Corvis¹, Philippe Négrier, Mathieu Lazerges

¹Laboratoire 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

The Journal of Physical Chemistry. B

|April 10, 2010

Summary

Researchers synthesized a novel lidocaine and L-menthol cocrystal. This stable compound is essential for developing pharmaceutical agents that maintain their thermodynamic integrity during manufacturing and storage.

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Area of Science:

Pharmaceutical Science
Materials Science
Crystallography

Background:

Lidocaine and L-menthol are widely used pharmaceutical compounds.
Cocrystal formation is a key strategy for improving drug properties.
Understanding phase behavior is critical for stable drug formulation.

Purpose of the Study:

To synthesize and characterize a novel cocrystal of lidocaine and L-menthol.
To determine the temperature-composition phase diagram of the lidocaine/L-menthol binary system.
To establish a method for preparing thermodynamically stable pharmaceutical mixtures.

Main Methods:

Cocrystal synthesis and structure determination.
Differential scanning calorimetry (DSC) for thermal analysis.
X-ray diffraction (XRD) for structural and phase analysis.

Main Results:

A novel, equimolar cocrystal of lidocaine and L-menthol was successfully synthesized.
The temperature-composition phase diagram revealed the cocrystal as the sole stable phase.
Preparation of binary mixtures must originate from the cocrystal for phase equilibrium.

Conclusions:

The lidocaine/L-menthol cocrystal is a thermodynamically stable entity.
This cocrystal is crucial for the development of stable pharmaceutical formulations.
The described preparation process ensures drug stability throughout its lifecycle.