Reversible interconversion of pharmaceutical salt polymorphs facilitated by mechanical methods

Abstract

Salification of the drug trimethoprim with enantiopure D- or L-lactic acid afforded salts with up to five times improved solubility. Both salts are polymorphic and we demonstrate fully reversible interconversion (cycling) between the drug polymorphs using mechanochemistry and slurry methods. We show drug polymorph interconversion requires both solvent contact and mechanical force, revealing strategies for cycling between solid material forms.

Description

This journal is © The Royal Society of Chemistry 2023

Keywords

Pharmaceutical Salts, Trimethoprim, Solubility Improvement, Mechanochemistry, Slurry Methods

Citation

Ma, L., Zheng, Q., Unruh, D. K., & Hutchins, K. M. (2023). Reversible interconversion of pharmaceutical salt polymorphs facilitated by mechanical methods. Chemical Communications, 59(50), 7779–7782. https://doi.org/10.1039/d3cc02188b

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