Reversible interconversion of pharmaceutical salt polymorphs facilitated by mechanical methods

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 sh...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2023-06, Vol.59 (5), p.7779-7782
Main Authors: Ma, Liulei, Zheng, Qixuan, Unruh, Daniel K, Hutchins, Kristin M
Format: Article
Language:English
Subjects:
Cycles
Lactic acid
Trimethoprim
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Summary: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. Fully reversible interconversion of pharmaceutical salt polymorphs is facilitated by a combination of mechanical force and solvent contact.
ISSN:1359-7345
1364-548X
DOI:10.1039/d3cc02188b