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From formulation to structure: 3D electron diffraction for the structure solution of a new indomethacin polymorph from an amorphous solid dispersion

Authors :
Helen W. Leung
Royston C. B. Copley
Giulio I. Lampronti
Sarah J. Day
Lucy K. Saunders
Duncan N. Johnstone
Paul A. Midgley
Source :
IUCrJ, Vol 11, Iss 5, Pp 744-748 (2024)
Publication Year :
2024
Publisher :
International Union of Crystallography, 2024.

Abstract

3D electron diffraction (3DED) is increasingly employed to determine molecular and crystal structures from micro-crystals. Indomethacin is a well known, marketed, small-molecule non-steroidal anti-inflammatory drug with eight known polymorphic forms, of which four structures have been elucidated to date. Using 3DED, we determined the structure of a new ninth polymorph, σ, found within an amorphous solid dispersion, a product formulation sometimes used for active pharmaceutical ingredients with poor aqueous solubility. Subsequently, we found that σ indomethacin can be produced from direct solvent evaporation using dichloromethane. These results demonstrate the relevance of 3DED within drug development to directly probe product formulations.

Details

Language :
English
ISSN :
20522525
Volume :
11
Issue :
5
Database :
Directory of Open Access Journals
Journal :
IUCrJ
Publication Type :
Academic Journal
Accession number :
edsdoj.4b8a69304af1467b8773d3c4b670d968
Document Type :
article
Full Text :
https://doi.org/10.1107/S2052252524008121