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Structure determination, thermal stability and dissolution rate of δ-indomethacin

Structure determination, thermal stability and dissolution rate of δ-indomethacin

Andrusenko, Iryna, Hamilton, Victoria, Lanza, Arianna E., Hall, Charlie L., Mugnaioli, Enrico, Potticary, Jason, Buanz, Asma ORCID: 0000-0002-2556-1256, Gaisford, Simon, Piras, Anna M., Zambito, Ylenia, Hall, Simon R. and Gemmi, Mauro (2021) Structure determination, thermal stability and dissolution rate of δ-indomethacin. International Journal of Pharmaceutics, 608:121067. ISSN 0378-5173 (doi:https://doi.org/10.1016/j.ijpharm.2021.121067)

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Abstract

The structure solution of the δ-polymorph of indomethacin was obtained using three-dimensional electron diffraction. This form shows a significantly enhanced dissolution rate compared with the more common and better studied α- and γ-polymorphs, indicating better biopharmaceutical properties for medicinal applications. The structure was solved in non-centrosymmetric space group P21 and comprises two molecules in the asymmetric unit. Packing and molecule conformation closely resemble indomethacin methyl ester and indomethacin methanol solvate. Knowledge of the structure allowed the rational interpretation of spectroscopic IR and Raman data for δ-polymorph and a tentative interpretation for still unsolved indomethacin polymorphs. Finally, we observed a solid-solid transition from δ-polymorph to α-polymorph that can be driven by similarities in molecular conformation.

Item Type: Article
Additional Information: Unmapped bibliographic data: DA - 2021/10/25/ [EPrints field already has value set] JO - International Journal of Pharmaceutics [Field not mapped to EPrints]
Uncontrolled Keywords: electron diffraction; structure determination; pharmaceutical compounds; polymorphism; bioavailability; indomethacin; non-steroidal anti-inflammatory drugs
Subjects: Q Science > QD Chemistry
R Medicine > RS Pharmacy and materia medica
Faculty / School / Research Centre / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > School of Science (SCI)
Last Modified: 02 Sep 2022 01:38
URI: http://gala.gre.ac.uk/id/eprint/35866

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