Andrusenko, I;
Hamilton, V;
Lanza, AE;
Hall, CL;
Mugnaioli, E;
Potticary, J;
Buanz, A;
... Gemmi, M; + view all
(2021)
Structure determination, thermal stability and dissolution rate of 6-indomethacin.
International Journal of Pharmaceutics
, 608
, Article 121067. 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.
| Type: | Article |
|---|---|
| Title: | Structure determination, thermal stability and dissolution rate of 6-indomethacin |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.ijpharm.2021.121067 |
| Publisher version: | http://dx.doi.org/10.1016/j.ijpharm.2021.121067 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| Keywords: | Electron diffraction, Structure determination, Pharmaceutical compounds, Polymorphism, Bioavailability, Indomethacin, Non-steroidal anti-inflammatory drugs |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10135913 |
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