ADMET and DMPK, Vol. 2 No. 1, 2014.
Original scientific paper
https://doi.org/10.5599/admet.2.1.33
The intrinsic aqueous solubility of indomethacin
John Comer
; Sirius Analytical Ltd., Forest Row, West Sussex RH18 5DW, UK
Sam Judge
; Sirius Analytical Ltd., Forest Row, West Sussex RH18 5DW, UK
Darren Matthews
; Sirius Analytical Ltd., Forest Row, West Sussex RH18 5DW, UK
Louise Towes
; Sirius Analytical Ltd., Forest Row, West Sussex RH18 5DW, UK
Bruno Falcone
; Unilever Centre for Molecular Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
Jonathan Goodman
; Unilever Centre for Molecular Informatics, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK
John Dearden
; School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, Byrom Street, Liverpool L3 3AF, UK
Abstract
A value of 8.8 μg/mL was measured for the intrinsic solubility of indomethacin. Evidence of a form with a solubility of about 77 μg/mL was also obtained. Solubility measurements were conducted using the CheqSol and Curve Fitting methods using a maximum pH of 9. It is also demonstrated that a published intrinsic solubility of 410 μg/mL was in error due to decomposition of indomethacin at pH 12. The decomposition of indomethacin at pH 12 was investigated. Decomposition products comprising p-chlorobenzoic acid and 5-Methoxy-2-methyl-3-indoleacetic acid were isolated and characterised.
Keywords
Indomethacin; solubility; CheqSol; p-chlorobenzoic acid; decomposition
Hrčak ID:
119017
URI
Publication date:
1.4.2014.
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