ADMET and DMPK  

The intrinsic aqueous solubility of indomethacin

John Comer, Sam Judge, Darren Matthews, Louise Towers, Bruno Falcone, Jonathan Goodman, John Dearden

Abstract


A value of 8.8 μg/mL was measured for the intrinsic solubility of indomethacin. Evidence of an amorphous 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.

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DOI: http://dx.doi.org/10.5599/admet.2.1.33

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ISSN 1848-7718