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Issue 19, 2015
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Crystallisation and physicochemical property characterisation of conformationally-locked co-crystals of fenamic acid derivatives

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Abstract

Polymorphism in drug compounds can cause significant problems for industrial-scale production and so a method for restricting the conformational freedom of the target compound whilst retaining desired chemical properties is highly beneficial to the pharmaceutical industry. Co-crystallisation is commonly used to alter the structure of an active pharmaceutical ingredient (API) without affecting its activity. A comprehensive co-crystal screen of four fenamic acid derivatives affords a strictly limited number of co-crystals. These show no evidence of polymorphism, although some of the parent APIs exhibit significant polymorphism. Two of these co-crystals, of mefenamic acid and tolfenamic acid with 4,4′-bipyridine, were previously unknown and are studied using X-ray diffraction. Co-crystals from this screen are fully characterised and display comparable solubility and stability with respect to the parent APIs; no phase transformations have been identified. A range of crystallisation techniques, including cooling and grinding methods, are shown to afford single polymorphic forms for each of the co-crystals.

Graphical abstract: Crystallisation and physicochemical property characterisation of conformationally-locked co-crystals of fenamic acid derivatives

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Supplementary files

Article information


Submitted
09 Feb 2015
Accepted
30 Mar 2015
First published
31 Mar 2015

CrystEngComm, 2015,17, 3610-3618
Article type
Paper
Author version available

Crystallisation and physicochemical property characterisation of conformationally-locked co-crystals of fenamic acid derivatives

K. E. Wittering, L. R. Agnew, A. R. Klapwijk, K. Robertson, A. J. P. Cousen, D. L. Cruickshank and C. C. Wilson, CrystEngComm, 2015, 17, 3610
DOI: 10.1039/C5CE00297D

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