Crystallisation and physicochemical property characterisation of conformationally-locked co-crystals of fenamic acid derivatives
| Autor: | Dyanne L. Cruickshank, Alexander Cousen, Karen Robertson, Kate Wittering, Anneke R. Klapwijk, Chick C. Wilson, Lauren R. Agnew |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Active ingredient
Mefenamic acid Chemistry Fenamic acid General Chemistry Condensed Matter Physics Combinatorial chemistry law.invention chemistry.chemical_compound Tolfenamic acid Polymorphism (materials science) law medicine Organic chemistry General Materials Science Crystallization Solubility medicine.drug |
| Zdroj: | Wittering, K, Agnew, L, Klapwijk, A R, Robertson, K, Cousen, A, Cruickshank, D & Wilson, C 2015, ' Crystallisation and physicochemical property characterisation of conformationally-locked co-crystals of fenamic acid derivatives ', CrystEngComm, vol. 17, no. 19, pp. 3610-3618 . https://doi.org/10.1039/C5CE00297D |
| DOI: | 10.1039/C5CE00297D |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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