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Título: | Polymorphic characterization and implications on biopharmaceutics properties of potential anti-inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica). |
Autor(es): | Caldeira, Tamires Guedes Guimarães, Dênia Antunes Saúde Lacerda, Dâmaris Laignier Rodrigues de Mussel, Wagner da Nova Yoshida, Maria Irene Souza, Jacqueline de |
Palavras-chave: | Differential scanning calorimetry Intrinsic dissolution Solubility X-ray powder diffraction |
Data do documento: | 2019 |
Referência: | CALDEIRA, T. G. et al. Polymorphic characterization and implications on biopharmaceutics properties of potential anti-inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica). Journal of Pharmacy and Pharmacology, v. 71, n. 6, p. 910-919, fev. 2019. Disponível em: <https://onlinelibrary.wiley.com/doi/full/10.1111/jphp.13080>. Acesso em: 10 fev. 2020. |
Resumo: | Objectives: To perform the polymorphic and physicochemical characterization of the potential anti-inflammatory drug, eremantholide C (EREC), as well as to evaluate the influence of these characteristics on its biopharmaceutics classification. Methods Eremantholide C was obtained from chloroformic extract of Lychnophora trichocarpha and crystallized in two distinct solvents: chloroform (EREC 1) and ethyl acetate (EREC 2). To evaluate the polymorphism, EREC samples were submitted to melting point, purity, infrared spectroscopy, differential scanning calorimetry (DSC), X-ray powder diffraction, optical microscopy and scanning electron microscopy analysis. In addition, EREC samples crystallized after intrinsic dissolution study were submitted to DSC and X-ray powder diffraction analysis. Key findings EREC 1 showed fusion at 234.7–241.6 °C, while EREC 2 showed fusion at 238.6–243.7 °C. No polymorphic transitions were observed during the intrinsic dissolution experiment. A single sharp endothermic peak was obtained for the EREC samples. X-ray diffraction showed no crystallographic differences between the EREC samples. EREC 1 and EREC 2 showed birefringence under polarized light and indefinite morphology; however, the shape of the crystals was common to the two samples. Conclusions: Eremantholide C does not present classical or morphological polymorphism; therefore, there is no influence of crystalline transitions in the solubility and consequently in its biopharmaceutics classification and oral absorption process. |
URI: | http://www.repositorio.ufop.br/handle/123456789/12197 |
Link para o artigo: | https://onlinelibrary.wiley.com/doi/full/10.1111/jphp.13080 |
DOI: | https://doi.org/10.1111/jphp.13080 |
ISSN: | 2042-7158 |
Aparece nas coleções: | DEFAR - Artigos publicados em periódicos |
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