Please use this identifier to cite or link to this item: http://www.repositorio.ufop.br/handle/123456789/12197
Title: Polymorphic characterization and implications on biopharmaceutics properties of potential anti-inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica).
Authors: Caldeira, Tamires Guedes
Guimarães, Dênia Antunes Saúde
Lacerda, Dâmaris Laignier Rodrigues de
Mussel, Wagner da Nova
Yoshida, Maria Irene
Souza, Jacqueline de
Keywords: Differential scanning calorimetry
Intrinsic dissolution
Solubility
X-ray powder diffraction
Issue Date: 2019
Citation: 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.
Abstract: 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
metadata.dc.identifier.uri2: https://onlinelibrary.wiley.com/doi/full/10.1111/jphp.13080
metadata.dc.identifier.doi: https://doi.org/10.1111/jphp.13080
ISSN: 2042-7158
Appears in Collections:DEFAR - Artigos publicados em periódicos

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