AI Article Synopsis

  • The study focused on characterizing the anti-inflammatory drug eremantholide C (EREC) by examining its polymorphic and physicochemical properties to understand its biopharmaceutical classification.
  • EREC was obtained from a natural source and crystallized in two solvents, with various analyses performed to assess its melting points, purity, and structural properties.
  • The results indicated that EREC does not exhibit polymorphism, meaning its crystallization process does not affect its solubility or how well it can be absorbed in the body when taken orally.*

Article 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.

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http://dx.doi.org/10.1111/jphp.13080DOI Listing

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