Université de Paris, Faculté de Santé, CNRS, Inserm, UTCBS, Chemical and Biological Technologies for Health Group (utcbs.cnrs.fr), 4 avenue de l'Observatoire, 75006 Paris, France.
CentraleSupélec, Laboratoire Structures, Propriétés et Modélisation des Solides (SPMS), UMR CNRS 8580, CentraleSupélec, Université Paris Saclay, 3 Rue Joliot Curie, 91190 Gif-sur-Yvette, France.
Eur J Pharm Biopharm. 2021 Dec;169:91-96. doi: 10.1016/j.ejpb.2021.09.008. Epub 2021 Sep 25.
The stable and metastable phase diagrams between the sinister and the rectus ibuprofen enantiomers were established by means of thermal analysis and X-ray powder diffraction experiments as a function of temperature. The results obtained allow proving for the first time the existence, for the stable system, of a solid solution by mixing the racemic ibuprofen with one of its enantiomers for low concentration of the enantiomer. Since the rectus ibuprofen is a non-active pharmaceutical agent which can be partially bio-converted into the sinister enantiomer, the present work offers a new approach for scalemic mixtures preparation in order to improve the benefit/risk ratio related to ibuprofen solid dosage form administration.
通过热分析和 X 射线粉末衍射实验，确定了（S）-和（R）-布洛芬对映异构体之间在稳定和亚稳定状态下的相图，作为温度的函数。所获得的结果首次证明，在稳定体系中，通过将外消旋布洛芬与其中一种对映异构体混合，在低对映异构体浓度下存在固溶体。由于（R）-布洛芬是非活性药物制剂，它可以部分生物转化为（S）-对映异构体，因此，目前的工作为制备手性混合物提供了一种新方法，以提高与布洛芬固体制剂给药相关的获益/风险比。
