Laboratoire Physico-Chimie Industrielle du Médicament, EA 4066, Université Paris Descartes, Sorbonne Paris Cité, Faculté des Sciences Pharmaceutiques et Biologiques, 4 Avenue de l'Observatoire, 75 006 Paris, France.
J Pharm Sci. 2011 Dec;100(12):5235-43. doi: 10.1002/jps.22727. Epub 2011 Sep 8.
The aim of this study was to investigate the solid dispersion phase behavior of s- or rs-ibuprofen in stearic acid. By means of thermal analysis, we have demonstrated the total immiscibility, in solid state, of the corresponding binary mixtures. This indicates that no specific interactions exist between the chosen excipient and active pharmaceutical ingredient (API) that lead to eutectic systems. Furthermore, based on calorimetric and X-ray diffraction experiments, we have showed that upon cooling of the molten state, only stearic acid recrystallizes in the presence of s-ibuprofen, whereas a quaternary phase mixture is obtained for the racemic ibuprofen/stearic acid preparation. The solubility of stearic acid in s-ibuprofen liquid in all proportions was also determined. Overall, the results presented here offer an approach for the study of API/excipient interactions.
本研究旨在探讨 s-或 rs-布洛芬在硬脂酸中的固体分散相行为。通过热分析，我们证明了相应二元混合物在固态下完全不混溶。这表明所选赋形剂和活性药物成分 (API) 之间不存在导致共晶体系的特定相互作用。此外，基于量热和 X 射线衍射实验，我们表明在熔融态冷却时，只有 s-布洛芬存在时硬脂酸才会重结晶，而外消旋布洛芬/硬脂酸制剂则得到四元相混合物。还确定了硬脂酸在 s-布洛芬液体中的所有比例下的溶解度。总的来说，这里呈现的结果为研究 API/赋形剂相互作用提供了一种方法。
