Département de Génie des Procédés, Faculté de Technologie, Laboratoire de Préparation, Modification et Applications des Matériaux Polymériques Multiphasiques, Université Ferhat Abbas Sétif-1, Sétif, Algérie.
Faculty of Exact Sciences, Laboratory of Materials and Catalysis, Djillali Liabès University of Sidi Bel Abbès, Sidi Bel Abbès, Algeria.
J Enzyme Inhib Med Chem. 2021 Dec;36(1):605-617. doi: 10.1080/14756366.2020.1869225.
The aim of this study was to prepare and characterise inclusion complexes of a low water-soluble drug, mefenamic acid (MA), with β-cyclodextrin (β-CD). First, the phase solubility diagram of MA in β-CD was drawn from 0 to 21 × 10 M of β-CD concentration. A job's plot experiment was used to determine the stoichiometry of the MA:β-CD complex (2:1). The stability of this complex was confirmed by molecular modelling simulation. Three methods, namely solvent co-evaporation (CE), kneading (KN), and physical mixture (PM), were used to prepare the (2:1) MA:β-CD complexes. All complexes were fully characterised. The drug dissolution tests were established in simulated liquid gastric and the MA water solubility at pH 1.2 from complexes was significantly improved. The mechanism of MA released from the β-CD complexes was illustrated through a mathematical treatment. Finally, two experiments confirmed the interest to use a (2:1) MA:β-CD complex.
本研究旨在制备并表征低水溶性药物甲芬那酸（MA）与β-环糊精（β-CD）的包合物。首先，绘制了 MA 在β-CD 中的相溶解度图，β-CD 浓度从 0 到 21×10 M。采用工作曲线实验确定 MA:β-CD 配合物（2:1）的化学计量比。通过分子建模模拟证实了该配合物的稳定性。采用溶剂共蒸发（CE）、捏合（KN）和物理混合物（PM）三种方法制备（2:1）MA:β-CD 配合物。对所有配合物进行了全面表征。在模拟胃液中建立了药物溶解试验，复合物在 pH 1.2 时的 MA 溶解度显著提高。通过数学处理阐明了 MA 从β-CD 配合物中释放的机制。最后，两项实验证实了使用（2:1）MA:β-CD 配合物的意义。
