Captopril is the first angiotensin I-converting enzyme inhibitor widely used for the treatment of hypertension. Based on the well-known benefits of cyclodextrin inclusion complexes, the present study investigated the ability of β-cyclodextrin to include captopril. Solid inclusion complexes of captopril with β–cyclodextrin in a 1:2 molar ratio were prepared by using the paste method of complexation. For comparison purposes, a simple physical mixture with the same molar ratio was also prepared. Fourier-transform infrared spectroscopy, scanning electron microscopy, X-ray diffraction and simultaneous thermal analysis were used to characterize the raw materials, physical mixture and solid inclusion complex. In order to provide the drug in a more accessible and patient-compliant form following masking its bitter taste, as well as ensuring the appropriate release kinetics, the investigated complex was formulated as orally disintegrating tablets. The study of captopril dissolution in both compendial and simulated saliva media suggested the Noyes Whitney model as the best mathematical model to describe the release phenomena. A clinical study on healthy volunteers also highlighted the taste improvement of the new formulation as compared to conventional tablets.

中文翻译：

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含有卡托普利-环糊精复合物的口腔崩解片的研制与表征。

卡托普利是第一种被广泛用于治疗高血压的血管紧张素转换酶抑制剂。基于环糊精包合物的众所周知的益处，本研究调查了β-环糊精包括卡托普利的能力。卡托普利与β-环糊精的摩尔比为1：2的固体包合物通过糊化法制备。为了比较，还制备了具有相同摩尔比的简单物理混合物。使用傅里叶变换红外光谱，扫描电子显微镜，X射线衍射和同步热分析来表征原料，物理混合物和固体包裹体。为了在掩盖苦味之后以更易于使用和患者顺应的形式提供药物，为了确保适当的释放动力学，将所研究的复合物配制成口服崩解片剂。卡托普利在药典和模拟唾液中的溶解研究表明，Noyes Whitney模型是描述释放现象的最佳数学模型。一项针对健康志愿者的临床研究还强调了与传统片剂相比，新制剂的味道有所改善。