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伊曲康唑液固复合制剂的处方设计与评价以提高其口服生物利用度。

Formulation and evaluation of liquisolid compacts of itraconazole to enhance its oral bioavailability.

作者信息

Thakkar Hetal P, Vasava Deepika, Patel Arpita A, Dhande Rahul D

机构信息

Department of Pharmacy, Faculty of Pharmacy, Kalabhavan Campus, The Maharaja Sayajirao University of Baroda, Vadodara 390001, Gujrat, India.

出版信息

Ther Deliv. 2020 Feb;11(2):83-96. doi: 10.4155/tde-2019-0050.

Abstract

Formulate and evaluate liquisolid compacts of Itraconazole, a biopharmaceutical classification system class II drug, which has poor bioavailability. PEG 600 was used as a nonvolatile solvent, Alfacel PH 200 as a carrier and Aerosil 200 as a coating material. The Itraconazole solution upon mixing with a carrier and coating material resulted in a dry powder, which was compressed into tablets. The optimized formulation exhibited a significantly higher drug dissolution (90.73% in 90 min) compared with conventional tablets and marketed capsules. The antifungal activity was retained in the formulation. Higher values of C and AUC of the formulation compared with the plain drug indicated enhancement in oral bioavailability. The formulation was stable at room temperature as well as in accelerated conditions.

摘要

对伊曲康唑(一种生物药剂学分类系统II类药物,生物利用度差)的液固分散体进行处方设计与评价。使用聚乙二醇600作为不挥发溶剂,Alfacel PH 200作为载体,气相二氧化硅200作为包衣材料。伊曲康唑溶液与载体和包衣材料混合后形成干粉,将其压制成片剂。与传统片剂和市售胶囊相比,优化后的制剂表现出显著更高的药物溶出度(90分钟内为90.73%)。该制剂保留了抗真菌活性。与原料药相比,该制剂的C值和AUC值更高,表明口服生物利用度有所提高。该制剂在室温及加速条件下均稳定。

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