Preparation and characterization of 9-nitrocamptothecin self-emulsifying microemulsion injection

作     者：吕娟丽 王坚成 张烜 张强 Juan-Li Lu;Jian-Cheng Wang;Xuan Zhang;Qiang Zhang

作者机构：北京大学药学院药剂学系 

基　　金：National Natural Science Foundation of China (GrantNo.30430760) the 985 projects (Phase II) of the State Key Labo-ratory of Natural and Biomimetic Drugs (Peking University, China) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2007年第16卷第3期

页      码：157-161页

摘      要：Aim To prepare a self-emulsifying microemulsion of 9-nitrocamptothecin （9-NC ME） for intravenous injection and investi- gation of its pharmacokinetic profiles in normal SD rats. Methods 9-NC ME was optimized in terms of droplet size and lack of drug precipitation following aqueous dilution using a pseudo-ternary phase diagram. Physicochemical properties of 9-NC ME were evaluated. 9-NC ME was intravenously administered via tail vein in healthy rats. Results A stable microemulsion was formulated consisted of soybean oil as oil phase, EPC/Tween-80 as emulsifier, and anhydrous ethanol as co-emulsifier. The droplets of the microemulsion were spherical shape with mean diameter of 38.3 ± 4.0 nm after 1：20 dilution with 5% glucose injection. The pharmacokinetic parameters of 9-NC ME after intravenous administration in rats were t1/2 of 0.97 ± 0.14 h, A UC0-8 of 372.77 ±49.62 ng·h·mL^-1 and MRT of 1.40 ± 0.21 h which were 1.4-fold, 1.65-fold, and 1.4-fold more than those of 9-NC solution （P〈0.01）. Conclusion The results suggested that 9-NC ME was a promising drug delivery system and it was expected to provide a novel 9-NC injection for cancer patients.

主 题 词：9-Nitrocamptothecin Self-emulsifying microemulsion Injection Pharmacokinetics 

学科分类：100702[100702] 1007[医学-药学类] 1006[医学-中西医结合类] 100602[100602] 10[医学] 

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