用于肺部给药的磷酸奥司他韦微粉的制备及肺组织分布初步考察

发布时间：2018-07-14 21:10

【摘要】：磷酸奥司他韦(1)是一种神经氨酸酶抑制剂类抗流感病毒药物。采用喷雾干燥方法制备了可用于肺部吸入给药的1微粉。通过正交设计得到的最优处方为:1 20%、亮氨酸20%、甘露醇60%,溶于去离子水中配成2%的溶液,喷雾干燥制得体积平均径为(2.907±0.105)μm、休止角为(29.2±2.0)°的微粉,产率为(58.1±3.2)%。使用Aerolizer~?吸入装置对装入胶囊的微粉进行雾化分散,测得其微细粒子分数为(36.2±2.8)%。大鼠肺部刺激性试验表明该微粉无明显肺部刺激性。肺组织分布试验表明1微粉肺部给药后大鼠肺部活性代谢产物奥司他韦羧酸含量高于口服同剂量1微粉溶液组。提示本研究制得的1微粉吸入后对呼吸道病毒感染可能会比口服发挥更好的治疗作用。
[Abstract]:Oseltamivir phosphate (1) is a neuraminidase inhibitor of influenza virus drugs. One micropowder which can be used for lung inhalation was prepared by spray drying method. The optimum formulation obtained by orthogonal design is: 1 / 120, leucine 20, mannitol 60, dissolved in deionized water into 2% solution, the average volume diameter is (2.907 卤0.105) 渭 m, the angle of repose is (29.2 卤2.0) 掳, the yield is (58.1 卤3.2) 掳, the average volume diameter is (2.907 卤0.105) 渭 m, the angle of repose is (29.2 卤2.0) 掳. Using Aerolizer? The fine particle fraction was (36.2 卤2.8). The pulmonary irritation test showed that the powder had no obvious pulmonary irritation. The lung tissue distribution test showed that the content of oseltamivir carboxylic acid in lung of rats after pulmonary administration of micropowder was higher than that in the same dose group. The results suggest that the 1 micropowder inhaled in this study may play a better role in the treatment of respiratory tract virus infection than oral administration.
【作者单位】：徐州医科大学江苏省新药研究与临床药学重点实验室;中国药科大学药学院;
【分类号】：R943;R96

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