应用多指标综合评价法优选胸腺五肽干粉吸入剂制备工艺  

Optimization of preparation process of thymopentin dry powder inhalation by multi-index evaluation

作　　者：王蕾[1] 唐星[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2009年第11期1057-1061,共5页Chinese Journal of New Drugs

摘　　要：目的:应用多指标综合评价法优选胸腺五肽干粉吸入剂的制备工艺。方法:采用正交试验设计,以喷雾干燥法制备胸腺五肽干粉吸入剂。以干粉吸入剂的收率、含水量、粉末空气动力径及体外沉积率作为考察指标,用Z分值法对各项指标进行综合评价,选出最佳制备工艺。结果:最佳工艺条件为雾化压力190 kPa、干燥风速0.7 m3.min-1、供液速度7.0 mL.min-1、入口温度110℃。按此工艺制得的3批干粉吸入剂平均收率为48.05%,含水量为0.44%,空气动力径为2.01μm,模拟肺部沉积率为47.45%。粒子形态为中空的近球形。3批样品室温放置6个月,外观、药物含量、粒径与体外沉积率均无明显变化。结论:正交试验结合多指标综合评价法用于优化胸腺五肽干粉吸入剂的制备工艺简单可行。Objective ：To optimize the preparation process of thymopentin （TP5） dry powder inhalation by multi-index evaluation. Methods：An orthogonal designed experiment was performed to prepare the spray-dried TP5 dry powders. The yield of the resultant powders, moisture contents, aerodynamic diameters and in vitro deposition were employed as evaluation indexes. The variable indexes were normalized by the method of Z-score to select the preferable process condition. Results：According to the Z-score results, the spray drying variables were optimized： atomizing pressure was 190 kPa;air flow was 0.7 m^3 · min^-1 ;feed flow rate was 7.0 mL· min ^-1 ;inlet temperature was 110 ℃. Under this condition,three batches of TP5 dry powder were prepared with the mean yield of 48.05% , moisture of 0.44% , aerodynamic diameters of 2.01 μm and in vitro deposition of 47.45%. The morphology of particles was hollow spherical. The powders showed good physical and chemical stability during a long-term storage of 6 months. Conclusion：Orthogonal design combined with multi-index evaluation proves to be available to optimize the preparation process for TP5 dry powder inhalation.

关 键 词：多指标综合评价法 胸腺五肽 干粉吸入剂 喷雾干燥 正交设计 

分 类 号：R943.4[医药卫生—药剂学]