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药学学报  2015 

蛋白及多肽药物干粉吸入剂研究新进展

, PP. 814-823

Keywords: 蛋白质及多肽类药物,干粉吸入剂,载体,肺部沉积率

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Abstract:

为成功设计蛋白及多肽类药物物理混合型干粉吸入剂提供理论和实践依据,本文综述和阐明了干粉吸入剂常用载体,药物微粉化制备技术,影响干粉吸入剂肺部沉积的处方工艺因素,包括载体性质、药物载体比例、混合顺序、混合方法和混合时间、药物载体相互作用,以及粉体学性质包括粒径大小和形态、密度、粉体流动性、带电性、分散性、吸湿性对肺部沉积率的影响。依据上述讨论和粉末分散的机制,提出了增加干粉吸入剂肺部沉积率的策略,包括加入载体细粉、加入黏附力控制物质和对药物微粉再加工等。因此,设计肺部沉积率高的蛋白及多肽药物的物理混合型干粉吸入剂需系统地研究药物与载体相互作用,阐明处方工艺及粉体学性质的影响。

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