蛋白及多肽药物干粉吸入剂研究新进展Recentprogressof-药学学报.PDF

814 药学学报 Acta Pharmaceutica Sinica 20 15, 50 (7): 814 823 白及多肽药物干粉吸入剂研究新进展 周洁雨, 张 兰, 毛世瑞* (沈阳药科大学药学院, 辽宁 沈阳 110016) 摘要: 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 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。 关键词: 蛋白质及多肽类药物; 干粉吸入剂; 载体; 肺部沉积率 中图分类号: R943 文献标识码: A 文章编号: 0513-4870 (20 15) 07-0814-10 Recent progress of dry powder inhalation of proteins and peptides * ZHOU Jie-yu, ZHANG Lan, MAO Shi-rui (School of Pharmacy, Shenyang Pharmaceutical University, Shenya ng 110016, China ) Abstract : To provide theoretical and practical basis for the successful formulation design of physically-mixed inhalation dry powder of proteins and peptides, related references were collected, analyzed and summarized. In this review drug micronization technology and commonly used carriers for inhalation dry powder preparation were introduced. For proteins and peptides, supercritical fluid technology and spray-drying are more suitable because of their capabilities of keeping drug activity. Being approved by U. S. Food and Dr