目的研究喷雾冷冻干燥法制备可吸入的蛋白颗粒。方法以干扰素α-2b为模型药、以甘露醇或乳糖为主要赋形剂,考察了喷雾冷冻干燥产品的粒径、形态、密度和吸湿性等粉体学性质,并测定了干扰素粉雾剂的体外沉积。结果喷雾冷冻干燥法制得的产品密度很小,有的敲击密度仅为0.016g·cm^-3;产品颗粒形态也为多孔性结构。样品的体外沉积较高,有的高达38.5%。结论喷雾冷冻干燥法可以制备超低密度的适于吸入给药的蛋白粉末。

OBJECTIVE To prepare protein loaded particles for administration via pulmonary delivery by spray freeze drying.METHODS Interferon α-2b was chosen as a model protein,and mannitol or lactose was used as main excipients.The particle size,morphology,density and hygroscopicity of obtained products were evaluated.And the deposition of interferon DPIs in vitro was determined using a twin stage impinger.RESULTS Spray freeze drying produced large porous particles with ultra low tap density(0.016 g·cm^-3) which possessed high in vitro deposition(up to 38.5%).CONCLUSION Spray freeze drying produce protein particles with ultra low density suitable for inhalation.