喷雾冷冻干燥法制备供吸入的超轻干扰素粉末

Preparation of Ultra Low Density Interferon α-2b Powder for Inhalation by Spray Freeze Drying

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.