两性霉素B脂质干粉吸入剂处方筛选与粉体学性质评价

Determination of the Prescription and Evaluation of Characters for Amphotericin B Liposomes Dry Powder Inhalation

目的考察两性霉素B脂质体干粉的体外性质,筛选合适的载体并确定最佳粉雾剂配比。方法通过薄膜分散法制备两性霉素B脂质体,分别经冷冻干燥和喷雾干燥法获得两性霉素B脂质体干粉。比较两种类型脂质干粉的粒径,以体外有效部位沉积率为指标,筛选载体组成及比例,确定最佳处方配比。结果冷冻干燥得到的脂质干粉具有较大的粉末粒径,喷雾干燥脂质干粉粒径较小。经过筛选发现,使用Inhalac230乳糖(含20%第三组分)做载体与干粉比例为1:1时具有较高的有效部位沉积率即二级分布率。其中冷冻干燥脂质体的有效部位沉积率为11.95%,喷雾干燥脂质干粉为20.08%。结论采用喷雾干燥法可以得到粒径小的脂质体干粉颗粒,体外实验证明具有较高的有效部位沉积率。

Objective To investigate the in vitro characters of Amphotericin B liposomes dry powder, select a suitable carrier and determ the best formulation of inhalation powders. Methods Amphotericin B liposomes dry powder was dehydrated by freeze drying and spray drying method;the particle size of the two kinds of powders was compared by determining the deposition rate of active parts. Resets The particle size of the powder prepared by freeze drying was larger than that by spray drying. The higher deposition rate was found at-the ratio of dry powder to the lactose carrier as Inhalac230 being 1 ： 1, which were 11.95% for freeze drying particles and 20.08% for spray drying powder . Conclusion The particles of dry powder prepared by spray drying method is smaller, and the deposition rate of active part is higher than that of freeze drying powders.