胰岛素吸入粉雾剂的制备及其体外沉积性质

Preparation and deposition properties of insulin dry powder inhalation

目的采用喷雾干燥法制备胰岛素吸入粉雾剂,并对其体外沉积性质做出评价。方法以产品收率,粉末的空气动力学径、休止角及水分含量为考察指标,采用正交设计Z综合评价法优化喷雾干燥制备方法中各工艺参数,同时采用双层液体碰撞器测定该工艺所制备的胰岛素吸入粉雾剂的有效部位沉积量,并通过扫描电镜观察产品的形态。结果优选出的工艺参数为:气流量为0.6 m3.min-1,进口温度为100℃,喷液速度为5.0 mL.min-1,泵压为130 kPa,溶液质量分数为0.75%。体外有效部位沉积质量高达60%。结论采用本法制备胰岛素肺部吸入粉雾剂重现性好,所得粉雾剂的有效部位沉积量高,提示大部分粒子能够到达肺部。

Objective To prepare insulin dry powders for inhalation by spray-drying method and investigate its deposition property in vitro.Methods The optimization of spray-drying method for the preparation parameters was performed by using orthogonal design and Z-score method which employed four indices including powder yield,aerodynamic diameter,angle of repose and moisture content.The in vitro deposition properties of the powders were assessed with a twin stage impinger.Results The optimized preparation parameters were obtained with a drying air flow rate of 0.6m^3·min^-1,an inlet temperature of 100℃,a liquid feed rate of 5.0 mL·min^-1,an atomizing air pressure of 130 kPa,and a solution concentration of 0.75%（W/W）.The in vitro deposition test showed that the respirable fraction was more than 60%.Conclusions Insulin dry powders for inhalation is successfully prepared by spray-drying method,and it can be predicted that most of the powders can get to the lung for its good deposition properties.