载体颗粒表面修饰对其表面能及粉雾剂性能的影响

目的研究载体的表面修饰对粉雾剂性能的影响。方法用不同的润滑剂对乳糖颗粒进行了表面修饰,并利用反向气相法测定了乳糖修饰前后的表面能,考察了表面能对干扰素α-2b粉雾剂沉积性能的影响。结果表面修饰后乳糖颗粒的流动性、表面光滑度都得到较大程度的改善,表面能也相应降低,而粉雾剂的性能得以提高。结论利用反向气相色谱法测定载体的表面能来预测粉雾剂的性能,可以为粉雾剂的处方设计和筛选提供一种快速有力的工具。

Effect of surface modification on surface energy of lactose and performance of dry powder inhalations

AIM: To investigate the effects of surface modification of lactose carrier on performance of dry powder inhalations (DPIs). METHODS: Modified lactose surface was prepared using a "particle smoothing" process to obtain smooth carrier surface and low surface energy with the presence of magnesium stearate, colloidal silica dioxide and talc. Inverse gas chromatography (IGC) was used to assess the surface energy of treated lactose, and the in vitro deposition of carrier-based IFNa-2b DPIs was evaluated with twin stage impinger. RESULTS: The flowing property of lactose was greatly improved and the surface energy decreased by the "particle smoothing" process. Decreasing surface energy resulted in greater aspiration fraction of IFNa-2b. CONCLUSION: IGC is a potentially useful tool for rapid formulation design and screening.