盐酸氨溴索干粉吸入剂理化性质及其初步稳定性考察

Study of Physicochemical Property and Stability of Ambroxol Hydrochloride Dry Powder Inhalations

目的:研究盐酸氨溴索干粉吸入剂的理化性质并考察其稳定性。方法:采用喷雾干燥法制备盐酸氨溴索干粉吸入剂;考察其吸湿性及临界相对湿度;观察其粒径分布、粉末形态;差示扫描量热(DSC)法分析吸入剂及其原料药和各辅料的特征峰;检测其排空率和沉积率;对制剂进行加速试验和长期试验以考察其稳定性。结果:所得干粉吸入剂的临界相对湿度约为64%,平均空气动力学径小于5μm,形态为粒径均匀的球形;DSC提示各样品特征峰未发生明显变化,即在喷雾干燥过程主药与辅料之间未发生相互作用;3批干粉吸入剂排空率均>90%,沉积率均>30%;稳定性试验中各指标在观察期内无明显变化。结论:所制盐酸氨溴索干粉吸入剂适合肺部吸入给药,且具有较好的稳定性。

OBJECTIVE： To study physicochemical property and stability of Ambroxol hydrochloride dry powder inhalations （AHDI）. METHODS： AHDI were prepared by spray-drying method. The humidity and critical relative moisture of inhalations were investigated. The particle size and powder morphology were also observed. The characteristic peak of inhalations, raw material and excipients were analyzed by DSC. The emptying rate and deposition rate of it were determined. The stability of it was determined by accelerated test and long-term test. RESULTS： The resultant powder inhalation exhibited the following properties： 64% critical relative humidity, d~, was 〈5 μm; DSC showed that there wasn＇t interaction between main component and excipients; emptying rate was 〉90%, and deposition rate was 〉30% for 3 patches; the accelerated test and the long-term test indicated that AHDI was stable. CONCLUSION： AHDI are stable and suitable for pulmonary delivery system.