前列地尔脂质体的制备及刺激性考察

Preparation of alprostadil liposomes and its test of irritation

目的 :制备前列地尔脂质体以减少其静脉注射的刺激性。方法 :采用逆相蒸发法制备前列地尔脂质体 ,用超滤膜测定脂质体的包封率及其释放、马尔文粒径仪测定平均粒径 ;并通过动物实验比较静脉注射的刺激性。结果 :前列地尔脂质体的包封率可达到 94 % ,超声后和高压匀质后的粒径为(732±s 35 )nm和 (6 7± 7)nm ,刺激性得到显著改善。结论 :前列地尔脂质体可以显著降低静脉注射引起的刺激性。

AIM: To prepare alprostadil liposomes for decreasing the irritation by iv. METHODS: Alprostadil liposomes were prepared by the reverse evaporating method. The entrapment efficiency and particle size were determined by the Zatasizer 3000HSA. The irritation of alprostadil liposomes was compared with alprostadil injections by animal experiment. RESULTS: The entrapment efficiency and particle size after ultrasonic and high pressure homogenization of the alprostadil liposomes were 94 % and (732± s 35) nm,(67±7) nm;the irritation of liposomes was significantly improved. CONCLUSION: Alprostadil liposomes can significantly decrease the irritation by iv.