表柔比星长循环脂质体冻干粉的制备  

Preparation of Lyophilized Epirubicin Long Circulation Liposome Powder

作　　者：周晖[1] 贺霞[2] 杨文涛[2] 姜伟化[2] 杨磊[2] 王东凯[2] 

机构地区：[1]中国医科大学附属第一医院药剂科,沈阳110001 [2]沈阳药科大学药学院,沈阳110016

出　　处：《医药导报》2014年第7期917-921,共5页Herald of Medicine

基　　金：沈阳市科学技术计划项目资助项目(F13-316-1-25)

摘　　要：目的对表柔比星长循环脂质体进行冷冻干燥以提高制剂稳定性,并对所得的冻干制剂进行初步质量评价。方法考察冻干保护剂种类、预冻时间及总干燥时间对制剂的影响;并考察表柔比星长循环脂质体冻干粉在温度为(25±2)℃、相对湿度(60±10)%条件下放置3个月的稳定性。结果以海藻糖为保护剂,保护剂与脂质体的比例为3∶1。预冻温度-70℃,预冻时间8 h,冷冻干燥时间24 h。表柔比星长循环脂质体冻干后粒径、包封率、含量基本不变;加速条件下放置3个月,冻干制剂的再分散性好,包封率>94%,含量>99%。结论将表柔比星长循环脂质体进行冷冻干燥,可以有效提高制剂的稳定性。Objective To improve the stability of epirubicin long circulation liposomes via lyophilizing technology and preliminarily evaluate their quality. Methods The effect of the various cryoprotectant,different pre-freezing and total drying time on the preparation was analyzed. The stability of the lyophilized powder was tested at （25±2） ℃ and （60±10）% relative humidity for 3 months. Results The protective agent trehalose to liposomes was 31. The freeze-drying was conducted with pre-freezing temperature at -70 ℃,precooling for 8 h and total drying for 24 h. There were no significant differences in particle size,encapsulation efficiency and drug content of lyophilized long-circulating liposomes compared with those un-lyophilized. After 3 months under the accelerated condition,it had good redispersibility, entrapment rate （〉94%） and drug content （〉99%） . Conclusion Lyophilizing the long-circulation epirubicin liposomes can effectively improve the stability of the preparation.

关 键 词：表柔比星 长循环脂质体 冷冻干燥 稳定性 

分 类 号：R979.1[医药卫生—药品] TQ460.1[医药卫生—药学]