摘要
目的制备胰岛素自复乳化给药系统并评价其质量。方法以自复乳的微观结构、体积平均粒径和自乳化速率为评价指标筛选较优处方,并考察其稳定性及体外释放特性。结果优选的处方组成为内水相-中链甘油三酸酯-亲脂乳化剂-亲水乳化剂(21∶24∶6∶9),平均粒径为6.74±0.55μm,包裹进入复乳的胰岛素为86.8%±8.2%;于25℃静置30 d后,其显微形态及平均粒径等指标均未见明显变化;8 h后胰岛素在体外的累计释放量达约80%,具一定缓释作用。结论成功制备了胰岛素自复乳化给药系统,可为蛋白多肽类药物的口服给药提供新的方法。
OBJECTIVE To prepare and evaluate insulin - loaded self - double - emulsifying drug delivery systems （SDEDDS）. METHODS The best formulation was optimized according to the microstructure, volume weighted mean droplet size, and self - emul- sifying rate of W/O/W transformed from SDEDDS. Meanwhile, the stability and release in vitro were assessed. RESULTS The best formulation was inner water phase - medium chain triglycerides - Abil EM90 - Labrasol with the weight ratio of 21 ： 24 ： 6 ： 9. The average oil globule size was 6.74 ±0.55 μm with 86.8% ± 8.2% insulin encapsulated in the formulation. There were no changes in the microscopic morphology and average oil globule size when it was stored at room temperature for 30 d. The cumulative release amount of insulin within 8 h in vitro was about 80%, exhibiting a certain sustained release effect. CONCLUSION We successfully prepared insulin -loaded SDEDDS,which may be a promising strategy for the orally administered peptide and protein drugs.
出处
《华西药学杂志》
CAS
CSCD
2016年第5期456-458,共3页
West China Journal of Pharmaceutical Sciences
关键词
自复乳化给药系统
乳化剂
油相
胰岛素
稳定性
体外释放:蛋白多肽
口服给药
Self - double - emulsifying drug delivery systems （SDEDDS）
Emulsifier
0il phase
Insulin
Stability
Release in vitro
Peptides and proteins
Oral administration
