酪丝亮肽多囊脂质体的制备和体外释放研究  

Preparation of tyroserlenutide multivesicular liposomes and drug release in vitro

作　　者：陶昱斐[1] 姚瑶[1] 丁燕飞[1] 陈若飞 肖灿[1] 

机构地区：[1]中南大学药学院,长沙410013 [2]深圳康哲药业股份有限公司,深圳518029

出　　处：《中国新药杂志》2008年第3期228-232,共5页Chinese Journal of New Drugs

摘　　要：目的：制备酪丝亮肽多囊脂质体,并考察其体外释药性能。方法：采用复乳法制备酪丝亮肽多囊脂质体,RP-HPLC法测定酪丝亮肽含量,以稳定性、包封率和体外释放为指标,正交试验设计法对酪丝亮肽多囊脂质体处方工艺进行优化。结果：酪丝亮肽多囊脂质体粒径均一,有80%的粒径分布在20-30μm,包封率达92.43%。酪丝亮肽多囊脂质体体外释放符合Korsmeyer-Peppas模型,37℃条件下在PBS介质中释药t1/2达111.5 h。结论：酪丝亮肽多囊脂质体稳定性好,包封率高,具有良好的缓释效果。Objective：To prepare tyroserlenutide sustained-release multivesicular liposomes and to study the drug release behavior invitro, nethods：Tyroserlenutide multivesicular liposomes was prepared by a two-step water-in-oil-in-water double emulsification process. RP-HPLC was used to determine the concentration of tyroserlenutide. The formulation and pharmaceutical process were optimized by orthogonal experimental design,with the factors of stability,encapsulation efficiency and invitro release behavior as the criteria. Results：The particle size of the optimized multivesicular liposomes was even and 80% of them was well-distributed in the range of 20 -30μm . The encapsulation efficiency was up to 92.43% and its drug-release profile in vitro was fitted to the model of Korsmeyer-Peppas with t1/2 up to 111.5 h in PBS buffer under 37℃. Conclusion：Tyroserlenutide multivesicular liposomes was prepared with good stability,high encapsulation efficiency and sustained-release character.

关 键 词：酪丝亮肽 多囊脂质体 缓释 

分 类 号：R943.41[医药卫生—药剂学] R979.1[医药卫生—药学]