正交试验优化5-氟尿嘧啶纳米粒的制备  

Optimization of orthogonal experiment for preparation of 5-fluorouracil nanoparticles

作　　者：仵文英[1] 赵暖暖[2] 代志军[1] 李兴华[1] 王娜[1] 

机构地区：[1]西安交通大学医学院第二附属医院药剂科,陕西西安710004 [2]西安交通大学医学院药学系,陕西西安710061

出　　处：《中国医院药学杂志》2014年第18期1554-1557,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:以包封率为指标优化5-氟尿嘧啶纳米粒的制备工艺。方法:以mPEG-PCL及PCL为载体,泊洛沙姆188为表面活性剂,采用复乳化/溶剂挥发法制备纳米粒。通过正交设计优化处方工艺,葡聚糖凝胶法分离游离药物,HPLC法测定纳米粒中5-氟尿嘧啶的包封率,并考察其体外释放度。结果:最佳工艺为:载体组成为mPEG-PCL与PCL的质量比1∶3,水浴温度为35℃,药载比为1∶5,表面活性剂质量体积百分比为2%,包封率均值为43.8%,24 h累积释放量为60%。结论:优化后的工艺可提高5-氟尿嘧啶包封率、增加纳米粒稳定性,体外药物释放具有良好的缓释效果。OBJECTIVE To study the preparation method of 5-fluorouracil nanoparticles and screen the optimal technological conditions by the encapsulation efficiencies.METHODS 5-fluorouracil nanoparticles were prepared by complex emulsion/solvent evaporation method with mPEG-PCL and PCL as the carrier,Poloxamer188 as surfactant.Then orthogonal design was adopted to screen the optimal conditions.Free drug was separated by Sephadex gel and the encapsulation efficiency of 5-fluorouracil was determined by HPLC.RESULTS The optimum conditions of 5-FU nanoparticles were as follows：the mass ratio of mPEG-PCL and PCL was 1∶3,temperature of water phase was 35℃,the ratio of 5-FU and carrier was 1∶5,the surfactant concentration was 2%.And the entrapment efficiency was 43.8%.In the release in vitro,the cumulative released drug from nanoparticles was 60%in 24 h.CONCLUSION The entrapment efficiency of 5-FU nanoparticles could be improved with the optimized condition.And it possesses good sustained release characteristics in vitro.

关 键 词：5-氟尿嘧啶 纳米粒 乳化/溶剂挥发法 包封率 

分 类 号：R943[医药卫生—药剂学]