快速膜乳化法制备胸腺法新长效缓释微球  

Preparation of Thymalfasin Loaded PLGA Microspheres by Premix Membrane Emulsification as Long-term Effective Formulation

作　　者：杨柳青[1,2] 王丽秋[1] 吴颉[2] 齐峰[2] 任玉[2] 陶安进 马亚平 马光辉[2] 

机构地区：[1]燕山大学环境与化学工程学院,河北秦皇岛066004 [2]中国科学院过程工程研究所生化工程国家重点实验室,北京100190 [3]深圳翰宇药业股份有限公司,广东深圳518057

出　　处：《过程工程学报》2014年第6期994-999,共6页The Chinese Journal of Process Engineering

基　　金：广东省中国科学院全面战略合作项目(编号:2011B090300012)

摘　　要：采用快速膜乳化技术结合溶剂蒸发法制备以生物可降解聚乳酸-羟基乙酸(PLGA)为载体的胸腺法新载药微球,考察了PLGA分子量、油相中PLGA和乳化剂浓度、外水相p H值和内水相体积等对微球包埋率和粒径的影响.结果表明,制备粒径均一的PLGA载药微球的优化条件为:PLGA分子量51 k Da,油相中PLGA和乳化剂浓度为100和10 g/L,内水相体积0.5 m L,外水相p H值为3.5.该条件下所制载药微球粒径均一性好(Span<0.7),药物包埋率高达80%以上,突释率24 h内低于20%,线性持续稳定释药时间长达30 d.Thymalfasin-loaded biodegradable poly（lactic-co-glycolic acid）（PLGA） microspheres were prepared by premix membrane emulsification technique combined with solvent evaporation method.The effects of concentrations of PLGA and Arlacel 83 in oil phase,p H value of external water phase and internal water volume on the drug encapsulation efficiency and size distribution of microcapsules were examined.The results showed that the optimized preparation conditions of thymalfasin loaded PLGA microspheres were molecular weight of PLGA 51 k Da,concentrations of PLGA and Arlacel 83 in oil phase 100 and 10 g/L,inner water volume 0.5 mL,and p H value of outer water phase 3.5.The microspheres prepared under the optimal conditions had narrow size distribution（Span〈0.7）,high drug encapsulation efficiency（above 80%）,low initial burst release（below 20% in initial 24 h） and constant release rate during 30 d.

关 键 词：胸腺法新 聚乳酸-羟基乙酸 微球 快速膜乳化 长效缓释 

分 类 号：R944.5[医药卫生—药剂学]