PLGA/PLA组合及微球混合对罗替戈汀微球体外释药特性的影响  

Influences of PLGA /PLA and microsphere blends on the release of rotigotine from the microspheres

作　　者：张静伟[1,2] 王爱萍[1,2] 李佩[1] 梁荣才[1] 刘万卉[1] 孙考祥[1] 

机构地区：[1]烟台大学药学院,烟台264005 [2]山东绿叶制药有限公司长效和靶向制剂国家重点实验室,烟台264003

出　　处：《中国新药杂志》2014年第4期465-469,共5页Chinese Journal of New Drugs

基　　金：国家重大基础研究计划(973)项目(2012CB724003);烟台大学基金(YX12B13和YX11Z1)

摘　　要：目的:考察PLGA/PLA及不同PLGA型号(末端基不同)组合和微球混合对罗替戈汀微球释药特性的影响。方法:采用乳化-溶剂挥发法制备罗替戈汀微球,对其载药量、粒径及体外释放等进行评价,并通过数学模型对体外释药曲线进行拟合。结果:PLGA/PLA组合制备的罗替戈汀微球释药与PLGA微球释药相似,均符合Logistic模型,与其组合比例无关;而PLGA微球/PLA微球混合后释药特性与混合比例相关。不同比例A/E型PLGA组合制备微球与不同比例A型PLGA微球/E型PLGA微球混合释药曲线变化趋势一致,与其混合比例相关,占优势比例的PLGA决定了其释药特性。结论:不同的高分子组合制备微球或不同高分子微球混合对微球释药特性有不同影响。Objective： To determine the effects of different types of poly （D, L-lactide-co-glycolide, PL- GA） with polylactide （PLA） and microsphere blending on the release of rotigotine loaded microsphere （RM）. Methods： RMs were prepared by an oil-in-water emulsion solvent evaporation technique and characterized for their drug load, size distribution and in vitro drug release. The release profiles were evaluated with different release kinetic equations. Results ： The release profiles of RMs prepared by PLGA/PLA combination were similar with PLGA microsphere, and did not relate to the ratio, which met the logistic equation. However, the drug-release profiles of PLGA and PLA microsphere blending depended on the ratio. The drug-release profiles of RMs prepared by PLGA （ carboxylic acid-terminated, A-type PLGA）/ester-capped PLGA （ E-type PLGA） combination were similar with A- type and E-type PLGA microsphere blending, which was relevant with the blending ratio. Conclusion： The feasible blending of polymers or microspheres with varied characteristics can modify drug release.

关 键 词：PLGA PLA 组合 微球混合 罗替戈汀 体外释放特性 

分 类 号：R943.41[医药卫生—药剂学] R971[医药卫生—药学]