丙氨瑞林微球制备工艺优化和体外释放研究  

Optimization of preparation technology of alarelin microspheres and exploration of its in vitro release characteristics

作　　者：张敏[1] 高静[2] 孙李平[3] 武鑫[1] 叶丽华[1] 高申[1] 

机构地区：[1]第二军医大学长海医院药学部,上海200433 [2]第二军医大学药学院药剂学教研室,上海200433 [3]成都军区司令部直工部,成都610000

出　　处：《药学服务与研究》2012年第5期358-361,共4页Pharmaceutical Care and Research

基　　金：国家自然科学基金资助项目(No.81000689;81172514;30873178);上海市自然科学基金资助项目(No.10ZR1437300)

摘　　要：目的:制备包封率高、可持续释药35d的丙氨瑞林微球。方法:以生物可降解聚合物聚乳酸-聚羟基乙酸(PLGA)为载体,采用W/O/W复乳溶剂挥发法制备缓释丙氨瑞林微球,以包封率为观察指标,用正交设计L9(34)对微球制备工艺进行优化。在pH=7.0的磷酸盐缓冲溶液中考察微球的体外释放。结果:经优化工艺制备的丙氨瑞林微球包封率为(93.2±1.6)%,90%的微球粒径分布范围为55～65μm。在选择的释放条件下,至35d时,药物累积释放92.3%,突释为9.7%。结论:该制备工艺简单、稳定。优化条件下制备的丙氨瑞林微球包封率高、粒径适宜、突释少。Objective： To prepare alarelin microspheres with high encapsulation rate and sustained release for 35 days. Methods：Poly（laetic-co-glycolic acid）（PLGA） which could be biodegraded was used as a carrier. Alarelin microspheres were prepared with the W/O/W double emulsion solvent evaporation method, encapsulation rate was used as evaluating indicators. Then, the preparation was optimized with orthogonal test EL9 （34 ）]. In vitro release of alarelin microspheres was investigated in the phosphate buffer solution（pH 7.0）. Results： The encapsulation rate of alarelin microspheres was （93.2 ± 1.6）%. Almost 90% of the particle diameter of alare｜in microspheres was distributed in 55-65 um. Under the selected release conditions, the cumulative drug release was 92.3~ and the burst release was 9.7~ within 35 days. Conclusion： This preparation process is simple and stable. The alarelin microspheres prepared with this optimized method have high encapsulation rate, appropriate particle diameter and low burst release rate.

关 键 词：丙氨瑞林 微球 工艺学 制药 体外释放 复乳溶剂挥发法 

分 类 号：R944.9[医药卫生—药剂学]