辛伐他汀聚乳酸微球的制备及药剂学性质  

Preparation and characteristics of simvastatin polylactic acid microspheres

作　　者：吴珍珍[1] 李馨儒[1] 胡应生[1] 杨卓理[1] 刘艳[1] 

机构地区：[1]北京大学药学院药剂学系,北京100083

出　　处：《中国新药杂志》2005年第11期1312-1315,共4页Chinese Journal of New Drugs

摘　　要：目的:制备辛伐他汀聚乳酸微球,并考察其药剂学性质。方法:采用乳化挥发法制备辛伐他汀聚乳酸微球,用光学显微镜考察微球的粒径,用扫描电镜观察微球的形状和表面形态,用差示扫描量热法(DSC)和红外光谱法研究药物在载体中的分散状态及相互作用。结果:辛伐他汀聚乳酸微球的算术平均粒径为(42.1±2.3)μm(n=500),载药量为(22.4±0.3)%(n=3),药物包封率为(80.7±0.6)%(n=3)。37℃时2种相对分子质量的聚乳酸(10 000和20 000)制备的微球体外累积释药量分别为92.68%和84.07%,释药动力学符合Higuchi方程。结论:辛伐他汀聚乳酸微球具有很好的缓控释能力。Objective： To characterize the simvastatin polylactic acid microspheres newly prepared. Methods：Simvastain polylactic acid microspheres were prepared by emulsifying solvent-evaporation process. The particle size and shape were examined by optical microscope;the morphology was observed by scanning electron microscope; the dispersion status of simvastatin and interactions between simavastatin and carriers were studied using DSC and IR. Results： The pharmaceutical properties of the simvastatin polylactic acid microspheres were as follows ： mean diameter of （42.1± 2.3）μm （ n = 500） , load efficiency of （22.4±0.3）%（n = 3）, encapsulation rate ot （80.7±0.6）% （u = 3）, in vitro accumulative release rate of 92.68% and 84.07% in 30 days, respectively, for the microspheres made of two polylactic acids with molecular weight of 10 000 and 20 000 at 37℃ . The in vitro simvastatin release from the microspheres was best described using Higuchi diffusion model. Conclusion：Simvastatin polylactic acid microspheres exhibited better controlled-release capacity.

关 键 词：辛戊他汀 聚乳酸微球 乳化挥发法 体外累积释药量 

分 类 号：R944.9[医药卫生—药剂学] R972.6[医药卫生—药学]