辛伐他汀聚乳酸微球的体外加速释放研究  

Accelerated release of simvastatin polylactic acid microspheres in vitro

作　　者：吴珍珍[1] 杨卓理[1] 李馨儒[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》2006年第7期525-528,共4页Chinese Journal of New Drugs

摘　　要：目的:考察聚乳酸微球体外长期释放和加速释放的相关性,建立辛伐他汀聚乳酸微球的体外加速释放方法。方法:用紫外分光光度法测定微球中辛伐他汀的含量。采用改良的摇瓶培养法分别在不同温度的介质中进行体外加速释放试验和长期释放试验。用点点相关法考察两者的相关性。结果:PLA10000和PLA20000制备的微球在37℃放置30 d内的释放分别达到92．68％和84．07％,微球在44℃,48℃和50℃下的释放均明显加速,释放动力学分别符合一级释药方程及Higuchi方程。辛伐他汀聚乳酸微球在48℃条件下的加速释放与在37℃的长期释放有良好的相关性。结论:辛伐他汀聚乳酸微球具有很好的缓释能力,采用体外加速试验的方法可以快速考察辛伐他汀聚乳酸微球的体外释药行为。Objective： To evaluate the correlation of in vitro accelerated release with the long-term release of polylactic acid （PLA） microspheres and establish a method to test the accelerated release in vitro of simvastatin PLA microspheres. Methods：The simvastatin concentration in the PLA microspheres was determined by a UV spectroscopy. The release of simvastatin from the PLA microspheres in PBS medium was monitored at different temperature using a modified incubation method. The accumulative release percentage of the long-term release was compared with the accumulative release percentage of the accelerated release at certain time points. Results：The accumulative release percentage of simvastatin microspheres prepared with PLA10000 and PLA20000 was 92.68% vs. 84.07% at 37 % within 30 days. The release in vitro of simvastatin PLA microspheres at 44 ℃, 48℃ and 50 ℃ was significantly accelerated. The release behavior obeyed both the first-order kinetics equation and Higuchi equation. The accelerated release at 48 % was correlated with the long-term release at 37 % well. Conclusion： Simvastatin PLA microspheres featured the sustained release. The accelerated release test in vitro is applied to predict the long-term release behavior of simvastatin PLA microspheres.

关 键 词：辛伐他汀 聚乳酸微球 加速释放 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]