局部用雷帕霉素聚乳酸乙醇酸共聚物缓释微球的制备及释药研究(1)
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[摘要]目的:介绍雷帕霉素(RAPA)聚乳酸乙醇酸共聚物(PLGA)缓释微球的制备方法,建立高效液相色谱法(HPLC)测定体系以检测微球中雷帕霉素含量,检测微球性状并进行体外释药实验。方法:以聚乳酸乙醇酸共聚物为载体,采用W/O/W 乳剂-扩散溶剂挥发法制备雷帕霉素缓释微球,扫描电镜检测微球外观及微球粒径,HPLC检测微球载药量、包封率及体外释药量。结果:所制微球光滑圆整,大小均一,平均粒径:(121.18±27.83)μm,载药率:(14.39 ± 1.32)%,包封率:(72.92±4.29)%,体外释放实验显示1～4天有突释,随后平稳释药至第10天累积释药率达80%。结论:采用制备工艺稳定,所制微球载药量及包封率均较高,形态完整,大小均一,体外释药较为平稳并且具有明显的缓释作用。
[关键词]雷帕霉素;缓释;微球;PLGA
[中图分类号]Q813.1[文献标识码]A[文章编号]1008-6455(2010)03-0334-04
Preparation and in vitro release study of rapamycin in poly(lactic-co-glycolic )acid microsphere for topical administration
PEI Jiao-miao,XUE Xiao-yan,LIU Bei,XIA Wei,LUO Xiao-xing,GUO Shu-zhong
(Institute of Plastic Surgery of People's Liberation Army,Xijing Hospitol,the Fourth Military Medical University,Xi'an 710032,Shaanxi,China)
Abstract:ObjectiveTo optimize the preparation technology of poly (lactide - co - glycolide) (PLGA) microspheres loaded with rapamycin (RAPA-PLGA-MS), establish a HPLC method for content determination of rapamycin in microspheres and study powder particle characteristics and in vitro release characteristics of RAPA-PLGA-MS ......
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