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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
引用本文:裴蛟淼,薛小燕,刘蓓,夏炜,罗晓星,郭树忠. 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[J]. 中国美容医学, 2010, 19(3): 334-337
作者姓名:裴蛟淼  薛小燕  刘蓓  夏炜  罗晓星  郭树忠
作者单位:1. 西京医院全军整形外科研究所
2. 药学系药理学教研室,陕西,西安,710032
基金项目:国家自然科学基金资助项目(编号:30830102),项目名称:局部基因诱导免疫耐受与局部用药防止异体复合组织移植急慢性排斥反应机制与应用研究
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

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. Preparation and in vitro release study of rapamycin in poly(lactic-co-glycolic)acid microsphere for topical administration[J]. Chinese Journal of Aesthetic Medicine, 2010, 19(3): 334-337
Authors:PEI Jiao-miao  XUE Xiao-yan  LIU Bei  XIA Wei  LUO Xiao-xing  GUO Shu-zhong
Affiliation:Institute of Plastic Surgery of People's Liberation Army/a>;Xijing Hospitol/a>;the Fourth Military Medical University/a>;Xi'an 710032/a>;Shaanxi/a>;China
Abstract:Objective To 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. Methods RAPA-PLGA-MS was prepared with PLGA as carriers by the water-in-oil-in-water (W/O/W) emulsion solvent evaporation method. Scanning electron miroscope (SEM) and HPLC were used to evaluate the ...
Keywords:rapamycin  controlled release  microspheres  PLGA  
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