氟维司群PLA-block-mPEG微球在大鼠体内的药动学研究  

Pharmacokinetics of PLA-block-mPEG Copolymer Microspheres Containing Fulvestrant in Rats

作　　者：王九成[1] 刘继三[1] 梁丹[1] 梁国正[1] 

机构地区：[1]西北工业大学理学院应用化学系,陕西西安710072

出　　处：《中国医药工业杂志》2009年第11期833-836,共4页Chinese Journal of Pharmaceuticals

摘　　要：分别以嵌段共聚物(聚乳酸-单甲氧基聚乙二醇,分子量比为40000∶2000)和非嵌段共聚物(聚乳酸-聚羟乙酸,分子量均为40000,摩尔比分别为75∶25、50∶50)作为载体材料,采用乳化-液中干燥法制备包载氟维司群的微球。大鼠单剂量(50mg/kg)皮下注射3种氟维司群微球,采用LC-MS/MS法测定血药浓度,计算药动学参数。结果表明,使用嵌段共聚物制备的微球,药-时曲线较平稳,释放效果较好。Fulvestrant microspheres entrapped by PLA-block-mPEG copolymer （molecular weight ratio 40 000 ： 2 000） and two kind of PLGA （molecule weight 40 000, molar ratio 75 ： 25 and 50 ：50） were prepared with emulsion in liquid drying method. Three kinds of fulvestrant microspheres were given subcutaneously to rats respectively, with single dosage of 50 mg/kg. The drug concentrations were determined by LC-MS/MS. The results showed that the fulvestrant microsphere prepared by PLA-block-mPEG copolymer had a smooth concentration-time chart. The releasing effect of the PLA-block-mPEG microsphere was better than that prepared by two kind of PLGA.

关 键 词：氟维司群 嵌段共聚物 微球 皮下注射 释放性质 药代动力学 

分 类 号：R969[医药卫生—药理学]