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硫酸长春新碱靶向缓释制剂的血浆蛋白结合率测定
引用本文:周辉年,陈刚,刘涛,何雯婷,李榆,任志俭,李玉民.硫酸长春新碱靶向缓释制剂的血浆蛋白结合率测定[J].中国医院药学杂志,2011(7).
作者姓名:周辉年  陈刚  刘涛  何雯婷  李榆  任志俭  李玉民
作者单位:兰州大学第二医院;兰州大学第二临床医学院;甘肃省消化系肿瘤重点实验室;
摘    要:目的:测定硫酸长春新碱靶向缓释制剂的血浆蛋白结合率,为该缓释制剂的药效学和临床研究提供相关参数。方法:采用平衡透析法测定硫酸长春新碱缓释制剂在Wistar大鼠血浆中的蛋白结合率,利用液-液萃取法提取药物,高效液相色谱法测定药物浓度。结果:硫酸长春新碱靶向缓释制剂在120h时达到最好平衡点,质量浓度为2.50,5.00,10.00,20.00,40.00和80.00mg.L-1的缓释制剂,血浆蛋白结合率分别为35.91%,40.01%,35.79%,32.55%,39.24%和41.34%。结论:硫酸长春新碱靶向缓释制剂中的高分子材料降解缓慢,故内部包裹药物可长期释放,同时,由于该制剂吸附和包裹药物的释放速率不同,导致血浆蛋白结合率在初期具有较大的波动性,但随着时间的延长,血浆蛋白结合率仍可达到稳定水平。

关 键 词:聚乳酸乙醇酸共聚物  硫酸长春新碱  血浆蛋白结合率  平衡透析法  

Determination of plasma protein binding rate of PLGA-VCR
ZHOU Hui-nian,CHEN Gang,LIU Tao,HE Wen-ting,LI Yu,REN Zhi-jian,LI Yu-min.Determination of plasma protein binding rate of PLGA-VCR[J].Chinese Journal of Hospital Pharmacy,2011(7).
Authors:ZHOU Hui-nian  CHEN Gang  LIU Tao  HE Wen-ting  LI Yu  REN Zhi-jian  LI Yu-min
Institution:ZHOU Hui-nian3,CHEN Gang3,LIU Tao2,HE Wen-ting2,LI Yu3,REN Zhi-jian3,LI Yu-min1,2(1.The Second Hospital of Lanzhou University,Gansu Lanzhou 730000,China,2.Key Laboratory of Digestive System Tumors,Gansu Province,3.School of Second Clinical Medical,Lanzhou University,China)
Abstract:OBJECTIVE To study the protein binding rate of PLGA-VCR in plasma of rats,and provide parameters for the study of PLGA-VCR in pharmacodynamics and clinical research.METHODS The protein binding rate of PLGA-VCR in plasma of Wistar rats was detected by equilibrium dialysis,purification of drugs was performed with liquid-liquid extraction,and determination of drugs concentration with high performance liquid chromatography.RESULTS The concentration of PLGA-VCR in both sides of dialysis bags reached the best bal...
Keywords:polylactic acid-polyglycolic acid copolymer  vincristine sulfate  plasma protein binding rate  equilibrium dialysis  
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