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银杏内酯B在血浆中的蛋白结合率研究
引用本文:陈卫东,梁艳,谢林,王雷,吴勇,汪电雷,刘晓东.银杏内酯B在血浆中的蛋白结合率研究[J].安徽医药,2012,16(2):154-157.
作者姓名:陈卫东  梁艳  谢林  王雷  吴勇  汪电雷  刘晓东
作者单位:安徽中医学院药学院药物代谢动力学研究室,安徽,合肥,230031;安徽省中药制剂工程技术研究中心;安徽省中药研究与开发重点实验室,安徽,合肥,230022;中国药科大学药物代谢动力学重点实验室,江苏,南京,210038;安徽省马鞍山市药品检验所,安徽,马鞍山,243000
基金项目:2010年安徽省科技厅科技计划项目
摘    要:目的测定银杏内酯B(ginkgolide B,GB)与大鼠和人的血浆蛋白结合率。方法将血浆样品加入内标23-羟基白桦酸,乙醚液液萃取后,高效液相色谱-质谱联用仪分析,采用平衡透析法测定GB在大鼠及人血浆中的血浆蛋白结合率。结果人和大鼠血浆中GB药物浓度在0.05~5.00 mg.L-1范围内血浆蛋白结合呈线性关系;GB与大鼠血浆蛋白结合率约为25%,与人血浆蛋白结合率约为20%。结论 GB的血浆蛋白结合率较低,在人血浆的蛋白结合率略低于大鼠,但不存在显著性差异;约80%的药物以游离态形式存在。

关 键 词:银杏内酯B  血浆蛋白结合率  平衡透析法

Protein binding ratio of Ginkgolide B in plasma
Institution:CHEN Wei-dong,LIANG Yan,XIE Lin,et al(1.Pharmacokinetic Laboratory in College of Pharmacy,Anhui University of Traditional Chinese Medicine,Hefei,Anhui 230031,China; 2.Anhui Province Engineering Research Center of Preparations,Hefei,Anhui 230022,China;3.Anhui Province Key Laboratory of R&D of Chinese Medicine,Hefei,Anhui 230022,China;4.Key Lab of Drug Metabolism and Pharmacokinetics,China Pharmaceutical University,Nanjing,Jiangsu 210038)
Abstract:Objective To determine protein binding ratio of ginkgolide B in rat and human plasma.Methods The plasma samples which were added with internal standard(IS,23-OH Betula Alba Acid) were extracted by aether and the extraction was assayed by high performance liquid chromatography-mass spectrometry detector.The equilibrium dialysis was carried out to determine the protein binding rate of ginkgolide B in rat and human plasma.Results The binding rates of GB to rat and human plasma protein were found to be about 25% and 20%,respectively,varying with the concentration of GB from 0.05 to 5.0 mg·L-1.Conclusion The plasma protein binding rate of ginkgolide B was low and the binding rate to rat plasma was a bit higher than that to human plasma,but the difference was negligible(P0.05).About 80% of the drugs exists in the free form.
Keywords:Ginkgolide B  plasma protein binding ratio  equilibrium dialysis
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