色谱

色谱

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药物间置换相互作用的毛细管电泳-迎头分析法研究

周大炜1,2,王怀锋1,李发美2   

  1. 1. College of Pharmaceuticals &Biotechnology, Tianjin University, Tianjin 300072, China; 2. Pharmaceutical College, Shenyang Pharmaceutical University, Shenyang 110016, China
  • 收稿日期:2004-03-09 修回日期:1900-01-01 出版日期:2005-03-30 发布日期:1988-12-25
  • 通讯作者: 周大炜
  • 基金资助:

Study on Drug Displacement Interactions by Capillary Electrophoresis-Frontal Analysis

ZHOU Dawei1,2, WANG Huaifeng1, LI Famei2   

  1. 1. College of Pharmaceuticals &Biotechnology, Tianjin University, Tianjin 300072, China; 2. Pharmaceutical College, Shenyang Pharmaceutical University, Shenyang 110016, China
  • Received:2004-03-09 Revised:1900-01-01 Online:2005-03-30 Published:1988-12-25

PDF

703

被引次数

6

摘要： 将18-甲基炔诺酮加到人血清白蛋白-酮洛芬平衡溶液中,室温孵育达平衡后应用毛细管电泳-迎头分析法研究了18-甲基炔诺酮和酮洛芬在人血清白蛋白分子上的置换相互作用。一大体积样品虹吸进样至未涂层毛细管(65 cm×50 μm i.d.,有效长度35 cm),进样时间80 s,毛细管两端高度差11 cm,工作电压10 kV,运行缓冲液为67 mmol/L磷酸盐缓冲液(pH 7.4),游离酮洛芬浓度由前沿峰的高度直接测定。当酮洛芬样品溶液中酮洛芬的总浓度分别为100 μmol/L和200 μmol/L时,随着18-甲基炔诺酮加入量的增加(18-甲基炔诺酮的浓度由0增至200 μmol/L),游离酮洛芬的浓度分别从22.4 增至26.4 μmol/L和从82.1增至106.2 μmol/L。由上面的结果可推论:高浓度的18-甲基炔诺酮可将酮洛芬从它的第二类结合位点上置换出来。

关键词: 毛细管电泳-迎头分析, 人血清白蛋白, 置换相互作用

Abstract: The interaction between 18-methyl norethindrone and ketoprofen including the displacement of ketoprofen from human serum albumin binding sites was investigated by capillary electrophoresis-frontal analysis method (CE-FA) at room temperature. A very large sample plug was introduced hydrostatically into the capillary (65 cm×50 μm i.d., effective length of 35 cm) over 80 s at a height difference of 11 cm. The working conditions for CE-FA separation are as follows: operating voltage, 10 kV; running buffer, 67 mmol/L phosphate, pH 7.4. The unbound ketoprofen concentration was directly measured from the height of the frontal peak. When the concentration of 18-methyl norethindrone was increased from 0 to 200 μmol/L, the unbound ketoprofen concentration was found to increase from 22.4 to 26.4 μmol/L at 100μmol/L total ketoprofen concentration and from 82.1 to 106.2 μmol/L at 200 μmol/L total ketoprofen concentration. From these data, it may be deduced that the administration of high concentration of 18-methyl norethindrone could displace ketoprofen from its secondary binding site.

Key words: displacement interaction , human serum albumin, capillary electrophoresis-frontal analysis