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三唑仑的蛋白结合及其与α1酸性糖蛋白浓度的相关性。

Triazolam protein binding and correlation with alpha-1 acid glycoprotein concentration.

作者信息

Kroboth P D, Smith R B, Sorkin M I, Silver M R, Rault R, Garry M, Juhl R P

出版信息

Clin Pharmacol Ther. 1984 Sep;36(3):379-83. doi: 10.1038/clpt.1984.191.

Abstract

On two occasions separated by a minimum of 1 wk, plasma was obtained from 12 patients (aged 18 to 73 yr) on dialysis after an overnight fast. Samples were assayed for albumin and alpha 1-acid glycoprotein (AGP) concentrations. 14C-Triazolam was added to each sample to a final concentration of 5 ng/ml. Protein binding was determined by equilibrium dialysis. Unbound triazolam ranged from 6.4% to 15.4% (mean = 10.0%). AGP concentrations ranged from 71.8 to 205.1 mg% (mean = 123.4 mg%). Triazolam binding ratio (bound/unbound concentration) correlated with AGP concentration (r2 = 0.69) but not with albumin concentration, age, or sex. This correlation was verified by adding AGP in varying amounts to control plasma.

摘要

在间隔至少1周的两个时间点,对12名接受透析的患者(年龄在18至73岁之间)进行过夜禁食后采集血浆。对样本检测白蛋白和α1-酸性糖蛋白(AGP)浓度。向每个样本中加入14C-三唑仑,使其终浓度达到5 ng/ml。通过平衡透析法测定蛋白结合率。未结合的三唑仑范围为6.4%至15.4%(平均值 = 10.0%)。AGP浓度范围为71.8至205.1 mg%(平均值 = 123.4 mg%)。三唑仑结合率(结合/未结合浓度)与AGP浓度相关(r2 = 0.69),但与白蛋白浓度、年龄或性别无关。通过向对照血浆中加入不同量的AGP验证了这种相关性。

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