Engelhardt G
Arzneimittelforschung. 1978;28(10):1714-23.
A series of non-steroid antiinflammatory drugs (NSAD) as well as substances with different spectra of pharmacological action were investigated with regard to the influence on binding of corticosterone to plasma protein in rats after repeated oral administration. At pharmacologically active doses, NSAD cause a time and dose dependent increase in rat plasma of the corticosterone fraction which can be ultra-filtrated. The effect on corticosterone binding to plasma protein largely parallels the antiinflammatory efficacy of the NSAD. This does not occur by a mere displacement of corticosterone from the plasma protein binding, but is apparently the consequence of a qualitative and/or quantitative change of the binding proteins. Organic acids, cytostatic or other drugs which strongly bind to plasma protein do not show any corresponding influence on the corticosterone binding to plasma protein under comparable conditions. The increase of the fraction of corticosterone which can be ultra-filtrated effected by the NSAD accelerates the excretion of corticosterone into the bile of rats. The phenomenon of decrease in binding of corticosteroids to plasma protein is discussed with respect to its importance for the mode of action of the NSAD.
研究了一系列非甾体抗炎药（NSAD）以及具有不同药理作用谱的物质在大鼠多次口服给药后对皮质酮与血浆蛋白结合的影响。在药理活性剂量下，NSAD导致大鼠血浆中可超滤的皮质酮部分呈时间和剂量依赖性增加。NSAD对皮质酮与血浆蛋白结合的影响在很大程度上与NSAD的抗炎功效平行。这并非仅仅是皮质酮从血浆蛋白结合位点上被置换所致，而显然是结合蛋白发生定性和/或定量变化的结果。在可比条件下，与血浆蛋白强烈结合的有机酸、细胞抑制剂或其他药物对皮质酮与血浆蛋白的结合未显示出任何相应影响。NSAD引起的可超滤皮质酮部分的增加加速了皮质酮向大鼠胆汁中的排泄。就其对NSAD作用方式的重要性而言，讨论了皮质类固醇与血浆蛋白结合减少的现象。
