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大鼠体内阿地芬宁的血浆水平及血脑屏障通透性

Adiphenine plasma levels and blood-brain barrier crossing in the rat.

作者信息

Michelot J, Moreau M F, Veyre A, Labarre P, Meyniel G

出版信息

Eur J Drug Metab Pharmacokinet. 1985 Oct-Dec;10(4):273-8. doi: 10.1007/BF03189754.

Abstract

Adiphenine was administered in 3H-labelled form in doses of 15 mumole/kg intravenously to male Wistar rats. Plasma and brain levels of the unchanged drug were measured. The elimination of the 3H-labelled compound from the plasma was monophasic with a half-life of 13 minutes. The unchanged drug was detectable in the plasma for 30 minutes after the injection. The time course of brain levels of unchanged drug paralleled that found in the plasma with a half-life of 9 to 12 minutes. In all experiments, brain and plasma levels of unchanged adiphenine correlate highly.

摘要

以3H标记形式的阿地芬宁,按15微摩尔/千克的剂量静脉注射给雄性Wistar大鼠。测定了未变化药物的血浆和脑内水平。3H标记化合物从血浆中的消除呈单相,半衰期为13分钟。注射后30分钟内可在血浆中检测到未变化的药物。未变化药物的脑内水平随时间的变化过程与血浆中的相似,半衰期为9至12分钟。在所有实验中,未变化的阿地芬宁在脑和血浆中的水平高度相关。

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