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静脉注射后大鼠体内4-碘安替比林-I125(放射性碘安替比林)的代谢

The metabolism of 4-iodantipyrine--I125 (RIAP) in rat organism after intravenous injection.

作者信息

Marciniak M, Bałtrukiewicz Z, Chaś J

出版信息

Acta Physiol Pol. 1984 Jul-Aug;35(4):355-65.

PMID:6545929
Abstract

Radioactive antipyrine labelled with I125 (RIAP) is used in radioisotope diagnostic methods for determination of the total water content of the organism, and cerebral and cardiac blood flow. The purpose of this study was to investigate RIAP metabolism in rats after intravenous administration. The distribution, excretion and passage with milk to the newborn animals were studied. Electrophoresis of the urine of the rats treated with this radioisotope was done as well. A rapid accumulation of the radioisotope in the thyroid was observed (the T 1/2 value was about 4 hours, and the greatest accumulation of RIAP was after 15 hours). The biological time of RIAP elimination from the thyroid was 5 days. I125 concentration in other organs was below 1% of the injected dose. Excretion was mainly with urine in three phases. In the urine of the rats two I125-containing fractions were found (a iodide fraction and an unidentified fraction). RIAP administration to lactating females caused passage of between 10 and 20% of the administered dose to pass to the newborns with milk. RIAP administration to pregnant rats raised this proportion by several per cent. Thyroid blockade with potassium iodide had no effect on RIAP passage with milk to the newborns. These results suggest a rapid loss of iodine from RIAP after intravenous injection.

摘要

用碘125标记的放射性安替比林(RIAP)用于放射性同位素诊断方法,以测定机体的总含水量以及脑血流量和心脏血流量。本研究的目的是调查静脉注射后大鼠体内RIAP的代谢情况。研究了其分布、排泄以及通过乳汁传递给新生动物的情况。还对用这种放射性同位素处理过的大鼠尿液进行了电泳分析。观察到放射性同位素在甲状腺中迅速蓄积(T 1/2值约为4小时,RIAP在15小时后蓄积最多)。RIAP从甲状腺消除的生物学时间为5天。其他器官中的碘125浓度低于注射剂量的1%。排泄主要分三个阶段通过尿液进行。在大鼠尿液中发现了两个含碘125的组分(一个碘化物组分和一个未鉴定组分)。给哺乳期雌性大鼠注射RIAP会导致10%至20%的给药剂量通过乳汁传递给新生动物。给怀孕大鼠注射RIAP会使这一比例提高几个百分点。用碘化钾阻断甲状腺对RIAP通过乳汁传递给新生动物没有影响。这些结果表明静脉注射后RIAP中的碘迅速流失。

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