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茶碱的分布研究:大鼠和马的微透析以及大鼠的全身放射自显影

Distribution studies of theophylline: microdialysis in rat and horse and whole body autoradiography in rat.

作者信息

Ingvast-Larsson C, Appelgren L E, Nyman G

机构信息

Department of Pharmacology and Toxicology, Swedish University of Agricultural Sciences, Uppsala.

出版信息

J Vet Pharmacol Ther. 1992 Dec;15(4):386-94. doi: 10.1111/j.1365-2885.1992.tb01030.x.

DOI:10.1111/j.1365-2885.1992.tb01030.x
PMID:1487837
Abstract

After intravenous administration of theophylline, microdialysis has been used for studying the non protein bound theophylline concentration in blood and in lung tissue in the rat as well as in two horses. The distribution pattern of 14C-theophylline in the rat was also investigated. When the distribution of theophylline was completed the time course of free drug in the interstitial fluid in lung tissue was in good agreement with the total concentration-time profile in plasma in both species. In the rat the free concentration of theophylline in the lung was slightly lower than the free concentration in the blood from 40 to 300 min. The in vivo protein binding in blood was 48.8 +/- 6.2% in the rats (n = 9) and 8-25% in the horses (n = 2). The whole body autoradiography study in rat showed that the concentration of radioactivity in the lung followed the blood concentration very closely up to 24 h after injection. The effect of theophylline in the lung can be assumed to be related to the plasma concentration of theophylline, since the concentration-time profile in plasma reflects the time course in the lung.

摘要

静脉注射茶碱后,微透析已被用于研究大鼠和两匹马血液及肺组织中未与蛋白结合的茶碱浓度。还研究了大鼠体内14C-茶碱的分布模式。当茶碱分布完成时,两个物种肺组织间质液中游离药物的时间进程与血浆中总浓度-时间曲线高度吻合。在大鼠中,40至300分钟内肺中茶碱的游离浓度略低于血液中的游离浓度。大鼠血液中的体内蛋白结合率为48.8±6.2%(n = 9),马为8 - 25%(n = 2)。大鼠全身放射自显影研究表明,注射后长达24小时,肺中放射性浓度与血液浓度密切相关。由于血浆中的浓度-时间曲线反映了肺中的时间进程,因此可以认为肺中茶碱的作用与血浆中茶碱浓度有关。

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