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[用³H标记的合成抗纤溶剂进行的药代动力学研究]

[Pharmacokinetic studies with 3H-labelled synthetic antifibrinolytics].

作者信息

Richter M, Markwardt F, Klöcking H P

出版信息

Pharmazie. 1982 Dec;37(12):851-3.

PMID:6984512
Abstract

In rabbits and rats pharmacokinetic studies on the anti-fibrinolytics 4-aminomethylbenzoic acid (PAMBA), trans-4-aminomethylcyclohexane-1-carboxylic acid (AMCA), and epsilon-aminocaproic acid (EACA) were carried out using the tritium labelled compounds. Following i. v. administration of PAMBA and EACA in rabbits a two-phasic plasma level and following AMCA a three-phasic plasma level was found within 7 h. The rate constants beta of 0.34 h-1, 0.44 h-1, and 1.08 h-1 for EACA, PAMBA, and AMCA, respectively, indicate a more rapid elimination of AMCA. Accordingly, the AUC-values for AMCA are considerably smaller than those for EACA and PAMBA after both i. v. and p. o. administration.

摘要

在兔子和大鼠身上,使用氚标记的化合物对抗纤维蛋白溶解剂4-氨甲基苯甲酸(PAMBA)、反式-4-氨甲基环己烷-1-羧酸(AMCA)和ε-氨基己酸(EACA)进行了药代动力学研究。给兔子静脉注射PAMBA和EACA后,7小时内血浆水平呈双相变化;给兔子静脉注射AMCA后,7小时内血浆水平呈三相变化。EACA、PAMBA和AMCA的消除速率常数β分别为0.34 h⁻¹、0.44 h⁻¹和1.08 h⁻¹,这表明AMCA的消除速度更快。因此,静脉注射和口服给药后,AMCA的AUC值均明显小于EACA和PAMBA的AUC值。

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