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己酮可可碱在大鼠体内的药代动力学研究/第二篇通讯:静脉注射后的消除(作者译)

[Studies on the pharmacokinetics of hexobendine in rats / 2nd communication: Elimination following i.v. administration (author's transl)].

作者信息

Kolassa N, Dörr B, Pfleger K

出版信息

Arzneimittelforschung. 1975 Oct;25(10):1567-70.

PMID:1243039
Abstract

The elimination of 14C and of 3H was studied in rats after i.v. administration of 0.22--0.33 mg/kg of 14C- or 0.67 mg/kg of 3H-labelled N,N'-dimethyl-N,N'-bis-[3-(3',4',5'-trimethoxy-benzoxy)-propyl]-ethylenediamine-dihydrochloride (hexobendine, Ustimon, Reoxyl), respectively. Regarding the obtained results shortcomings in methods are discussed which may falsify the elimination pattern of radioactively labelled substances. Under certain experimental conditions (closed metabolism chamber with absorption of CO2 or H2O, respectively) 99-100% of the administered radioactivity were detected in the excretion products. The appearance of 14CO2 in the expired air was prevented when the bile duct was cannulated and the bile was drained to the outside before reaching the gut with its probably decarboxylating bacteria.

摘要

在大鼠静脉注射分别为0.22 - 0.33毫克/千克的14C标记或0.67毫克/千克的3H标记的N,N'-二甲基-N,N'-双-[3-(3',4',5'-三甲氧基-苯氧基)-丙基]-乙二胺二盐酸盐(己酮可可碱,Ustimon,Reoxyl)后,研究了14C和3H的消除情况。针对所得结果,讨论了可能会歪曲放射性标记物质消除模式的方法缺陷。在某些实验条件下(分别带有吸收CO2或H2O的封闭代谢室),在排泄产物中检测到99 - 100%的给药放射性。当胆管插管并且胆汁在到达带有可能进行脱羧作用细菌的肠道之前被引流到体外时,呼出气体中14CO2的出现受到了抑制。

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