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氚标记长春乙酯的药代动力学数据。

Pharmacokinetic data on tritium labelled ethyl apovincaminate.

作者信息

Vereczkey L, Zólyomi G, Szporny L

出版信息

Arzneimittelforschung. 1976;26(10a):1929-33.

PMID:1037218
Abstract

Absorption, tissue distribution and excretion of tritium labelled ethyl apovincaminate (RGH-4405, Cavinton) were studied. Both oral and i.p. administration resulted in a relatively rapid elimination of tritium activity, suggesting that neither the original drug nor its metabolites remained in the organism of rat. 50% of radioactivity was recovered in urine and 30% in faeces during 48 h. At this time only liver and kidneys contained measurable quantities of radioactivity among the organs tested. Biliary route of elimination seemed to be important, since 20% and 4% of radioactivity appeared in bile during 9 h following i.p. and p.o. administration, respectively. Enterohepatic circulation was of no consequence. Radioactivity was hardly adsorbed to or absorbed by blood cells and was almost completely bound by plasma protein(s).

摘要

研究了氚标记的阿朴长春胺乙酯(RGH - 4405,卡温顿)的吸收、组织分布及排泄情况。口服和腹腔注射给药后,氚活性均相对快速消除,这表明原药及其代谢产物均未留存于大鼠体内。在48小时内,50%的放射性在尿液中回收,30%在粪便中回收。此时,在所检测的器官中,只有肝脏和肾脏含有可测量的放射性。排泄的胆汁途径似乎很重要,因为腹腔注射和口服给药后9小时内,分别有20%和4%的放射性出现在胆汁中。肝肠循环没有影响。放射性几乎不被血细胞吸附或吸收,几乎完全与血浆蛋白结合。

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