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N-乙烯基-2-吡咯烷酮在大鼠体内的处置

Disposition of N-vinyl-2-pyrrolidinone in the rat.

作者信息

McClanahan J S, Lin Y C, Digenis G A

出版信息

Drug Chem Toxicol. 1984;7(2):129-48. doi: 10.3109/01480548408998411.

Abstract

The disposition of N-[14C-vinyl]-2-pyrrolidinone was studied in male Sprague-Dawley rats following a single iv injection. Plasma levels of the intact compound dropped rapidly within the first 6 hours after dosing with a half life of 1.90 hours. Urinary excretion by 12 hours represented 74.9% of a 5 microCi dose while 18.7% was excreted into the bile by 6 hours. 14C-activity attributed to the intact compound was found to be less than 0.59% of the dose in the urine and less than 0.46% in the bile. Tissue distribution studies showed that the liver and small intestines and contents contained the highest accumulation of 14C-activity up to 6 hours after administration of N-[14C-vinyl]-2-pyrrolidinone. Urine analyses performed for metabolite elucidation indicated that 12% of the radioactivity dosed was incorporated into acetate and the major remaining portion in species which appeared to be water soluble acidic compounds.

摘要

在雄性斯普拉格-道利大鼠单次静脉注射N-[14C-乙烯基]-2-吡咯烷酮后,对其处置情况进行了研究。给药后最初6小时内,完整化合物的血浆水平迅速下降,半衰期为1.90小时。12小时时尿液排泄量占5微居里剂量的74.9%,而6小时时18.7%排泄到胆汁中。在尿液中,归因于完整化合物的14C活性不到剂量的0.59%,在胆汁中不到0.46%。组织分布研究表明,在给予N-[14C-乙烯基]-2-吡咯烷酮后6小时内,肝脏、小肠及其内容物中14C活性的积累量最高。为阐明代谢产物而进行的尿液分析表明,给药放射性的12%被整合到乙酸盐中,其余主要部分存在于似乎是水溶性酸性化合物的物质中。

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