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9-氨基吖啶在经口或静脉给药的大鼠以及局部给药的猴子体内的处置情况。

Disposition of 9-aminoacridine in rats dosed orally or intravenously and in monkeys dosed topically.

作者信息

el Dareer S M, Kalin J R, Tillery K F, Hill D L

出版信息

J Toxicol Environ Health. 1985;15(6):789-99. doi: 10.1080/15287398509530705.

DOI:10.1080/15287398509530705
PMID:4057283
Abstract

Following administration of [14C]-labeled 9-aminoacridine ([14C]9AA) hydrochloride either orally or intravenously to rats, the excretion of radioactivity was similar, with 20-26% of the dose appearing in the urine and 57-68% in the feces. The pattern of tissue distribution was also similar for the two routes. This information suggests that absorption of the oral doses was extensive and that, for both routes of administration, biliary excretion accounted for most of the radioactivity in the feces. Biliary excretion of radioactivity derived from [14C]9AA was confirmed in an experiment involving rats with inserted biliary cannulas. For these rats, 49.5% of the dose administered appeared in the bile in 4 h. The major urinary and biliary metabolite of [14C]9AA of rats was identified as an O-beta-glucuronide of hydroxylated 9AA. Absorption of 9AA through the skin could not be conclusively demonstrated. For monkeys dosed topically with [14C]9AA, only small amounts of radioactivity (a total of less than 0.8% of the dose) appeared in the urine and various tissues in 24 h.

摘要

给大鼠口服或静脉注射[14C]标记的盐酸9-氨基吖啶([14C]9AA)后,放射性排泄情况相似,剂量的20%-26%出现在尿液中,57%-68%出现在粪便中。两种给药途径的组织分布模式也相似。这一信息表明口服剂量的吸收广泛,并且对于两种给药途径,胆汁排泄是粪便中大部分放射性的来源。在一项涉及插入胆管插管的大鼠的实验中,证实了源自[14C]9AA的放射性的胆汁排泄。对于这些大鼠,给药剂量的49.5%在4小时内出现在胆汁中。大鼠[14C]9AA的主要尿液和胆汁代谢物被鉴定为羟基化9AA的O-β-葡萄糖醛酸苷。无法确凿证明9AA可通过皮肤吸收。对于局部给予[14C]9AA的猴子,24小时内尿液和各种组织中仅出现少量放射性(总量少于剂量的0.8%)。

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