Badger D A, Smith R L, Bao J, Kuester R K, Sipes I G
Department of Pharmacology and Toxicology and Center for Toxicology, The University of Arizona, 1501 N. Campbell Ave., Tucson 85721, USA.
Food Chem Toxicol. 2002 Dec;40(12):1757-65. doi: 10.1016/s0278-6915(02)00183-7.
The primary objective of these studies was to determine the absorption, distribution, metabolism and excretion of isoeugenol following oral and intravenous administration to male Fischer-344 rats. Following a single oral dose of [14C]isoeugenol (156 mg/kg, 50 microCi/kg), greater than 85% of the administered dose was excreted in the urine predominantly as sulfate or glucuronide metabolites by 72 h. Approximately 10% was recovered in the feces, and less than 0.1% was recovered as CO(2) or expired organics. No parent isoeugenol was detected in the blood at any of the time points analyzed. Following iv administration (15.6 mg/kg, 100 microCi/kg), isoeugenol disappeared rapidly from the blood. The t(1/2) was 12 min and the Cl(s) was 1.9 l/min/kg. Excretion characteristics were similar to those of oral administration. The total amount of radioactivity remaining in selected tissues by 72 h was less than 0.25% of the dose following either oral or intravenous administration. Results of these studies show that isoeugenol is rapidly metabolized and is excreted predominantly in the urine as phase II conjugates of the parent compound.
这些研究的主要目的是确定异丁香酚经口和静脉给药雄性Fischer-344大鼠后的吸收、分布、代谢和排泄情况。单次经口给予[14C]异丁香酚（156毫克/千克，50微居里/千克）后，到72小时时，超过85%的给药剂量以硫酸盐或葡萄糖醛酸代谢物的形式主要经尿液排泄。约10%在粪便中回收，作为二氧化碳或呼出有机物回收的不到0.1%。在分析的任何时间点血液中均未检测到母体异丁香酚。静脉给药（15.6毫克/千克，100微居里/千克）后，异丁香酚迅速从血液中消失。半衰期为12分钟，清除率为1.9升/分钟/千克。排泄特征与经口给药相似。经口或静脉给药后，到72小时时选定组织中残留的放射性总量不到给药剂量的0.25%。这些研究结果表明，异丁香酚迅速代谢，并主要以母体化合物的II相缀合物形式经尿液排泄。
