Abstract

1. Triclocarban is a residue-producing antibacterial agent used in a variety of consumer products. These studies investigated the disposition and metabolism of [¹⁴C]triclocarban.

2. In male rats following a single gavage administration of 50, 150, and 500 mg/kg, excretion was primarily via feces (feces, 85–86%; urine, 3–6%) with no apparent dose-related effect. In male rats, 29% of the administered dose was excreted in bile suggesting some of the fecal excretion is from the absorbed dose which was excreted to the intestine via bile.

3. The tissue retention of radioactivity was low in male rats (24 h, 3.9%; 72 h, 0.1%).

4. Disposition pattern following gavage administration of 50 mg/kg in female rats and male and female mice were similar to male rats.

5. Plasma elimination half-life of triclocarban in rats following gavage administration was shorter (∼2 h) compared to that based on total radioactivity (≥9 h) which included all products of triclocarban.

6. Absorption following a single dermal application of 1.5 or 3% was low (≤3%) in rodents.

7. Hydroxylated and conjugated metabolites of triclocarban predominated in bile.

8. In hepatocytes, clearance of triclocarban in mouse and human was similar and was faster than in rat.

摘要

1. 三氯卡班是一种产生残留物的抗菌剂，可用于多种消费品。这些研究调查了[ ¹⁴ C]三氯卡班的处置和代谢。

2. 在雄性大鼠一次管饲50、150和500 mg / kg时，排泄主要是通过粪便（粪便占85–86％；尿占3–6％）而没有明显的剂量相关作用。在雄性大鼠中，29％的给药剂量通过胆汁排泄，这表明粪便中的一些排泄是通过胆汁排泄到肠道的吸收剂量。

3. 雄性大鼠的放射性组织保留率低（24 h，3.9％； 72 h，0.1％）。

4. 雌性大鼠和雄性和雌性小鼠强饲法施用50 mg / kg后的处置方式与雄性大鼠相似。

5. 与包括所有三氯卡班产品的总放射性（≥9小时）相比，强饲法给药后大鼠的三氯卡班血浆消除半衰期更短（〜2 h）。

6. 在啮齿动物中，单次皮肤施用1.5％或3％后的吸收率很低（≤3％）。

7. 在胆汁中占主导地位的三氯卡班的羟基化和共轭代谢产物。

8. 在肝细胞中，三氯卡班在小鼠和人体内的清除率相似，并且比大鼠快。