Pharmacokinetics of triclosan following oral ingestion in humans
Pharmacokinetics of triclosan following oral ingestion in humans
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DOI：
10.1080/15287390600631706
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发表时间：
2006-10-15
影响因子：
2.6
通讯作者：
Ekstrand, Jan
中科院分区：
文献类型：
--
作者：
Sandborgh-Englund, Gunilla;Adolfsson-Erici, Margaretha;Ekstrand, Jan
在过去十年中，含有三氯生的个人卫生产品的数量迅速增加，三氯生是当今牙膏中最常用的抗菌化合物之一。然而，三氯生暴露的程度尚未得到很好的描述。产生三氯生耐药病原微生物或选择耐药菌株的潜在风险是一些令人关注的领域。本研究的目的是：(1)获得血浆和尿液中三氯生的基线水平信息，(2)研究单剂量摄入三氯生后的药代动力学模式。10名健康志愿者通过吞咽一种口腔漱口水溶液，暴露于单次口服剂量4毫克的三氯生。在接触三氯生前和接触后8 d内随访血浆和尿液中的三氯生。血浆中三氯生浓度迅速升高，在1 ~ 3小时内达到最大浓度，血浆终末半衰期为21小时。主要部分在服药后24小时内排出。尿中累积排泄量在受试者之间存在差异，口服剂量的24% ~ 83%在服药后4天排出。总之，三氯生似乎很容易从胃肠道吸收，并且在人体中有快速的周转。该物质的高脂溶性引起了有关分布特性和积累的问题。本研究的结果为进一步了解三氯生在人体内的毒性动力学特性奠定了基础。
The number of personal hygiene products containing triclosan has increased rapidly during the last decade, and triclosan is one of the most common antibacterial compounds used in dentifrices today. However, the extent of triclosan exposure has not yet been well described. The potential risks of generating triclosan-resistant pathogenic microorganisms or of the selection of resistant strains are some areas of concern. The aim of the present study was to (1) obtain information on baseline levels of triclosan in plasma and urine, and (2) study the pharmacokinetic pattern of triclosan after a single-dose intake. Ten healthy volunteers were exposed to a single oral dose of 4 mg triclosan by swallowing an oral mouthwash solution. Triclosan in plasma and urine was followed before and up to 8 d after exposure. Triclosan levels in plasma increased rapidly, with a maximum concentration within 1 to 3 h, and the terminal plasma half-life was 21 h. The major fraction was excreted within the first 24 h. The accumulated urinary excretion varied between the subjects, with 24 to 83% of the oral dose being excreted during the first 4 d after exposure. In conclusion, triclosan appears to be readily absorbed from the gastrointestinal tract and has a rapid turnover in humans. The high lipid solubility of the substance gives rise to questions regarding distribution properties and accumulation. The findings of the present study form a basis for greater understanding of the toxicokinetic properties of triclosan in humans.