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三氯生在人体口服后的药代动力学。

Pharmacokinetics of triclosan following oral ingestion in humans.

作者信息

Sandborgh-Englund Gunilla, Adolfsson-Erici Margaretha, Odham Göran, Ekstrand Jan

机构信息

Institute of Odontology, Karolinska Institutet, Huddinge, Sweden.

出版信息

J Toxicol Environ Health A. 2006 Oct;69(20):1861-73. doi: 10.1080/15287390600631706.

DOI:10.1080/15287390600631706
PMID:16952905
Abstract

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.

摘要

在过去十年中,含三氯生的个人卫生用品数量迅速增加,三氯生是当今牙膏中使用最普遍的抗菌化合物之一。然而,三氯生的暴露程度尚未得到充分描述。产生耐三氯生病原微生物或选择耐药菌株的潜在风险是一些令人担忧的领域。本研究的目的是:(1)获取血浆和尿液中三氯生基线水平的信息,以及(2)研究单次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口腔漱口液口服单剂量4毫克三氯生。在暴露前及暴露后长达8天的时间内对血浆和尿液中的三氯生进行跟踪监测。血浆中三氯生水平迅速升高,在1至3小时内达到最高浓度,血浆终末半衰期为21小时。大部分在最初24小时内排出。累积尿排泄量在受试者之间有所不同,暴露后前4天内排出的口服剂量为24%至83%。总之,三氯生似乎易于从胃肠道吸收,在人体内周转迅速。该物质的高脂溶性引发了关于其分布特性和蓄积的问题。本研究结果为更好地理解三氯生在人体内的毒代动力学特性奠定了基础。

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