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人体通过牙膏接触三氯生不会改变 CYP3A4 活性或甲状腺激素的血浆浓度。

Human exposure to triclosan via toothpaste does not change CYP3A4 activity or plasma concentrations of thyroid hormones.

机构信息

Department of Applied Environmental Science, Stockholm University, Stockholm, Sweden.

出版信息

Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):339-44. doi: 10.1111/j.1742-7843.2009.00455.x. Epub 2009 Jul 20.

Abstract

Triclosan is an antibacterial compound commonly used in cosmetics and personal care products for everyday use. As previously shown, triclosan is found in the plasma, urine and milk from large parts of different human populations. Recent studies have revealed that triclosan is able to activate the human pregnane X receptor in vitro and thus possibly affecting metabolism of drugs in humans via the induction of CYP3A4. Besides, triclosan has been shown to affect thyroid hormonal levels in rats in vivo. In the present study, we investigated if an everyday exposure to triclosan via triclosan-containing toothpaste for 14 days in 12 adult humans caused an increase in plasma 4beta-hydroxycholesterol, indicative of CYP3A4 induction, and/or alterations in thyroid hormonal status. The plasma triclosan concentrations increased from 0.009-0.81 ng/g to 26-296 ng/g (ranges) upon exposure. Despite this, there were no significant changes in plasma levels of either plasma 4beta-hydroxycholesterol or thyroid hormones during the exposure. This indicates that the normal use of triclosan-containing toothpaste is not likely to alter metabolism of drugs via CYP3A4 induction or cause adverse events because of thyroid disturbances in humans.

摘要

三氯生是一种抗菌化合物,常用于日常使用的化妆品和个人护理产品。如前所述,三氯生存在于不同人群的血浆、尿液和牛奶中。最近的研究表明,三氯生能够在体外激活人孕烷 X 受体,从而可能通过诱导 CYP3A4 来影响人类药物的代谢。此外,三氯生已被证明会在体内影响大鼠的甲状腺激素水平。在本研究中,我们调查了 12 名成年人在 14 天内每天使用含有三氯生的牙膏是否会导致血浆 4β-羟胆固醇增加,表明 CYP3A4 诱导,以及/或甲状腺激素状态的改变。暴露后,血浆三氯生浓度从 0.009-0.81ng/g 增加到 26-296ng/g(范围)。尽管如此,在暴露期间,血浆 4β-羟胆固醇或甲状腺激素的水平均没有显著变化。这表明,正常使用含三氯生的牙膏不太可能通过 CYP3A4 诱导改变药物代谢,也不会因为甲状腺紊乱而在人类中引起不良反应。

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