Systemic exposure to parabens: Pharmacokinetics, tissue distribution, excretion balance and plasma metabolites of [¹⁴C]-methyl-, propyl- and butylparaben in rats after oral, topical or subcutaneous administration

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• 作者：Nicolas Aubert ; ^{nicolas.aubert@fr.citoxlab.com} ; Thibault Ameller ; Jean-Jacques Legrand
• 关键词：AUC ; area under the plasma&ndash ; time curve ; BP ; butylparaben ; CIR ; US Cosmetic Ingredient Review ; Cmax ; maximal plasma concentration ; EP ; ethylparaben ; GLP ; good laboratory practice ; LOD ; limit of detection ; LOQ ; limit of quantification ; MP ; methylparabe
• 刊名：Food and Chemical Toxicology
• 出版年：2012
• 期刊代码：20_02786915
• 类别：pha
• 出版时间：March-April, 2012
• 卷：50
• 期：3-4
• 页码：445-454
• 文件大小：593 K

摘要

Parabens (PB) are preservatives used in food, drugs and personal care products preventing microbial and fungal contamination. We investigated ADME profiles of [¹⁴C]-methyl-, propyl- or butylparaben (MP, PP, BP) following single oral, dermal or subcutaneous (BP) doses at 100 mg/kg to Sprague-Dawley rats. Plasma C_max and AUC values after oral or subcutaneous doses were 4- to 10-fold higher relative to respective values after dermal administration. t_max ranged from 0.5, 2 or 8 h after oral, subcutaneous or dermal administration, respectively. MP produced higher blood C_max and AUC levels relative to those after PP or BP. Following oral or subcutaneous administration, urinary excretion was predominant (>70%, mainly during the first 24 h), less than 4%were eliminated in the feces, 2%were retained in the tissues and carcasses. Following dermal application, >50%of the dose was unabsorbed, 14-27%or <2%were respectively excreted in the urine or feces, respectively. Overall, parabens were well absorbed after oral and subcutaneous, and partially absorbed after dermal administration. All administration routes produced a single peak in the plasma, corresponding to that of para-hydroxybenzoic acid (PHBA) suggesting that PB produce no significant systemic exposure of mammalian organisms after oral, topical or subcutaneous administration.