对氯间甲酚、对氯间甲酚、氯百里酚、混合甲酚、间甲酚、邻甲酚、对甲酚、异丙基甲酚、百里酚、邻异丙基甲苯-5-醇和香芹酚安全性评估的最终报告。

Final report on the safety assessment of sodium p-chloro-m-cresol, p-chloro-m-cresol, chlorothymol, mixed cresols, m-cresol, o-cresol, p-cresol, isopropyl cresols, thymol, o-cymen-5-ol, and carvacrol.

作者信息

Andersen Alan

机构信息

Cosmetic Ingredient Review, Washington, DC 20036, USA.

出版信息

Int J Toxicol. 2006;25 Suppl 1:29-127. doi: 10.1080/10915810600716653.

Abstract

Sodium p-Chloro-m-Cresol, p-Chloro-m-Cresol (PCMC), Mixed Cresols, m-Cresol, o-Cresol, p-Cresol, Isopropyl Cresols, Thymol, Chlorothymol, o-Cymen-5-ol, and Carvacrol are substituted phenols used as cosmetic biocides/preservatives and/or fragrance ingredients. Only PCMC, Thymol, and o-Cymen-5-ol are reported to be in current use, with the highest concentration of use at 0.5% for o-Cymen-5-ol in perfumes. The use of PCMC in cosmetics is restricted in Europe and Japan. Cresols can be absorbed through skin, the respiratory tract, and the digestive tract; metabolized by the liver; and excreted by the kidney as glucuronide and sulfate metabolites. Several of these cresols increase the dermal penetration of other agents, including azidothymidine. In acute oral toxicity studies, LD50 values were in the 200 to 5000 mg/kg day-1 range across several species. In short-term studies in rats and mice, an o-Cresol, m-Cresol, p-Cresol or m-Cresol/p-Cresol mixture at 30,000 ppm in the diet produced increases in liver and kidney weights, deficits in liver function, bone marrow hypocellularity, irritation to the gastrointestinal tract and nasal epithelia, and atrophy of female reproductive organs. The no observed effect levels (NOEL) of o-Cresol was 240 mg/kg in mink and 778 mg/kg in ferrets in short-term feeding studies, with no significant dose-related toxicity (excluding body weight parameters). In mice, 0.5% p-Cresol, but neither m-Cresol nor o-Cresol, caused loss of pigmentation. Short-term and subchronic oral toxicity tests performed with various cresols using mice, rats, hamsters, and rabbits resulted in no observed adverse effect levels (NOAELs) for mice of 625 ppm and rats of 50 mg/kg day-1, although the NOEL was 2000 ppm in a chronic study using rats. In rabbits, < or =160 mg/kg PCMC was found to produce irritation and erythema, but no systemic effects. Hamsters dosed with 1.5% p-Cresol in diet for 20 weeks had a greater incidence of mild and moderate forestomach hyperplasia as compared to the control. Acute inhalation toxicity studies using rats yielded LC50 values ranging from >20 mg/m(3) for o-Cresol to >583 mg/m(3) for PCMC. No deaths were recorded in mice given o-Cresol at 50 mg/m(3). Cats exposed (short-term) to 9 to 50 mg/m(3) of o-Cresol developed inflammation and irritation of the upper respiratory tract, pulmonary edema, and hemorrhage and perivascular sclerosis in the lungs. Rats exposed (subchronic) to o-Cresol at 9 mg/m(3) had changes in leukocytes, spinal cord smears, nervous activity, liver function, blood effects, clinical signs, and neurological effects. In guinea pigs, exposure to 9 mg/m(3) produced changes in hemoglobin concentrations and electrocardiograms (EKGs). Rats exposed (subchronic) to 0.05 mg/m(3) Mixed Cresols by inhalation exhibited central nervous system (CNS) excitation, denaturation of lung protein, and decreased weight gain. All cresols appear to be ocular irritants. Numerous sensitization studies have been reported and most positive reactions were seen with higher concentrations of Cresol ingredients. Developmental toxicity is seen in studies of m-Cresol, o-Cresol, and p-Cresol, but only at maternally toxic levels. In a reproductive toxicity study of a mixture of m-Cresol and p-Cresol using mice under a continuous breeding protocol, 1.0% caused minimal adult reproductive and significant postnatal toxicity in the presence of systemic maternal toxicity. The o-Cresol NOAEL was 0.2% for both reproductive and general toxicity in both generations. Cresol ingredients were generally nongenotoxic in bacterial, fruit fly, and mammalian cell assays. Thymol did not induce primary lung tumors in mice. No skin tumors were found in mice exposed dermally to m-Cresol, o-Cresol, or p-Cresol for 12 weeks. In the trypthan blue exclusion assay, antitumor effects were observed for Thymol and Carvacrol. Clinical patch testing with 2% PCMC may produce irritant reactions, particularly in people with multiple patch test reactions, that are misinterpreted as allergic responses. o-Cresol, p-Cresol, Thymol, Carvacrol, and o-Cymen-5-ol caused no dermal irritation at or above use concentrations. In two predictive patch tests, PCMC did not produce a sensitization reaction. Overall, these ingredients are not significant sensitizing or photosensitizing agents. The Cosmetic Ingredient Review (CIR) Expert Panel noted some of these ingredients may increase the penetration of other cosmetic ingredients and advised cosmetic formulators to take this into consideration. The CIR Expert Panel concluded that the toxic effects of these ingredients are observed at doses higher than would be available from cosmetics. A concentration limitation of 0.5% was chosen to ensure the absence of a chemical leukoderma effect. For p-Cresol and Mixed Cresols (which contain p-Cresol), the Panel considered that the available data are insufficient to support the safety of these two ingredients in cosmetics. Studies that would demonstrate no chemical leukoderma at concentrations of use of p-Cresol and Mixed Cresols, or would demonstrate a dose response from which a safe concentration could be derived, are needed.

摘要

对氯间甲酚、对氯间甲酚(PCMC)、混合甲酚、间甲酚、邻甲酚、对甲酚、异丙基甲酚、百里酚、氯百里酚、邻伞花烃 -5-醇和香芹酚均为取代酚类,用作化妆品杀菌剂/防腐剂和/或香料成分。据报道,目前仅使用PCMC、百里酚和邻伞花烃 -5-醇,邻伞花烃 -5-醇在香水中的最高使用浓度为0.5%。在欧洲和日本,化妆品中对PCMC的使用受到限制。甲酚可通过皮肤、呼吸道和消化道吸收;在肝脏中代谢;并以葡萄糖醛酸和硫酸盐代谢物的形式通过肾脏排泄。其中几种甲酚会增加其他物质(包括叠氮胸苷)的皮肤渗透性。在急性经口毒性研究中,多个物种的半数致死剂量(LD50)值在200至5000 mg/kg·天 -1范围内。在对大鼠和小鼠的短期研究中,饲料中30,000 ppm的邻甲酚、间甲酚、对甲酚或间甲酚/对甲酚混合物会导致肝脏和肾脏重量增加、肝功能缺陷、骨髓细胞减少、胃肠道和鼻上皮刺激以及雌性生殖器官萎缩。在短期喂养研究中,邻甲酚对水貂的未观察到有害作用水平(NOEL)为240 mg/kg,对雪貂为778 mg/kg,无明显的剂量相关毒性(不包括体重参数)。在小鼠中,0.5%的对甲酚会导致色素沉着丧失,但间甲酚和邻甲酚均不会。使用小鼠、大鼠、仓鼠和兔子对各种甲酚进行的短期和亚慢性经口毒性试验结果显示,小鼠的未观察到有害作用水平(NOAEL)为625 ppm,大鼠为50 mg/kg·天 -1,尽管在一项使用大鼠的慢性研究中NOEL为2000 ppm。在兔子中,发现≤160 mg/kg的PCMC会产生刺激和红斑,但无全身影响。在饲料中添加1.5%对甲酚喂养20周的仓鼠,与对照组相比,轻度和中度前胃增生的发生率更高。使用大鼠进行的急性吸入毒性研究得出的半数致死浓度(LC50)值范围为:邻甲酚>20 mg/m³,PCMC>583 mg/m³。给予50 mg/m³邻甲酚的小鼠未记录到死亡。短期暴露于9至50 mg/m³邻甲酚的猫出现上呼吸道炎症和刺激、肺水肿以及肺部出血和血管周围硬化。亚慢性暴露于9 mg/m³邻甲酚的大鼠在白细胞、脊髓涂片、神经活动、肝功能、血液影响、临床体征和神经学影响方面出现变化。在豚鼠中,暴露于9 mg/m³会导致血红蛋白浓度和心电图(EKG)发生变化。通过吸入亚慢性暴露于0.05 mg/m³混合甲酚的大鼠表现出中枢神经系统(CNS)兴奋、肺蛋白变性和体重增加减少。所有甲酚似乎都是眼部刺激物。已报道了大量致敏研究,大多数阳性反应出现在较高浓度的甲酚成分中。在间甲酚、邻甲酚和对甲酚的研究中观察到发育毒性,但仅在母体毒性水平出现。在一项使用小鼠按照连续繁殖方案对间甲酚和对甲酚混合物进行的生殖毒性研究中,1.0%在存在全身母体毒性的情况下导致最小的成年生殖毒性和显著的产后毒性。邻甲酚在两代中的生殖毒性和一般毒性的NOAEL均为0.2%。在细菌、果蝇和哺乳动物细胞试验中,甲酚成分通常无遗传毒性。百里酚未在小鼠中诱发原发性肺癌。经皮暴露于间甲酚、邻甲酚或对甲酚12周的小鼠未发现皮肤肿瘤。在台盼蓝排斥试验中,观察到百里酚和香芹酚具有抗肿瘤作用。用2% PCMC进行的临床斑贴试验可能会产生刺激性反应,特别是在有多次斑贴试验反应的人群中,这些反应会被误解为过敏反应。邻甲酚、对甲酚、百里酚、香芹酚和邻伞花烃 -5-醇在使用浓度及以上时未引起皮肤刺激。在两项预测性斑贴试验中,PCMC未产生致敏反应。总体而言,这些成分不是显著的致敏或光致敏剂。化妆品成分审查(CIR)专家小组指出,其中一些成分可能会增加其他化妆品成分的渗透性,并建议化妆品配方师予以考虑。CIR专家小组得出结论,这些成分的毒性作用在高于化妆品中可能存在的剂量时才会观察到。选择0.5%的浓度限制以确保不存在化学性白斑病效应。对于对甲酚和混合甲酚(其中含有对甲酚),该小组认为现有数据不足以支持这两种成分在化妆品中的安全性。需要进行研究以证明在对甲酚和混合甲酚的使用浓度下不会出现化学性白斑病,或者能够证明剂量反应关系从而得出安全浓度。

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