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Metabolism and disposition of 2-hydroxy-4-methoxybenzophenone, a sunscreen ingredient, in Harlan Sprague Dawley rats and B6C3F1/N mice; a species and route comparison.
Xenobiotica ( IF 1.3 ) Pub Date : 2019-10-31 , DOI: 10.1080/00498254.2019.1680906
Esra Mutlu 1 , C Edwin Garner 2 , Christopher J Wegerski 2 , Jacob D McDonald 2 , Barry S McIntyre 1 , Melanie Doyle-Eisele 2 , Suramya Waidyanatha 1
Affiliation  

2-Hydroxy-4-methoxybenzophenone (HMB) is a common ingredient in personal care products and used as an UV stabilizer. In these studies, disposition and metabolism of [14C]HMB in rats and mice was assessed following single gavage administration (10, 100, or 500 mg/kg), single IV administration (10 mg/kg), or dermal application (0.1, 1, 10, or 15 mg/kg).Following gavage administration, [14C]HMB was well absorbed and excreted mainly in urine (39-57%) and feces (24-42%) with no apparent difference between doses, species or sexes. Distribution of HMB in tissues was minimal in rats (0.36%) and mice (<0.55%).Distribution of HMB following dermal application was comparable to that following gavage administration; no differences between doses, sexes, or species were observed but absorption varied between dose vehicles. Light paraffin oil had the highest absorption and excretion (98% of the HMB dose absorbed).In rats, HMB slowly appeared in the systemic circulation (Tmax ∼2-6 h) and had poor bioavailability (F%<1).Urine metabolites for both species and all routes included HMB, HMB-glucuronide, 2,4-dihydroxybenzophenone (DHB), DHB-glucuronide, and DHB-sulfates, and novel minor dihydroxy metabolites including 2,5-dihydroxy-4-methoxybenzophenone.In vitro hepatic metabolism in mice differed from human and in vivo metabolism especially for phase II conjugates.

中文翻译:

防晒成分2-羟基-4-甲氧基二苯甲酮在Harlan Sprague Dawley大鼠和B6C3F1 / N小鼠中的代谢和分布;物种和路线比较。

2-羟基-4-甲氧基二苯甲酮(HMB)是个人护理产品中的常见成分,并用作紫外线稳定剂。在这些研究中,通过单次强饲法(10、100或500 mg / kg),单次IV给药(10 mg / kg)或经皮肤施用(0.1, 1、10或15 mg / kg)。在管饲法给药后,[14C] HMB被很好地吸收并排泄,主要在尿液(39-57%)和粪便(24-42%)中发生,剂量,种类或剂量之间没有明显差异。性别。在大鼠(0.36%)和小鼠(<0.55%)中,HMB在组织中的分布极少。皮肤施用后HMB的分布与强饲法后相当。没有观察到剂量,性别或种类之间的差异,但是吸收在剂量载体之间变化。
更新日期:2019-10-31
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