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过氧化苯甲酰:经皮渗透与代谢处置

Benzoyl peroxide: percutaneous penetration and metabolic disposition.

作者信息

Nacht S, Yeung D, Beasley J N, Anjo M D, Maibach H I

出版信息

J Am Acad Dermatol. 1981 Jan;4(1):31-7. doi: 10.1016/s0190-9622(81)70004-5.

Abstract

The transepidermal penetration and metabolic disposition of 14C-benzoyl peroxide were assessed in vitro (excised human skin) and in vivo (rhesus monkey). In vitro, the benzoyl peroxide penetrated into the skin, through the stratum corneum or the follicular openings, or both, and was recovered on the dermal side as benzoic acid. In vivo, benzoic acid was recovered from urine in amounts equivalent to 45% and 98% of the radiolabel following, respectively, topical and intramuscular administration of small amounts of 14C-benzoyl peroxide. We conclude that benzoyl peroxide penetrates as such into the skin layers and is converted therein to benzoic acid, which, in turn is absorbed into the systemic circulation. Renal clearance of the metabolite is sufficiently rapid as to preclude its hepatic conjugation with glycine, since following topical administration to rhesus monkeys, no hippuric acid was found in the urine, as could have been expected had a significant amount of benzoic acid passed through the liver.

摘要

在体外(离体人皮肤)和体内(恒河猴)评估了14C-过氧化苯甲酰的经皮渗透和代谢情况。在体外,过氧化苯甲酰通过角质层或毛囊开口或两者进入皮肤,并在真皮侧以苯甲酸形式回收。在体内,分别对恒河猴局部和肌肉注射少量14C-过氧化苯甲酰后,从尿液中回收的苯甲酸量分别相当于放射性标记物的45%和98%。我们得出结论,过氧化苯甲酰本身可渗透到皮肤层中,并在其中转化为苯甲酸,苯甲酸进而被吸收进入体循环。该代谢物的肾脏清除速度足够快,可防止其在肝脏与甘氨酸结合,因为对恒河猴局部给药后,尿液中未发现马尿酸,而如果有大量苯甲酸通过肝脏,本应可以预期到马尿酸的存在。

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