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对人类志愿者进行皮肤涂抹后,N,N-二乙基间甲苯甲酰胺的吸收、代谢及排泄情况。

Absorption, metabolism, and excretion of N,N-diethyl-m-toluamide following dermal application to human volunteers.

作者信息

Selim S, Hartnagel R E, Osimitz T G, Gabriel K L, Schoenig G P

机构信息

Biological Test Center, Irvine, California 92714, USA.

出版信息

Fundam Appl Toxicol. 1995 Apr;25(1):95-100. doi: 10.1006/faat.1995.1043.

Abstract

The absorption, metabolism, and excretion of N,N-diethyl-m-toluamide (DEET) in male human volunteers following dermal application of [14C]DEET was studied. DEET was applied to two groups of six volunteers either as the undiluted technical grade material or as a 15% solution in ethanol. The material was applied over a 4 x 6-cm area on the volar surface of the forearm and was left in contact with the skin for 8 hr, then rinsed off the skin. Application sites also were tape stripped at 1, 23, and 45 hr after rinsing. Serial blood samples and all urine and feces were collected for 5 days after application. Aliquots of these materials were analyzed for total radioactivity in order to define absorption and excretion patterns. Urine samples also were analyzed by HPLC to characterize the metabolic profile and/or to identify metabolites. Absorption of DEET as evidenced by plasma radioactivity occurred within 2 hr after dose application. Elimination of radioactivity from plasma was rapid and quantifiable levels of radioactivity were observed in plasma for only 4 hr after the end of the 8-hr exposure period. Urine was the principal route of excretion of radioactivity and accounted for an average of 5.61 and 8.33% of the applied dose in the undiluted DEET and 15% DEET in ethanol groups, respectively. Excretion of radioactivity in the feces was less than 0.08% of the applied dose in both groups. DEET did not accumulate in the superficial layers of the skin as evidenced by low amounts of radioactivity in the tape strippings.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

研究了男性人类志愿者经皮涂抹[¹⁴C]避蚊胺(DEET)后,DEET的吸收、代谢及排泄情况。将DEET以未稀释的工业级原料或15%乙醇溶液的形式涂抹于两组各六名志愿者身上。该物质涂抹于前臂掌侧4×6厘米的区域,与皮肤接触8小时,然后从皮肤上冲洗掉。冲洗后1、23和45小时,对涂抹部位进行胶带剥离。涂抹后5天收集系列血样以及所有尿液和粪便。分析这些物质的等分试样中的总放射性,以确定吸收和排泄模式。尿液样本也通过高效液相色谱法进行分析,以表征代谢谱和/或鉴定代谢物。剂量应用后2小时内,血浆放射性证明DEET发生了吸收。血浆中放射性的消除很快,在8小时暴露期结束后,血浆中仅在4小时内观察到可量化的放射性水平。尿液是放射性排泄的主要途径,在未稀释DEET组和15%乙醇DEET组中,分别占施用剂量的5.61%和8.33%。两组粪便中放射性排泄均小于施用剂量的0.08%。胶带剥离中放射性含量低,证明DEET未在皮肤表层蓄积。(摘要截短于250字)

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