市售驱蚊剂中避蚊胺(DEET)的经皮渗透及溶剂影响。

J Stinecipher, J Shah
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引用次数: 60

摘要

N,N-二乙基-m-甲苯酰胺(DEET)是许多商业驱蚊剂中的有效成分,被认为是使用后引起广泛的局部和全身不良反应的原因。许多研究者研究了皮肤对纯避蚊胺的吸收;然而,关于避蚊胺在商业驱蚊剂中的吸收以及避蚊胺浓度对其经皮肤吸收的影响,文献中仅有一篇报道。本研究的第一个目的是评估Everglades(95%)、击退猎鹿者(52.25%)、Off Skintastic(6.65%)和Skedaddle(6.2%)四种商业产品避蚊胺的渗透特性,与纯避蚊胺(约100%)相比。第二个目的是研究避蚊胺的溶剂乙醇对避蚊胺渗透的影响,并研究其增强避蚊胺皮肤吸收的潜力。使用Franz扩散池的无限剂量技术,对商用驱蚊剂和含有不同百分比乙醇的溶液中的避蚊胺进行了人体皮肤渗透研究。从每一种情况下的渗透剖面中获得稳态通量(Jss)、滞后时间(tL)、扩散系数(D)、渗透率(P)和皮肤/车辆分配系数(K)等渗透参数。避蚊胺的累计渗透量排序为:整齐避蚊胺(100%)= Everglades(95%) >击退(52.25%)> Skedaddle (6.2%) = Off skinintastic(6.65%)。纯DEET的通量值最高,为63.20 +/- 24.52微克/cm2-h, Off Skintastic的通量值最低,为21.12 +/- 14.75微克/cm2-h。每种产品的tL和D值与纯避蚊胺相似。在36 h结束时,30-45%乙醇溶液的避蚊胺渗透总量显著高于纯避蚊胺和60-90%乙醇溶液。30-45%乙醇溶液避蚊胺的Jss、P和K值显著高于75-90%乙醇溶液避蚊胺的Jss、P和K值,而tL和D值与75% -90%乙醇溶液避蚊胺的相似。因此,在商业驱蚊剂的皮肤应用后,避蚊胺有可能被大量吸收,而乙醇作为溶剂可能会增强避蚊胺的渗透。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Percutaneous permeation of N,N-diethyl-m-toluamide (DEET) from commercial mosquito repellents and the effect of solvent.

N,N-Diethyl-m-toluamide (DEET), the active ingredient in many commercial mosquito repellents, is thought to be responsible for a wide range of local and systemic adverse reactions following its use. Many investigators have studied the dermal absorption of pure DEET; however, there is only one report in the literature on the absorption of DEET from commercial mosquito repellents and the effect of concentration of DEET on its absorption through skin. The first objective of the present study was to evaluate the permeation characteristics of DEET from four commercial products, Everglades (95%), Repel Deerhunters (52.25%), Off Skintastic (6.65%), and Skedaddle (6.2%), as compared to pure DEET (approximately 100%). The second objective was to study the effects of ethanol, the solvent for DEET, on the permeation of DEET and investigate its potential for enhancing the dermal absorption of DEET. Permeation studies of DEET from commercial mosquito repellents and from solutions containing various percentages of ethanol were conducted across human skin using an infinite dose technique with a Franz diffusion cell. Permeation parameters such as steady-state flux (Jss), lag time (tL), diffusion coefficient (D), permeability (P), and skin/ vehicle partition coefficient (K) were obtained from the permeation profiles in each case. The cumulative amount of DEET permeated can be ranked according to the following order: neat DEET (100%) = Everglades (95%) > Repel (52.25%) > Skedaddle (6.2%) = Off Skintastic (6.65%). Pure DEET exhibited the highest flux value of 63.20 +/- 24.52 micrograms/cm2-h, while Off Skintastic had the lowest value of 21.12 +/- 14.75 micrograms/cm2-h. The tL and D values for each of the products were similar to that of pure DEET. The total amount of DEET permeated from 30-45% ethanolic solutions at the end of 36 h was significantly higher than that from pure DEET and from the 60-90% ethanolic solutions. The Jss, P, and K values of DEET from the 30-45% ethanolic solutions were significantly higher than those from the 75-90% ethanolic solutions, while the tL and D values were similar for each solution. Therefore, there is potential for significant absorption of DEET after the dermal application of commercial mosquito repellents, and ethanol, used as a solvent, may enhance the permeation of DEET.

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