Bronaugh R L, Maibach H I
J Invest Dermatol. 1985 Mar;84(3):180-3. doi: 10.1111/1523-1747.ep12264716.
The percutaneous absorption of 2-nitro-p-phenylene-diamine, 4-amino-2-nitrophenol, nitrobenzene, p-nitroaniline, and 2,4-dinitrochlorobenzene was measured through human and monkey skin. Human studies were performed with excised skin in diffusion cells. Absorption through monkey skin was measured by in vivo and in vitro techniques. Results were compared with those from previously reported human in vivo studies on 2,4-dinitrochlorobenzene and nitrobenzene. Rapid penetration was observed with all compounds, with maximum absorption occurring the first few hours. No significant differences in absorption were found in values obtained by the different procedures except for the highly volatile (and therefore difficult to compare) compound nitrobenzene. A comparison of the human and monkey in vitro data showed a trend toward increased absorption through monkey skin, but the increase was not statistically significant. The monkey in vivo and in vitro results showed that absorption of all compounds except nitrobenzene was slightly less in the in vitro studies; however, the values were not significantly different. The relative volatility of these nitroaromatic compounds was measured by the loss of compound from epidermal discs at various time intervals. The greatest loss of applied material occurred with nitrobenzene; however, substantial amounts of the other compounds were lost, particularly during the first minute after application as the acetone vehicle evaporated. Monkey skin was found to be a good model for human skin for the determination of the percutaneous absorption of these compounds, and in vitro measurements of absorption agreed reasonably well with values obtained by in vivo techniques. A good correlation was not observed between the absorption of these compounds and their solubility properties.
通过人体和猴皮肤测定了2-硝基对苯二胺、4-氨基-2-硝基苯酚、硝基苯、对硝基苯胺和2,4-二硝基氯苯的经皮吸收情况。人体研究使用扩散池中切除的皮肤进行。通过体内和体外技术测定了猴皮肤的吸收情况。将结果与先前报道的关于2,4-二硝基氯苯和硝基苯的人体体内研究结果进行了比较。观察到所有化合物均快速渗透，最大吸收发生在最初几个小时。除了高挥发性（因此难以比较）的化合物硝基苯外，不同方法获得的值在吸收方面没有显著差异。人体和猴体外数据的比较显示，通过猴皮肤的吸收有增加的趋势，但增加没有统计学意义。猴体内和体外结果表明，除硝基苯外，所有化合物在体外研究中的吸收略少；然而，这些值没有显著差异。通过在不同时间间隔表皮盘中化合物的损失来测量这些硝基芳香族化合物的相对挥发性。应用材料损失最大的是硝基苯；然而，其他化合物也有大量损失，特别是在应用后第一分钟丙酮载体蒸发时。发现猴皮肤是用于测定这些化合物经皮吸收的人体皮肤的良好模型，体外吸收测量值与体内技术获得的值相当吻合。未观察到这些化合物的吸收与其溶解性之间有良好的相关性。
