Príborský J, Mühlbachová E
Institute of Pharmacology, Medical Faculty of Hygiene, Charles University, Prague, Czechoslovakia.
J Pharm Pharmacol. 1990 Jul;42(7):468-72. doi: 10.1111/j.2042-7158.1990.tb06597.x.
The in-vitro permeability characteristics of human skin have been examined and compared with results in laboratory animals using various types of penetration enhancers. The study was focused on evaluation of predictable validity of the data obtained in animals mostly used in permeation studies. The results in man using the same penetration enhancers were about 30% of the value in the rat. The least potent enhancer was dimethylsulphoxide and the maximum efficacy was observed with sodium laurylsulphate in the rat experiments while in man the results were approximately equal when using any of the studied enhancers. Comparison of the results of experiments performed with N-methyl-2-pyrrolidone in several laboratory animals and man showed that the skin permeability in man is approximately 4 times lower than with the rat. Man and guinea-pig were not significantly different in these experiments. There were no significant differences in laurocapram penetration enhancing effect in the concentration range 0.1 to 0.5%, but there was an optimum concentration of laurocapram of 1%. The results showed quantitative differences in percutaneous absorption in various animal species in comparison with man. These differences should be considered in selecting a suitable model for preclinical drug evaluation. The guinea-pig skin penetration seems to be most similar to that in man.
已对人体皮肤的体外渗透特性进行了研究，并使用各种类型的渗透促进剂将其与实验动物的结果进行了比较。该研究的重点是评估在渗透研究中最常用的动物身上获得的数据的可预测有效性。在人体中使用相同渗透促进剂的结果约为大鼠结果的30%。在大鼠实验中，效力最低的促进剂是二甲基亚砜，而月桂基硫酸钠的效果最佳；而在人体中，使用任何一种所研究的促进剂时结果大致相同。在几种实验动物和人体中用N-甲基-2-吡咯烷酮进行实验的结果比较表明，人体皮肤的渗透率比大鼠低约4倍。在这些实验中，人和豚鼠没有显著差异。在0.1%至0.5%的浓度范围内，月桂氮卓酮的渗透促进效果没有显著差异，但月桂氮卓酮的最佳浓度为1%。结果表明，与人体相比，不同动物物种的经皮吸收存在定量差异。在选择合适的临床前药物评价模型时应考虑这些差异。豚鼠的皮肤渗透似乎与人体最为相似。
