Gazith J, Schalla W, Bauer E, Schaefer H
J Invest Dermatol. 1978 Aug;71(2):126-30. doi: 10.1111/1523-1747.ep12546709.
Penetration kinetics of 8-methoxypsoralen (8-MOP) into human skin have been investigated under in vitro conditions. The dependence of the resulting tissue concentration on time of penetration, drug concentration in the applied preparation and vehicle composition has been studied. Tissue concentration of the drug was found to increase with time of penetration; however, in both horny layer and epidermis, this increase was followed by a significant decrease in concentration, (after 100 to 300 min), although a large amount of unpenetrated drug was present on the horny layer surface at all times. In contrast to this, 8-MOP accumulated in the lower corium and subcutis and reached concentrations higher then those found in the upper corium and epidermis. This accumulation of the drug is a consequence of the in vitro conditions and its amount is proportional to that amount that under in vivo conditions would have been taken up by the capillary system. Penetration was dependent on vehicle characteristics and was found to increase with increasing polarity of the vehicle. The penetration was found to be directly proportional to the applied concentration; however, the percentage of the drug that actually penetrated was inversely proportional to the applied concentration.
在体外条件下研究了8-甲氧基补骨脂素（8-MOP）渗透入人皮肤的动力学。研究了所得组织浓度与渗透时间、所用制剂中药物浓度以及赋形剂组成的关系。发现药物的组织浓度随渗透时间增加；然而，在角质层和表皮中，这种增加之后浓度会显著下降（100至300分钟后），尽管角质层表面始终存在大量未渗透的药物。与此相反，8-MOP积聚在真皮下层和皮下组织中，其浓度高于真皮上层和表皮中的浓度。药物的这种积聚是体外条件的结果，其数量与在体内条件下会被毛细血管系统摄取的数量成正比。渗透取决于赋形剂的特性，并且发现随着赋形剂极性的增加而增加。发现渗透与所用浓度成正比；然而，实际渗透的药物百分比与所用浓度成反比。
