Schaefer H, Stüttgen G
Arzneimittelforschung. 1976;26(3):432-5.
The absolute concentrations of an antimycotic drug, econazole, 1-[2,4-dichloro-beta-(p-chlorobenzyloxy)-phenethyl]-imidazole nitrate, in the different layers of the skin are reported when the agent is applied to human skin in vitro and in vivo. The drug was tritium-labelled and incorporated into an ointment to give a 1% concentration as it is used in the therapy of dermatomycoses. This ointment was applied to the skin surface. After fixed time intervals, the skin was sliced parallel to the surface and the amount in each layer determined by liquid scintillation counting. In the in vivo investigations, the excretion of the drug in the urine was also determined. The results reveal that though up to 90% of the drug remain on the surface, about 20 mug/ml epidermal tissue and 1.5 mug/ml dermal tissue can be achieved. The amount which is excreted in the urine is equivalent to the quantity which enters the skin, i.e., the penetrating drug is absorbed by the circulatory system.
当抗真菌药物益康唑（1-[2,4-二氯-β-(对氯苄氧基)-苯乙基]-咪唑硝酸盐）在体外和体内应用于人体皮肤时，报告了其在皮肤不同层中的绝对浓度。该药物用氚标记，并配制成软膏，使其浓度为1%，这是其在皮肤真菌病治疗中的使用浓度。将此软膏涂抹于皮肤表面。在固定的时间间隔后，将皮肤平行于表面切片，并通过液体闪烁计数法测定各层中的药物量。在体内研究中，还测定了药物在尿液中的排泄情况。结果表明，尽管高达90%的药物残留在表面，但表皮组织中可达到约20微克/毫升，真皮组织中可达到1.5微克/毫升。尿液中排泄的药物量与进入皮肤的量相当，即穿透皮肤的药物被循环系统吸收。
