Kammerau B, Klebe U, Zesch A, Schaefer H
Arch Dermatol Res (1975). 1976 Mar 10;255(1):31-42. doi: 10.1007/BF00581675.
The penetration, permeation, and resorption of radioactively labelled 8-Methoxypsoralen was investigated in human skin. Siultaneously, the effects to time and ointment carrier on the penetration kinetics were ascertained. The carriers tested were: vaseline, aqueous wool-wax alcohol ointment, aqueous hydrophilic ointment and polyethylene glycol ointment. The absolute concentrations of 8-Methoxypsoralen were estimated in the horny layer, epidermis and dermis. With the most advantageous carrier, aqueous wool-wax alcohol ointment, 4-6X10(-5) M and 10(-5) M were attained in the epidermis and dermis, respectively. Moreover, it was shown that the substance penetrates rapidly (10 min) into the epidermis and dermis and the high concentrations reached constant over a period of 16 h. Only with a formulation of aqueous wool-wax alcohols is any accumulation at all achieved in the deeper areas of the horny layer. A uniform decrease in drug concentration with increasing depth of the horny layer is found with the other 3 vehicles, whereby slight variations in concentrations pertain from carrier to carrier. 4 h after local application, 8-Methoxypsoralen can be detected in the urine. Regardless of the ointment base employed, 8-Methoxypsoralen is no longer detectable in the urine 40 h after application. In comparison to the oral therapy, the same magnitude of percutaneous resorption into the central compartment is to be derived from the data, if half the body surface is treated locally.
对放射性标记的8-甲氧基补骨脂素在人体皮肤中的渗透、透皮吸收及再吸收进行了研究。同时，确定了时间和软膏基质对渗透动力学的影响。所测试的基质有：凡士林、含水羊毛脂醇软膏、水性亲水性软膏和聚乙二醇软膏。对8-甲氧基补骨脂素在角质层、表皮和真皮中的绝对浓度进行了估算。使用最有利的基质——含水羊毛脂醇软膏时，表皮和真皮中的浓度分别达到4-6×10⁻⁵M和10⁻⁵M。此外，结果表明该物质能迅速（10分钟）渗透到表皮和真皮中，且高浓度在16小时内保持恒定。只有使用含水羊毛脂醇制剂时，角质层较深区域才会有任何蓄积。使用其他3种基质时，随着角质层深度增加，药物浓度均匀降低，不同基质的浓度略有差异。局部用药4小时后，可在尿液中检测到8-甲氧基补骨脂素。无论使用何种软膏基质，用药40小时后尿液中均无法检测到8-甲氧基补骨脂素。与口服疗法相比，如果对身体一半表面积进行局部治疗，从数据中可得出经皮吸收进入中心室的量相当。
