Zesch A, Schaefer H
Arch Dermatol Forsch. 1975 Jul 18;252(4):245-56.
Absolute concentrations in the horny layer, epidermis, and dermis of therapeutical doses of topically applied hydrocortisone to human skin (in vivo) are reported. Using vaseline as vehicle 2-10(-4) molar concentrations are found in the epidermis and 3-10(-5) molar concentrations in the dermis. Further, three vehicles revealed minor concentrations. Comparison of the results with similar in vitro-investigations, reported earlier, allow to judge the resorption rate by the intact capillary system. Uptake of hydrocortisone by the vessels is observed. With high rates of penetration vasoconstriction seems to limit the resorption, while this is not the case with low rates, for instance with polyethyleneglycol as vehicle. Thus a differing drug liberation from the vehicle causes qualitatively different permeation kinetics. The elimination by urine, however, was practically the same. It is concluded that different vehicles may cause different therapeutic concentrations of the drug in the skin, but equal systemic side effects.
报告了局部应用氢化可的松治疗剂量对人体皮肤（体内）角质层、表皮和真皮中的绝对浓度。以凡士林为载体时，表皮中发现浓度为2×10⁻⁴摩尔，真皮中为3×10⁻⁵摩尔。此外，三种载体显示出较低的浓度。将结果与早期报道的类似体外研究进行比较，可以判断完整毛细血管系统的吸收速率。观察到氢化可的松被血管摄取。在高渗透率时，血管收缩似乎会限制吸收，而在低渗透率时则不然，例如以聚乙二醇为载体时。因此，载体中药物释放的差异导致了定性不同的渗透动力学。然而，尿液排泄情况实际上是相同的。得出的结论是，不同的载体可能会导致药物在皮肤中产生不同的治疗浓度，但全身副作用相同。
