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[局部应用雌激素的渗透动力学与分布(作者译)]

[Penetrations kinetics and distribution of topically applied estrogens (author's transl)].

作者信息

Wendker H, Schaefer H, Zesch A

出版信息

Arch Dermatol Res (1975). 1976 Jul 26;256(1):67-74. doi: 10.1007/BF00561181.

Abstract

The penetration into the single layers of human skin in vitro of 17 alpha-estradiol, 17 beta-estradiol and estriol was investigated. The radiolabeled substances were incorporated into 4 standard ointments and into an alcoholic solution mixture. After application to the skin and after different penetration periods, the horny layer was taken off by adhesive tape stripping. The epidermis and the dermis were separated by slicing them down parallel to the skin surface in a freeze microtome. In each single layer, the amount of substance was determined and calculated relative to the applied quantity and in absolute concentrations (mug per tissue weight and molarity). Besides the expected dependence of the penetration on the type of ointment, there is a distinct dependence on the chemical structure: estriol penetrates considerably slower and in less concentrations into the living layers of the human skin than the estradiols. Furthermore, estriol reaches the dermis only in low concentrations so that this substance may be termed epidermotropic. 17 alpha-estriol which has only weak sexhormone properties in humans penetrates as well as the sexhormone 17 beta-estradiol.

摘要

研究了17α-雌二醇、17β-雌二醇和雌三醇在体外对人皮肤单层的渗透情况。将放射性标记的物质掺入4种标准软膏和一种乙醇溶液混合物中。将其涂抹于皮肤后,在不同的渗透时间后,通过胶带剥离去除角质层。在冷冻切片机中,将表皮和真皮沿与皮肤表面平行的方向切片分离。在每一层中,测定并计算相对于涂抹量的物质含量以及绝对浓度(每组织重量微克数和摩尔浓度)。除了预期的渗透对软膏类型的依赖性外,还存在对化学结构的明显依赖性:与雌二醇相比,雌三醇渗透到人体皮肤活层的速度要慢得多,浓度也低得多。此外,雌三醇仅以低浓度到达真皮,因此这种物质可称为亲表皮性的。在人体中仅具有弱性激素特性的17α-雌三醇的渗透情况与性激素17β-雌二醇相同。

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