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皮质类固醇的经皮吸收:年龄、部位及皮肤切片对氢化可的松在无毛小鼠皮肤中渗透速率的影响。

Percutaneous absorption of corticosteroids: age, site, and skin-sectioning influences on rates of permeation of hairless mouse skin by hydrocortisone.

作者信息

Behl C R, Flynn G L, Linn E E, Smith W M

出版信息

J Pharm Sci. 1984 Sep;73(9):1287-90. doi: 10.1002/jps.2600730925.

Abstract

As part of a long-range plan to decipher the mechanism of mass transfer of corticosteroids across skin, the permeation of [3H]hydrocortisone through hairless mouse skin was characterized by in vitro diffusion cell techniques. Age and anatomical site-related behaviors were explored mainly with whole skin but also with skin stripped of its horny layer. Permeability of the mouse skin was low shortly after birth and increased during the singular normal hair cycle exhibited by the SKH-hr-1 mouse strain. The return to a hairless state over a period of 20-35 d was accompanied by decreased permeability of hydrocortisone. A permeability coefficient of approximately 2 X 10(-4) cm/h was found for the mature mouse. For whole skin, there was no difference in the permeabilities of dorsal and abdominal skin sections, but for stratum corneum-free membranes and dermal membranes, the abdominal site appeared to be more permeable, which is consistent with its thinner dimensions. Totally stripped skin and isolated dermis are approximately 500 and approximately 1000 times more permeable than intact skin, respectively; the unaltered stratum corneum of the hairless mouse is thus shown to be the major barrier to the mass transfer of hydrocortisone.

摘要

作为解析皮质类固醇经皮传质机制长期计划的一部分,采用体外扩散池技术对[3H]氢化可的松在无毛小鼠皮肤中的渗透情况进行了表征。主要通过全皮并结合去除角质层的皮肤来探究年龄和解剖部位相关的渗透行为。SKH-hr-1小鼠品系在单一正常毛发生长周期中,出生后不久小鼠皮肤的渗透性较低,随后渗透性增加。在20 - 35天的时间内恢复到无毛状态的过程中,氢化可的松的渗透性降低。成熟小鼠的渗透系数约为2×10(-4) cm/h。对于全皮而言,背部和腹部皮肤切片的渗透性没有差异,但对于无角质层的皮肤膜和真皮膜,腹部部位的渗透性似乎更高,这与其更薄的尺寸相符。完全去除表皮的皮肤和分离的真皮的渗透性分别比完整皮肤高约500倍和约1000倍;因此,无毛小鼠未改变的角质层被证明是氢化可的松传质的主要屏障。

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