Johnson M E, Blankschtein D, Langer R
Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge 02139, USA.
J Pharm Sci. 1995 Sep;84(9):1144-6. doi: 10.1002/jps.2600840922.
The permeabilities of many steroids through human skin have been previously measured and reported in the literature. Analysis of these data reveals that significant discrepancies exist between the measurements of Scheuplein et al. and those of other groups. Six of the 14 steroids which were examined by Scheuplein et al., aldosterone, corticosterone, estradiol, hydrocortisone, progesterone, and testosterone, have also been examined by other groups. For each of these steroids, the permeability measurements of Scheuplein et al. are lower than those reported by other groups by factors of between 5.0 and 77. Eight independent measurements of the permeability of estradiol are in good agreement with one another, but are greater than the value reported by Scheuplein et al. by factors of between 11 and 20. Several possible sources of experimental error, including the variability of the skin samples, the differences in the experimental temperature, the establishment of steady-state conditions, the use of radiolabeled drugs, and the skin preparation technique, have been considered and do not appear to account for the magnitude of the observed discrepancies nor for the fact that the data of Scheuplein et al. are consistently lower than those reported by other groups.
此前已有文献报道了多种甾体激素透过人体皮肤的渗透率。对这些数据的分析表明,舍普林等人的测量结果与其他研究小组的测量结果之间存在显著差异。舍普林等人检测的14种甾体激素中,有6种,即醛固酮、皮质酮、雌二醇、氢化可的松、孕酮和睾酮,也被其他研究小组检测过。对于每种甾体激素,舍普林等人测得的渗透率均低于其他研究小组报告的值,两者相差5.0至77倍。对雌二醇渗透率的8次独立测量结果彼此吻合良好,但比舍普林等人报告的值高出11至20倍。已考虑了几个可能的实验误差来源,包括皮肤样本的变异性、实验温度的差异、稳态条件的建立、放射性标记药物的使用以及皮肤制备技术,但这些因素似乎既不能解释所观察到的差异程度,也不能解释舍普林等人的数据始终低于其他研究小组报告的数据这一事实。