Lyrenäs S, Carlström K, Bäckström T, von Schoultz B
Br J Obstet Gynaecol. 1981 Feb;88(2):181-7.
Equivalent doses of oestradiol-17 beta were given orally and percutaneously to eight post-menopausal women and three men. The resultant serum levels of unconjugated immunoreactive oestrogens and total oestrone were followed during 48 hours after hormone administration. A single percutaneous dose of 4 mg oestradiol-17 beta resulted in increased serum levels of oestradiol-17 beta in all individuals. Compared to oral administration the increase in serum oestrogen levels was quite slow and they were maintained for 48 hours. In contrast to the rapid and very marked increase in serum total oestrone following oral administration of oestradiol-17 beta, only a moderate increase was obtained after percutaneous administration and there was a tendency to a biphasic pattern. Topical administration of oestradiol-17 beta might have physiological advantages as the steroid will reach the peripheral circulation without passing the entero-hepatic circulation.
对8名绝经后女性和3名男性口服和经皮给予等量的17β-雌二醇。在激素给药后48小时内监测所产生的血清中未结合免疫反应性雌激素和总雌酮水平。经皮单次给予4mg 17β-雌二醇后,所有个体的血清17β-雌二醇水平均升高。与口服给药相比,血清雌激素水平升高相当缓慢且维持48小时。与口服17β-雌二醇后血清总雌酮迅速且显著升高相反,经皮给药后仅出现中度升高,且有呈双相模式的趋势。17β-雌二醇局部给药可能具有生理优势,因为该类固醇无需经过肠肝循环即可进入外周循环。