Schwenk M, Frank B, Bolt H M, Winne D
Arzneimittelforschung. 1981;31(8):1254-7.
Mixtures of (14C)-estrone and (3H)-estrone-sulfate (10 micrograms and 13 micrograms, respectively) were instilled into the lumina of intact jejunal loops of rats. Estrone was faster absorbed into portal blood than was estrone-sulfate (72% vs. 17% in 30 min). In portal blood the chemical forms derived from estrone were: unchanged estrone (72%), estrone-glucuronide (14%), estrone-sulfate (5%) and estradiol (9%); no estriol was formed. The chemical forms of estrone sulfate were: estrone-sulfate (86%), estrone (6%), estrone-glucuronide (2%), estradiol (2%) and estradiol-sulfate (4%). These metabolites were also found in the lumen. It is concluded that the intestinal first-pass effects do not significantly influence the hormonal activities of the two estrogens.
将(14C)-雌酮和(3H)-雌酮硫酸盐的混合物(分别为10微克和13微克)注入大鼠完整空肠肠袢的肠腔。雌酮比雌酮硫酸盐更快地被吸收进入门静脉血(30分钟内分别为72%对17%)。门静脉血中源自雌酮的化学形式为:未变化的雌酮(72%)、雌酮葡糖醛酸苷(14%)、雌酮硫酸盐(5%)和雌二醇(9%);未形成雌三醇。雌酮硫酸盐的化学形式为:雌酮硫酸盐(86%)、雌酮(6%)、雌酮葡糖醛酸苷(2%)、雌二醇(2%)和雌二醇硫酸盐(4%)。这些代谢产物在肠腔中也有发现。结论是,肠道首过效应不会显著影响这两种雌激素的激素活性。