Schwenk M, Schiemenz C, del Pino V L, Remmer H
Naunyn Schmiedebergs Arch Pharmacol. 1982 Dec;321(3):223-5. doi: 10.1007/BF00505490.
The intestinal absorption and biotransformation of ethinylestradiol and of ethinylestradiol glucuronide in rats were studied using a jejunal loop preparation in situ. Radioactivity associated with ethinylestradiol almost completely appeared in the venous outflow within 80 min. Forty two percent was present as unchanged compound, 56% in the glucuronide fraction and 2% as sulfate ester. Absorption of ethinylestradiol glucuronide was about 20 times slower than absorption of the nonconjugated molecule. The data indicate, that intestinal absorption of ethinylestradiol involves several superimposed kinetics and that glucuronidation in the gut may result in a decreased bioavailability of the compound.
采用原位空肠袢制备法，对大鼠体内乙炔雌二醇及其葡萄糖醛酸结合物的肠道吸收和生物转化进行了研究。与乙炔雌二醇相关的放射性物质在80分钟内几乎完全出现在静脉流出物中。42%为未变化的化合物，56%在葡萄糖醛酸结合物部分，2%为硫酸酯。乙炔雌二醇葡萄糖醛酸结合物的吸收比未结合分子的吸收慢约20倍。数据表明，乙炔雌二醇的肠道吸收涉及多种叠加动力学，且肠道中的葡萄糖醛酸化可能导致该化合物的生物利用度降低。
