Heimer G M, Englund D E
Ups J Med Sci. 1984;89(2):107-15. doi: 10.3109/03009738409178470.
This study was done to evaluate the absorption of a single oral dose of 12 mg oestriol (Triovex, Leo AB, Sweden) and to confirm the hypothesis that the enterohepatic recirculation can prolong the plasma oestriol elevation obtained. Twelve menopausal women, six of whom had been cholecystectomized earlier, were given 12 mg oestriol orally. Fatty meals were given immediately after drug administration and then at four hourly intervals. Fat was given to induce the bileflow and provide oestriol to the intestine for deconjugation and enterohepatic recycling. One of the non-cholecystectomized women also remained fasting for 24 hours after oestriol administration. Plasma concentrations of unconjugated oestriol were measured by a specific RIA-method. In all women the plasma oestriol levels were considerably elevated for 24 hours. In the non-cholecystectomized women the plasma oestriol levels fluctuated in relation to meals whereas in the cholecystectomized women the fluctuations were not as pronounced, indicating that the release of biliary oestriol metabolites is the source of intestinal degradation and reabsorption to the systemic circulation. Fasting also gave increased and stable plasma oestriol levels. After a high oral dosage of oestriol, the enterohepatic recycling renders oestriol an enhanced potency since the plasma oestriol elevation time is prolonged.
本研究旨在评估单次口服12毫克雌三醇(Triovex,瑞典Leo AB公司)的吸收情况,并证实肠肝循环可延长所获得的血浆雌三醇升高时间这一假设。12名绝经后女性口服12毫克雌三醇,其中6名女性此前已接受胆囊切除术。给药后立即给予高脂餐,随后每4小时给予一次。给予脂肪以诱导胆汁流动,并为肠道提供雌三醇进行去结合和肠肝循环。1名未接受胆囊切除术的女性在给予雌三醇后也禁食24小时。采用特异性放射免疫分析法测定血浆中未结合雌三醇的浓度。所有女性的血浆雌三醇水平在24小时内均显著升高。未接受胆囊切除术的女性血浆雌三醇水平随进餐而波动,而接受胆囊切除术的女性波动不明显,这表明胆汁中雌三醇代谢产物的释放是肠道降解和再吸收进入体循环的来源。禁食也使血浆雌三醇水平升高且稳定。口服高剂量雌三醇后,由于血浆雌三醇升高时间延长,肠肝循环使雌三醇的效力增强。