Pharmacokinetics of an Equol Supplement in Humans

Shaw Watanabe, Naoto Otaki, M. Uehara, Kazuharu Suzuki, T. Ueno, Shigeto Uchiyama, S. Mizuno
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引用次数: 5

Abstract

Equol, a metabolite of daidzein, is considered to be the most effective estrogen modifier in the human body. The production of equol depends on an individual's intestinal flora, however, so an equol supplement has been developed for nonproducers. To examine the pharmacokinetics in humans of a newly developed equol supplement made from fermented soy germ by Lactococcus sp. Equol supplements were given to 18 adults (20-22 yr) in three doses (one 10-mg dose, one 30-mg dose, or three 10-mg doses per day) to investigate the pharmacokinetics and physiological effects. Equol reached a peak in plasma at 30 or 60 min after supplement intake, and the average plasma half-life was 83 min. Plasma concentrations of equol were always higher in females than in males. Less than 5% of the highest plasma concentration remained in the plasma after 2 days. Up to 56% of the orally administered equol was excreted in urine within 1 day. This short-term, high-dose equol exposure yielded no observable adverse effect in both feeling and biochemical markers. For equol nonproducers, this newly developed equol supplement may yield more beneficial effects of isoflavones.
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人体内雌马酚补充剂的药代动力学
雌马酚是大豆苷元的代谢物,被认为是人体内最有效的雌激素调节剂。然而,雌马酚的产生取决于个体肠道菌群,因此为不产生雌马酚的人开发了一种雌马酚补充剂。为了研究由乳球菌(Lactococcus sp.)发酵大豆胚芽制成的一种新开发的马酚补充剂在人体内的药代动力学。研究人员给18名20-22岁的成年人服用了三种剂量的马酚补充剂(每天一次10毫克、一次30毫克或三次10毫克),以研究其药代动力学和生理效应。雌马酚在补充后30或60分钟血浆中达到峰值,平均血浆半衰期为83分钟。雌马酚的血浆浓度始终高于男性。2天后,血浆中保留的最高血药浓度不到5%。高达56%的口服马雌酚在1天内通过尿液排出。这种短期、高剂量的马雌酚暴露在感觉和生化指标上没有产生可观察到的不良影响。对于不生产雌马酚的人来说,这种新开发的雌马酚补充剂可能产生更多的异黄酮有益效果。
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