Suzuki H, Furukawa H, Miyazaki H, Hashimoto M
Radioisotopes. 1977 Mar;26(3):152-7.
Absorption, distribution, excretion and metabolism of SC-11800EE, a combined steroid preparation consisting of SC-11800(ethynodiol diacetate)as gestagen and ethinyl estradiol (EE)as estrogen in 20:1 (w:w), were studied with the use of 14C-SC-11800 and 3H-EE by radiometry in female rats and by the whole body autoradiography in female normal and pregnant mice. The gestagen orally given with EE was rapidly absorbed from digestive tracts and distributed in tissues in various levels. Gestagen levels in liver and kidney exceeded that in plasma. About 75% of dosed radioactivity was excreted in feces largely via bile and more than 20% in urine within 72 hr after administration. The gestagen was metabolized extensively to more polar products and their conjugates. The pharmacokinetic behavior of the gestagen given with EE did not alter after repeated administrations for 7 days, but was slightly different from that without EE, possibly due to the estrogen effect. The pharmacokinetic behavior of the estrogen was independent from the gestagen given simultaneously. The distribution of the gestagen given with EE revealed by the whole body autoradiography in normal mice were essentially consistent with the radiometric results in rats and that in the pregnant mice showed that the gestagen in fetus was virtually nil under the present conditions.
对SC - 11800EE（一种由作为孕激素的SC - 11800（双醋炔诺醇）和作为雌激素的炔雌醇（EE）按20:1（重量比）组成的复方甾体制剂）的吸收、分布、排泄和代谢进行了研究。在雌性大鼠中采用放射测量法，在雌性正常和怀孕小鼠中采用全身放射自显影法，使用14C - SC - 11800和3H - EE进行研究。与EE一起口服给予的孕激素迅速从消化道吸收，并以不同水平分布于组织中。肝脏和肾脏中的孕激素水平超过血浆中的水平。给药后72小时内，约75%的给药放射性主要通过胆汁经粪便排出，超过20%经尿液排出。孕激素被广泛代谢为极性更强的产物及其结合物。与EE一起给予的孕激素在重复给药7天后其药代动力学行为未改变，但与未与EE一起给药时略有不同，这可能是由于雌激素的作用。雌激素的药代动力学行为与同时给予的孕激素无关。在正常小鼠中通过全身放射自显影显示的与EE一起给予的孕激素的分布与大鼠中的放射测量结果基本一致，而在怀孕小鼠中的结果表明，在当前条件下胎儿中的孕激素几乎为零。
