Täuber U, Kuhnz W, Hümpel M
Research Laboratories, Schering AG, Berlin, West Germany.
Am J Obstet Gynecol. 1990 Oct;163(4 Pt 2):1414-20. doi: 10.1016/0002-9378(90)91358-j.
The pharmacokinetic and protein-binding properties of gestodene and ethinyl estradiol have been investigated after single and multiple dosing in several studies in 83 healthy, young women. After oral administration, gestodene is completely absorbed and bioavailable and exhibits dose-linear pharmacokinetics. During long-term pill use, serum levels of gestodene were four to five times higher than after single administration, showing a periodic increase from day 1 to day 10 during each cycle. Ultrafiltration studies revealed that 75.3% of total serum gestodene is bound to sex hormone-binding globulin, 24.1% is bound to albumin, and only 0.6% is not protein bound. Thus gestodene levels during steady state are explained by an increase in sex hormone binding-globulin as a result of concomitant administered ethinyl estradiol and a specific binding of gestodene to this protein. Serum levels of ethinyl estradiol during single and multiple administration were identical and were not different from those observed with another preparation containing 30 micrograms of ethinyl estradiol.
在针对83名健康年轻女性开展的多项研究中，对孕二烯酮和炔雌醇进行了单剂量和多剂量给药后的药代动力学及蛋白结合特性研究。口服给药后，孕二烯酮可被完全吸收并具有生物利用度，且呈现出剂量线性药代动力学特征。在长期服用避孕药期间，孕二烯酮的血清水平比单次给药后高出四至五倍，在每个周期内从第1天到第10天呈周期性升高。超滤研究显示，血清中总孕二烯酮的75.3%与性激素结合球蛋白结合，24.1%与白蛋白结合，只有0.6%未与蛋白结合。因此，稳态期间孕二烯酮水平的升高是由于同时服用炔雌醇导致性激素结合球蛋白增加以及孕二烯酮与该蛋白的特异性结合所致。单次和多次给药期间炔雌醇的血清水平相同，且与另一含30微克炔雌醇制剂所观察到的水平无异。
