During a cross-over study, the pharmacokinetics of ethinylestradiol (EE) and 3-keto-desogestrel (KDG) were investigated on days 7 and 22 of one cycle of treatment with two biphasic formulations containing 50 micrograms EE (7 tablets) and 50 micrograms EE + 125 micrograms desogestrel (DG) (15 tablets) (50/50 EE) or 40 micrograms EE + 25 micrograms DG (7 tablets) and 30 micrograms EE + 125 micrograms DG (15 tablets) (40/30 EE). Peak serum levels and areas under the curve of EE increased significantly by 50% between days 7 and 22 of those taking 50/50 EE, while during treatment with 40/30 EE, no difference was found between days 7 and 22. Both formulations caused identical KDG levels on day 22. There were only slight differences in the effects of both preparations on sex-hormone-binding globulin (SHBG; +150 to +160%) and on corticosteroid-binding globulin (CBG; +130 to +150%) on day 7. On day 22, the changes were more pronounced with 50/50 EE (SHBG, +310%; CBG, +240%) than with 40/30 EE (SHBG, +250%; CBG, +180%). On day 22 after discontinuation of treatment, the SHBG and CBG levels were still significantly above the control values. Using both formulations, LH and FSH levels were significantly suppressed on day 22, while on day 7 no significant reduction was observed. The rise in the EE levels between days 7 and 22 of 50/50 EE intake and the time course of the EE concentrations during treatment with 40/30 EE appear to be due to an inhibition of hepatic metabolism by the contraceptive steroids, as EE is nearly exclusively bound to albumin which does not change.

译文

:在交叉研究中,在一个疗程的第7天和第22天研究了乙炔雌二醇(EE)和3-酮-去氧孕烯(KDG)的药代动力学,其中两种双相制剂分别含有50毫克EE(7片)和50毫克微克EE 125微克去氧孕烯(15片)(50/50 EE)或40微克EE 25微克DG(7片)和30微克EE 125微克DG(15片)(40/30 EE)。在服用50/50 EE的患者的7至22天之间,血清峰值水平和EE曲线下的面积显着增加了50%,而在使用40/30 EE的患者中,在7和22天之间没有发现差异。第22天的KDG水平相同。在第7天,两种制剂对性激素结合球蛋白(SHBG; 150%至160%)和对皮质类固醇结合球蛋白(CBG; 130%至150%)的作用仅有微小差异。在第22天,与使用40/30 EE(SHBG,250%; CBG,180%)相比,使用50/50 EE(SHBG,310%; CBG,240%)的变化更为明显。在停药后第22天,SHBG和CBG水平仍显着高于对照值。使用这两种配方,LH和FSH水平在第22天被显着抑制,而在第7天未观察到显着降低。在50/50 EE摄入量的第7天到22天之间,EE水平升高以及在用40/30 EE治疗期间EE浓度随时间变化的过程似乎是由于避孕类固醇抑制了肝代谢,因为EE是几乎只与不变的白蛋白结合。

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