Schubert W, Cullberg G
Department of Obstetrics and Gynecology, Ostra Sjukhuset, University of Gothenburg, Sweden.
Acta Obstet Gynecol Scand. 1987;66(6):543-7. doi: 10.3109/00016348709015732.
Ovulation inhibition and bleeding control with a combination of 0.5 mg 17 beta-estradiol cyclo-octyl acetate (E2COA) and 0.15 mg desogestrel was investigated in 10 regularly menstruating women for 21 days. In half the group the treatment was extended for 7 days (days 22-28) with 0.03 mg desogestrel in order to evaluate any posttreatment influence on the gonadotropin levels. E2COA, beeing a long-chain fatty ester dissolved in oil, was expected to be resorbed from the intestinal wall via the lymphatic system. By incorporating it in the chylomicrons, E2COA would thereby avoid the unfavourable first liver pass. The serum levels of progesterone were suppressed during treatment. No increase in 17 beta-estradiol (E2) concentration was found; levels remained low and even during medication. No peak values of gonadotropins were seen. Thus follicular hormonal activity and ovulation was inhibited by this combination. Bleeding control was, however unacceptable in all volunteers. The addition of desogestrel during the fourth investigation week apparently did not induce any hormonal differences. The estrogenic activity is shown by the low, even S-E2 levels, but the dosage of E2COA seems to be too low in relation to progestogen dosage. Further studies will have to be performed in order to find the ideal combination.
对10名月经周期规律的女性进行了为期21天的研究，以探究0.5毫克17β - 雌二醇环辛酯（E2COA）与0.15毫克去氧孕烯联合使用对排卵的抑制作用和出血控制情况。在该组的一半受试者中，治疗延长7天（第22 - 28天），给予0.03毫克去氧孕烯，以评估治疗后对促性腺激素水平的任何影响。E2COA是一种溶解于油中的长链脂肪酸酯，预计可通过淋巴系统从肠壁吸收。通过将其纳入乳糜微粒，E2COA可避免不利的首过肝效应。治疗期间孕酮的血清水平受到抑制。未发现17β - 雌二醇（E2）浓度升高；水平在用药期间一直保持较低。未观察到促性腺激素的峰值。因此，这种联合用药抑制了卵泡的激素活性和排卵。然而，所有志愿者的出血控制情况均不理想。在第四个研究周添加去氧孕烯显然未引起任何激素差异。低且稳定的S - E2水平显示出雌激素活性，但相对于孕激素剂量，E2COA的剂量似乎过低。为找到理想的联合用药方案，还需进行进一步研究。
