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口服去氧孕烯和3-酮-去氧孕烯后血清中3-酮-去氧孕烯的水平。

Serum levels of 3-keto-desogestrel after oral administration of desogestrel and 3-keto-desogestrel.

作者信息

Hasenack H G, Bosch A M, Käär K

出版信息

Contraception. 1986 Jun;33(6):591-6. doi: 10.1016/0010-7824(86)90047-8.

Abstract

In a cross-over study with orally administered desogestrel (0.150 mg) plus ethinyloestradiol (0.030 mg) and 3-keto-desogestrel (0.150 mg) plus ethinyloestradiol (0.030 mg) in ten women under steady-state conditions, the serum levels of 3-keto-desogestrel were monitored by radioimmunoassay. No statistically significant differences between treatment groups were found with respect to the areas under the curve of the serum levels versus time (AUC), peak heights and peak times. The individual AUCs for 3-keto-desogestrel after dosing with desogestrel (plus EE) or 3-keto-desogestrel (plus EE) show a similar degree of variation. The biotransformation of desogestrel into 3-keto-desogestrel is rapid and appears not to be limited by the metabolic capacity of the normal liver.

摘要

在一项交叉研究中,对10名处于稳态的女性口服去氧孕烯(0.150毫克)加炔雌醇(0.030毫克)以及3 - 酮 - 去氧孕烯(0.150毫克)加炔雌醇(0.030毫克)后,通过放射免疫分析法监测3 - 酮 - 去氧孕烯的血清水平。在血清水平随时间变化的曲线下面积(AUC)、峰值高度和峰值时间方面,各治疗组之间未发现统计学上的显著差异。服用去氧孕烯(加炔雌醇)或3 - 酮 - 去氧孕烯(加炔雌醇)后,3 - 酮 - 去氧孕烯的个体AUC显示出相似程度的变化。去氧孕烯向3 - 酮 - 去氧孕烯的生物转化迅速,且似乎不受正常肝脏代谢能力的限制。

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