Sahlberg B L, Landgren B M, Axelson M
J Steroid Biochem. 1987 May;26(5):609-17. doi: 10.1016/0022-4731(87)90014-8.
Conjugated ethynyl and endogenous steroids in plasma and urine from two women taking an oral contraceptive (Conlumin) containing 1 mg norethindrone and 50 micrograms mestranol have been analyzed by methods based on anion and ligand exchange chromatography and gas chromatography-mass spectrometry. Conjugated norethindrone and its reduced metabolites with 3 alpha,5 alpha, 3 alpha,5 beta, 3 beta,5 beta and 3 beta,5 alpha configurations were identified in the fluids. The quantitatively major metabolites in plasma were a disulphate of the 3 alpha,5 alpha isomer and a monosulphate of the 3 alpha,5 beta isomer. The renal clearance of the former compound was low. The major urinary metabolite of norethindrone was the 3 alpha,5 beta isomer conjugated with glucuronic or sulphuric acid. Disulphates constituted only a small portion of urinary ethynyl steroids. Metabolic profiles of endogenous neutral steroids in plasma and urine during the contraceptive cycle were compared with profiles during a physiological menstrual cycle. The concentrations of steroids in plasma during contraception were similar to those during the follicular and mid phases of the menstrual cycle, whereas levels of progesterone metabolites were higher in the luteal phase. The urinary excretion of steroids was 15-30% lower during the contraceptive cycle, due to a decrease in excretion of C21O5 steroids, 11-oxygenated androgens and etiocholanolone. The increase of urinary progesterone metabolites seen during the luteal phase was not observed during contraception, but the excretion of 5 beta-pregnane-3 alpha,20 alpha-diol glucuronide was higher than during the follicular and mid phases of the menstrual cycle.
采用基于阴离子和配体交换色谱以及气相色谱 - 质谱联用的方法，对两名服用含1毫克炔诺酮和50微克炔雌醇甲醚口服避孕药（Conlumin）的女性血浆和尿液中的共轭乙炔基及内源性甾体进行了分析。在这些体液中鉴定出了具有3α,5α、3α,5β、3β,5β和3β,5α构型的共轭炔诺酮及其还原代谢产物。血浆中定量占主要的代谢产物是3α,5α异构体的二硫酸盐和3α,5β异构体的单硫酸盐。前一种化合物的肾清除率较低。炔诺酮的主要尿代谢产物是与葡萄糖醛酸或硫酸结合的3α,5β异构体。二硫酸盐仅占尿中乙炔基甾体的一小部分。将避孕药周期中血浆和尿液内源性中性甾体的代谢谱与生理月经周期中的代谢谱进行了比较。避孕期间血浆中甾体的浓度与月经周期卵泡期和中期相似，而黄体期孕酮代谢产物的水平较高。避孕周期中甾体的尿排泄量降低了15 - 30%，这是由于C21O5甾体、11 - 氧化雄激素和本胆烷醇酮的排泄减少所致。在避孕期间未观察到黄体期出现的尿孕酮代谢产物增加情况，但5β - 孕烷 - 3α,20α - 二醇葡萄糖醛酸的排泄量高于月经周期的卵泡期和中期。
