Stanczyk F Z, Brenner P F, Mishell D R, Ortiz A, Gentzschein E K, Goebelsmann U
Contraception. 1978 Dec;18(6):615-33. doi: 10.1016/0010-7824(78)90046-x.
A sensitive and reliable radioimmunoassay (RIA) for the measurement of norethindrone (NET) in serum has been established employing anti-11 alpha-hydroxynorethindrone 11-hemisuccinyl-bovine serum albumin serum in conjunction with norethindrone-3-(0-carboxymethyl) oximino-[125I]-iodohistamine. Of a number of ring A reduced NET metabolites, only 17 beta-hydroxy-17 alpha-ethinyl-5 beta-estran-3-one (43%) and 17 alpha-ethinyl-5 alpha-estrane-3 beta, 17 beta-diol (15.7%) cross-reacted appreciably in this RIA. Ethinyl estradiol (EE2) and mestranol (MEE2) exhibited cross-reactions of only 1.1 and 0.4%, respectively. Serum NET levels were measured in four groups of 3 women, each ingesting either 1 mg NET plus 0.05 mg MEE2 (Norinyl 1 + 50 or Ortho Novum 1/50), 0.5 mg NET plus 0.035 mg EE2 (Brevicon) or only 0.35 mg NET (Micronor) daily for 5 consecutive days. Peak serum NET levels were observed within 1/2 to 4 hours after oral intake and fell precipitously thereafter. After reaching a maximum, serum NET concentrations declined in a manner consistent with at least two disposition phases. The average half-life for the first disposition phase was 2.3, 3.4, 3.9 and 4.4 hours in subjects ingesting Norinyl 1 + 50, Ortho Novum 1/50, Brevicon and Micronor, respectively. Peak and 3-hour post-ingestion serum NET concentrations were dose-related but showed considerable subject-to-subject variations. Following discontinuation of tablet intake, serum NET levels remained detectable (greater than 0.05 ng/ml) for at least 5 days in all 3 women who had taken Ortho Novum 1/50, but in none of the other 9 volunteers. These results suggest that different preparations of identical doses and combinations of oral contraceptive steroids may yield different serum NET profiles. However, due to considerable subject-to-subject variations, larger numbers of subjects are required for a conclusive investigation.
已建立一种灵敏可靠的放射免疫分析法（RIA），用于测定血清中的炔诺酮（NET），该方法采用抗11α - 羟基炔诺酮11 - 半琥珀酰 - 牛血清白蛋白血清，结合炔诺酮 - 3 -（邻羧甲基）肟基 - [125I] - 碘组胺。在多种A环还原的NET代谢物中，只有17β - 羟基 - 17α - 乙炔基 - 5β - 雌甾 - 3 - 酮（43%）和17α - 乙炔基 - 5α - 雌甾烷 - 3β，17β - 二醇（15.7%）在该RIA中表现出明显的交叉反应。乙炔雌二醇（EE2）和炔雌醇甲醚（MEE2）的交叉反应分别仅为1.1%和0.4%。对四组每组3名女性的血清NET水平进行了测定，她们分别连续5天每天服用1 mg NET加0.05 mg MEE2（诺雷得1 + 50或 Ortho Novum 1/50）、0.5 mg NET加0.035 mg EE2（短效避孕片）或仅0.35 mg NET（迷你避孕丸）。口服后1/2至4小时观察到血清NET水平峰值，此后急剧下降。达到最大值后，血清NET浓度以符合至少两个处置阶段的方式下降。在服用诺雷得1 + 50、Ortho Novum 1/50、短效避孕片和迷你避孕丸的受试者中，第一个处置阶段的平均半衰期分别为2.3、3.4、3.9和4.4小时。摄入后峰值和3小时的血清NET浓度与剂量相关，但个体间差异较大。停止服用片剂后，在所有服用Ortho Novum 1/50的3名女性中，血清NET水平在至少5天内仍可检测到（大于0.05 ng/ml），但在其他9名志愿者中均未检测到。这些结果表明，相同剂量和组合的口服避孕甾体药物的不同制剂可能产生不同的血清NET谱。然而，由于个体间差异较大，需要更多受试者进行确定性研究。
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