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炔诺酮(17α-乙炔基-17β-羟基-4-雌甾烯-3-酮)和乙炔雌二醇(17α-乙炔基-1,3,5,(10)-雌甾三烯-3,17β-二醇)的放射免疫测定。该甾体口服后在人体血浆中炔诺酮测定的应用。

Radioimmunoassay of norethindrone (17 alpha-ethynyl-17 beta-hydroxy-4-estren-3-one) and ethynyl-estradiol (17 alpha-ethynyl-1,3,5, (10)-estratien-3, 17 beta-diol). Application to human plasma determination of norethindrone after oral administration of this steroid.

作者信息

Pasqualini J R, Castellet R, Portois M C, Hill J L, Kincl F A, Cortes-Prieto J

出版信息

Reproduccion. 1975 Jul-Dec;2(3-4):197-205.

PMID:1232004
Abstract

The experiment conditions for the evaluation of Norethindrone (17 alpha-Ethynyl-17 beta-hydroxy-4-estren-3-one, NET) and Ethynyl-estradiol (17 alpha-ethynyl-1, 3, 5 (10) estratrien-3, 17 beta-diol, EE) by radioimmunoassay are described. A minimal quantity of 25 pg of these two steroids could be evaluated using different reduced metabolites of NET, very little cross reaction is observed with 200 pg of these metabolites. No effect was observed with estradiol for the EE-antiserum. The NET-antiserum was used to evaluate this steroid and ethynodiol diacetate after oral administration to female volunteers. Maximal values in the plasma (2-3% of the administered dose) was found between 1-3 h after administration and at 24 h a concentration of 0.1-0.3% still remained in the plasma.

摘要

描述了通过放射免疫测定法评估炔诺酮(17α-乙炔基-17β-羟基-4-雌甾烯-3-酮,NET)和炔雌醇(17α-乙炔基-1,3,5(10)雌甾三烯-3,17β-二醇,EE)的实验条件。使用NET的不同还原代谢物可评估这两种甾体的最小量为25皮克,观察到与200皮克这些代谢物的交叉反应非常少。对于EE抗血清,未观察到雌二醇有影响。NET抗血清用于评估该甾体以及口服给予女性志愿者后的双醋炔诺醇。给药后1 - 3小时血浆中出现最大值(为给药剂量的2 - 3%),并且在24小时时血浆中仍残留0.1 - 0.3%的浓度。

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引用本文的文献

1
Clinical pharmacokinetics of oral contraceptive steroids.口服避孕甾体激素的临床药代动力学。
Clin Pharmacokinet. 1983 Mar-Apr;8(2):95-136. doi: 10.2165/00003088-198308020-00001.
2
Bioavailability of norethindrone in human subjects.
Eur J Clin Pharmacol. 1978 Mar 17;13(1):35-9. doi: 10.1007/BF00606680.