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Norgestimate,一种具有最少雄激素活性的孕激素的临床前评价
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作者 张云山 《国外医学(计划生育分册)》 北大核心 1994年第1期30-32,共3页
Norgestimate(NGM)是一种新的具有高度选择性的促孕活性及最低的雄激素活性的孕激素。在家兔,NGM与子宫孕激素受体结合,剌激子宫内膜,抑制排卵。NGM直接作用于靶器官,当注入宫腔的,可剌激家兔子宫内膜,而注入培养中的分散的大鼠垂体细胞... Norgestimate(NGM)是一种新的具有高度选择性的促孕活性及最低的雄激素活性的孕激素。在家兔,NGM与子宫孕激素受体结合,剌激子宫内膜,抑制排卵。NGM直接作用于靶器官,当注入宫腔的,可剌激家兔子宫内膜,而注入培养中的分散的大鼠垂体细胞中,则抑制LHRH对LH释放的刺激作用。NGM无雌激素活性,相反,与其它孕激素一样,抑制雌激素的作用。而与其它一些孕激素不同的是,NGM相对无雄激素活性。与左旋18甲基炔诺酮(LNG)及gestodene和比,NGM及其17-去乙酰代谢物对雌激素受体的亲和力很弱,当其作为未成熟大鼠前列腺生长的刺激物时,未显示出雄激素活性。NGM缺乏与人类性激素结合球蛋白的亲和力,这一点是其具有最低的雌激素活性的更有力的证据。 展开更多
关键词 norgestimate 孕激素 药理学
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Quantification of 17-desacetyl norgestimate in human plasma by liquid chromatography–tandem mass spectrometry (LC–MS/MS) and its application to bioequivalence study
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作者 Ashish Saxena Arun Kumar Gupta +3 位作者 V.Praveen Kumar M.Sundaramoorthi Nainar Manoj Bob Ravisekhar Kasibhatta 《Journal of Pharmaceutical Analysis》 SCIE CAS 2015年第2期93-100,共8页
A rapid and sensitive ultra-performance liquid chromatography–tandem mass spectrometry(UPLC–MS/MS) method was developed and validated for the estimation of 17-desacetyl norgestimate in human plasma using solid-pha... A rapid and sensitive ultra-performance liquid chromatography–tandem mass spectrometry(UPLC–MS/MS) method was developed and validated for the estimation of 17-desacetyl norgestimate in human plasma using solid-phase extraction technique. 17-desacetyl norgestimate D6 was used as the internal standard. Simple gradient chromatographic conditions and mass spectrometric detection enabled accurate and precise measurement of 17-desacetyl norgestimate at sub-picogram levels. The proposed method was validated for a linear range of 20–5000 pg/m L with a correlation coefficient Z 0.9988. The intra-run and inter-run precision and accuracy were within 10%. The overall recoveries for 17-desacetyl norgestimate and 17-desacetyl norgestimate D6 were 96.30% and 93.90%, respectively. The total run time was 4.5 min. The developed method was applied for the determination of the pharmacokinetic parameters of 17-desacetyl norgestimate following a single oral administration of a norgestimate and ethinyl estradiol0.250 mg/0.035 mg tablets in 35 healthy female volunteers. 展开更多
关键词 17-desacetyl norgestimate UPLC–MS/MS Human plasma
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