单剂药物动力学Nestorone,潜在的女用避孕。
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普拉萨德PV,巴希尔M, Sitruk-Ware R, Kumar N
单剂药物动力学Nestorone,潜在的女用避孕。
类固醇。2010年3月,75 (3):252 - 64。doi: 10.1016 / j.steroids.2009.12.011。Epub 2010年1月11日。
- PubMed ID
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20064539 (在PubMed]
- 文摘
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一种合成黄体酮Nestorone正在开发女性节育。这个研究来确定的分布、代谢、排泄出现Nestorone ((3) H Nestorone)在成年雌性老鼠。老鼠皮下注射(南卡罗来纳州)的单剂量400 microCi (3) H Nestorone /公斤。其分布和血液中浓度,血浆和其他组织在定义的时间确定。消除的排泄物进行(3)H Nestorone。分析了放射性物质在所有样本液体闪烁计数器。代谢物分析是由高效液相色谱和LC / MS分析等离子体,尿液和粪便样本。(3)H Nestorone皮下注射后,放射性物质的平均峰值浓度(C (max))在血液和血浆58.1和95.5 ng电化学当量(3)H Nestorone / g,分别在2 H postdose (T (max))。之后,药物的浓度逐渐下降通过与终端96 - h postdose消除半衰期(t (1/2)) 15.6 h。(3) h Nestorone-derived放射性物质是广泛分布在大多数组织由0.5 h,达到平均最大浓度2 h postdose。大约81.4%和7.62%的服用剂量是通过粪便和尿液排出,分别。 In vivo metabolism of (3)H Nestorone resulted into a total of 19 metabolites. Among them, two metabolites viz., 17alpha-deacetyl-Nestorone (M9) and 4,5-dihydro-17alpha-deacetyl-Nestorone (M19) were identified by HPLC and LC/MS analysis. Metabolite profiling of plasma samples showed that most of the circulating radioactivity was associated with unchanged parent drug, and M19. The M19 was a major metabolite in the profiled urine and feces samples. Presence of large proportion of drug/drug-related material in feces suggested that the biliary excretion is a main elimination route of (3)H Nestorone. The distribution, metabolism, and excretion profiles of (3)H Nestorone obtained in this study provide a fairly good insight about its fate in women.
