代谢norgestimate由人类胃肠粘膜和肝微粒体体外。
文章的细节
-
引用
复制到剪贴板 -
马登,DJ
代谢norgestimate由人类胃肠粘膜和肝微粒体体外。
J类固醇生物化学杂志。1991年4月,38 (4):497 - 503。0960 - 0760 . doi: 10.1016 / (91) 90338 - 6。
- PubMed ID
-
2031863 (在PubMed]
- 文摘
-
孕激素口服避孕药的代谢norgestimate研究了体外使用人类肠道粘膜和人类肝脏微粒体。使用放射性代谢物分离高效液相色谱法(HPLC)和被co-chromatography真实的标准,通过质谱分析。组织学正常的结肠从接受各种切除术6例,黏膜2有机玻璃(美国)两院之间的安装。2 h后增加[3 h] norgestimate粘膜室,超过95%的放射性物质存在于室。代谢物分析显示38.1 + / - 11.6%(平均+ / - SD;n = 8)的药物现在norgestimate, 49.2 + / - 14.5%, 17-deacetyl norgestimate和8.1 + / - 4.5%,共轭代谢物。少量的3-keto norgestimate、甲基炔诺酮和无特征代谢物被发现。Norgestimate也是由胃组织代谢与17-deacetyl Norgestimate再次被发现的主要代谢物。从6人类肝脏微粒体准备。代谢研究在5 h NADPH的缺失和存在的时间进程。 Deacetylation to 17-deacetyl norgestimate took place in the absence of the cofactor. In the presence of NADPH, after 5 h incubation only 30.5 +/- 14.6% (mean +/- SD) of steroid present was norgestimate. The major metabolite formed was 17-deacetyl norgestimate which accounted for 39.3 +/- 20.5%. Less than 2% was present as 3-keto norgestimate but 10.0 +/- 2.3% was identified as norgestrel and 15.5 +/- 8.9% as uncharacterized metabolites. We also examined the microsomal breakdown of [3H]17-deacetyl norgestimate. This was NADPH and oxygen dependent. Norgestrel and other metabolites were formed. This study has demonstrated that norgestimate is rapidly deacetylated by both gut wall and liver. The deacetylated metabolite can then be further metabolized.
DrugBank数据引用了这篇文章
- 药物反应
-
反应 细节
