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地索高诺酮是一种口服的孕激素,它代谢为3-酮-地索高诺酮,后者具孕激素效应,体内外研究已证实地索高诺酮迅速转化为其活性代谢物,Hasenack等近年报告了10例口服地索高诺酮(+乙炔雌二醇EE_2)和口服3-酮-地索高诺酮(+EE_2)的交叉试验,他们发现口服上述二药后3-酮-地索高诺酮的曲线下面积(AUC)相似,他们认为此药生物转化迅速,似乎不受肝脏代谢能力的限制,但同一对象给地索高诺酮后血中3-酮-地索高诺酮的AUC是给3-酮-地索高诺酮AUC的49.7～129.7%。为了正确评价3-酮-地索高诺酮的生物利用度,作者测定了口服和静注3-酮-地索高诺酮后
Desopostone is an oral progestin that is metabolized to 3-keto-desogestrel, which has a progestin effect, and in vivo and in vitro studies have shown that desopostone is rapidly converted to its active metabolite In recent years, Hasenack et al. Reported 10 oral crossover trials of sogassone (+ ethinyl estradiol EE 2) and oral 3-keto-desosogostone (+ EE 2). They found that oral administration of 3- The area under the curve (AUC) for keto-desosoogone was similar, and they considered the drug to be rapidly biotranslated and appeared to be unrestricted by the liver’s metabolic capacity, but the same subject gave 3-keto- The AUC of sorbitol was 49.7 to 129.7% for the 3-keto-descorpine AUC. In order to properly evaluate the bioavailability of 3-keto-desogestrel, the authors measured the effects of oral and intravenous 3-keto-desosolnolone