【摘要】 本文应用[~3H)标记化合物。采用高效液相(HPLC)反相色谱及放射检测技术,研究了醋炔诺酮肟(NETO-AC),醋炔诺酮(NET-AC)经口给药后在兔体内的药代动力学过程。实验结果表明,NETO-AC和NET-AC在兔体内迅速吸收并水解,原型药NETO-AC和含乙酰基的代谢产物NET-AC的血浓甚低,而不含乙酰基的代谢产物炔诺酮肟(NETO)和炔诺酮(NET)的血浓较高,后二者是NETO-AC在兔体内发挥药理作用的主要形式,其体内处置方式符合口服二室模型。更多还原

【Abstract】 Pharmacokinetic studies of norethindrone-oxime(NETO-AC) and nore-thindrone acetate(NET-AC) were carried out after an oral administration of labelled steroids to rabbits. Radioactivities in serum samples were counted after reverse phase HPLC separation. The experimental results indicate that NETO-AC and NET-AC were quickly absorbed and hydrolyzed. The serum concentrations of the original drug NETO-AC and its acetylated metabolite NET-AC are quite low, and those of non-acetylated products NETO and NET are obviously higher. Therefore, the latter two metabolites are the main ones which exert pharmacolgical actions on the body. Their disposition could be described as two-compartment model. NET-AC was hyd-rolysed into NET in rabbits. The blood concentrations of NET within 12 hours are higher than those of the original drug NET-AC. The serum concentration-time curve of NET was also adequately fitted by a two-compartment model.更多还原