兔口服炔诺酮肟和炔诺酮的药代动力学

PHARMACOKINETICS OF NORETHINDRONE-OXIME AND NORETHINDRONE IN RABBITS AFTER ORAL ADMINISTRATION

本文用高效液相色谱分离、液闪测定放射性的方法,测定了兔口服炔诺酮肟(NETO)和炔诺酮(NET)的血浓,并比较了二者的药代动力学参数。结果表明:二者吸收迅速,从血中的消除均呈快慢两个时相。NETO在兔体内一部分迅速转变为NET,另一部分则以原药形式存在,24 h内NETO与其代谢产物NET在血清中的浓度大致各占一半。兔口服NETO与NET后,血浓—时间曲线符合二室模型,NETO的达峰时间比NET短,二者有显著差异(P<0.05),其它动力学参数无明显差异(P>0.05)。

After oral administration of [~3H]-labelled norethindrone-oxime (NETO) or norethindrone (NET) to rabbits, the blood concentrations of NETO and NET were determined by measuring the radioactivity after separation with HPLC. The pharmaeokinetie parameters of the compounds were also compared. Experimental results indicate that both NETO and NET were quickly absorbed. Their elimination from blood revealed a fast and a slow phase. One portion of NETO was metabolized to NET, and the remainder was excreted in unchanged form. The amount of NETO and its metabolite, NET, in serum were about equal within 24 hours. The serum concentration-time curves of NETO and NET adquatety fitted to a two-compartment model. There was sighifieant difference between NETO and NET in Tmax (P&lt;0.05). But no signifieant differences in other parameters (P&gt;0,05) were observed.