孕妇及非孕妇口服不同剂量RU 486后的药物动力学研究  

Pharmacokinetic Study on RU 486 and Its Metabolites After Oral Administration of Various Doses in Pregnant and.Non-pregnant Women

作　　者：石永恩 叶智厚 贺昌海[1] 张国庆[1] 江乃雄 史美贞 许建秋[1] 白秀梅[1] 

机构地区：[1]上海市计划生育科学研究所 [2]上海市计算技术研究所

出　　处：《生殖与避孕》1992年第1期8-14,共7页Reproduction and Contraception

摘　　要：非孕妇(n=9)及早孕妇(n=36)口服不同剂量RU 486后,以HPLC测定服药后RU486及其代谢产物RU 42633、RU 42848和RU 42698的血浆浓度,结果显示不论妊娠与否,药物的吸收及代谢都很迅速;服药后20 min 即可测得血浆中的RU 486及其代谢产物;母药达峰时间Tmax 均为1～2h,其峰浓度Cmax 对数与剂量对数之间呈显著正相关。服相同剂量后,非孕组药-时曲线水平及药时曲线下面积AUC 大于早孕组,但两组间并无显著性差异(P>0.05)。无论非孕组及早孕组,口服25 mg、100 mg 和200 mg后,RU 486代谢符合二室开放模型,口服400 mg 和600mg 后则呈非线性动力学过程。Plasma levels of RU 486 and its metabolites,RU 42633,RU 42643,RU 42698 weredetermined by HPLC in non-pregnant(n=9)and early pregnant women(n=36)orallyadministered with different doses of RU 486.The results showed that absorption and initia-tion of metabolism of RU 486 were rapid in both groups,as indicated by the fact thatRU 486 and its three metabolites could be measured in plasma 20 min after administration,and that Tmax of RU 486 was between 1～2 h.There was a positive correlation(P<0.01)between the logarithm of Cmax and that of the corresponding doses orally administered ineach group.The plasma drug-time curve of each dose in non-pregnant group was higherthan that in pregnant group,and so was the AUC.However,there was no significant dif-ference in these two parameters between the two groups(p>0.05).Metabolism of RU 486was in agreement with two-compartment open model after orally administration of 25 mg,100 mgand 200mg,and presented as a process of non-linear kinetics after intake of 400mgand 600 mg,in both pregnant and non-pregnant women.

关 键 词：RU486 药物动力学 妊娠 

分 类 号：R969.1[医药卫生—药理学]