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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 concentrations of RU486 and its metabolites RU 42633, RU 42848 and RU 42698 after oral administration of different doses of RU 486 were measured by HPLC in non-pregnant women (n = 9) and early pregnant women (n = 36). The results showed that regardless of pregnancy or not, Drug absorption and metabolism are very rapid; measured RU486 and its metabolites in plasma after 20 min; mother peak drug peak time Tmax are 1 ~ 2h, the peak concentration Cmax logarithm of dose There was a significant positive correlation between them. After taking the same dose, the AUC of the non-pregnant group and the area under the curve of the time of the medicine were higher than those of the first trimester group, but there was no significant difference between the two groups (P> 0.05). RU486 metabolism was in accordance with two-compartment open model after oral administration of 25 mg, 100 mg and 200 mg in both non-pregnant group and early pregnancy group. Non-linear kinetics were observed after 400 mg and 600 mg orally.