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目的比较中国妇女单次及连续肌注cyclofem后血中醋酸甲羟孕酮(MPA)的药代动力学变化 ,为长期应用该长效避孕针的安全性提供依据。方法9名健康育龄妇女每月一次肌注cyclofem微晶水混悬剂(醋酸甲羟孕酮25mg+环戊丙酸雌二醇5mg) ,持续一年。于用药第1、6和12个月的临注射前和注射后不同时间取血 ,采用自身对照比较此三个给药周期MPA的药代动力学特征。结果首次及第6、12次注射后 ,血中MPA分别于3.4±0.9、4.3±2 2及3 7±2.6天达峰浓度 ;MPA平均峰值血药水平(Cmax)为3.75±1.27、5.54±1.79及5.55±1.80nmol/L ;AUC0 -28 分别为55.84±28.15、95.45±26.56及98.81±21.84nmol/(L·d)。MPA的药代动力学存在明显的个体差异。三个给药周期MPA体内平均滞留时间(MRT)无显著变化 ,分别为11.98±1.08、12.77±0.47和12.43±0.64天。与首次注射后相比 ,第6个给药周期MPA的Cmax 和AUC0 -28显示有增高的倾向 ,但在其后6个月中 ,上述参数未见明显差别。结论连续使用每月一次避孕针cyclofem并不引起受试者体内MPA的明显蓄积
Objective To compare the pharmacokinetics of medroxyprogesterone acetate (MPA) in Chinese women after single and continuous intramuscular injection of cyclofem to provide basis for the long-term application of the long-acting contraception needle. Methods Nine healthy women of childbearing age were injected once a month with cyclofem microcrystalline water suspension (25 mg medroxyprogesterone acetate plus 5 mg estradiol cypionate) for one year. Pharmacokinetic characteristics of MPA in the three administration cycles were compared before and at different times after injection on the 1st, 6th and 12th month after administration. Results After the first and sixth and sixth injections, MPA in blood reached peak concentrations of 3.4 ± 0.9, 4.3 ± 2 2 and 37 ± 2.6 days, respectively; mean peak plasma MPA levels (Cmax) were 3.75 ± 1.27 and 5.54 ± 1.79 and 5.55 ± 1.80nmol / L respectively; AUC0-28 were 55.84 ± 28.15,95.45 ± 26.56 and 98.81 ± 21.84nmol / (L · d), respectively. There are significant individual differences in the pharmacokinetics of MPA. There were no significant changes in the mean MRT of MPA in three administration cycles, which were 11.98 ± 1.08, 12.77 ± 0.47 and 12.43 ± 0.64 days, respectively. Compared with the first injection, the Cmax and AUC0 -28 of MPA in the sixth administration cycle showed an increasing tendency, but no significant difference was observed in the above 6 months after the first injection. CONCLUSIONS: Continuous use of monthly cyclodextrins did not cause significant accumulation of MPA in the subjects