中国妇女单次及多次注射cyclofem 后血中醋酸甲羟孕酮的药代动力学

摘要/Abstract

摘要： 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25 mg+环戊丙酸雌二醇5 mg), 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(C_max)为3.75±1.27、5.54±1.79 及5.55±1.80 nmol/L;AUC_0-28 分别为55.84±28.15、95.45±26.56 及98.81±21.84 nmol/(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C_max 和AUC_0-28 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。

关键词: 醋酸甲羟孕酮, cyclofem, 药代动力学

Abstract: Aim Pharmaco kinetic profiles of medroxy progesterone acetate after single and multiple administ ration of cyclofem in Chinese women were analy sed to provide pharmacokinetic data for safety evaluation on chronic treatment of this long-acting injectable contraceptive.Methods Nine healthy women received once-a-month injectable cont raceptive cyclofem (aqueous microcry stalline suspension containing 25 mg medroxy progeste rone acetate and 5 mg cypionate)for up to 1 year.Blood samples were collected immediately prior to drug administ ration and to consecutive time points after injection.Int raindividual compa rison was applied in this long itudinal study.Results after 1st, 6th and 12th injection, the maximum concent rations were observed on day 3.4±0.9, 4.3±2.2 and 3.7±2.6, reespectively.C_max of 1st, 6th and 12th treatment cycles were 3.75±1.27, 5.54±1.79 and 5.55±1.80 nmol/L, while A UC0-28were 55.84±28.15, 95.45±26.56 and 98.81±21.84 nmol/(L·d), respectively.There was significant interindividual varia tion in the pharmacokinetic prof ile of MPA after int ramuscular injection of cyclofem.No meaning ful change was observed in MRT.There was a tendency of increase in C_max and AUC_0-28 of MPA during First six mo nths of treatment, whereas no statistically significant difference be tw ee n 6th and 12th injection.Conclusion No obvious drug accumulation was occured after long-term use of cyclofem.

Key words: medroxy progesterone acetate, cyclofem, once-a-month injectable contraceptive, Pharmacokinetics

中图分类号:

R979.21

周晓飞, 邵庆翔, 韩学军, 翁梨驹, 桑国卫. 中国妇女单次及多次注射cyclofem 后血中醋酸甲羟孕酮的药代动力学[J]. 中国临床药理学与治疗学, 1998, 3(1): 9-13.

ZHOU Xiao-Fei, SHAO Qing-Xiang, HAN Xue-Jun, WENG Li-Ju, SANG Guo-Wei. Pharmacokinetics of medroxyprogesterone acetate after single and multiple injection of cyclofem in Chinese women[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 1998, 3(1): 9-13.

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