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目的比较米索前列醇不同给药途径(口服、舌下和阴道)药动学特征。方法采用平行试验设计,30名中国健康女性志愿受试者随机分为3组,分别空腹口服、舌下含服和阴道给予400μg米索前列醇片,采用液相色谱-串联质谱法测定受试者血浆中米索前列醇活性代谢物米索前列酸的浓度。结果受试者空腹口服、舌下含服和阴道给药后的主要药动学参数:tm ax分别为(0.18±0.05),(0.40±0.14)和(5.05±1.80)h,mρax分别为(1 424±380),(783±285)和(302±198)ng.L-1,t1/2分别为(0.61±0.32),(0.82±0.18)和(5.27±4.38)h,AUC0-t分别为(698±138),(824±302)和(1 313±691)ng.h.L-1,AUC0-∞分别为(709±143),(846±306)和(1 816±727)ng.h.L-1。结论米索前列醇片经不同途径给药后的药动学有较大差异。空腹口服给药后吸收迅速,米索前列酸达峰最快,舌下含服给药tm ax略有延长,阴道给药tm ax明显滞后。达峰浓度以空腹口服给药最高,舌下含服次之,阴道给药最低。与空腹口服和舌下含服相比,阴道给药AUC最高,但个体差异较大。
Objective To compare the pharmacokinetic characteristics of misoprostol with different routes of administration (oral, sublingual and vaginal). Methods Using the parallel experimental design, 30 Chinese healthy female volunteers were randomly divided into three groups: 400 μg misoprostol tablets were given orally, sublingually and vaginally, respectively. The results of liquid chromatography-tandem mass spectrometry Concentration of misoprostol, the active metabolite of misoprostol in plasma. Results The main pharmacokinetic parameters of tm ax after oral administration, sublingual administration and vaginal administration were (0.18 ± 0.05), (0.40 ± 0.14) and (5.05 ± 1.80) h respectively, and mρax were ( 1 424 ± 380), (783 ± 285) and (302 ± 198) ng.L-1, respectively, and t1 / 2 were 0.61 ± 0.32, 0.82 ± 0.18 and 5.27 ± 4.38 h, (698 ± 138), (824 ± 302) and (1 313 ± 691) ng.hL-1, and the AUC0-∞ were 709 ± 143, 846 ± 306 and 1816 ± 727 ng .hL-1. Conclusion The misoprostol tablets have different pharmacokinetics after administration by different routes. Fasting oral administration after absorption rapidly, misoprostol peak fastest, sublingual administration tm ax slightly prolonged vaginal administration tm ax was significantly delayed. Peak concentration of fasting oral administration of the highest sublingual sub-second vaginal administration the lowest. Compared with fasting oral and sublingual ingestion, vaginal administration AUC highest, but individual differences.