甲硝唑片在健康人体中的药动学及生物等效性研究  

Pharmacokinetics and bioequivalence of metronidazole tablet in healthy volunteers

作　　者：冯仕银 蔡林芮[1] 陈卓[1] 苏旭[1] 邹琴[1] 郭伟一 王晶[1] 余勤 FENG Shi-yin;CAI Lin-rui;CHENG Zhuo;SU Xu;ZOU Qin;GUO Wei-yi;WANG Jing;YU Qin(Institute of Drug Clinical Trial·GCP,West China Second University Hospital,Sichuan University,Chengdu 610041,China)

机构地区：[1]四川大学华西第二医院国家药物临床试验机构,成都610041

出　　处：《中国新药杂志》2019年第10期1203-1207,共5页Chinese Journal of New Drugs

摘　　要：目的:研究甲硝唑在人体的药动学特征,评价在空腹和餐后条件下单次口服甲硝唑受试制剂与参比制剂的生物等效性。方法:采用开放、随机、双周期、交叉设计,健康志愿者各24名分别在空腹和餐后服用0.2 g甲硝唑受试制剂和参比制剂后,采用LC-MS/MS法测定甲硝唑的血药浓度。使用Phoenix WinNonlin 8.0版中的非房室模型分析,计算药动学参数并评价2种甲硝唑片空腹及餐后服用的生物等效性。结果:在空腹和餐后条件下中国健康志愿者口服受试制剂和参比制剂后的主要药动学参数(AUC_(0-∞),AUC_(0-t),C_(max))的几何均数比值90%置信区间均在80.00%～125.00%的范围内。餐后给药T_(max)稍延长,其他药动学参数基本一致。结论:在空腹和餐后条件下甲硝唑受试制剂与参比制剂具有生物等效性。Objective:To study the pharmacokinetic parameters of metronidazole tablets in human,and evaluate the bioequivalence between a single test and reference dose of metronidazole tablet in healthy volunteers under fasting and fed conditons.Methods:An open,randomized,two-period crossover design was performed in 24 healthy volunteers.Twenty-four healthy volunteers were given a single oral dose of 0.2 g domestic or imported metronidazole tablet under fasting and fed conditions,respectively.Metronidazole in plasma was determined by a LC-MS/MS method.By means of Phoenix WinNonlin 8.0 software,pharmacokinetic parameters were calculated using a non-compartmental mode.And then estimate the bioequivalence between a single test and reference dose of metronidazole tablet in healthy volunteers under fasting and fed conditons.Results:The 90%CIs of the GMR of AUC0-∞,AUC0-tand Cmaxbetween the test and reference drug fell within the limit ranges of 80.00%~125.00%under fasting and fed conditions,respectively.Tmaxis increased under fed condition,but other parameters are nearly the same.Conclusion:The domestic metronidazole tablets are proved to be bioequivalent to imported metronidazole tablets both under fasting and fed conditions.

关 键 词：甲硝唑 空腹 餐后 液相-质谱/质谱检测法 生物等效性 

分 类 号：R927.1[医药卫生—药学]