【摘要】 目的 评价在空腹和高脂高热量饮食情况下甲硝唑片在中国健康受试者中的药代动力学特征。方法 本方案按单中心、随机、开放、单剂量的试验设计。空腹和高脂高热量饮食条件下共入组47例中国健康受试者，单次口服甲硝唑片200 mg,给药前后按规定时间点采集静脉血样。用高效液相色谱串联质谱法测定血浆中甲硝唑的浓度并计算药代动力学参数。结果 甲硝唑片空腹和高脂高热量饮食后的主要药代动力学参数如下：C_max分别为（4 799.13±1 195.32）和（4 044.17±773.98）ng·mL^-1,t_max分别为1.00和2.25 h,t_1/2分别为（9.11±1.73）和（9.37±1.79）h, AUC_0-t分别为（5.59±1.19）×10⁴和（5.51±1.18）×10⁴ng·mL^-1·h, AUC_0-∞分别为（5.79±1.33）×10⁴和（5.74±1.32）×10⁴ng·mL^-1·h;高脂饮食后服药较空腹条件下服药，t_max延迟1.25 h（P<0.01）,C_max、AUC_0-t、AUC_0-∞虽有不同程度的较少或降低，但影响较小（均P>0.05）。结论 高脂餐饮食对甲硝唑的药代动力学参数影响较小，虽然不会显著改变药物的吸收程度，但是会使达峰时间明显延迟。更多还原

【Abstract】 Objective To evaluate the effects of high-fat diet on the pharmacokinetics of metronidazole in Chinese healthy adult subjects.Methods This program is designed according to a single-center,randomized,open,single-dose trial.Forty-seven healthy subjects were assigned to receive single dose of metronidazole tablets 200 mg in either fasting and high-fat diet state,and blood samples were taken at different time points,respectively.The concentrations of metronidazole in plasma were determined by high performance liquid chromatographymass spectromentry.Results The main pharmacokinetic parameters of metronidazole in fasting state and high-fat diet state were as follows:C_max were（4 799.13±1 195.32） and（4 044.17±773.98）ng·mL^-1;t_max were 1.00 and 2.25 h;t_1/2 were（9.11±1.73） and（9.37±1.79） h;AUC_0-t were（5.59±1.19） × 10⁴ and（5.51±1.18） × 10⁴ ng · mL^-1·h;AUC_0-∞ were（5.79±1.33） ×10⁴ and（5.74±1.32） × 10⁴ ng·mL^-1·h.Compared to the fasting state,the t_max of the drug taken after a high fat diet was delayed by 1.25 h（P<0.01）,C_max,AUC_0-t,AUC_0-∞ were less or decreased in different degrees,but the effects were small（all P> 0.05）.Conclusion High-fat diet has little effects on the pharmacokinetic parameters of metronidazole,which does not significantly change the degree of drug absorption,but can significantly delay the time to peak.更多还原