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目的研究甲磺酸帕珠沙星片在中国健康受试者多次给药的药动学。方法 12名健康受试者男女各半,口服甲磺酸帕珠沙星片,每天2次,每次500mg,连续用药至第7天,收集第1天和第7天血、尿样本,用LC-MS/MS方法测定帕珠沙星的血、尿浓度。结果受试者多次口服甲磺酸帕珠沙星第1天和第7天主要药动学参数分别是,C_(max)为(9.79±2.18)、(9.37±1.58)mg/L;AUC_(0-t)为(25.44±3.86)、(25.23±5.06)h·mg/L;t_(1/2)为(1.81±0.28)、(1.78±0.23)h;T_(max)为(0.72±0.27)、(0.73±0.31)h;多剂给药后第1天和第7天原型药物尿中累积排泄百分率分别为(71.93±23.20)、(87.41±16.10)%。第1天与第7天主要药动学参数比较差异均无统计学意义。结论多次连续给药后第1天和第7天主要药动学参数结果相似,药物在体内无蓄积,口服给药耐受性良好。
Objective To study the pharmacokinetics of pazufloxacin mesylate tablets administered multiple times in healthy Chinese subjects. Methods Twelve male and female healthy volunteers were divided into two groups. Pazufloxacin mesylate tablets were orally administered twice a day for 500mg once daily for 7 days. Blood and urine samples were collected on day 1 and day 7 with LC-MS / MS method for the determination of pazufloxacin blood and urine concentrations. Results The main pharmacokinetic parameters of pazufloxacin mesylate on day 1 and 7 were orally (9.79 ± 2.18) and (9.37 ± 1.58) mg / L, respectively; the AUC_ (0-t) were (25.44 ± 3.86) and (25.23 ± 5.06) h · mg / L respectively; t 1/2 was 1.81 ± 0.28 and 1.78 ± 0.23 h respectively; T max was 0.72 ± 0.27) and (0.73 ± 0.31) h, respectively. The cumulative urinary excretion rates of the first day and the seventh day after the multidrug administration were (71.93 ± 23.20) and (87.41 ± 16.10)%, respectively. There was no significant difference in the main pharmacokinetic parameters between the first day and the seventh day. Conclusions The results of the main pharmacokinetic parameters on the 1st and the 7th day after repeated administrations were similar. The drug did not accumulate in the body and was well tolerated by oral administration.