三种氟喹诺酮类抗菌药的药物动力学研究

PHARMACOKINETICS STUDY ON THREE FLUOROQUINOLONES

本文报道氟喹诺酮类药物诺氟沙星、依诺沙星和氧氟沙星的药物动力学研究结果。健康志愿者空腹口服单剂400mg的诺氟沙星、依诺沙星和氧氟沙星后,采用微生物法测定其血、尿浓度,氧氟沙星的体内过程符合二室模型,依诺沙星和诺氟沙星符合一室模型,口服诺氟沙星、依诺沙星和氧氟沙星的消除半衰期分别为3.5、4.8和5.4h,平均血峰浓度各为1.2、3.1和5.8mg/L,达峰时间各为1.6、1.2和1.1h, AUC分别为6.0、18.1和36.7h·mg/L。 三种药物单次给药后尿浓度均高,有效尿药浓度维持时间长,尤以氧氟沙星为著。给药后12h内诺氟沙星、依诺沙星和氧氟沙星以药物原形自尿中排出给药量的28％、47％和75％。 根据三者的药物动力学参数拟订了治疗各种感染的给药方案。

Clinical pharmacokinetics study of Norfloxacin, Enoxacin and Ofloxacin was carried out in 8 volunteers after oral administration of 400mg Norfloxacin, Enoxacin and Ofloxacin. Ofloxacin obeyed the two compartment model kinetics in serum, Norfloxacin and Enoxacin obeyed the one. The mean peak serum concentration of Norfloxacin, Enoxacin and Ofloxacin was 1.2, 3.1 and 5.8mg/L respectively.The elimination half life was 3.5, 4.8 and 5.4h and the area under curve was 6.0, 18.1 and 36.7h·mg/L. The urinary recovery rate of Norfloxacin, Enoxacin and Ofloxacin over 12h was 28%, 47% and 75%. Based on their pharmacokinetic characteristics, a therapeutic regimen is suggested for use in the treatment of various infections.