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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。
This article reports the fluoroquinolones norfloxacin, enoxacin and ofloxacin pharmacokinetic studies. Healthy volunteers oral administration of a single dose of 400mg of norfloxacin, enoxacin and ofloxacin after a single oral dose of microbiological determination of the blood and urine concentrations of ofloxacin in vivo process in line with two-compartment model, enoxaparin Star and norfloxacin are in a one-compartment model. The elimination half-lives of oral norfloxacin, enoxacin and ofloxacin were 3.5, 4.8 and 5.4 h, respectively, with mean peak plasma concentrations of 1.2, 3.1 and 5.8 mg / L, reaching 1.6, 1.2 and 1.1 h at peak time, with AUC of 6.0, 18.1 and 36.7 h · mg / L, respectively. After a single administration of three drugs, urinary concentrations were high, the effective concentration of urine to maintain a long time, especially of Ofloxacin. Norfloxacin, enoxacin and ofloxacin excreted 28%, 47%, and 75% of their dosing volume from the urine in drug form within 12 hours after administration. According to the three pharmacokinetic parameters developed for the treatment of various infections dosing regimen.