Privitera G, Nicastro G, Imbimbo B P, Cesana M, Visconti M, Lombardi F, Tagliabue G, Faleschini E, Colturani F, Franzini P
Institute of Hygiene, University of Milan, Italy.
Antimicrob Agents Chemother. 1993 Dec;37(12):2545-9. doi: 10.1128/AAC.37.12.2545.
Rufloxacin is a new once-daily antibacterial fluoroquinolone with a long half-life. The aim of the present study was to evaluate the plasma and biliary kinetics and biliary and urinary excretion of rufloxacin in patients with extrahepatic cholestasis. Twelve patients with total external percutaneous transhepatic biliary drainage were given a single oral dose of 400 mg of rufloxacin. Plasma, bile, and urine samples and fractions were collected over 72 h after drug administration. Rufloxacin and its major metabolite, the N-desmethyl derivative, were measured by high-performance liquid chromatography. Maximum rufloxacin concentrations in plasma and bile (means +/- standard deviations) were 4.05 +/- 1.38 micrograms/ml and 8.24 +/- 7.16 micrograms/ml, respectively, and were reached in 4.2 +/- 3.0 h and 4.2 +/- 3.5 h, respectively. The terminal elimination half-life of rufloxacin in plasma was 45.1 +/- 13.5 h. Apparent plasma clearance was 31.3 +/- 10.5 ml/min, while biliary clearance was 0.4 +/- 0.2 ml/min and renal clearance was 12.7 +/- 6.0 ml/min. In 72 h, 0.9% +/- 0.8% of the dose given was recovered in bile and 27.2% +/- 12.0% was recovered in urine. Biliary concentrations exceeded the MICs of most common biliary tract pathogens for at least 24 h after administration. The broad antibacterial spectrum of rufloxacin and its high and prolonged biliary concentrations suggest that this drug may be useful for treatment of biliary tract infections.
芦氟沙星是一种新型的每日一次服用的抗菌氟喹诺酮类药物，半衰期长。本研究的目的是评估芦氟沙星在肝外胆汁淤积患者中的血浆和胆汁动力学以及胆汁和尿液排泄情况。12例经皮经肝胆道外引流的患者口服单剂量400mg芦氟沙星。给药后72小时内收集血浆、胆汁、尿液样本及各部分样本。采用高效液相色谱法测定芦氟沙星及其主要代谢产物N-去甲基衍生物。血浆和胆汁中芦氟沙星的最大浓度（均值±标准差）分别为4.05±1.38μg/ml和8.24±7.16μg/ml，分别在4.2±3.0小时和4.2±3.5小时达到。芦氟沙星在血浆中的终末消除半衰期为45.1±13.5小时。表观血浆清除率为31.3±10.5ml/min，胆汁清除率为0.4±0.2ml/min，肾脏清除率为12.7±6.0ml/min。在72小时内，给药剂量的0.9%±0.8%在胆汁中回收，27.2%±12.0%在尿液中回收。给药后至少24小时内，胆汁浓度超过大多数常见胆道病原体的最低抑菌浓度。芦氟沙星的广谱抗菌活性及其高且持久的胆汁浓度表明，该药可能对治疗胆道感染有用。
