Sorgel F, Metz R, Naber K, Seelmann R, Muth P
Department of Pediatrics, University of Essen, Federal Republic of Germany.
J Antimicrob Chemother. 1988 Oct;22 Suppl D:155-67. doi: 10.1093/jac/22.supplement_d.155.
The pharmacokinetics of fleroxacin after oral administration of 400 mg fleroxacin in twelve healthy volunteers were investigated. All drug analysis was carried out by HPLC. Pharmacokinetic analysis was done by non-compartmental methods. We found that fleroxacin achieves high plasma levels of 5.2 +/- 1.1 mg/l after 1.2 +/- 0.7 h. The high AUC-value of 60.4 +/- 8.4 mg.h/l is the result of complete absorption and the long half-life of 10.8 +/- 1.6 h. The total, renal and non-renal clearance of fleroxacin were 107.9 +/- 15.1, 67.6 +/- 11.8 and 40.3 +/- 14.5 ml/min respectively. The volume of distribution Vd beta/F was 101.4 +/- 21.9 or 1.32 +/- 0.28 l/kg. Fleroxacin penetrated well into saliva (66%), nasal secretions (223%), tears (69%) and sweat (43%). On the basis of these findings once a day administration deserves consideration in the further clinical development of fleroxacin.
在12名健康志愿者口服400毫克氟罗沙星后，对其药代动力学进行了研究。所有药物分析均通过高效液相色谱法进行。药代动力学分析采用非房室方法。我们发现，氟罗沙星在1.2±0.7小时后达到5.2±1.1毫克/升的高血浆水平。60.4±8.毫克·小时/升的高AUC值是完全吸收和10.8±1.6小时的长半衰期的结果。氟罗沙星的总清除率、肾清除率和非肾清除率分别为107.9±15.1、67.6±11.8和40.3±14.5毫升/分钟。分布容积Vdβ/F为101.4±21.9或1.32±0.28升/千克。氟罗沙星能很好地渗透到唾液（66%）、鼻分泌物（223%）、泪液（69%）和汗液（43%）中。基于这些发现，在氟罗沙星的进一步临床开发中，每日给药一次值得考虑。
