Single and multiple dose pharmacokinetics of fleroxacin.
Single and multiple dose pharmacokinetics of fleroxacin.
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氟罗沙星的单剂量和多剂量药代动力学。
DOI：
10.1093/jac/22.supplement_d.145
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发表时间：
1988
影响因子：
5.2
通讯作者：
D. Dell
中科院分区：
文献类型：
--
作者：
E. Weidekamm;R. Portmann;C. Partos;D. Dell
研究了健康男性志愿者单次和多次给药氟罗沙星的药代动力学。这种新的三氟喹诺酮的特点是消除半衰期长，约为10小时，血浆浓度高，口服200 mg后超过2 mg/l。这两个参数是每日一次给药方案的先决条件。发现给药剂量（100-2500 mg）与所得AUC值之间存在良好的线性关系（r = 0.998）。分布容积（Vss）超过1 l/kg，反映了良好的组织渗透性。未结合药物的肾脏清除率为104 ml/min，在3天内，56%的剂量可从尿液中以原型药物形式回收。800或1200 mg氟罗沙星每日一次多次给药，持续10天，导致药物在血浆中蓄积1.4倍。该值与理论预测的蓄积一致，因此可以排除非线性、时间依赖性药代动力学。给药的片剂具有完全生物利用度（F = 1.0），因此可以排除显著的首过代谢。
Pharmacokinetics of fleroxacin following single and multiple dosing were studied in healthy male volunteers. The characteristics of this new trifluorinated quinolone are the long elimination half-life of approximately 10 h and the high plasma concentrations, which exceed 2 mg/l after an oral dose of 200 mg. These two parameters are a prerequisite for a once daily dosage regimen. A good linear relationship (r = 0.998) was found between administered doses (100-2500 mg) and resulting AUC values. The volume of distribution (Vss) exceeded 1 l/kg and reflects the good tissue penetration. Renal clearance of unbound drug was 104 ml/min and within three days 56% of the dose could be recovered from urine as unchanged drug. Multiple dosing of 800 or 1200 mg fleroxacin once daily over ten days resulted in an accumulation of the drug in the plasma by a factor of 1.4. This value is in agreement with the theoretically predicted accumulation and thus non-linear, time-dependent pharmacokinetics can be excluded. The administered tablets were completely bioavailable (F = 1.0) and a significant first pass metabolism can therefore be excluded.