Farinotti R, Trouvin J H, Bocquet V, Vermerie N, Carbon C
Department of Pharmacy, Hôpital Bichat, Paris, France.
Antimicrob Agents Chemother. 1988 Oct;32(10):1590-2. doi: 10.1128/AAC.32.10.1590.
The pharmacokinetics of ofloxacin were investigated in eight healthy male volunteers. A single infusion (200 mg over 0.5 h) was performed on day 1, followed by a washout period of 2 weeks. Repeated administrations were performed for 4 days (200 mg every 12 h). Pharmacokinetic parameters were determined from the plasma decay curves of the single and the last of the multiple administrations. Ofloxacin kinetics after the single dose were best described by a two-phase curve with a total body clearance of 241.6 +/- 43.3 ml min-1, a volume of distribution of 112 +/- 23.1 liters, and an elimination half-life of 5.4 +/- 0.8 h. The extrapolated area under the curve (AUC0-infinity) was 14 +/- 2.3 mg.h liter-1. The pharmacokinetics were not significantly modified by repeated administration, demonstrated mainly by the AUC0-12 value of the last infusion (13.4 +/- 2.2 mg.h liter-1). We conclude that, with intravenous multiple doses every 12 h, the steady state is reached within 24 to 36 h and no abnormal accumulation or changes in pharmacokinetic parameters occur.
在8名健康男性志愿者中研究了氧氟沙星的药代动力学。第1天进行单次输注（0.5小时内输注200毫克），随后有2周的洗脱期。重复给药4天（每12小时200毫克）。根据单次给药和多次给药最后一次给药后的血浆衰减曲线确定药代动力学参数。单次给药后氧氟沙星的动力学最好用双相曲线描述，全身清除率为241.6±43.3毫升·分钟-1，分布容积为112±23.1升，消除半衰期为5.4±0.8小时。曲线下面积外推值（AUC0-∞）为14±2.3毫克·小时·升-1。多次给药未显著改变药代动力学，主要由最后一次输注的AUC0-12值（13.4±2.2毫克·小时·升-1）证明。我们得出结论，每12小时静脉注射多次剂量，在24至36小时内达到稳态，药代动力学参数无异常蓄积或变化。
