Bergan T, Thorsteinsson S B, Solberg R, Bjornskau L, Kolstad I M, Johnsen S
Am J Med. 1987 Apr 27;82(4A):97-102.
The pharmacokinetics of ciprofloxacin, after administration of single oral doses of 100, 250, 500, and 1,000 mg, and an intravenous dose of 100 mg, were determined in 12 healthy volunteers (six women and six men). Serum concentrations were determined by high-pressure liquid chromatography, and urine samples were assayed microbiologically. The peak serum concentrations and the total areas under the serum concentration curves increased in proportion to the size of the oral dose. The pharmacokinetics of ciprofloxacin were described by a dose-independent linear relationship. The apparent oral bioavailability was 85 percent, based on comparison of the total areas under the serum concentration curves of the 100-mg dose. The serum concentrations during steady state were not significantly higher than after the first dose. The serum half-life ranged from 3.0 to 3.4 hours after the oral doses, and was 2.9 hours after the intravenous dose. The elimination-phase apparent distribution volume coefficient, delta d,area, was 2.76 liters/kg, and the total body clearance was 42.0 liters/hour. The 24-hour urinary excretion was 42.2 +/- 15.6 percent after the 100-mg intravenous dose and 42.5 +/- 17.6 percent after the 500-mg twice-daily oral dose during steady state.
在12名健康志愿者（6名女性和6名男性）中测定了单次口服100、250、500和1000mg环丙沙星以及静脉注射100mg环丙沙星后的药代动力学。血清浓度通过高压液相色谱法测定，尿样采用微生物学方法检测。血清峰浓度和血清浓度曲线下总面积与口服剂量大小成比例增加。环丙沙星的药代动力学呈剂量无关的线性关系。基于100mg剂量血清浓度曲线下总面积的比较，环丙沙星的表观口服生物利用度为85%。稳态时的血清浓度并不显著高于首剂后。口服给药后血清半衰期为3.0至3.4小时，静脉给药后为2.9小时。消除相表观分布容积系数δd,area为2.76升/千克，全身清除率为42.0升/小时。100mg静脉给药后24小时尿排泄率为42.2±15.6%，稳态时500mg每日两次口服给药后为42.5±17.6%。
