Brumfitt W, Franklin I, Grady D, Hamilton-Miller J M, Iliffe A
Antimicrob Agents Chemother. 1984 Nov;26(5):757-61. doi: 10.1128/AAC.26.5.757.
Twelve male subjects, aged 19 to 40 years, shown to be healthy by examination and laboratory tests, took 500 mg of ciprofloxacin every 12 h for 7 days. After the first and the last dose, blood and urine samples were taken and drug concentrations were determined by bioassay. There was a significant buildup in mean concentrations in serum from day 1 to day 7; mean peak levels (attained after 1 to 2 h) were 1.9 and 2.8 micrograms/ml, respectively. The terminal half-life was 3.5 to 4 h. About 40% of the drug was excreted into the urine during the 12-h period after dosing; minimum mean concentrations in urine were 105 micrograms/ml on day 1 and 174 micrograms/ml on day 7. Considerable amounts of ciprofloxacin were found in the feces on day 7 (185 to 2,220 micrograms/g). Marked changes in the aerobic part of the fecal flora were observed as a result of taking ciprofloxacin: coliforms were absent on day 7, and concentrations of streptococci and staphylococci were significantly reduced. There was no overgrowth by yeasts. One week later the fecal flora had returned to a state similar to that found before treatment. Anaerobes were little affected quantitatively but acquired resistance to ciprofloxacin. Side effects were mild and transient.
12名年龄在19至40岁之间的男性受试者，经体格检查和实验室检测显示健康，每12小时服用500毫克环丙沙星，持续7天。在首次和末次给药后，采集血样和尿样，并通过生物测定法测定药物浓度。从第1天到第7天，血清中的平均浓度有显著升高；平均峰值水平（在1至2小时后达到）分别为1.9和2.8微克/毫升。终末半衰期为3.5至4小时。给药后12小时内，约40%的药物经尿液排出；第1天尿液中的最低平均浓度为105微克/毫升，第7天为174微克/毫升。在第7天的粪便中发现了大量环丙沙星（185至2220微克/克）。服用环丙沙星导致粪便需氧菌群发生显著变化：第7天未检测到大肠菌群，链球菌和葡萄球菌的浓度显著降低。未出现酵母菌过度生长的情况。一周后，粪便菌群恢复到治疗前的类似状态。厌氧菌在数量上受影响较小，但获得了对环丙沙星的耐药性。副作用轻微且短暂。
