Black H R, Israel K S, Wolen R L, Brier G L, Obermeyer B D, Ziege E A, Wolny J D
Antimicrob Agents Chemother. 1979 Feb;15(2):165-70. doi: 10.1128/AAC.15.2.165.
Cinoxacin was almost completely absorbed when given orally and was found to be approximately 60 to 70% protein bound. Peak serum concentrations were reached within 2 h, and detectable serum concentrations persisted up to 12 h after administration of 0.25-, 0.5-, and 1-g multiple oral doses. Although food delayed the absorption and caused a 30% reduction in mean peak serum concentrations, the overall 24-h urinary recovery was not significantly altered. Approximately 50 to 55% of the drug was excreted in the urine as unchanged drug. At 12 h, urine concentrations were still above the minimal inhibitory concentration for most common gram-negative urinary pathogens. Cinoxacin was well tolerated when administered to 23 volunteers from 10 to 28 days. Resistance among fecal isolates initially susceptible to cinoxacin was not observed in nine volunteers who were administered 0.5 g every 12 h for 4 to 28 days.
环丙沙星口服后几乎完全被吸收，发现其蛋白结合率约为60%至70%。口服0.25克、0.5克和1克多次剂量后，2小时内达到血清峰值浓度，给药后12小时内仍可检测到血清浓度。尽管食物会延迟吸收并导致平均血清峰值浓度降低30%，但24小时的总体尿液回收率没有显著变化。约50%至55%的药物以原形经尿液排泄。12小时时，尿液浓度仍高于大多数常见革兰氏阴性尿路病原体的最低抑菌浓度。对23名志愿者给药10至28天，环丙沙星耐受性良好。在每12小时服用0.5克、持续4至28天的9名志愿者中，未观察到最初对环丙沙星敏感的粪便分离株产生耐药性。
