Wise R, Mortiboy D, Child J, Andrews J M
Department of Medical Microbiology, City Hospital National Health Service Trust, Birmingham, United Kingdom.
Antimicrob Agents Chemother. 1996 Jan;40(1):47-9. doi: 10.1128/AAC.40.1.47.
A single 200-mg oral dose of trovafloxacin (CP-99,219) was given to each of eight healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharides-induced inflammatory fluid, and urine over the subsequent 36 h. The mean maximum concentration observed in plasma was 2.9 micrograms/ml at a mean time of 0.75 h postdose. The mean maximum concentration observed in inflammatory fluid was 1.2 micrograms/ml at 4.0 h postdose. The mean elimination half-life in plasma was 7.8 h. The overall penetration into inflammatory fluid was 64%, as assessed by determining the ratio of the area under the concentration-time curves. Recovery of the dose in urine within the first 36 h postdose was 5.0% of the administered dose. Our results indicate that trovafloxacin, at a dosage of 200 mg once or twice daily, should be adequate for the treatment of systemic infections caused by most common bacterial pathogens.
给8名健康男性志愿者每人单次口服200毫克曲伐沙星（CP - 99,219），并在随后36小时内测定血浆、斑蝥素诱导的炎性渗出液及尿液中的药物浓度。给药后平均0.75小时血浆中观察到的平均最大浓度为2.9微克/毫升。给药后4.0小时炎性渗出液中观察到的平均最大浓度为1.2微克/毫升。血浆中的平均消除半衰期为7.8小时。通过测定浓度-时间曲线下面积的比值评估，药物进入炎性渗出液的总体渗透率为64%。给药后前36小时尿液中药物剂量回收率为给药剂量的5.0%。我们的结果表明，曲伐沙星每日一次或两次、每次200毫克的剂量应足以治疗由最常见细菌病原体引起的全身感染。
