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克林沙星的药代动力学和炎性液体渗透情况

Pharmacokinetics and inflammatory fluid penetration of clinafloxacin.

作者信息

Wise R, Jones S, Das I, Andrews J M

机构信息

Department of Microbiology, City Hospital NHS Trust, Birmingham, United Kingdom.

出版信息

Antimicrob Agents Chemother. 1998 Feb;42(2):428-30. doi: 10.1128/AAC.42.2.428.

Abstract

A single 200-mg dose of clinafloxacin was given orally to each of nine healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharidin-induced inflammatory fluid, and urine over the following 24 h (48 h in the case of urine). The mean maximum concentration in plasma was 1.34 microg/ml at a mean time of 1.8 h postdose. The mean maximum concentration in the inflammatory fluid was 1.3 microg/ml at 3.8 h postdose. The mean elimination half-life of clinafloxacin in plasma was 5.65 h. The overall penetration into the inflammatory fluid was 93.1%, as assessed by determining the ratio of area under the concentration-time curves. Recovery of clinafloxacin in urine was 58.8% by 24 h and 71.8% by 48 h postdose.

摘要

给9名健康男性志愿者每人口服200毫克单剂量的克林沙星,然后在接下来的24小时内(尿液情况为48小时)测量血浆、斑蝥素诱导的炎性液体和尿液中的药物浓度。血浆中的平均最大浓度在给药后1.8小时时为1.34微克/毫升。炎性液体中的平均最大浓度在给药后3.8小时时为1.3微克/毫升。克林沙星在血浆中的平均消除半衰期为5.65小时。通过测定浓度-时间曲线下面积的比值评估,其进入炎性液体的总体渗透率为93.1%。给药后24小时,尿液中克林沙星的回收率为58.8%,48小时时为71.8%。

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