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氟罗沙星在健康受试者中的代谢及药代动力学

The metabolism and pharmacokinetics of fleroxacin in healthy subjects.

作者信息

Griggs D J, Wise R, Kirkpatrick B, Ashby J P

机构信息

Department of Microbiology, Dudley Road Hospital, Birmingham, UK.

出版信息

J Antimicrob Chemother. 1988 Oct;22 Suppl D:191-4. doi: 10.1093/jac/22.supplement_d.191.

DOI:10.1093/jac/22.supplement_d.191
PMID:3144537
Abstract

A 400 mg dose of fleroxacin was administered orally to six healthy male volunteers. Concentrations of fleroxacin and the N-demethyl and N-oxide metabolites were determined in serum and urine by HPLC. The serum metabolite levels were negligible. The N-oxide metabolite was measured in the serum of five subjects but did not exceed 4% of the corresponding fleroxacin level. N-demethyl fleroxacin was not detected (less than 0.1 mg/l). The urinary recovery of fleroxacin was 49.5% over 72 h; the N-demethyl and N-oxide metabolites accounted for 6.9% and 5.7%, respectively, of the administered dose.

摘要

给6名健康男性志愿者口服400毫克氟罗沙星。采用高效液相色谱法测定血清和尿液中氟罗沙星及其N - 去甲基和N - 氧化代谢物的浓度。血清代谢物水平可忽略不计。在5名受试者的血清中检测到了N - 氧化代谢物,但未超过相应氟罗沙星水平的4%。未检测到N - 去甲基氟罗沙星(低于0.1毫克/升)。72小时内氟罗沙星的尿回收率为49.5%;N - 去甲基和N - 氧化代谢物分别占给药剂量的6.9%和5.7%。

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