Wise R, Lister D, McNulty C A, Griggs D, Andrews J M
J Antimicrob Chemother. 1986 Nov;18 Suppl D:71-81. doi: 10.1093/jac/18.supplement_d.71.
The pharmacokinetics and tissue penetration of five quinolones were studied in volunteers. The compounds were norfloxacin (400 mg po), enoxacin (400 mg iv and 600 mg po), ciprofloxacin (100 mg iv and 500 mg po), ofloxacin (600 mg po) and pefloxacin (400 mg iv). Of the oral agents studied ofloxacin and ciprofloxacin were the most rapidly absorbed (Tmax = 1.2 h) and enoxacin the least (Tmax = 1.9 h). The serum levels attained were highest in the case of ofloxacin (after allowing for the higher dose administered). The serum half-lives were norfloxacin 3.75 h, ciprofloxacin 3.9 h (po), 4.0 h (iv), ofloxacin 7.0 h, enoxacin 6.2 h (po), 5.1 h (iv) and pefloxacin 10.5 h. All agents penetrated blister fluid readily. The 24 h urine recovery was 62% for oral enoxacin, 46.4% for iv enoxacin (plus 12.2% for oxo-enoxacin), 27% for norfloxacin, 30.6% for oral ciprofloxacin, 75.7% for iv ciprofloxacin, 73% for ofloxacin and 4.9% for pefloxacin (plus 9.2% for the norfloxacin metabolite and 17.8% for pefloxacin N-oxide).
在志愿者中研究了5种喹诺酮类药物的药代动力学和组织穿透性。这些化合物分别为诺氟沙星（口服400mg）、依诺沙星（静脉注射400mg和口服600mg）、环丙沙星（静脉注射100mg和口服500mg）、氧氟沙星（口服600mg）和培氟沙星（静脉注射400mg）。在所研究的口服药物中，氧氟沙星和环丙沙星吸收最快（达峰时间Tmax = 1.2小时），依诺沙星吸收最慢（Tmax = 1.9小时）。在给予较高剂量的情况下，氧氟沙星达到的血清水平最高。血清半衰期分别为：诺氟沙星3.75小时、环丙沙星口服3.9小时、静脉注射4.0小时、氧氟沙星7.0小时、依诺沙星口服6.2小时、静脉注射5.1小时、培氟沙星10.5小时。所有药物均能轻易穿透水疱液。口服依诺沙星24小时尿液回收率为62%，静脉注射依诺沙星为46.4%（氧代依诺沙星加12.2%）、诺氟沙星为27%、口服环丙沙星为30.6%、静脉注射环丙沙星为75.7%、氧氟沙星为73%、培氟沙星为4.9%（诺氟沙星代谢物加9.2%，培氟沙星N - 氧化物加17.8%）。
