Hamel B, Mottet N, Audran M, Costa P, Bressolle F
Laboratoire de Pharmacocinétique Clinique, Faculté de Pharmacie, Université Montpellier I, France.
J Antimicrob Chemother. 2000 Dec;46(6):993-6. doi: 10.1093/jac/46.6.993.
The objective of this study was to determine the concentrations of enoxacin and its oxo-metabolite in human prostatic tissue after multiple oral doses (400 mg bd) in 13 patients. On the first day of treatment, elimination half-lives were 6.8 h for enoxacin and 7.1 h for its metabolite; they were increased on day 4 (10.3 and 13.2 h, respectively). The ratios of drug concentration in prostatic tissue and plasma averaged 2.2 for enoxacin and 1.4 for its metabolite. In conclusion, concentrations of enoxacin achieved within the prostatic tissue were higher than plasma concentrations suggesting that there was an active transport mechanism.
本研究的目的是测定13例患者多次口服给药（400mg，每日两次）后，人前列腺组织中依诺沙星及其氧代代谢物的浓度。治疗第一天，依诺沙星的消除半衰期为6.8小时，其代谢物为7.1小时；第4天半衰期延长（分别为10.3和13.2小时）。前列腺组织与血浆中药物浓度之比，依诺沙星平均为2.2，其代谢物为1.4。总之，前列腺组织中依诺沙星的浓度高于血浆浓度，提示存在主动转运机制。
