吉米沙星片剂单剂及多剂临床药物动力学研究  

Research on the pharmacokinetics of single dose and multipledose of gemifloxacin in healthy Chinese male subjects

作　　者：曹国英 施耀国 张菁 郁继诚 郭蓓宁 

机构地区：[1]Institute of Antibiotics, Huashan Hospital, Fudan University

出　　处：《中国临床药理学与治疗学》2007年第10期1173-1173,共1页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：AIM: To investigate the pharmacokinetics and safety of gemifloxacin in healthy Chinese subjects and provide some theoretic bases for its reasonable application in clinic. METHODS:(1) 12 healthy Chinese male subjects were enrolled in this study with an open label, 3-period cross-over oral single dosing pharmacokinetic study. The subjects sequentially took 3 doses of gemifloxacin (160, 320 and 480 mg) according to the randomization schedule. (2)20 subjects were chosen to participate in a randomized, double blind, multiple dosing pharmacokinetic study. The subjects were orally given 320 mg gemifloxacin or matching placebo once daily for 7 consecutive days. Clinical observation and laboratory test were performed during the study for the assessment of adverse events. The concentrations of gemifloxacin in serum and urine were determined by high performance liquid chromatogram (HPLC). The pharmacokinetic parameters were analysed by 3P97 analysis software. RESULTS: (1)The pharmacokinetic courses following single crossover oral dose of 160, 320 and 480 mg were all in accordance with the two-compartment model. The Cmax were (0.70±0.19), (1.40±0.32) and (1.84±0.35) mg/L, respectively. The mean times to reach Cmax were (1.2±0.4), (1.1±0.4) and (1.4±0.4) h, respectively. The values of t1/2β were (7.0±1.0), (6.7±0.8) and (6.9±0.8) h, respectively. The AUC0-∞ were (4.1±0.6), (7.5±1.1) and (11.7±1.7) mg·L-1·h, respectively. The accumulation urinary excretion at 48 hours post dosing were 39%±69%, 38%±7% and 36%±5%, respectively. The concentrations and AUCs of gemifloxacin had a linear pharmacokinetics with dose manner. (2) The results from multiple dosing of 320 mg for 7 days showed that the pharmacokinetic course following the last dose on day 7 was in accordance with one following the first dose on day 1, which were in accordance with the two-compartment model. The Cmax was (1.6±0.3) mg/L on day 1 and (1.6±0.3) mg/L on day 7. The mean times to reach Cmax were (0.9±0.4) and (1.1±0.3) h, respectively. The AIM： To investigate the pharmacokinetics and safety of gemifloxacin in healthy Chinese subjects and provide some theoretic bases for its reasonable application in clinic. METHODS： （1） 12 healthy Chinese male subjects were enrolled in this study with an open label, 3-period crossover oral single dosing pharmacokinetic study. The subjects sequentially took 3 doses of gemifloxacin （ 160, 320 and 480 mg） according to the randomization schedule. （2）20 subjects were chosen to participate in a randomized, double blind, multiple dosing pharmacokinetic study. The subjects were orally given 320 mg gemifloxacin or matching placebo once daily for 7 consecutive days. Clinical observation and laboratory test were performed during the study for the assessment of adverse events. The concentrations of gemifloxacin in serum and urine were determined by high performance liquid chromatogram （HPLC）. The pharmacokinetic parameters were analysed by 31797 analysis software. RESULTS： （1）The pharmacokinetic courses following single crossover oral dose of 160, 320 and 480 mg were all in accordance with the two-compartment model.

关 键 词：吉米沙星片剂 单剂 多剂 临床药物动力学 

分 类 号：R978.1[医药卫生—药品]