【摘要】 目的　研究左氧氟沙星注射液及口服片剂单次给药的药动学。方法　选 18名男性健康受试者 ,分别随机交叉给予左氧氟沙星注射液 2 0 0mg(注射时间 6 0min)及 2 0 0mg口服片剂 ;另选 18名健康受试者 ,分别随机交叉给予左氧氟沙星注射液30 0mg ,注射时间分别为 6 0及 90min。采用反相高效液相色谱法测定血及尿药浓度。 结果　左氧氟沙星 2 0 0mg注射液与2 0 0mg口服片剂的主要药动学参数cmax分别为 (3.0 6± 0 .32 ) ,(2 .5 0± 0 .39)mg·L-1;AUC分别为 (17.79± 1.6 2 ) ,(17.0 2±1.79)mg·h·L-1;t1/ 2 β分别为 (5 .6 0± 0 .31) ,(5 .73± 0 .48)h ;48h尿药累积排泄百分率分别为 (72 .5 8± 8.6 6 ) %和 (71.5 0±6 .75 ) %。经计算口服片剂的绝对生物利用度为 (96 .0 3± 9.35 ) %。左氧氟沙星注射液 30 0mg ,注射时间分别为 6 0及 90min的主要药动学参数cmax分别为 (4 .6 3± 0 .5 9) ,(4 .2 1± 0 .6 6 )mg·L-1;AUC分别为 (2 9.17± 2 .6 6 ) ,(2 9.0 4± 3.76 )mg·h·L-1;t1/ 2 β分别为 (6 .0 5± 0 .30 ) ,(5 .96± 0 .48)h ;48h尿药累积排泄百分率分别为 (74.5 0± 9.32 ) %和 (77.6 8± 8.86 ) %。两组中的主要参数经配对t检验除cmax有显著性差异 (P <0 .0 5 )外 ,其余均无显著性差异 (P <0更多还原

【Abstract】 OBJECTIVE To study the pharmacokinetics of single oral administration and intravenous infusion of levofloxacin in Chinese healthy volunteers.METHODS Intravenous infusion of levofloxacin 200 mg within 60 min, or the same dose of levofloxacin tablet orally was given to 18 male healthy volunteers in randomized self control crossover study. To another 18 healthy subjects,infusion of levofloxacin 300 mg was given intravenously within 60 min and 90 min, respectively. The concentrations of levofloxacin in serum and urine were assayed by HPLC.RESULTS The mean pharmacokinetic parameters of 200 mg levofloxacin injection and tablet were c max (3.06±0.32) mg·L -1 and (2.50±0.39) mg·L -1 , AUC (17.79±1.62) mg·h·L -1 and (17.02±1.79) mg·h·L -1 , t 1/2β (5.60±0.31) h and (5.73±0.48) h,respectively.The 48 hour cumulative urinary excretion rates were (72.58± 8.66 )% and (71.50±6.75)% respectively.The absolutely bioavailibility was (96.03±9.35)%.In 300 mg group, the main pharmacokinetic parameters of infusion 60 min and 90 min were as follows: c max (4.63±0.59) mg·L -1 and (4.21±0.66) mg·L -1 , AUC (29.17±2.66) mg·h·L -1 and (29.04±3.76) mg·h·L -1 , t 1/2β (6.05±0.30) h and (5.96±0.48) h,respectively. The 48 h cumulative urinary excretion rates were (74.50±9.32)% and (77.68±8.86)% respectively.The main pharmacokinetic parameters showed no significant difference except the c max .No adverse events were noted in any of the above studies.CONCLUSION It suggested that there were the same pharmacokinetic behavior in 200 mg and 300 mg dose groups.The absolutely bioavailibility of levofloxacin tablet was (96.03±9.35)%.更多还原