左氧氟沙星注射液及口服片剂在健康人体内的药动学研究  

Pharmacokinetic study of levofloxacin in Chinese healthy volunteers

作　　者：张莉[1] 李家泰[1] 吕媛[1] 李曼宁[1] 张永龙[1] 刘燕[1] 李天云[1] 张建伟[1] 

机构地区：[1]北京大学临床药理研究所,北京100083

出　　处：《中国药学杂志》2001年第12期834-837,共4页Chinese Pharmaceutical Journal

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 (POBJECIIVE: 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 rain, 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 cmax (3.06 ± 0.32) mg&middotL-1 and (2.50 ± 0.39) mg&middotL-1, AUC (17.79 ± 1.62) mg&middoth&middotL-1 and (17.02 ± 1.79) mg&middoth&middot L-1, t1/2β (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: cmax (4.63 ± 0.59) mg&middotL-1 and (4.21 ± 0.66) mg&middotL-1, AUC (29.17 ± 2.66) mg&middoth&middotL-1 and (29.04 ± 3.76) mg&middoth&middotL-1, t1/2β(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 cmax. 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)%.

关 键 词：左氧氟沙星 高效液相色谱法 药代动力学 抗菌药 

分 类 号：R969.1[医药卫生—药理学] R978.19[医药卫生—药学]