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

 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200 mg（注射时间60 min）及200 mg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300 mg, 注射时间分别为60及90 min。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200 mg注射液与200 mg口服片剂的主要药动学参数c_max分别为（3.06±0.32），(2.50±0.39) mg·L^-1；AUC分别为(17.79±1.62)，(17.02±1.79) mg·h·L^-1；t_1/2β分别为(5.60±0.31)，(5.73±0.48) h；48 h尿药累积排泄百分率分别为(72.58±8.66)%和（71.50±6.75）%。经计算口服片剂的绝对生物利用度为（96.03±9.35）%。左氧氟沙星注射液300 mg, 注射时间分别为60及90 min的主要药动学参数c_max分别为（4.63±0.59），（4.21±0.66）mg·L^-1；AUC分别为（29.17±2.66），（29.04±3.76） mg·h·L^-1；t_1/2β分别为（6.05±0.30），（5.96±0.48）h；48 h尿药累积排泄百分率分别为（74.50±9.32）%和（77.68±8.86）%。两组中的主要参数经配对t检验除c_max有显著性差异(P＜0.05)外，其余均无显著性差异(P＜0.05)。结论 200 mg左氧氟沙星片剂的口服吸收良好，绝对生物利用度为(96.03±9.35)%；给予相同剂量左氧氟沙星300 mg而注射时间不同（60及90min）的药动学过程基本一致，因此临床可根据具体情况调整给药时间。

Pharmacokinetic study of levofloxacin in Chinese healthy volunteers

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)%.