单剂静脉输注左氧氟沙星的人体药动学研究

Pharmacokinetics of levofloxacin after a single intravenous administration in human

目的:研究健康成年志愿者单剂静脉输注600mg左氧氟沙星后的药动学特征。方法:用高效液相色谱法测定10例受试者单剂静脉输注600mg左氧氟沙星后的血药浓度,并用非房室模型计算其药动学参数。结果:受试者接受单剂静脉输注600mg左氧氟沙星后的药动学参数Cmax为(7.5±2.1)mg·mL-1;AUC0-36为(51.1±9.8)mg·mL-1.h;t1/2为(6.8±0.7)h;Vd为(2.0±0.4)L.kg-1;λ为(0.100±0.010)h-1;t1/2为(6.8±0.7)h;MRT为(8.3±1.3)h;CL为(196.7±38.3)mL·min-1。结论:单次静脉输注600mg左氧氟沙星后,Cmax为4.1～10.3mg·mL-1,t1/2为6.0～8.1h,MRT为6.6～11.0h;男女受试者Cmax、Vd差异具显著性,但经体质量校正后这种差异不明显。

OBJECTIVE To study the pharmacokintics of levofloxacin in healthy Chinese volunteers after a single intraveous injection at dose of 600 mg. METHODS The plasma concentrations of levofloxacin was determined by a validated HPLC method, and pharmacokinetic parameter calculation was performed using a non-compartmental analysis. RESULTS The main pharmacokinetic parameters were as follows：Cmax was （7. 5±2.1） mg·L^-1; AUC0-36 was（51.1±9. 8） mg·L^-1·h; t1/2 was （6. 8±0. 7）h,Vd was （2.0±0.4） L·kg^-1）, λ was （0. 100±0.010） h^-1,MRT was （8.3±1.3） h,CL was （196.7±38.3） mL·min^-1. CONCLUSION After a single intravenous injection of 600 mg of levofloxaein, the range of Cmax, t1/2 and MRT were （4. 1-10. 3） mg·L^-1, （6. 0±8.1） h, （6. 6-11.0） h, respectively. Sexual differences were showed in Cmax and Vd. but the differences were not significant after adjustment with weight.