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目的:研究左氧氟沙星注射液多剂量给药在健康人体内的药代动力学.方法:10名健康男性受试者给予左氧氟沙星注射液200mg,注射时间为60min,连续给药7天,其中第1天及第7天给药1次,第2到6天每天给药2次,间隔12h 采用反相高效液相色谱法测定血及尿药浓度.结果:第一次给药的主要药物动力学参数:C_(max)(2.4±0.4)mg/L;AUC_(0-∞)(16.1±1.4)mg·h·L~(-1);T1/3β(6.3±0.3)h.血药浓度于第3天达稳态,稳态后最后一次给药的主要药物动力学参数:C_(ssmax)(2.9±0.4)mg/L;C_(ssmin)(0.71+0.19)mg/L;C_(av)(1.40±0.29)mg/L;AUC_(ss0-12)(17±3)mg·h·L~(-1),T1/2β(6.2±0.8)h.24h内平均尿累积排泄百分率为(88±5)％.累积比为1.20,波动系数为1.30.第一次给药与最后一次给药T1/2β及AUC差异无显著性(P>0.05).整个试验期间,受试者未出现明显的不良反应.结论:左氧氟沙星注射液200mg连续给药7天,药物在体内无明显蓄积.
OBJECTIVE: To study the pharmacokinetics of levofloxacin injection in healthy volunteers.Methods: Ten healthy male subjects were given 200 mg levofloxacin injection for 60 minutes and administered for 7 consecutive days. The first day And once a day on the 7th day, on the 2nd to 6th day, the medicine was administered twice a day, and the blood and urine concentration was measured by RP-HPLC at 12h intervals.RESULTS: The main pharmacokinetic parameters : Cmax 2.4 ± 0.4 mg / L; AUC 0-∞ (16.1 ± 1.4) mg · h · L -1; On the third day, the main pharmacokinetic parameters for the last administration after steady state were as follows: C (ssmax) (2.9 ± 0.4) mg / L; C ssmin (0.71 + 0.19) mg / L; ) (1.40 ± 0.29) mg / L, the mean cumulative urinary excretion rate of AUC_ (ss0-12) (17 ± 3) mg · h · L -1 and T1 / 2β (88 ± 5)%, the cumulative ratio was 1.20 and the coefficient of variation was 1.30.The difference between T1 / 2β and AUC in the first administration and the last administration was insignificant (P> 0.05) .Throughout the experiment, There was obvious adverse reaction.Conclusion: 200mg levofloxacin injection for 7 consecutive days, no significant drug accumulation in the body.