普卢利沙星片的健康人体药动学

Pharmacokinetics of the Active Metabolite of Prulifloxacin in Healthy Human

目的健康志愿受试者口服普卢利沙星片后，测定血浆中其活性代谢物（UFX）并作药动学研究。方法10名受试者分别单剂量和多剂量稳态时服用普卢利沙星片（相当于200mg UFX），采集血浆和尿液样品，液相色谱分离荧光检测UFX浓度，3P97软件计算药动学参数。结果单剂量时测得UFX的主要药动学参数分别为Cmax（1．64±0．29）μg·ml^-1，tmax（0．7±0．2）h，AUC0-36（6．87±1．78）h·μg·ml^-1，AUC0-∞（7．14±1．79）h·μg·ml^-1，t1／2（7．54±0．59）h，MRT（8．76±0．65）h；0—36h尿液累积排泄量为（56．85±9．12）％。稳态时测得uFx的主要药动学参数分别为Cmax（1．26±0．41）μg·ml^-1，tmax（0.8±0.3）h，AUC0-36（7．77±2．73）hμg·ml^-1，AUC0-∞（8．10±2．70）h·μg·ml^-1，t1／2（7．71±1．13）h，MRT（9．85±1．40）h。结论健康志愿受试者口服普卢利沙星片后，在体内转化为活性代谢物（UFX）发挥作用，主要经尿液排泄。每日2次，每次2片（相当于200mg UFX），在体内无积蓄。男女健康受试者的主要药动学参数无显著性差异。

AIM To study the pharmacokinetics of prulifloxacin tablets in healthy Chinese volunteers. METHODS Single dose and steady state of prulifloxacin tablets equivalent to 200 mg of metabolite （UFX） were given to each of 10 healthy volunteers. The concentrations of UFX in plasma and urine were determined by HLPC-FLD. The pliarmacokinetic parameters were calculated by 3P97 software （compartment model）. RESULT The main pliarmacokinetic parameters （^-x ± s） of UFX after po a single dose of prulifloxacin tablets equivalent to 200 mg UFX were as follows： Cmax（1.64±0.29）μg·ml^-1,tmax（0.7±0.2）h,AUC0-36（6.87±1.78）h·μg·ml^-1,AUC0-∞（7.14±1.79）h·μg·ml^-1,t1/2（7.54±0.59）h,MRT（8.76±0.65）h. Accumulative excretion rate of UFX in urine tluoughout 0 -36 h period were （56.85 ± 9.12） %. The main pharmacokinetic parameters at steady state at the same dose were as follows： Cmax（1.26±0.41）μg·ml^-1,tmax（0.8±0.3）h,AUC0-36（7.77±2.73）hμg·ml^-1,AUC0-∞（8.10±2.70）h·μg·ml^-1,t1/2（7.71±1.13）h,MRT（9.85±1.40）h, MRT（9.85 ± 1.40）h. CONCLUSION After po prulifloxacin tablets to healthy volunteers, they were transformed to active metabolite（UFX）. Urine is the main pathway for the elimination. The absorption rate and elimination rate of UFX were not changed after multiple oral administration. There was no accumulation of drug in plasma to be found after the adininistration with the 200 mg UFX,q. 12 h regimen and no difference in pharmacokinetics of UFX in male and female volunteers was observed.