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目的进行健康志愿者普卢利沙星片单次和多次口服给药活性代谢物NM394人体药代动力学研究。方法采用三交叉试验设计,12名健康志愿者随机分为3组,普卢利沙星片132.1mg,264.2mg和396.3mg分别单次口服或264.2mg每日2次,连续7日口服。采集肘静脉血,HPLC法测定NM394血浓度,DAS软件计算药动力学参数。结果普卢利沙星片单次口服给药NM394主要药动学参数Cmax为0.64±0.25μg·mL-1,1.06±0.35μg·mL-1和1.45±0.44μg·mL-1,Tmax为0.94±0.22h,1.02±0.17h和0.98±0.23h,t12为8.37±0.70h,7.70±0.82h和7.78±0.77h,AUC0-24为2.93±0.78μg·mL-1·h,4.39±1.05μg·mL-1·h和5.55±1.32μg·mL-1·h,AUC0-∞为3.32±0.84μg·mL-1·h,4.82±1.06μg·mL-1·h和6.10±1.38μg·mL-1·h;连续多次口服给药NM394主要药动学参数Cmax为1.20±0.33μg·mL-1,Tmax为0.67±0.12h,t127.38±1.03h,AUC0-24为5.58±1.25μg·mL-1·h和AUC0-∞为6.09±1.24μg·mL-1·h。结论普卢利沙星片单次口服给药NM394Cmax和AUC呈良好剂量依赖性;单次和多次给药NM394药动学特征无明显差异;多次给药NM394体内无蓄积。
OBJECTIVE: To study the pharmacokinetics of promethazine in single and multiple oral administration of the active metabolite NM394 in healthy volunteers. Methods A triple-crossover trial was designed. Twelve healthy volunteers were randomly divided into three groups. Prulifloxacin tablets (132.1 mg, 264.2 mg and 396.3 mg) were orally administered orally or 264.2 mg twice daily for 7 consecutive days. Elbow venous blood was collected, the blood concentration of NM394 was determined by HPLC, and the pharmacokinetic parameters were calculated by DAS software. Results The pharmacokinetic parameters Cmax of prulifloxacin single oral administration of NM394 were 0.64 ± 0.25μg · mL-1, 1.06 ± 0.35μg · mL-1 and 1.45 ± 0.44μg · mL-1, and the Tmax was 0.94 ± 0.22h, 1.02 ± 0.17h and 0.98 ± 0.23h, t12 was 8.37 ± 0.70h, 7.70 ± 0.82h and 7.78 ± 0.77h, AUC0-24 was 2.93 ± 0.78μg · mL-1 · h, 4.39 ± 1.05μg · mL-1 · h and 5.55 ± 1.32 μg · mL-1 · h with AUC0-∞ of 3.32 ± 0.84μg · mL-1 · h, 4.82 ± 1.06μg · mL-1 · h and 6.10 ± 1.38μg · mL- 1 · h. The main pharmacokinetic parameters of NM394 administered orally for consecutive times were Cmax 1.20 ± 0.33μg · mL-1, Tmax 0.67 ± 0.12h, t127.38 ± 1.03h, AUC0-24 5.58 ± 1.25μg · mL-1 · h and AUC0-∞ of 6.09 ± 1.24 μg · mL-1 · h. Conclusion Prolifloxacin single oral administration of NM394Cmax and AUC in a good dose-dependent manner; single and multiple administration of NM394 pharmacokinetic characteristics no significant difference; multiple administration of NM394 no accumulation in vivo.