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目的研究健康受试者单次和多次口服普卢利沙星片后的药动学过程。方法采用多周期试验设计,10名健康受试者单次po(200,400,600mg)和多次po(400mg)普卢利沙星片;采用HPLC测定普卢利沙星活性代谢物噻丁啶-喹啉羧酸衍生物(NM394)的血药浓度。用DAS2.0程序计算主要药动学参数,并进行统计分析。结果健康志愿者单次及多次口服普卢利沙星片后,其活性代谢物NM394符合一级吸收一级消除的二室模型。主要药动学参数:单次给药低、中、高3种剂量普卢利沙星血浆活性代谢物NM394的消除半衰期及体内平均驻留时间相近,ρmax、AUC0-t和AUC0-∞均值与剂量呈良好的线性;多次给药ρsasv为(1.02±0.18)mg·L-1,DF为(2.17±0.48),AUCs0s-36为(15.69±3.20)mg·h·L-1,AUCs0s-∞为(16.38±3.34)mg·h·L-1,t1/2α为(1.23±0.58)h,t1/2β为(7.95±3.28)h。结论普卢利沙星片单次(低、中、高3种剂量)与多次(中剂量)po给药的主要药动学参数(t1/2、V/F、CL/F)无显著性差异(P>0.05),体内药物无蓄积现象。
Objective To study the pharmacokinetics of prulifloxacin tablets in healthy subjects after single and multiple oral administrations. Methods A multi-period trial was designed. Prulifloxacin tablets of po (200,400,600 mg) and po (400 mg) were given to 10 healthy volunteers. The activity of thulidine-quinolinecarboxylate, an active metabolite of prulifloxacin, Blood concentration of acid derivative (NM394). The main pharmacokinetic parameters were calculated using the DAS 2.0 program and statistically analyzed. Results After administration of prulifloxacin tablets to healthy volunteers, the active metabolite NM394 conformed to the two-compartment model of primary absorption elimination. The main pharmacokinetic parameters: single administration of low, medium and high doses of prussianacin plasma active metabolite NM394 elimination half-life and the average residence time in the same, ρmax, AUC0-t and AUC0-∞ mean and dose (1.02 ± 0.18) mg · L-1 for multiple administrations, (2.17 ± 0.48) for DF, and (15.69 ± 3.20) mg · h · L-1 for AUCs0s-36. The AUCs0s-∞ (16.38 ± 3.34) mg · h · L-1, t1 / 2α was (1.23 ± 0.58) h and t1 / 2β was (7.95 ± 3.28) h. Conclusion The main pharmacokinetic parameters (t1 / 2, V / F, CL / F) of prulifloxacin single (low, medium and high doses) and multiple Difference (P> 0.05), no accumulation of drug in vivo.