瑞巴匹特治疗消化性溃疡剂量时的药物动力学

Pharmacokinetics of Rebamipide with Curative Dose in the Patients with Peptic Ulcer

目的 观察瑞巴匹特治疗消化性溃疡患者体内药代动力学及其治疗效果。方法 2 0例消化性溃疡患者分别单剂量(6 0 0mg)和多剂量 (6 0 0mg,qd ,4周 )口服瑞巴匹特 ,观察该药的治疗效果 ,并用高效液相色谱法测定口服后不同时间的血药浓度 ,模拟房室模型并计算药代动力学参数。结果 瑞巴匹特治疗消化性溃疡有效率 10 0 % ;单剂量和多剂量口服后的血药浓度 -时间曲线均符合一级吸收开放二室模型 ,主要药动学参数Cmax分别为 (0 .5 6± 0 .2 4)和 (0 .6 2± 0 .2 9)mg·L-1,Tmax 为(1.75± 0 .92 )和 (1.88± 1.0 5 )h ,T1/ 2 β 分别为 (1.86± 1.38)和 (1.96± 1.45 )h ,AUC0 -∞ 为 (2 .48± 1.0 6 )和 (2 .85± 1.45 )mg·h·L-1,除Cmax 和AUC0 -∞ 外 ,其他参数经统计学分析无明显差别 (P >0 .0 5 ) ;连续用药 4周后体内蓄积因子为 1.15。

Aim To investigate the curative effects and the pharmacokinetics of rebamipide in 20 patients with peptic ulcer.Methods The patients were treated with rebamipide 600mg·d -1 and the therapeutic courses were all one month.After one month, all of the patients were spy out with gastroscopy. The rebamipide concentrations in plasma were determined by high performance liquid chromatographic method following a single oral dose of 600mg rebamipide and multiple dose of 600mg·d -1 ×4 weeks.The pharmacokinetic parameters were computed with PKBP-N 1 program.Results After one month of medication,the total effective rate was 100%.Following a single and multiple dose oral rebamipide,the concentration-time curves of the domestic and imported products fitted to two compartment open model.There was no significant difference for each pharmacokinetic parameters between two doses (P>0.05) but C max and AUC 0-∞ ·C max of single and multiple rebamipide tablet were (0.56±0.24) and (0.62±0.29)mg·L -1 , with that T max were (1.75±0.92) and (1.88±1.05)h,T 1/2β were (1.86±1.38) and (1.96±1.45)h,AUC 0-∞ were (2.48±1.06) and (2.85±1.45)mg·h·L -1 .The storage rate was 1.15.Conclusion Rebamipide tablet is safe and effective to cure peptic ulcer.