国产妥舒沙星片与进口妥舒沙星片人体生物等效性研究

Bioequivalence of domestic and imported tosufloxacin tosylate tablets

目的 进行国产妥舒沙星片与进口妥舒沙星片的人体生物等效性研究。方法 12名健康志愿者随机自身交叉给药 ,分别单次口服 3 0 0mg国产妥舒沙星片与进口片剂 ,采用高效液相色谱紫外检测法 ,测定血浆及尿液中药物浓度。经 3p97药代动力学计算程序处理计算参数 ,并进行双单侧t检验确定是否生物等效。结果 该药体内过程符合口服给药一室模型 ,国产片与进口片的主要药代动力学参数分别为Tmax(1.188± 0 .43 9)和 (1.3 3 2± 0 .5 81)h ,Cmax(1.5 0 1± 0 .5 96)和 (1.3 45± 0 .5 0 6)mg/L ,AUC0 -∞(8.845± 3 .410 )和 (8.971±3 .3 87)mg·h/L ,用梯形法计算所得的AUC0 -t分别为 (10 .13 3± 3 .92 7)和 (9.80 3± 3 .3 43 )mg·h/L ,由AUC0 -t计算国产片的相对生物利用度为 (10 2 .5± 13 .6) %。结论 两种制剂具有生物等效性。

Objective: To study the bioequivalence of domestic and imported tosufloxacin tosylate. Metheds: A dose of 300mg domestic or imported tosufloxacin tosylate was randomly given to 12 healthy volunteers in two way cross over design . The pharmacokinetic parameters were calculated with the aid of 3p97 pharmacokinetics software. The bioequivalence of the domestic and imported tablets were calculated by analysis of variance, two one sided t test. Results: The plasma and urine concentrations of tosufloxacin tosylate was determined by high performance liquid chromatography (HPLC) method. The concentration time curve of the two preparations was fitted to a one compartment model. The main pharmacokinetic parameters of domestic and imported tosufloxacin tosylate were as follows: T max (1.188±0.439) and (1.332±0.581)h; C max (1.501±0 596) and (1.345±0.506)mg/L; AUC 0～∞ (8.845±3.410) and (8.971±3.387)mg·h/L; AUC 0～24 (10.133±3.927) and (9.803±3.343)mg·h/L, respectively. The relative bioavailability of the domestic drug was (102.5±13.6)%. Conclusion: The domestic and imported tablets were bioequivalent.