甲苯磺酸妥舒沙星分散片在健康人体中的生物等效性研究

Bioequivalence of tosufloxacin tosylate tablets in healthy Chinese volunteers

目的:评价受试制剂甲苯磺酸妥舒沙星分散片与参比制剂甲苯磺酸妥舒沙星片在中国健康人体内的生物等效性。方法:入选18名男性健康志愿者,随机交叉单剂量口服甲苯磺酸妥舒沙星分散片或甲苯磺酸妥舒沙星片0.3 g,HPLC法测定血浆中妥舒沙星浓度。经DAS 2.0药代动力学计算程序处理参数,并进行双单侧t检验确定是否生物等效。结果:甲苯磺酸妥舒沙星分散片和甲苯磺酸妥舒沙星片的药动学参数分别如下:t1/2分别为(5.17±1.96)和(5.13±2.10)h;tmax分别为(0.89±0.19)和(0.86±0.20)h;Cmax分别为(0.53±0.09)和(0.51±0.09)μg/mL;AUC0-24 h分别为(1.75±0.67)和(1.76±0.66)μg.h.mL-1;AUC0→∞分别为(1.98±0.74)和(1.98±0.76)μg.h.mL-1。甲苯磺酸妥舒沙星分散片受试制剂相对于参比制剂的相对生物利用度F为(101.1±15.6)%。结论:经统计学分析,受试制剂甲苯磺酸妥舒沙星分散片与参比制剂甲苯磺酸妥舒沙星片具有生物等效性。

AIM： To evaluate the bioequivalence of tosufloxacin test tablets and reference tablets in healthy Chinese volunteers. METHODS： Eighteen healthy male Chinese volunteers were enrolled and orally administrated 0.3 g tosufloxacin test tablets or reference tablets,the concentration of tosufloxacin in plasma were determined by HPLC.The pharmacokinetic parameters were calculated with the aid of DAS 2.0 pharmacokinetics software.The bioequivalence of the test and reference tablets were calculated by analysis of variance,two one sided t-test.RESULTS：The pharmacokinetic parameters of tosufloxacin test tablets and reference tablets were as following：t1/2（5.17±1.96） and（5.13±2.10） h;tmax（0.89±0.19） and（0.86±0.20） h;Cmax（0.53±0.09） and（0.51±0.09） μg/mL;AUC0-24 h（1.75±0.67） and（1.76±0.66） μg·h·mL-1;AUC0→∞（1.98±0.74） and（1.98±0.76） μg·h·mL-1,respectively.The relative bioavailability of two formulations was（101.1±15.6） %.CONCLUSION： The results of statistical analysis demonstrated that the two preparations were bioequivalent.