盐酸替扎尼定口服液在中国健康人体内的生物等效性研究  

Bioequivalence Study of Tizanidine Hydrochloride Oral Liquid in Healthy Chinese Volunteers

作　　者：姜敏生 朱琦涛 华玉 尹咸淼 宋欢 丁峰 郭东生 甘方良 JIANG Min-sheng;ZHU Qi-tao;GUO Dong-sheng(School of Pharmacy,Xianning Medical College,Hubei University of Science and Technology,Xianning Hubei 437100,China)

机构地区：[1]湖北科技学院医学部药学院,湖北咸宁437100 [2]咸宁市中心医院临床药理机构办公室

出　　处：《湖北科技学院学报(医学版)》2025年第2期103-106,共4页Journal of Hubei University of Science and Technology(Medical Sciences)

摘　　要：目的研究盐酸替扎尼定口服液在中国健康人体内的药动学特征,进一步评价其生物等效性。方法按照两序列四周期完全重复交叉设计,66例健康志愿者分为空腹36例和餐后30例,每周期分别使用受试制剂(T,100mL∶40mg)或参比制剂(R,4mg)的一种,采用UPLC-MS/MS方法检测血浆中替扎尼定的药物浓度,最后使用药动学软件计算其药动学相关参数和评价其生物等效性。结果空腹试验受试制剂和参比制剂的替扎尼定C_(max)、AUC_(0-t)、AUC_(0-∞)分别为(4.129±2.538)和(3.980±2.227)ng/mL、(11.4±8.3)和(11.1±8.0)h·ng/mL、(11.6±8.4)和(11.3±8.2)h·ng/mL;餐后试验受试制剂和参比制剂的替扎尼定C_(max)、AUC_(0-t)、AUC_(0-∞)分别为(3.655±2.065)和(3.073±2.144)ng/mL、(11.2±6.4)和(10.5±5.9)ng/mL、(11.4±6.5)和(10.7±6.0)ng/mL。药动学参数最小二乘几何均值比的90%置信区间均落在80%~125%。结论盐酸替扎尼定受试制剂和参比制剂在空腹和餐后试验具有生物等效性。Objective To study the pharmacokinetic characteristics of tizanidine hydrochloride oral solution in healthy Chinese volunteers and further evaluate its bioequivalence.Methods According to a two sequence four cycle completely repeated crossover design,66 healthy volunteers(fasting 36 and postprandial 30)were treated with either the test formulation(T,100mL∶40mg)or the reference formulation(R,4mg)per cycle.The drug concentration in plasma was detected using UPLC-MS/MS method.Finally,pharmacokinetic software was used to calculate its pharmacokinetic parameters and evaluate its bioequivalence.Results The C_(max),AUC_(0-t),and AUC_(0-∞) of the test and reference formulations of tizanidine in the fasting test were(4.129±2.538)and(3.980±2.227)ng/mL,(11.4±8.3)and(11.1±8.0)h·ng/mL,(11.6±8.4)and(11.3±8.2)h·ng/mL,respectively.The C_(max),AUC_(0-t),and AUC_(0-∞) of tizanidine in the postprandial trial and reference formulation were(3.655±2.065)and(3.073±2.144)ng/mL,(11.2±6.4)and(10.5±5.9)ng/mL,(11.4±6.5)and(10.7±6.0)ng/mL,respectively.The 90%confidence interval of the least squares geometric mean ratio of pharmacokinetic parameters falled within the judgment range of 80%-125%.Conclusion The test and reference formulations of tizanidine hydrochloride have bioequivalence in fasting and postprandial trials.

关 键 词：盐酸替扎尼定口服液 UPLC-MS/MS 生物等效性 药动学 

分 类 号：R969.1[医药卫生—药理学]