酮咯酸氨丁三醇片仿制药与原研药的生物等效性评价  

The bioequivalence between generic and original ketorolac tromethamine tablet

作　　者：蔡颖[1] 黄红谦[1] 韦传姑 CAI Ying;HUANG Hongqian;WEI Chuangu(National Drug Clinical Trial Institute,the First Affiliated Hospital of Hainan Medical College,Haikou 570100,Hainan,China)

机构地区：[1]海南医学院第一附属医院国家药物临床试验机构,海南海口570100

出　　处：《中南医学科学杂志》2023年第1期65-68,共4页Medical Science Journal of Central South China

基　　金：海南省新药临床评价技术平台建设(2020ZX09201029)。

摘　　要：目的探讨酮咯酸氨丁三醇(KT)片仿制药(受试剂)与原研药(参比剂)的生物等效性。方法采用随机、开放、单剂量、双周期、双交叉对照试验,80例健康志愿者均分为空腹组和餐后组,均口服受试剂或参比剂。采用高效液相色谱法检测不同时间血浆KT质量浓度;计算血浆KT药代动力学参数;并对两种制剂进行生物等效性评价和安全性评价。结果参比剂最大质量浓度(C_(max))、0时到最后时间点质量浓度-时间曲线下面积(AUC_(0-t))、0时到无限时间质量浓度-时间曲线下面积(AUC0-inf)空腹组为0.60 mg/L、3.66 h·mg/L、3.97 h·mg/L,餐后组为0.65 mg/L、4.26 h·mg/L、4.46 h·mg/L。受试剂C_(max)、AUC_(0-t)、AUC0-inf空腹组为0.58 mg/L、3.51 h·mg/L、3.80 h·mg/L,餐后组为0.62 mg/L、4.02 h·mg/L、4.20 h·mg/L。空腹和餐后条件下,受试剂和参比剂C_(max)、AUC_(0-t)、AUC0-inf及其90%CI均落在80%~125%范围内,符合生物等效性要求,无严重或重度不良事件发生。结论健康受试者空腹或餐后口服KT片受试剂、参比剂具有生物等效性,安全性良好。Aim To explore the bioequivalence between thegeneric(test product)and the original(reference product)ketorolac tromethamine(KT)tablets.Methods According to randomized,open,single-dose,double-cycle anddouble-cross controlled trial,80 healthy volunteers were averagely divided into fasting group and postprandial group.All were given test product or reference product.The blood concentration of KT was detected by high performance liquid chromatography at different times.The pharmacokinetics parameters of plasma KT were calculated.Theevaluation of bioequivalence and safety in the two products was conducted.Results The C_(max),AUC_(0-t)and AUC0-infof reference product in the fasting group were 0.60 mg/L,3.66 h·mg/L and 3.97 h·mg/L,while those in the postprandial group were 0.65 mg/L,4.26 h·mg/L and 4.46 h·mg/L.C_(max),AUC_(0-t)and AUC0-infof test product in the fasting group were 0.58 mg/L,3.51 h·mg/L and 3.80 h·mg/L,while those in postprandial groupwere 0.62 mg/L,4.02 h·mg/L and 4.20 h·mg/L.Under fasting and postprandial conditions,C_(max),AUC_(0-t),AUC0-infand 90%CI of the test product and reference product were all within 80%-125%,meeting the requirements of bioequivalence,withoutserious or severe adverse events.Conclusion Under fasting and postprandial conditions,there is bioequivalence between oral test and reference KT tablets in healthy objects,with good safety.

关 键 词：酮咯酸氨丁三醇片 药代动力学 生物等效性 安全性 

分 类 号：R917[医药卫生—药物分析学]