格列吡嗪片在中国健康受试者中的生物等效性研究  

Bioequivalence study of glipizide tablets in Chinese healthy subjects

作　　者：郑飞浪[1,2] 程林忠[2] 李海菊[2] 杨璐[2] 刘泽源 王素玲[2] ZHENG Fei-lang;CHENG Lin-zhong;LI Hai-ju;YANG Lu;LIU Ze-yuan;WANG Su-ling(Department of Pharmacy,Heping Hospital Affiliated to Changzhi Medical College,Changzhi 046000,Shanxi Province,China;Drug Clinical Trial Institution,Heping Hospital Affiliated to Changzhi Medical College,Changzhi 046000,Shanxi Province,China;Medical Institution Conducting Clinical Trials for Human Used Drug,The Fifth Medical Center of the General Hospital of the Chinese People's Liberation Army,Beijing 100039,China)

机构地区：[1]长治医学院附属和平医院药剂科,山西长治046000 [2]长治医学院附属和平医院药物临床试验机构,山西长治046000 [3]中国人民解放军总医院第五医学中心药物临床试验机构,北京100039

出　　处：《中国临床药理学杂志》2024年第11期1628-1632,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究2种格列吡嗪片制剂在中国健康受试者的生物等效性。方法用单剂量、随机、开放、两周期、自身交叉对照试验设计,空腹试验、餐后试验各入组28例健康受试者,2个周期分别口服格列吡嗪片受试制剂或参比制剂5 mg。用液相色谱串联质谱法测定给药后不同时间点格列吡嗪的血药浓度,用非房室模型计算药代动力学参数,评价2种制剂的生物等效性。结果空腹试验中格列吡嗪受试制剂和参比制剂的主要药代动力学参数:C_(max)分别为(551.60±91.26)和(518.10±105.10)ng·mL^(-1),AUC_(0-t)分别为(3074.33±861.91)和(3026.77±934.25)h·ng·mL^(-1),AUC_(0-∞)分别为(3204.85±990.78)和(3166.35±1107.36)h·ng·mL^(-1)。餐后试验中格列吡嗪受试制剂和参比制剂的主要药代动力学参数C_(max)分别为(517.30±98.97)和(472.80±114.48)ng·mL^(-1),AUC_(0-t)分别为(3001.12±830.87)和(2932.79±736.35)h·ng·mL^(-1),AUC_(0-∞)分别为(3067.00±918.84)和(2997.44±819.14)h·ng·mL^(-1)。受试制剂与参比制剂主要药代动力学参数C_(max)、AUC_(0-t)和AUC_(0-∞)经对数转换后几何均值比值的90%置信区间均在80.00%~125.00%。空腹组与餐后组均未发生严重不良事件。结论2种格列吡嗪片在空腹及餐后状态下均具有生物等效性,且安全性良好。Objective To study the bioequivalence of two glipizide tablets in healthy Chinese subjects.Methods Randomized,open,single-administration,two-period,self-cross-over trial design was used in the study.There were 28 Chinese healthy subjects in the fasted state and28 in the fed state,complete repeat cross single dose oral glipizide tablets test preparation or reference preparation 5 mg.The plasma concentration of glipizide was determined by liquid chromatography/tandem mass spectrometry at different time points after administration.The noncompartmental model was used to calculate the pharmacokinetic parameters and evaluate the bioequivalence of the two formulations.Results The main pharmacokinetic parameters of glipizide in the fasted state were as follows:C_(max)were(551.60±91.26)and(518.10±105.10)ng·mL^(-1);AUC_(0-t)were(3074.33±861.95)and(3026.77±934.25)h·ng·mL^(-1);AUC_(0-∞)were(3204.85±990.78)and(3166.35±1107.36)h·ng·mL^(-1).The parameters of glipizide in the fed state were as follows:C_(max)were(517.30±98.97)and(472.80±114.48)ng·mL^(-1);AUC_(0-t)were(3001.12±830.87)and(2932.79±736.35)h·ng·mL^(-1);AUC_(0-∞)were(3067.00±918.84)and(2997.44±819.14)h·ng·mL^(-1).The 90%confidence interval of the C_(max),AUC_(0-t)and AUC_(0-∞)of the test formulation and the reference formulation were from 80.00%to 125.00%.The incidence of adverse events in fasted group and fed group was no serious adverse events.Conclusion The two glipizide tablets were bioequivalent under fasted and fed conditions,and good security.

关 键 词：格列吡嗪片 生物等效性 药代动力学 安全性 

分 类 号：R977.15[医药卫生—药品]