头孢克洛干混悬剂在中国健康受试者中的生物等效性研究  

Bioequivalence study of cefaclor for suspension in Chinese healthy subjects

作　　者：李海菊[1,2] 程林忠[1] 常生 张红莲 王素玲[1] 杨璐[1] LI Hai-ju;CHENG Lin-zhong;CHANG Sheng;ZHANG Hong-lian;WANG Su-ling;YANG Lu(MedicalInstitution Conducting Clinical Trials for Human Used Drug,Heping Hospital Affliated to Changzhi MedicalCollege,Changzhi 046000,Shangxi Province,China;Department of Pharmacy,Changzhi Medical College,Changzih0i46000,Shangxi Province,China;Shijiazhuang No.4 Pharmaceutical Company Limited,Shijiazhuangg 052160,Hebei Province,China)

机构地区：[1]长治医学院附属和平医院药物临床试验机构,山西长治046000 [2]长治医学院药学系,山西长治046000 [3]石家庄四药有限公司,河北石家庄052160

出　　处：《中国临床药理学杂志》2023年第9期1287-1291,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究在中国健康受试者中头孢克洛干混悬剂的药代动力学,评估国产受试制剂与原研参比制剂的生物等效性。方法采用单剂量、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36例健康受试者,2个周期分别口服头孢克洛干混悬剂受试制剂和参比制剂0.125 g,在给药前后按设计的时间点采集静脉血。用液相色谱串联质谱法测定血浆中的头孢克洛浓度,用SAS 9.4软件计算药代动力学参数,并进行生物等效性分析。结果空腹试验受试制剂和参比制剂的头孢克洛Cmax分别为(7277.82±1501.52)和(7470.28±1647.19)ng·mL^(-1),AUC_(0-t)分别为(5867.31±650.95)和(5856.08±673.84)ng·mL^(-1)·h,AUC0-∞分别为(5907.58±652.96)和(5895.61±676.11)ng·mL^(-1)·h。餐后试验受试制剂和参比制剂的头孢克洛Cmax分别为(1894.29±381.99)和(1964.57±551.52)ng·mL^(-1),AUC0-t分别为(5072.71±638.83)和(5101.20±674.18)ng·mL^(-1)·h,AUC_(0-∞)分别为(5115.37±642.61)和(5149.54±696.66)ng·mL^(-1)·h。空腹试验和餐后试验Cmax、AUC0-t和AUC0-∞的几何均值比(受试制剂/参比制剂)及其90%置信区间在80.00%~125.00%。结论在空腹和餐后给药条件下,2种头孢克洛干混悬剂在中国健康受试者体内均具有生物等效性,且安全性良好。Objective To study the pharmacokinetics of two cefaclor for suspension in Chinese subjects and then to evaluate the bioequivalence.Methods Randomized,open,single-administration,two-period,self-cross-over trial design was used in the study.There were 36 Chinese healthy subjects in the fasted state and 36 in the fed state.Each subject was given a single administration of test and reference preparation of cefaclor for suspension(each 0.125 g),and blood samples were taken at different time points,repectively.The concentrations of cefaclor in plasma were determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated and the bioequivalence was evaluated by SAS 9.4.Results The main pharmacokinetic parameters of cefaclor in the fasted state were as follows:Cmax were(7277.82±1501.52)and(7470.28±1647.19)ng:mL^(-1);AUCo-t were(5867.31±650.95)and(5856.08±673.84)ng·mL^(-1)·h;AUC0-αwere(5907.58±_652.96)and(5895.61±676.11)ng:mL^(-1).h.The parameters of cefaclor in the fed state were as follows:Cmax were(1894.29±381.99)and(1964.57±551.52)ng:mL^(-1);AUC_(o-t)were(5072.71±638.83)and(5101.20±674.18)ng·mL^(-1).h;AUC_(o-t)were(5115.37±642.61)and(5149.54±696.66)ng·mL-1.h.The 90%CIs of Cmax,AUC_(o-t)and AUC o-αwere in 80.00%-125.00%both in the fasted state and fed state.Conclusion The two cefaclor for suspension were bioequivalent and safe in healthy subjects both in the fasted state and fed state.

关 键 词：头孢克洛干混悬剂 药代动力学 生物等效性 安全性 

分 类 号：R97[医药卫生—药品]