雷贝拉唑对氯吡格雷在大鼠体内药动学的影响  

Effects of Rabeprazole on Pharmacokinetics of Clopidogrel in Rats

作　　者：王军[1] 付翠香[1] 吴伟明[1] 王增寿[1] 胡国新[2] 

机构地区：[1]温州医学院附属第二医院药学部,浙江温州325027 [2]温州医学院药学院药理学教研室,浙江温州325027

出　　处：《中国现代应用药学》2013年第4期364-368,共5页Chinese Journal of Modern Applied Pharmacy

基　　金：温州市科技计划项目(Y20100262)

摘　　要：目的研究雷贝拉唑对氯吡格雷在大鼠体内的药动学的影响。方法将16只大鼠随机分成2组,单独给予氯吡格雷(Ⅰ组)和联用雷贝拉唑(Ⅱ组),于给药后不同时间点采集血样,HPLC-DAD法测定血浆中氯吡格雷代谢产物SR26334的浓度,用DAS药动学软件对SR26334血药浓度-时间数据采用非房室模型分析,求得氯吡格雷在大鼠体内主要的药动学参数,并对其进行统计分析。结果与单用组比较,联用雷贝拉唑组的主要药动学参数(AUC(0-48),AUC(0-∞),MRT(0-48),t1/2,CL/F,Cmax差异均无统计学意义(P>0.05),tmax由(1.17±0.41)h减少为(0.58±0.20)h(P<0.01)。结论雷贝拉唑加快氯吡格雷在体内代谢为SR26334的速度,但对于其代谢程度没有显著性影响。OBJECTIVE To study the effect of rabeprazole on pharmacokinetics of clopidogrel in rats. METHODS A total of 16 rats were divided into two groups： one was administrated with clopidogre, and another with the combination of rabeprazole. Concentrations of clopidogre＇s metabolite SR26334 in plasma were determined by HPLC-DAD. The plasma concentration-time data of SR26334 were analyzed by DAS program according to non-compartment model. The main pharmacokinetic parameters of SR26334 were obtained and compared with SPSS software between two groups. RESULTS There was no significant difference between the single-drug group and the combined rabeprazole group in the main pharmacokinetics parameters of SR26334, such as AUC（0.48）, AUC（0-∞）, MRT（0.48）, t1/2, CL/F, Cmax （P〉0.05）. Compared with single-drug group, the tmax in combined rabeprazole group significantly decreased from （1.17±0.41）h to （0.58±0.20）h （P〈0.01）. CONCLUSION There is no effect of rabeprazole on pharmacokinetics of clopidogrel in rats. But rabeprazole can accelerate clopidogrel metabolism for SR26334 in vivo. But it has not significant influence to the degree of metabolism.

关 键 词：氯吡格雷 雷贝拉唑 SR26334 药动学 

分 类 号：R945.1[医药卫生—微生物与生化药学]