血栓通注射液对大鼠体内细胞色素P450酶活性的影响  

Influence of Xueshuantong Injection on P450 Activities Using a Cocktail Method

作　　者：刘史佳[1,2] 居文政[2] 陈为烤[1] 许黎君[1] 熊宁宁[2] 谈恒山[3] 

机构地区：[1]南京中医药大学药学院,南京210009 [2]南京中医药大学附属医院临床药理科,南京210029 [3]南京军区总医院,南京210002

出　　处：《中国药学杂志》2010年第2期115-118,共4页Chinese Pharmaceutical Journal

基　　金：科技部"十一五"支撑计划课题(2006BAI14B07)

摘　　要：目的用Cocktail探针药物法,研究血栓通注射液对大鼠肝细胞细胞色素P450(CYP450)的影响。方法分别以茶碱、氯唑沙宗和咪哒唑仑作为CYP1A2,CYP2E1及CYP3A4的探针药,将大鼠随机分为低剂量和高剂量两组,每日尾静脉注射血栓通注射液,采用高效液相色谱法测定连续使用血栓通注射液前后大鼠血浆中相应的探针药物的浓度及其药动学参数。结果连续注射14 d后,与用药前比较,茶碱、氨苯砜的血药浓度及其药动学参数未见显著性改变;但低剂量组和高剂量组中氯唑沙宗的AUC0t-减少,mρax明显降低,CL/F显著增加,t1/2和Vd/F变化不明显。高剂量组中tm ax有所降低(P<0.05)。结论连续注射血栓通注射液14 d后,对CYP2E1酶活性有显著诱导作用,而对CYP3A4、CYP1A2酶活性无影响。OBJECTIVE To evaluate the effects of Xueshuantong Injection on P450 activities by Cocktail probe drugs in rats. METHODS Three probe drugs （theophylline, dapsone, chlorzoxazone） were simultaneously given to rats after middle and high dosing of Xueshuantong injection. The plasma concentrations of the three probes were measured By HPLC and their corresponding pharmacokinetic parameters were calculated. RESULTS There were no differences on theophylline and dapsone plasma concentrations and the corresponding pharmacokinetie parameters in rats between before and after Xueshuantong injection administration for 14 d. But AUC0-4 and the concentration of chlorzoxazone were decreased significantly （P 〈 0. 05） and the CL/F was increased in rats after Xueshuantong Injection for 14 consecutive days. No influences were observed on t1/2 and Vd/F. CONCLUSION Xueshuantong injection can induce CYP2E1 activity significantly, but it shows no effect on CYP3A4 and CYP1A2.

关 键 词：COCKTAIL 探针药物 血栓通注射液 细胞色素P450 

分 类 号：R965[医药卫生—药理学]