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该研究旨在探究溶栓胶囊、血脂康胶囊、心元胶囊和松龄血脉康胶囊对氯吡格雷活性代谢产物药动学的影响.在中国,中药制剂溶栓胶囊、血脂康胶囊、心元胶囊和松龄血脉康胶囊广泛用于心血管疾病的临床治疗,且常与抗血小板药物氯吡格雷联合使用.我们模拟人体给药对大鼠体内四种中药制剂对氯吡格雷活性代谢产物药动学的影响进行了研究.单独口服氯吡格雷(7.5 mg/kg)或口服溶栓胶囊(75 mg/kg)、血脂康胶囊(60 mg/kg)、心元胶囊(120 mg/kg)或松龄血脉康胶囊(150 mg/kg)后口服氯吡格雷(7.5 mg/kg)后采集血样获得活性代谢产物药动学参数.与对照组相比,合用血脂康胶囊后,活性代谢产物衍生物的药时曲线下面积(AUC0-t明显减小25.4％,但t1/2和Vz/F分别明显增加43.6％和70.7％.与对照组相比,合用溶栓胶囊、心元胶囊和松龄血脉康胶囊后,活性代谢产物药动学参数虽有变化,但变化无统计学意义.该研究表明血脂康胶囊对活性代谢产物的形成和代谢均有一定影响.氯吡格雷抗血小板活性会在联合使用血脂康胶囊初期减弱,此外长期联合使用会导致副作用.“,”In the present study,we aimed to examine the effects of Rong Shuan capsule,Xue Zhi Kang capsule,Xin Yuan capsule and Songling Xue Mai Kang capsule on the pharmacokinetics of clopidogrel active metabolite (CAM).The traditional Chinese medicines (TCMs) Rong Shuan capsule,Xue Zhi Kang capsule,Xin Yuan capsule and Songling Xue Mai Kang capsule are widely used to treat cardiovascular disease in China.They are often prescribed in combination with clopidogrel,a common anti-platelet Western drug.We investigated the influence of the four TCMs on CAM pharmacokinetics following administration at human dose in rats.Pharmacokinetic parameters were determined following oral (PO) administration of clopidogrel (7.5 mg/kg) with or without Rong Shuan capsule (75 mg/kg,PO),Xue Zhi Kang capsule (60 mg/kg,PO),Xin Yuan capsule (120 mg/kg,PO),or Songling Xue Mai Kang capsule (150 mg/kg,PO).Compared with the animals in the control group,Xue Zhi Kang capsule significantly decreased the area under the plasma concentration-time curve (A UC0-t) of the CAM derivative by 25.4％.However,the t1/2 and Vz/F of CAM derivative were significantly increased by 43.6％ and 70.7％,respectively.It was also observed that the pharmacokinetic parameters were altered in groups pretreated with Rong shuan capsule,Xin yuan capsule or Songling Xue mai kang capsule compared with the control group,but not significant.This study indicated that Xue Zhi Kang capsule had an effect on the formation and metabolism of CAM.Therefore,in the beginning of co-administration of Xue Zhi Kang capsule and clopidogrel,the anti-platelet efficacy might be compromised because of the decreased formation of CAM.Otherwise,long-time co-administration might lead to side effects by the prolongation of the t1/2 and Vz/F increase of CAM.