灯盏乙素的大鼠药代动力学和血小板聚集抑制率的相关性研究

Correlationship between pharmacodynamic manifestations of scutellarin in rats and Inhibition of platelet aggregation

目的:探讨灯盏花素注射液中灯盏乙素血药浓度与其药效学的相关性,为临床合理用药提供科学依据。方法:Wistar大鼠随机分为3.75、7.5和15 mg/kg三个剂量组,尾静脉注射灯盏花素注射液。给药前和给药后不同时间点取血测定三组血药浓度和ADP诱导的血小板聚集率,用统计学方法计算两者的相关性。结果:瞬时血药浓度(C)与ADP诱导的血小板聚集抑制率(Y)进行线性回归,相关系数r均>0.7。经统计学处理,各给药剂量下的瞬时血药浓度均与ADP诱导的大鼠血小板聚集抑制率呈显著正相关(P<0.01)。结论:灯盏乙素明显抑制ADP诱导的血小板聚集,并且其血药浓度与药效呈现一定的关系。本试验为灯盏乙素用于防治血栓性疾病提供了进一步的科学依据。

Objective： To explore the correlationship of plasma concentration of scutellarin in breviscapine and its pharmacodynamics,providing scientific evidence for rational clinical utilization of the medicine.Methods： Wistar rats were randomly divided into three groups,receiving 3.75,7.5 and 15 mg/kg of breviscapine,respectively.The rat plasma samples were collected before and after dosing and plasma concentrations of scutellarin were determined.The inhibition of ADP-induced platelet aggregation was also calculated and the relationship of the inhibition of platelet aggregation and plasma concentrations of scutellarin was investigated.Results： There was positive correlation between plasma concentrations（C） and the inhibition of platelet aggregation activity（Y） among all three doses（r0.7,P0.01）.Conclusion： The Results： show that scutellarin can inhibit ADP-induced platelet aggregation and there is a good correlation with plasma concentration and anti coagulation effects.Thus,the results of this study will serve as a good clinical evidence for the prevention and treatment of thrombosis.