灯盏细辛注射液多成分血浆蛋白结合率测定  

Determination of plasma protein binding rate of multicomponent in Dengzhanxixin injection

作　　者：周玲[1] 居文政[2] 刘子修[1] 谈恒山[3,4] 

机构地区：[1]南京中医药大学药学院,江苏南京210002 [2]南京中医药大学附属医院临床药理科,江苏南京210029 [3]南京中医药大学 [4]南京军区总医院,江苏南京210002

出　　处：《中国药理学通报》2011年第5期719-722,共4页Chinese Pharmacological Bulletin

基　　金：国家重大新药创制资助项目(No2008ZX09312-004);江苏省中医药领军人才资助项目(NoLJ200906)

摘　　要：目的建立同时检测灯盏细辛注射液中6个成分在大鼠血浆中药物浓度的方法,并测定其体外血浆蛋白结合率。方法采用平衡透析法测定血浆蛋白结合率,采用HPLC法测定各成分的血药浓度及游离药物浓度,生物样本用乙酸乙酯液提取的方法。结果在低、中、高3种浓度下,绿原酸、咖啡酸、1,5-O-二咖啡酰奎宁酸、灯盏乙素、3,5-二-O-咖啡酰奎宁酸、3,4-二-O-咖啡酰奎宁酸的平均血浆蛋白结合率分别为(76.94±3.72)%、(91.57±0.96)%、(83.32±3.73)%、(91.66±0.71)%、(95.73±0.67)%、(94.21±0.65)%。结论采用HPLC法对灯盏细辛注射液中的多个成分进行分离,方法简便、可靠、稳定。6个成分在大鼠体外均有较高的血浆蛋白结合率。Aim To establish a detection method for determination of concentration of six major compounds in Dengzhanxixin injection in rat plasma and to study the plasma protein binding rate.Methods The equilibrium dialysis was carried out to determine the plasma protein binding rate of multicomponent in Dengzhanxixin injection,and the drug concentration was detected by HPLC method.The biological samples were all handled with acetic ether-extracting.Results The average plasma protein binding rates of six compounds at low,middle and high concentrations were as follows,respectively：caffeotannic acid was（76.94±3.72）%,caffeic acid was（91.57±0.96）%,1,5-DCQA was（83.32±3.73）%,scutellarin was（91.66±0.71）%,3,5-DCQA was（95.73±0.67）%,3,4-DCQA was（94.21±0.65）%.Conclusions The HPLC method is used for the first time to determine the concentration of multicomponent in Dengzhanxixin injection.The method is simple,reliable and stable.The six major compounds in Dengzhanxixin injection have high capacity in binding to plasma protein in rat in vitro.

关 键 词：灯盏细辛注射液 绿原酸 咖啡酸 1 5-DCQA 灯盏乙素 3 5-DCQA 3 4-DCQA 平衡透析法 

分 类 号：R-332[医药卫生] R282.71