黄芩苷及其含药血清在大鼠体内的药动学、药效学相关性研究  

Studies on correlation between pharmacodynemics and pharmacokenitics characteristics of baicalin using serum pharamoclogical test in rats

作　　者：宋珏[1] 路通[2] 谢林[3] 王广基[3] 刘晓东[3] 

机构地区：[1]安徽医科大学药学院药剂教研室 [2]中国科学院上海药物研究所药物代谢研究中心,上海201203 [3]中国药科大学药物代谢动力学重点实验室

出　　处：《中国临床药理学与治疗学》2006年第12期1350-1354,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家中医药管理局资助项目(№02-032P32);国家"863"项目(№2003AA2Z347A)

摘　　要：目的：以黄芩苷含药血清对PC12细胞氧化损伤的保护作用为药效指标，研究黄芩苷的体内药动学及药效学过程的相关性。方法：大鼠灌胃后，测定不同取血点血清样本中的黄芩苷含量，运用血清药理学方法，观察血清样本对H2O2诱导PC12细胞氧化损伤模型的保护作用，对浓度．时间、效应．时间曲线进行相关分析，建立药动．药效结合模型；观察不同浓度黄芩苷溶液的保护作用，获得黄芩苷体外抗氧化作用的量效关系。结果：黄芩苷含药血清对PC12细胞氧化损伤有明显保护作用，且具有时间依赖性。效应-时间曲线的Emax为98％，fmax为15min；浓度-时间曲线的Cmax为9．39μg·ml^-1，fmax亦为15min，以Log（AUC）-AUE作图，图形近似呈“S”形。体外实验中，黄芩苷浓度在0．16～10μg·ml^-1范围内有抑制作用，且作用随剂量增加而增大。结论：黄芩苷体内、外均具有抗氧化作用，且效应的时效关系与血清中黄芩苷的时量关系呈正相关。AIM： To study the correlation between pharmacodynemics and phannacokenitics characteristics of baicalin using serum pharamnoclogical test in vitro. METHODS： After administration of baicalin in rats, the drug-contained serum was obtained at different time and each sample was divided into two portions. One portion was respectively added into the cultured PC12 cells, which bad been treated with H2O2, and the viability was determined by MTT colormetric microassay. The other was used to determine the concentration of baicalin in each serum sample. Then the relationship among concentration,time and effect could be established. Furthermore, the relationship of concentration-effect of bacalin solution was also investigated in vitro. RESULTS： Exact antioxidant effects of baicalin solution and drug-contained serum could be shown in vitro test. The curves of time-effect and time-concentration were both peaked at 15 min after oral administration. CONCLUSION： The protection rate of the baicalin-contained serum had a positive correlation with the AUC of baicalin in serum.

关 键 词：黄芩苷 PC12细胞 血清药理学 药动-药 效结合模型 

分 类 号：R969.1[医药卫生—药理学]