愈风宁心片中葛根素在小鼠体内的药动学和生物利用度研究  

Studies on Pharmacokinetics and Bioavailability of Puerarin in Yufeng Ningxin Tablet in Mice

作　　者：吴燕红[1] 苏子仁[1] 赖小平[1] 姚红[2] 林吉[1] 

机构地区：[1]广州中医药大学,广州510405 [2]广州医学院,广州510182

出　　处：《中药新药与临床药理》2004年第4期259-261,共3页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：广东省自然科学基金重点项目(编号022313);广东省科技攻关项目(编号20020209);国家中医药管理局项目(编号0304P44)。

摘　　要：目的测定口服愈风宁心片在小鼠体内葛根素的药-时曲线,并与葛根素静注相比较,计算其体内药动学参数和生物利用度。方法将NIH小鼠随机分成不同的时间组,采用6%高氯酸水溶液沉淀血浆蛋白,HPLC法测定小鼠血浆中的葛根素含量,用PKsolutions2.0(非房室模型)程序计算药动学参数和生物利用度。结果小鼠静脉注射(0.01g/kg)葛根素注射液主要药动学参数分别是t1/2=98.359min,CL=35.548mL·min-1,AUC(0-∞)=281.3μg·min·mL-1;小鼠灌胃愈风宁心片(相当于葛根素0.2g/kg)主要药动学参数分别是t1/2=35.562min,CL=898.685mL·min-1,Cmax=9.3μg·mL-1,Tmax=30min,AUC(0-∞)=222.5μg·min·mL-1,与静脉注射相比较,生物利用度为3.95%。结论小鼠口服愈风宁心片,葛根素在小鼠体内吸收极少。提高愈风宁心片口服的生物利用度,将提高临床用药有效性。Objective To evaluate the pharmacokinetic parameters and bioavailability of puerarin in Yufeng Ningxin tablets in mice by determining dose-time curve and by comparing with the pharmacokinetics of puerarin injection.Methods NIH mice were randomized into different groups. 6 %HClO4 was used to precipitate plasma protein and the plasma concentration of puerarin in mice was determined by HPLC.The PK solutions 2.0 program,a non-compartmental model software,was applied to calculate the pharmacokinetic parameters and bioavailability.Results The main pharmacokinetic parameters of puerarin injection by i.v.in mice were:t1/2=98.359 min,CL=35.548 mL·min-1,AUC(0-∞)=281.3 μg·min·mL-1;the main pharmacokinetic parameters of puerarin in Yufeng Ningxin tablets by o.p.were:t1/2 =35.562 min,CL=898.685 mL·min-1,Cmax=9.3 μg·mL-1,Tmax=30 min,AUC(0-∞)=222.5 μg·min·mL-1 ,F(bioavailability value)=3.95 %comparing to puerarin injection.Conclusion As compared with puerarin injection,the absorptive content of puerarin in Yufeng Ningxin tablets is very poor and the bioavailability is also low,indicating that enhancement of bioavailability of Yufeng Ningxin tablets will be beneficial to the clinical application.

关 键 词：愈风宁心片 葛根素 药动学参数 生物利用度 

分 类 号：R285.5[医药卫生—中药学] R969.1[医药卫生—中医学]