黄连解毒散超微细粉中黄芩苷在家兔体内的药代动力学研究  

Pharmacokinetic Study of the Baicalin from Ultramicro-pulverised Powder of Huanglian jiedusan(HLJDS) in Rabbits

作　　者：马玉芳[1] 林雪玲[1] 俞道进[1] 姚金水[1] 黄小红[1] 黄一帆[1] 

机构地区：[1]福建农林大学动物科学学院/动物保健研究所,福州350002

出　　处：《畜牧兽医学报》2007年第12期1368-1372,共5页ACTA VETERINARIA ET ZOOTECHNICA SINICA

基　　金：国际科技合作重点项目(2003DF030008);福建省科技厅重点项目(2004N031);福建省自然科学基金项目(B0710002)

摘　　要：采用高效液相色谱法测定灌胃给予黄连解毒散超微细粉和细粉的家兔血浆中黄芩苷的浓度,血药浓度-时间数据经药代动力学分析软件(Pharmaceutical Kinetics Software,PKS)处理,比较黄连解毒散超微细粉和普通细粉中黄芩苷在家兔体内的药代动力学参数。结果如下:黄连解毒散超微细粉组、普通细粉组黄芩苷的药代动力学最佳模型均为二室开放模型。黄连解毒散超微细粉主要药动学参数:Ka=0.497 h-1,t1/2α=2.556 h,t1/2β=8.46 h,AUC0→∞=3.401μg.h/mL,Vd=6.752 L/kg,Tpeak=3.005 h,Cmax=0.311μg/mL;黄连解毒散普通细粉主要药动学参数:Ka=0.419 h-1,t1/2α=2.74 h,t1/2β=5.83 h,AUC0→∞=2.611μg.h/mL,Vd=12.890 L/kg,Tpeak=3.645 h,Cmax=0.215μg/mL。与细粉比较,黄连解毒散超微细粉中黄芩苷的相对生物利用度提高了30.26%。上述结果表明,黄连解毒散经超微粉碎后吸收相增大,可显著提高其有效成分黄芩苷的生物利用度。High performance liquid chromatography（HPLC） was applied to determine the concentrations of plamsa baicalin in two groups of rabbits after administering the ultramicro-pulverised powder and the ordinary powder of HLJDS （in water suspension） by gastrogavage respectively. The plasma concentration-time data of baicalin were dealt with Pharmaceutical Kinetics Software （PKS）. Pharmacokinetics characteristics of both the ultramicro-pulverised powder and ordinary powder of HLJDS were compared. The results showed that the best pharmacokinetic model of baicalin in either group was two-compartment open model. The main pharmacokinetic parameters of baicalin of ultramicro-pulverised powder were as follows. Ka=0.497h^-1,＇t1/2α=2.556h,t1/2β=8.46h,AUC0→∞=3.401μg·h/mL,Vd=6.752L/kg,Tpeak=3.005h,Cmax=0.311μg/mL; The main pharmacokinetic parameters of baicalin of the ordinary powder were as follows： Ka=0.419h^-1,t1/2α=2.74h,t1/2β=5.83h,AUC0→∞=2.611μg·h/mL,Vd=12.890L/kg,Tpeak=3.645h,Cmax=0.215μg/mL. As compared to the baicalin from ordinary powder, the relative bioavailability of baicalin from ultramicro-pulverised powder was increased by 30.26 %. These data presented above indicated that the bioavailbility of baicalin from HLJDS could be greatly improved after processing and preparing by the technique of ultromicro-pulverization.

关 键 词：黄连解毒散 超微细粉 黄芩苷 药代动力学 生物利用度 

分 类 号：S859.7[农业科学—临床兽医学] S853.7[农业科学—兽医学]