蛇床子素在兔体内的药动学研究  

Pharmacokinetics of osthol in the rabbits

作　　者：郑立卿[1] 张丹参[1,2] 张力[1] 薛贵平[1] 武海霞[1] 

机构地区：[1]河北北方学院药理教研室,河北张家口075000 [2]河北医科大学,河北石家庄051500

出　　处：《中成药》2010年第10期1698-1702,共5页Chinese Traditional Patent Medicine

基　　金：河北省自然科学基金资助项目(2004000653);河北省中医药管理局资助项目(2009065)

摘　　要：目的:研究蛇床子素在兔体内的药代动力学特点。方法:18只新西兰兔分成3组经ip分别给15、30和60mg/kg蛇床子素,以RP-HPLC法测定家兔在5、10、20、30、45、60、75、90、110和125min时血浆中蛇床子素浓度,用3P87软件处理血药浓度-时间数据,分析房室模型和药代动力学参数。结果:家兔ip蛇床子素15、30、60mg/kg的时量曲线属一室开放一室模型。AUC有明显的剂量依赖关系,半衰期、峰浓度和AUC相邻剂量间有显著性差异(P<0.05),剂量越大消除越快。家兔iv本品15mg/kg的时量曲线属二室模型,但其消除快于ip。蛇床子素血浆蛋白结合率为76%。结论:蛇床子素在家兔体内吸收快、起效快、蛋白结合率较高、消除快。在考察浓度范围内,蛇床子素ip在兔体内符合线性动力学过程。AIM：To study the characteristic of pharmacokinetics of osthol in rabbits.METHODS：Eighteen New Zealand rabbits were assigned into three groups and given osthol solution containing the concentration of 15,30 and 60 mg/kg,respectively.The plasma osthol concentrations at 5,10,20,30,45,60,75,90,110 and 125 min were detected by RP-HPLC and used to analyze the pharmacokinetic parameters in the compartment model by 3 p87 programme.RESULTS：The elimination process of osthol 15,30 and 60 mg/kg,ip in rabbit plasma corresponded with one-compartment with first order,and the experiment showed that Cmax t1/2（Ke） and AUC had markedly dosedependent relation,difference in half-life,peak area and AUC between three osthol concentration.The more the high concentration,the more the rapidly eliminate dose-dependent curve in the condition of 15 mg/kg,iv.fitted with two-compartment model and had rapid elimination rate the average of plasma protein binding rate with osthol was up to 76%.CONCLUSION：Osthol could be absorbed quickly,be taken effect quickly,the plasma protein binding rate is high and be eliminated quickly and the pharmocokinetics of osthol ip fits linear process during experiment concentrations.

关 键 词：蛇床子素 药动学 反相高效液相色谱 血药浓度 血浆蛋白结合率 家兔 

分 类 号：R966[医药卫生—药理学]