强痛宁在试验犬血浆中的药代动力学特征及药动-药效同步模型的建立  

Pharmacokinetics characteristic and pharmacokinetics-pharmacodynamic synchronous model of Qiangtongning in plasma of dogs

作　　者：范宏刚[1] 高利[1] 肖建华[1] 卢德章[1] 马海鵾 胡魁[1] 刘焕奇[1] 王洪斌[1] 

机构地区：[1]东北农业大学动物医学学院,黑龙江哈尔滨150030

出　　处：《中国兽医学报》2009年第8期1047-1051,共5页Chinese Journal of Veterinary Science

基　　金：国家自然科学基金资助项目(30671552);黑龙江省自然科学基金重点项目(ZJH0503-01);黑龙江省研究生创新科研资助项目(YJSCX2007-0065HLJ)

摘　　要：采用高效液相色谱法（HLCP）测定犬血浆中强痛宁血药浓度,以探讨强痛宁在犬血浆中代谢规律及药效、毒副作用与血药浓度之间的关系。给试验犬静脉注射2μg/kg强痛宁后,血药经时过程符合无吸收的三室开放性模型,t1/2π为1.591 min、t1/2α为7.892 min、t1/2β为140.283 min;kel为0.009 02 min;V1为153.372 mL/kg、VB为306.535 mL/kg;CL为2.379 mL·kg^-1·min^-1;AUC为906.040μg·min^-1;TCP为237.503 min。同时建立了强痛宁与镇痛效果、脉搏脉搏血氧饱和度、心率、呼吸频率等监测指标之间的药动—药效同步模型,直观、快捷地描述了强痛宁血浆药物浓度与药效之间的量时—量效关系,最终根据构建的模型及线性回归方程,得出了保证犬安全（脉搏脉搏血氧饱和度〉85%）且有良好的术中、后镇痛效果的强痛宁血药质量浓度范围分别为4-4.77μg/L和2.0-4.77μg/L;术后镇痛最低有效质量浓度为2μg/L。This study established a method using the high performance liquid chromatography to determine the concentration of Qiangtongning in plasma. The concentration-time course in plasma can be described by a three-compartment open model without absorption after the experimental dogs were injected intravenously Qiangtongning （2 μg/kg,b, w）. The results were as follaw： t1/2 = 1. 591 min, t1/2α = 7. 892 min, t1/2β = 140. 283 min; kel = 0. 009 02 min^-1 ;V1=153. 372 mL/kg,VB306. 535 mL/kg;CL=2. 379 mL· kg^-1 ·min^-1 ; AUC=960. 040 μg· min· L^-1 ;TCP= 237. 503 rain,indicating that the simultaneous pharmacokineticspharmacodynamics model was built and the dose-time and dose-efficacy relationships between plasma concentration of drug and pharmacodynamics were described directly. It is determined that the minimal efficacious plasma concentration of Qiangtongning for operative analgesia of experimental dogs is 4-4.77 μg/L,2. 0-4. 77 μg/L and for postoperative analgesia is 2 μg/L.

关 键 词：强痛宁 犬 血浆 药代动力学特征 药动-药效同步模型 

分 类 号：S859.7[农业科学—临床兽医学]