1、 DrugBodypharmacodynamicspharmacokinetics 研究内容研究内容吸收吸收(absorption)代谢代谢(metabolism)排泄排泄(excretion)分布分布(distribution)生物利用度肝肠循环首关消除滤 过Simple diffusionmembraneHigh pH(more basic side)Low pH(more acidic side)At steady state,an acidic drug will accumulate on the more basic side of the membrane and a basic
2、 drug on the more acidic sideSimple diffusionpH 7.0pH 7.4Epithelial cell in GI tractGI tract:limit the absorptionKidney:promote the renal excretionLiver:promote the biliary excretionBrain:limit entry to brainFunction as a barrier system to protect cellsGlomerular filtrationTubular secretionTubular r
3、eabsorptionIonized,polar,water-solubleCompetitive inhibitionPlasma protein bindingLipid solubilityPolarity 一室模型 0123456781010010002000实 测值-拟 合 曲 线CA4P/nmol.ml-1时 间 (h)e-ket -tdtdc303.2ke -t303.2kedtdcDrug concentration in bloodDrug concentration in bloodTime Time 0406080100151050100Zero-order elimin
4、ation First-order elimination =024681012141618101001000 8mg/kg 4mg/kg 2mg/kgConcentration(ng/mL)t/min消除动力学的临床意义消除动力学的临床意义今有今有A、B两种不同药物，给一位患者静脉注射，测得其剂量与半衰期数两种不同药物，给一位患者静脉注射，测得其剂量与半衰期数据如下，请问下列叙述哪一项是正确的据如下，请问下列叙述哪一项是正确的A 说明药物说明药物B是以零级过程消除是以零级过程消除 B 两种药物都以一级过程消除两种药物都以一级过程消除 C 药物药物B是以一级过程消除是以一级过程消除 D 药物药物A是以一级过程消除是以一级过程消除 E A、B都以零级过程消除都以零级过程消除剂剂量量（mg）药药物物A的的t1/2（h）药药物物B的的t1/2（h）40 10 3.47 60 15 3.47 80 20 3.47 tCuUnit:(mg/mL)min,(mg/L)h,(ng/L)min,(ng/mL)h,etcCtHalf life,（t1/2）Half life,（t1/2）-303.2keThe meaning of Vd
