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 ba
2、sic 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 secretionTu
3、bular reabsorptionIonized, 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 0406080100151050100Z
4、ero-order elimination 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
