《Biopharmaceutics and Pharmacokinetics》课程教学大纲 一、课程基本信息 英文名称 Biopharmaceutics andPharmacokinetics 课程代码 PHAR1091 课程性质 专业必修课程 授课对象 医18药学全英文 学 分 2.5 学 时 36 主讲救师 崔京浩阮建清 修订日期 2021.6.25 指定散材 Applied Biopharmaceutics Pharmacokinetics (7th version) 二、课程目标 (一)总体目标： Biopharmaceutics and Pharmacokinetics is a major required courses for pharmaceutical students.This course aims to provide professional information to students and benefit for an overall understanding of pharmaceutical science,familiar with the professional discipline knowledge,to grasp the concept of biopharmaceutics and pharmacokinetics,improve the capability to solve professional problems in drug development and pharmaceutical practices.To develop a sense of discipline identity of biopharmaceutics and pharmacokinetics,to clarify the direction and good learning objectives of future professional learning,and provide guidance for personal professional career development. (二)课程目标： Biopharmaceutics and Pharmacokinetics is very important in pharmaceutical area,which is a discipline that investigates the fate of drug in the body dynamically.This course describes factors affecting the absorption,distribution,and metabolism,and excretion of drugs.The students will be able to demonstrate
《Biopharmaceutics and Pharmacokinetics》课程教学大纲 一、课程基本信息 英文名称 Biopharmaceutics andPharmacokinetics 课程代码 PHAR1091 课程性质 专业必修课程 授课对象 医 18 药学全英文 学 分 2.5 学 时 36 主讲教师 崔京浩 阮建清 修订日期 2021.6.25 指定教材 Applied Biopharmaceutics & Pharmacokinetics（7th version） 二、课程目标 （一）总体目标： Biopharmaceutics and Pharmacokinetics is a major required courses for pharmaceutical students. This course aims to provide professional information to students and benefit for an overall understanding of pharmaceutical science,familiar with the professional discipline knowledge, to grasp the concept of biopharmaceutics and pharmacokinetics, improve the capability to solve professional problems in drug development and pharmaceutical practices.To develop a sense of discipline identity of biopharmaceutics and pharmacokinetics, to clarify the direction and good learning objectives of future professional learning, and provide guidance for personal professional career development. （二）课程目标： Biopharmaceutics and Pharmacokinetics is very important in pharmaceutical area,which is a discipline that investigates the fate of drug in the body dynamically. This course describes factors affecting the absorption, distribution, and metabolism, and excretion of drugs. The students will be able to demonstrate
an understanding of the differential and integrated equations associated with pharmacokinetic models and assess factors which affect the absorption,distribution,metabolism and excretion of drugs.At the same time,they will be able to describe the techniques used to determine drug concentrations in biological and formulation matrices and calculate appropriate dosing regimens using appropriate criteria. 课程目标1：(chapter1,2,4,5,6,7,8,9,10) 1.1 Master the definition of pharmacokinetics,research contents and basic pharmacokinetic parameters, grasp the calculation methods of pharmacokinetic parameters for different administration routes of one- compartment model.Understand the blood drug concentration-time curve and estimation of pharmacokinetic parameters of multi-compartment model,familiar with to identify compartment model.Master the basic concepts related to multi-dose administration,drug accumulation and blood concentration fluctuation. 1.2 Master the characteristics of nonlinear pharmacokinetics and Michaelis-Menten kinetics equation, approach the basic concept of statistical moment and the estimation of pharmacokinetic parameters. 课程目标2：(chapter11,12,14,15,16) 2.1 Understand the significance of biopharmaceutics and pharmacokinetics to new drug research and development and clinical application. 2.2 Master the structure and properties of biofilms,drug transport mechanism,drug absorption pathways in different parts,and factors affecting drug absorption including physiology,drugs,dosage forms and preparations. 2.3 Master the basic concepts of drug distribution,excretion and metabolism;skilled with the factors that affect drug distribution,the types of drug metabolic reactions and the factors that affect drug metabolism.To master the characteristics and influencing factors of renal excretion and other excretory pathways of drugs
an understanding of the differential and integrated equations associated with pharmacokinetic models and assess factors which affect the absorption, distribution, metabolism and excretion of drugs. At the same time, they will be able to describe the techniques used to determine drug concentrations in biological and formulation matrices and calculate appropriate dosing regimens using appropriate criteria. 课程目标 1：(chapter 1,2,4,5,6,7，8,9,10） 1.1 Master the definition of pharmacokinetics, research contents and basic pharmacokinetic parameters, grasp the calculation methods of pharmacokinetic parameters for different administration routes of onecompartment model. Understand the blood drug concentration-time curve and estimation of pharmacokinetic parameters of multi-compartment model, familiar with to identify compartment model. Master the basic concepts related to multi-dose administration, drug accumulation and blood concentration fluctuation. 1.2 Master the characteristics of nonlinear pharmacokinetics and Michaelis–Menten kinetics equation, approach the basic concept of statistical moment and the estimation of pharmacokinetic parameters. 课程目标 2：(chapter 11,12,14，15，16） 2.1 Understand the significance of biopharmaceutics and pharmacokinetics to new drug research and development and clinical application. 2.2 Master the structure and properties of biofilms, drug transport mechanism, drug absorption pathways in different parts, and factors affecting drug absorption including physiology, drugs, dosage forms and preparations. 2.3 Master the basic concepts of drug distribution, excretion and metabolism;skilled with the factors that affect drug distribution, the types of drug metabolic reactions and the factors that affect drug metabolism.To master the characteristics and influencing factors of renal excretion and other excretory pathways of drugs
2.4 Understand the application of pharmacokinetics in clinical pharmacy and new drug research and development,master the design of drug administration regimen,the detection of therapeutic drugs and the individualized design of drug administration regimen.Familiar with the research contents of new drugspharmacokinetics,the basic requirements of bioavailability,research methods and evaluation methods of bioequivalence. (三)课程目标与毕业要求、课程内容的对应关系 表1：课程目标与课程内容、毕业要求的对应关系表 程 对应 目 课程子目标 对应课程内容 毕业 标 要求 1 Introduction to biopharmaceutics and 具备 pharmacokinetics. 药动 2 Mathematical fundamentals in 学基 课 1.1 Master the definition of pharmacokinetics,research contents and basic pharmacokinetic parameters,grasp pharmacokinetics. 础理 the calculation methods of pharmacokinetic parameters for different administration routes of one- 4 One compartment open model: 论、 目 compartment model.Understand the blood drug concentration-time curve and estimation of 标 pharmacokineticparameters of multi-compartment model,familiar with to identify compartment model. Intravenous bolus administration. 基本 Master the basic concepts related to multi-dose administration,drug accumulation and blood concentration 5 Multi-compartment models: 知 Intravenous bolus administration fluctuation. 6 Intravenous infusion 基本 8.Pharmacokinetics of oral 技 absorption 能。 9.Multiple-dosage regimens
2.4 Understand the application of pharmacokinetics in clinical pharmacy and new drug research and development, master the design of drug administration regimen, the detection of therapeutic drugs and the individualized design of drug administration regimen. Familiar with the research contents of new drugspharmacokinetics, the basic requirements of bioavailability, research methods and evaluation methods of bioequivalence. （三）课程目标与毕业要求、课程内容的对应关系 表 1：课程目标与课程内容、毕业要求的对应关系表 课 程 目 标 课程子目标 对应课程内容 对应 毕业 要求 课 程 目 标 1 1.1 Master the definition of pharmacokinetics,research contents and basic pharmacokinetic parameters, grasp the calculation methods of pharmacokinetic parameters for different administration routes of onecompartment model. Understand the blood drug concentration-time curve and estimation of pharmacokinetic parameters of multi-compartment model, familiar with to identify compartment model. Master the basic concepts related to multi-dose administration, drug accumulation and blood concentration fluctuation. 1 Introduction to biopharmaceutics and pharmacokinetics. 2 Mathematical fundamentals in pharmacokinetics. 4 One compartment open model: Intravenous bolus administration. 5 Multi-compartment models: Intravenous bolus administration 6 Intravenous infusion 8. Pharmacokinetics of oral absorption 9. Multiple-dosage regimens 具备 药动 学基 础理 论、 基本 知 识、 基本 技 能
具备 药动 学基 础理 1.2Master the characteristics of nonlinear pharmacokinetics and 论 Michaelis -Menten kinetics equation,approach the basic concept of 10.Nonlinear pharmacokinetics 基本 statistical moment and the estimation of pharmacokinetic parameters.. 知 技 从事 药物 研究 工作 15.Biopharmaceutic 的知 Considerations in Drug Product 识和 1.3 Understand the application of pharmacokinetics in clinical pharmacy and new drug research and Design and In Vitro Drug Product 能 development,master the design of drug administration regimen,the detection of therapeutic drugs and the Performance 。 individualized design of drug administration regimen.Familiar with the research contents of new drugs 具备 pharmacokinetics,the basic requirements of bioavailability.research methods and evaluation methods of 16.Drug Product Performance.In 从事 bioequivalence. Vivo:Bioavailability and 药物 Bioequivalence 动力 学与 药剂 学方 面工 作的 知识
1.2Master the characteristics of nonlinear pharmacokinetics and Michaelis–Menten kinetics equation, approach the basic concept of statistical moment and the estimation of pharmacokinetic parameters.。 10. Nonlinear pharmacokinetics 具备 药动 学基 础理 论、 基本 知 识、 基本 技 能。 1.3 Understand the application of pharmacokinetics in clinical pharmacy and new drug research and development, master the design of drug administration regimen, the detection of therapeutic drugs and the individualized design of drug administration regimen. Familiar with the research contents of new drugs pharmacokinetics, the basic requirements of bioavailability, research methods and evaluation methods of bioequivalence. 15. Biopharmaceutic Considerations in Drug Product Design and In Vitro Drug Product Performance 16. Drug Product Performance, In Vivo: Bioavailability and Bioequivalence 具备 从事 药物 研究 方面 工作 的知 识和 能 力。 具备 从事 药物 动力 学与 生物 药剂 学方 面工 作的 知识
和能 力。 具备 药学 基础 7.Drug elimination,dlearance. 理 and renal clearance 2.1 Understand the significance of biopharmaceutics and pharmacokinetics to new drug research and 11.Physiologicdrug distribution 论、 基本 development and clinical application. and protein binding 12.Drug elimination and hepatic 知 clearance 识、 本 课 技 能。 标 具备 2 从事 药品 体内 2.2 Master the structure and properties of biofilms.drug transport mechanism.drug absorption pathways in 评价 different parts,and factors affecting drug absorption including physiology,drugs.dosage forms and 14.Physiologic Factors 方面 Related to Drug Absorption preparations. 工作 的知 识和 能 力。 具备 2.3 Master the basic concepts of drug distribution,excretion and metabolism:skilled with the factors that 11.Physiologic Drug 从事 affect drug distribution,the types of drug metabolic reactions and the factors that affect drug metabolism.To Distribution and Protein 临床 master the characteristics and influencing factors of renal excretion and other excretory pathways of drugs. Binding 合理 用药
和能 力。 课 程 目 标 2 2.1 Understand the significance of biopharmaceutics and pharmacokinetics to new drug research and development and clinical application. 7. Drug elimination, clearance, and renal clearance 11. Physiologic drug distribution and protein binding 12. Drug elimination and hepatic clearance 具备 药学 基础 理 论、 基本 知 识、 基本 技 能。 2.2 Master the structure and properties of biofilms, drug transport mechanism, drug absorption pathways in different parts, and factors affecting drug absorption including physiology, drugs, dosage forms and preparations. 14. Physiologic Factors Related to Drug Absorption 具备 从事 药品 体内 评价 方面 工作 的知 识和 能 力。 2.3 Master the basic concepts of drug distribution, excretion and metabolism;skilled with the factors that affect drug distribution, the types of drug metabolic reactions and the factors that affect drug metabolism.To master the characteristics and influencing factors of renal excretion and other excretory pathways of drugs. 11. Physiologic Drug Distribution and Protein Binding 具备 从事 临床 合理 用药
方面 工作 的知 识和 能 力。 三、教学内容 第一章Introduction to Biopharmaceutics and Pharmacokinetics 1.教学目标 (1)Understanding the definition of biopharmaceutics and pharmcokinetics,and relationship with drug product performance. (2)Describe the role of biopharmaceutics and pharmcokinetics in a new drug development and clinical application. 2.教学重难点 (1)The definition of biopharmaceutics and pharmacokinetics. (2)The application of biopharmaceutics and pharmacokinetics in new drug development and clinical drug application. 3.教学内容 Drug Product Performance,Biopharmaceutics,Pharmacokinetics,Pharmacodynamics,Clinical Pharmacokinetics,Measurement of Drug Concentrations,Basic Pharmacokinetics and Pharmacokinetic Models
方面 工作 的知 识和 能 力。 三、教学内容 第一章 Introduction to Biopharmaceutics and Pharmacokinetics 1.教学目标 (1) Understanding the definition of biopharmaceutics and pharmcokinetics, and relationship with drug product performance. (2) Describe the role of biopharmaceutics and pharmcokinetics in a new drug development and clinical application. 2.教学重难点 (1) The definition of biopharmaceutics and pharmacokinetics. (2) The application of biopharmaceutics and pharmacokinetics in new drug development and clinical drug application. 3.教学内容 Drug Product Performance, Biopharmaceutics, Pharmacokinetics, Pharmacodynamics, Clinical Pharmacokinetics, Measurement of Drug Concentrations, Basic Pharmacokinetics and Pharmacokinetic Models
4.教学方法 (1)Teaching method:Relevant concepts and theoretical framework,combined with typical drug examples. (2)Discussion method:Flipped classroom will be encouraged. 5.教学评价 Take quick summary test,discuss with selected learning questions and frequently asked questions. 第二章Mathematical Fundamentals in Pharmacokinetics 1.教学目标 (1)Learn to algebraically solve mathematicalexpressions related topharmacokinetics. (2)Express the calculated andtheoretical pharmacokineticvalues in proper units. (3)Define various modelsrepresenting rates and orderof reactions and calculatepharmacokinetic parameters(eg,zero-and first-order)fromexperimental data based onthese models. 2.教学重难点 (1)Mathematicalexpressions related topharmacokinetics (2)Rates and orderof reactions and calculatepharmacokinetic parameters(eg,zero-and first-order) fromexperimental data 3.教学内容 Calculus,Graphs,Mathematical Expressions and Units,Units for Expressing Blood Concentrations, Measurement and Use of Significant Figures,Rates and Orders of Processes. 4.教学方法
4.教学方法 (1) Teaching method: Relevant concepts and theoretical framework, combined with typical drug examples. (2) Discussion method: Flipped classroom will be encouraged. 5.教学评价 Take quick summary test, discuss with selected learning questions and frequently asked questions. 第二章 Mathematical Fundamentals in Pharmacokinetics 1.教学目标 (1) Learn to algebraically solve mathematicalexpressions related topharmacokinetics. (2) Express the calculated andtheoretical pharmacokineticvalues in proper units. (3) Define various modelsrepresenting rates and orderof reactions and calculatepharmacokinetic parameters(eg, zero- and first-order) fromexperimental data based onthese models. 2.教学重难点 (1) Mathematicalexpressions related topharmacokinetics (2) Rates and orderof reactions and calculatepharmacokinetic parameters(eg, zero- and first-order) fromexperimental data 3.教学内容 Calculus, Graphs, Mathematical Expressions and Units, Units for Expressing Blood Concentrations, Measurement and Use of Significant Figures, Rates and Orders of Processes. 4.教学方法
(1)Teaching method:Relevant concepts and theoretical framework,combined with typical drug examples. (2)Discussion method:Flipped classroom was encouraged. 5.教学评价 Take quick summary test,discuss with selected learning questions and frequently asked questions. 第三章0ne-Compartment0 pen Model:Intravenous Bolus Administration 1.教学目标 (1)Describe a one-compartmentmodel,IV bolus injection. (2)Provide the pharmacokineticterms that describe a onecompartment model,IV bolusinjection,and the underlyingassumptions. (3)Explain how drugs follow onecompartment kinetics usingdrug examples that follow onecompartment kinetics. (4)Calculate pharmacokineticparameters from drugconcentration-time data using aone-compartment model. (5)Calculate the IV bolus doseof a drug using the onecompartment model equation. 2.教学重难点 (1)The definition of pharmacokinetic compartment model,the significance of one compartment model for intravenous bolus administration. (2)The calculation of pharmacokinetic parameters. 3.教学内容 Elimination rate constant,apparent volume of distribution,clearance,clinical application,calculation of k from urinary excretion data
(1) Teaching method: Relevant concepts and theoretical framework, combined with typical drug examples. (2) Discussion method: Flipped classroom was encouraged. 5.教学评价 Take quick summary test, discuss with selected learning questions and frequently asked questions. 第三章 One-Compartment Open Model: Intravenous Bolus Administration 1.教学目标 (1) Describe a one-compartmentmodel, IV bolus injection. (2) Provide the pharmacokineticterms that describe a onecompartment model, IV bolusinjection, and the underlyingassumptions. (3) Explain how drugs follow onecompartment kinetics usingdrug examples that follow onecompartment kinetics. (4) Calculate pharmacokineticparameters from drugconcentration–time data using aone-compartment model. (5) Calculate the IV bolus doseof a drug using the onecompartment model equation. 2.教学重难点 (1) The definition of pharmacokinetic compartment model,the significance of one compartment model for intravenous bolus administration. (2) The calculation of pharmacokinetic parameters. 3.教学内容 Elimination rate constant, apparent volume of distribution, clearance, clinical application, calculation of k from urinary excretion data
4.教学方法 (1)Teaching method:Relevant concepts and theoretical framework,combined with typical drug examples. (2)Discussion method:Flipped classroom was encouraged. 5.教学评价 Take quick summary test,discuss with selected learning questions and frequently asked questions. 第四章Multicompartment Models:Intravenous Bolus Administration 1.教学目标 (1)Define the pharmacokineticterms used in a two-and threecompartment model. (2)Explain using examples whydrugs follow one-compartment,two-compartment,or threecompartment kinetics. (3)Use equations and graphto simulate plasma drugconcentration at varioustime periods after an IV bolusinjection of a drug that followsthe pharmacokinetics of a twoand three-compartment modeldrug. (4)Estimate two-compartmentmodel parameters by using themethod of residuals. 2.教学重难点 Whydrugs follow one-compartment,two-compartment,or threecompartment kinetics,estimate two- compartmentmodel parameters by using themethod of residuals. 3.教学内容 Two-Compartment Open Model,Clinical Application,Three-Compartment Open Model,Determination of Compartment Models,Practical Problem 4.教学方法 (1)Teaching method:Relevant concepts and theoretical framework,combined with typical drug examples
4.教学方法 (1) Teaching method: Relevant concepts and theoretical framework, combined with typical drug examples. (2) Discussion method: Flipped classroom was encouraged. 5.教学评价 Take quick summary test, discuss with selected learning questions an d frequently asked questions. 第四章 Multicompartment Models: Intravenous Bolus Administration 1.教学目标 (1) Define the pharmacokineticterms used in a two- and threecompartment model. (2) Explain using examples whydrugs follow one-compartment,two-compartment, or threecompartment kinetics. (3) Use equations and graphto simulate plasma drugconcentration at varioustime periods after an IV bolusinjection of a drug that followsthe pharmacokinetics of a twoand three-compartment modeldrug. (4) Estimate two-compartmentmodel parameters by using themethod of residuals. 2.教学重难点 Whydrugs follow one-compartment,two-compartment, or threecompartment kinetics, estimate twocompartmentmodel parameters by using themethod of residuals. 3.教学内容 Two-Compartment Open Model, Clinical Application, Three-Compartment Open Model, Determination of Compartment Models, Practical Problem 4.教学方法 (1) Teaching method: Relevant concepts and theoretical framework, combined with typical drug examples
(2)Discussion method:Flipped classroom was encouraged. 5.教学评价 Take quick summary test,discuss with selected learning questions and frequently asked questions. 第五章I ntravenous Infusion 1.教学目标 (1)Describe the concept of steadystate and how it relates tocontinuous dosing. (2) Determine optimum dosing foran infused drug by calculatingpharmacokinetic parametersfrom clinical data. (3) Calculate loading doses tobe used with an intravenousinfusion. (4) Describe the purpose of aloading dose. 2.教学重难点 Pharmacokinetic parameters for one-compartment model drugs after intravenous infusion,loading dose,estimation of drug clearance and Vo. 3.教学内容 One-compartment model drugs,infusion method for calculating patient elimination half-life,loading dose plus iv infusion-one-compartment model,estimation of drug clearance and Vo from infusion data. 4.教学方法 (1)Teaching method:Relevant concepts and theoretical framework,combined with typical drug examples. (2)Discussion method:Flipped classroom was encouraged. 5.教学评价
(2) Discussion method: Flipped classroom was encouraged. 5.教学评价 Take quick summary test, discuss with selected learning questions and frequently asked questions. 第五章 Intravenous Infusion 1.教学目标 (1) Describe the concept of steadystate and how it relates tocontinuous dosing. (2) Determine optimum dosing foran infused drug by calculatingpharmacokinetic parametersfrom clinical data. (3) Calculate loading doses tobe used with an intravenousinfusion. (4) Describe the purpose of aloading dose. 2.教学重难点 Pharmacokinetic parameters for one-compartment model drugs after intravenous infusion, loading dose,estimation of drug clearance and VD. 3.教学内容 One-compartment model drugs, infusion method for calculating patient elimination half-life,loading dose plus iv infusion-one-compartment model,estimation of drug clearance and VD from infusion data. 4.教学方法 (1) Teaching method: Relevant concepts and theoretical framework, combined with typical drug examples. (2) Discussion method: Flipped classroom was encouraged. 5.教学评价