课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

1. Introduction to Biopharmaceutics and Pharmacokinetics

授课时间

100分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(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.技能（能力）目标：

(1) Learn basic English terms in biopharmaceutics and pharmacokinetics.

(2) Improve the skills in listening and speaking English in pharmacokinetics.

(3) Apply the knowledge to practices.

二、授课内容（依据教学大纲）及时间分配

Lecture I:

Drug Product Performance, Biopharmaceutics, Pharmacokinetics, Pharmacodynamics, Clinical Pharmacokinetics, Measurement of Drug Concentrations—50 min

Lecture II:

Basic Pharmacokinetics and Pharmacokinetic Models—50 min

三、教学重点与难点

1．教学重点

(1) The definition of biopharmaceutics and pharmacokinetics.

(2) The application of biopharmaceutics and pharmacokinetics in new drug development and clinical drug application.  

2.教学难点

Basic Pharmacokinetics and Pharmacokinetic Models.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Review the major concepts and materials covering the chapters.  

(2) Work on problems with students together to emphasize the basic principles covered in the chapters

(3) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

 1. What is the significance of the plasma level–time curve? How does the curve relate to the pharmacologic activity of a drug?  

2. What is the purpose of pharmacokinetic models?

七、学习资源、课外自主学习参考

(可以列出供学生进一步学习、拓展本章节内容的网站、著作、期刊的名称及内容等)

1. Applied Biopharmaceutics and Pharmacokinetics – Leon Shargel, Sussana Wu- Pong, Andrew B.C. Yu, 7th Edition, Mc Graw Hill Inc; Chapter -1

2. Concepts in Clinical Pharmacokinetics, 6th Edition

By William J. Spruill, William E. Wade, Joseph T. DiPiro, Robert A. Blouin, and Jane M. Pruemer 2014; Chapter -1 and Chapter -2  

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

2.Mathematical Fundamentals in Pharmacokinetics

授课时间

100分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(1) Learn to algebraically solve mathematical expressions related to pharmacokinetics.

(2) Express the calculated and theoretical pharmacokinetic values in proper units.

(3) Define various models representing rates and order of reactions and calculate pharmacokinetic parameters (eg, zero- and first-order) from experimental data based on these models.

2.技能（能力）目标：

(1) Learn basic English terms in Zero-Order Process and First-Order Process  

(2) Improve the skills in listening and speaking English in pharmacokinetics

二、授课内容（依据教学大纲）及时间分配

Lecture I:

Calculus, Graphs, Mathematical Expressions and Units, Units for Expressing Blood Concentrations, Measurement and Use of Significant Figures—50 min

Lecture II:

Rates and Orders of Processes—50 min

三、教学重点与难点

1．教学重点

(1) Mathematical expressions related to pharmacokinetics

(2) Rates and order of reactions and calculate pharmacokinetic parameters (eg, zero- and first-order) from experimental data

2.教学难点

Rates and order of reactions and calculate pharmacokinetic parameters (eg, zero- and first-order) from experimental data.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Use case study to explain the pharmacokinetic parameters (eg, zero- and first-order).

(2) Review the major concepts and materials covering the chapters.  

(3) Work on problems with students together to emphasize the basic principles covered in the chapters

(4) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

 How many half-lives (t1/2) would it take for 99.9% of any initial concentration of a drug to decompose? Assume first-order kinetics.  

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

3.One Compartment Open Model: Intravenous Bolus Administration

授课时间

200分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(1) Describe a one-compartment model, IV bolus injection.

(2) Provide the pharmacokinetic terms that describe a one compartment model, IV bolus injection, and the underlying assumptions.

(3) Explain how drugs follow one compartment kinetics using drug examples that follow one compartment kinetics.

(4) Calculate pharmacokinetic parameters from drug concentration–time data using a one-compartment model.

(5) Calculate the IV bolus dose of a drug using the one compartment model equation.

2.技能（能力）目标：

(1) Learn basic English terms in one-compartment model

(2) Improve the skills in listening and speaking English in pharmacokinetics

(3) Be able to calculate the IV bolus dose of a drug using the one compartment model equation

二、授课内容（依据教学大纲）及时间分配

Lecture I & II:

Elimination rate constant, apparent volume of distribution—100 min  

Lecture III & IV:

clearance, clinical application, calculation of k from urinary excretion data—100 min

三、教学重点与难点

1．教学重点

(1) The definition of pharmacokinetic compartment model, the significance of one compartment model for intravenous bolus administration.

(2) The calculation of pharmacokinetic parameters.

2.教学难点

 The calculation of pharmacokinetic parameters.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Use case study to explain the principles and applications of pharmacokinetic compartment model

(2) Review the major concepts and materials covering the chapters.  

(3) Work on problems with students together to emphasize the basic principles covered in the chapters

(4) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

The first learning question in chapter 3.

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

4.Multicompartment Models: Intravenous Bolus Administration

授课时间

100分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(1) Define the pharmacokinetic terms used in a two- and three compartment model.

(2) Explain using examples why drugs follow one-compartment, two-compartment, or three compartment kinetics.

(3) Use equations and graph to simulate plasma drug concentration at various time periods after an IV bolus injection of a drug that follows the pharmacokinetics of a two and three-compartment model drug.

(4) Estimate two-compartment model parameters by using the method of residuals.

2.技能（能力）目标：

(1) Learn basic English terms in Multicompartment models

(2) Improve the skills in listening and speaking English in pharmacokinetics

二、授课内容（依据教学大纲）及时间分配

Lecture I & II:

Two-Compartment Open Model, Clinical Application—90 min

Three-Compartment Open Model, Determination of Compartment Models, Practical Problem—10 min

三、教学重点与难点

教学重难点

Why drugs follow one-compartment, two-compartment, or three compartment kinetics, estimate two-compartment model parameters by using the method of residuals.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Use case study to explain the principles and applications of Two-Compartment Open Model

(2) Review the major concepts and materials covering the chapters.  

(3) Work on problems with students together to emphasize the basic principles covered in the chapters

(4) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

The second learning question in chapter 4.

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

5.Intravenous Infusion

授课时间

100分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(1) Describe the concept of steady state and how it relates to continuous dosing.

(2) Determine optimum dosing for an infused drug by calculating pharmacokinetic parameters from clinical data.

(3) Calculate loading doses to be used with an intravenous infusion.

(4) Describe the purpose of a loading dose.

2.技能（能力）目标：

(1) Be able to calculate pharmacokinetic parameters from clinical data.

(2) Improve the skills in listening and speaking English in pharmacokinetics

二、授课内容（依据教学大纲）及时间分配

Lecture I & II:

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—100 min

三、教学重点与难点

教学重难点

Pharmacokinetic parameters for one-compartment model drugs after intravenous infusion, loading dose,estimation of drug clearance and V_D.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Use case study to explain the principles and applications of one-compartment model drugs after intravenous infusion, loading dose.

(2) Review the major concepts and materials covering the chapters.  

(3) Work on problems with students together to emphasize the basic principles covered in the chapters

(4) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

1. The first and second learning questions in chapter 5.

2. The  two examples in PPT.

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

6.Drug Elimination, Clearance and Renal Clearance

授课时间

100分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(1) Describe the main routes of drug elimination from the body.

(2) Understand the importance of the role of clearance as a PK parameter.

(3) Define clearance and its relationship to a corresponding half-life and a volume of distribution, differentiate between clearance and renal clearance.

2.技能（能力）目标：

(1) Learn basic English terms in drug elimination

(2) Improve the skills in listening and speaking English in pharmacokinetics

二、授课内容（依据教学大纲）及时间分配

Lecture I & II:

Drug elimination, drug clearance, clearance models, the kidney, renal clearance, determination of renal clearance, relationship of clearance to elimination half-life and volume of distribution—100 min

三、教学重点与难点

教学重难点

The definition and significance of drug elimination, clearance, renal clearance, determination of renal clearance, relationship of clearance to elimination half-life and volume of distribution.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Use case study to explain the principles and applications of drug elimination.

(2) Review the major concepts and materials covering the chapters.  

(3) Work on problems with students together to emphasize the basic principles covered in the chapters

(4) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

The first learning question in chapter 6.

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

第六学期

授课章节

7. Drug Elimination, Clearance and Renal Clearance

授课时间

100分钟

一、教学目标：含知识目标、技能（能力）目标

1．知识目标：

(1) Describe the main routes of drug elimination from the body.

(2) Understand the importance of the role of clearance as a PK parameter.

(3) Define clearance and its relationship to a corresponding half-life and a volume of distribution, differentiate between clearance and renal clearance.

2.技能（能力）目标：

(1) Learn basic English terms in drug elimination

(2) Improve the skills in listening and speaking English in pharmacokinetics

二、授课内容（依据教学大纲）及时间分配

Lecture I & II:

Drug elimination, drug clearance, clearance models, the kidney, renal clearance, determination of renal clearance, relationship of clearance to elimination half-life and volume of distribution—100 min

三、教学重点与难点

教学重难点

The definition and significance of drug elimination, clearance, renal clearance, determination of renal clearance, relationship of clearance to elimination half-life and volume of distribution.

四、教学方法选择

1.理论课堂教学

A.多媒体教学：（简要列出本章节多媒体教学设计特点及优势）

(1) Use case study to explain the principles and applications of drug elimination.

(2) Review the major concepts and materials covering the chapters.  

(3) Work on problems with students together to emphasize the basic principles covered in the chapters

(4) Test could push students usually.

B.互动教学：（根据实际情况列出案例/实例讨论、分析讨论、分组讨论、翻转课堂等互动教学内容标题）

(1) Ask questions during case studies before and after introducing basic concepts

(2) Discuss the complicated concepts

(3) Solve problems together with students

2.实验课教学

No applicable.

五、更新或补充内容提要

课后总结：按照实际进度对知识点分详略进行讲解

Emphasize the key concept and adjust the amount of materials in each section

六、复习思考题

The first learning question in chapter 6.

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

8.Pharmacokinetics of Oral Absorption

授课时间

100分钟

一 教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

1 Define oral drug absorption and describe the absorption process.

2 Introduce two general approaches used for studying absorption kinetics and their similarities and differences.

3 Understand the basic principles for physiologically based absorption kinetics.

4 Describe the oral one compartment model and explain how this model simulates drug absorption from the gastrointestinal tract.

5 Calculate the pharmacokinetic parameters of a drug that follows the oral one compartment model, the fraction of drug absorbed in a one-compartment model using the Wagner–Nelson method.

（二）技能（能力）目标：

Methods of study for oral drug absorption.

二 授课内容（依据教学大纲）及时间分配

1 Chapter objectives and main contents（5min）；Drug Transportation Process，Relationship between Biopharmacokinetics and Pharmacokinetics（10min）；

2 Introduction (10min), Basic Principles of Physiologically Based Absorption Kinetics (25min),

 3 Pharmacokinetics of drug absorption (5min), Significance of Absorption (10min), rate Constants (5min), first-order Absorption Model and calculation  (30 min).

三 教学重点与难点

1 教学重点

Understand the oral drug absorption principles and process, the basic principles for physiologically based absorption kinetics, calculate the pharmacokinetic parameters of a drug that follows the oral one compartment model.

2 教学难点

 Calculate the pharmacokinetic parameters of a drug that follows the oral one compartment model.

四 教学方法选择

A. 多媒体教学：

Improve students' comprehension based on lots of pictures, tables and examples.

互动教学：

Discuss with students about oral drug absorption based on biological factors, drug factors and dosage form factors.

五 更新或补充内容提要

NO

六 复习思考题

1 Learning questions (discussion!)

2 Application questions in text book: 1, 3, 5, 7, 8, 9

七 学习资源、课外自主学习参考

1 国内期刊：药学学报，中国药学杂志，中国医院药学杂志，等

2 国外期刊：Molecular Pharmaceutics，Clinical Pharmacokinetics， European Journal of Pharmaceutical Sciences,European Journal of Pharmaceutics and Biopharmaceutics,International Journal of Pharmaceutics, Journal of Pharmaceutical Sciences, Drug Metabolism And Pharmacokinetics, Journal Of Pharmaceutical And Biomedical Analysis, Biopharmaceutics & Drug Disposition, European Journal of Drug Metabolism and Pharmacokinetics, etc….

3  刘建平主编，生物药剂学与药物动力学教材，人民卫生出版社，第五版

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

9.Multiple-Dosage Regimens

授课时间

100分钟

一 教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

1  Define drug accumulation, accumulation index and drug accumulation t1/2

2  Explain the principle of superposition and its assumptions in multiple-dose regimens.

3  Calculate the steady-state Cmax and Cmin after multiple IV bolus dosing of drugs, k and VD of aminoglycosides in multiple-dose regimens.

（二）技能（能力）目标：

To master the characteristics and clinical significance of multiple-dosage regimens..

二 授课内容（依据教学大纲）及时间分配

 1 Chapter objectives and main contents（5min）；The superposition principle（15min）； Drug accumulation（30min）,

2  Repetitive intravenous injections（30min）；Intermittent intravenous infusion（5min）；Multiple-oral-dose regimen（10min）；Loading dose（5min）.

三 教学重点与难点

1 教学重点

The definition of drug accumulation and evaluate related pharmacokinetic parameters.

2 教学难点

Drug accumulation, repetitive intravenous injections, intermittent intravenous infusion, estimation of k and VD of aminoglycosides in clinical situations, multiple-oral-dose regimen, loading dose, dosage regimen schedules.

四 教学方法选择

1多媒体教学：

结合临床用药特点的典型案例，提高学生对多剂量给药的理解与掌握。

2 互动教学：

课堂提问和讨论，探究单剂量给药与多剂量给药的差异，多剂量给药在临床药学中的作用。

五 更新或补充内容提要

无

六 复习思考题

1. Definitions: steady state plasma drug concentration, mean steady state plasma drug concentration, plateau amplitude, plateau fraction, accumulation coefficient, fluctuation degree.

2. What is the difference in in vivo process between single dose and multiple dose administration?

3. The influence of multi-dose administration route on steady-state plasma concentration?

七 学习资源、课外自主学习参考

同第八章。

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

10.Nonlinear Pharmacokinetics

授课时间

100分钟

一 教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

1  Describe the differences between linear pharmacokinetics and nonlinear pharmacokinetics.

2  Explain how to detect nonlinear kinetics using AUCversusdoses plots.

3  Learn to apply Michaelis–Menten equation and graphical methods to calculate Vmax and KM.

（二）技能（能力）目标：

Familiar with drug characteristics and kinetic parameter calculation under nonlinear pharmacokinetics.

二 授课内容（依据教学大纲）及时间分配

1  Chapter objectives and main contents（5min）；

2  Linear Pharmacokinetics, Nonlinear Pharmacokinetics & properties(25min); Why Nonlinear PK of drug(15min);PK parameters calculation (35min), Application of Nonlinear PK(15min);

3  Discussion (5min).

三 教学重点与难点

1 教学重点

The necessity to study Nonlinear Pharmacokinetics, how to determine Nonlinear Pharmacokinetics, the properties of Nonlinear Pharmacokinetics, calculation of related PK parameters.

2 教学难点

The properties of Nonlinear Pharmacokinetics, calculation of related PK parameters.

四 教学方法选择

1  多媒体教学：

结合典型药物案例，提高学生对非线性药物动力学的理解与重要性。

2 互动教学：

课堂提问和讨论，探究线性药物动力学与非线性药物动力学给的临床用药特点。

五 更新或补充内容提要

无

六 复习思考题

1.  What is nonlinear pharmacokinetics? How does it differ from linear pharmacokinetics?

2.  Analyze the relationship between dose and nonlinear pharmacokinetic half-life, AUC, CL and steady-state plasma concentration.

七 学习资源、课外自主学习参考

同第八章。

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

11.Physiologic Drug Distribution and Protein Binding

授课时间

200分钟

一 教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

 1  Describe the physiology of drug distribution in the body.

 2  Explain how drug distribution is affected by blood flow, protein, and tissue binding.

 3  Describe how drug distribution can affect the apparent volume of distribution.

 4  Explain how volume of distribution, drug clearance, and half-life can be affected by protein binding.

（二）技能（能力）目标：

提高药动学研究中综合考虑各种生理学因素对药物分布与蛋白结合影响的能力。

二 授课内容（依据教学大纲）及时间分配

1  Chapter objectives and main contents（5min）；

2  Physiologic factors of distribution（45 min）,

3  Apparent volume distribution（40min）,discussion （5min）；

4  Protein binding of drugs（25min）, Effect of protein binding on the apparent volume of distribution（35min）, Relationship of plasma drug–protein binding to distribution and elimination（15min）, determinants of protein binding（15min）, Kinetics of protein binding（5min），Clinical Significance of Drug–protein Binding（7min），

5  Discussion（3min）

三 教学重点与难点

1教学重点

 The physiology of drug distribution in the body, factors affect drug distribution, the definition and significance of drug protein binding in vivo, the relationship between drug distribution, drug clearance and half-life of elimination.

2教学难点

The definition and significance of drug protein binding , and the relationship between drug distribution and protein binding in patients.  

四 教学方法选择

多媒体教学：

尽可能采用更多的与药物体内分布相关的基础研究与临床应用案例，提高学生对药影响物体内分布生理学因素的认识，尤其是在不同疾病条件下安全合理用药的必要性。

互动教学：

预先布置学生了解影响药物体内分布的因素，通过课堂讨论与提问，加深和巩固本章节知识点。

五 更新或补充内容提要

无

六 复习思考题

1. How does a physical property, such as partition coefficient, affect drug distribution?

2. What are the causes of a long distribution half-life for a body organ if blood flow to the tissue is rapid?

3. How long does it take for a tissue organ to be fully

equilibrated with the plasma? How long for a tissue organ to be half-equilibrated?

4. When a body organ is equilibrated with drug from the

plasma, the drug concentration in that organ should be the same as that of the plasma. True or false?

5. What is the parameter that tells when half of the protein-binding sites are occupied?

6. Do all drugs that bind proteins lead to clinically significant interactions?

7. Which macromolecules participate in drug–protein binding?

8. How does drug–protein binding affect drug elimination?

9. What are the factors to consider when adjusting the

drug dose for a patient whose plasma protein concentration decreases to half that of normal?

10. How does one distinguish between the distribution phase and the elimination phase after an IV injection of a drug?

七 学习资源、课外自主学习参考

同第八章。

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

12.Drug Elimination and hepatic clearance

授课时间

100分钟

一 教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

 1  Describe the pathways for drug elimination in the body.

 2  Describe the role of hepatic blood flow, drug protein binding, and intrinsic clearance on hepatic clearance.

 3  Describe the biotransformation of drugs in the liver and which enzymatic processes are considered “phase I reactions” and “phase II reactions.”

（二）技能（能力）目标：

提高学生理解分析影响药物体内代谢与消除过程及因素的能力。

二 授课内容（依据教学大纲）及时间分配

 1  Chapter objectives and main contents（5min）；

 2  Route of drug administration and extrahepatic drug metabolism（20min）, Hepatic clearance, extrahepatic metabolism, enzyme kinetics（10min）；Anatomy and physiology of the liver（5min）；

 3  Hepatic enzymes involved in the biotransformation of drugs（15min）, Drug biotransformation reactions（15min）, pathways of drug biotransformation（5min）, biliary excretion of drugs（5min）, role of transporters on hepatic clearance and bioavailability（8min）；

 4  Discussion（2min）

三 教学重点与难点

1教学重点

 Understanding the definition of drug  elimination and hepatic clearance, factors affecting Drug Elimination, biotransformation pathway of drug in vivo.

2教学难点

The factors involves in  elimination and hepatic clearance, the mechanism of drug elimination in different organs in vivo.  

四 教学方法选择

多媒体教学：采用药物消除、代谢、排泄在新药研究与临床应用的案例，增强学生对药物体内过程的理解。

互动教学：提问讨论药物发生药物消除（代谢、排泄）的意义？

五 更新或补充内容提要

无

六 复习思考题

 1  How does the route of drug administration affect drug elimination?

 2  Why does the rate of drug elimination for some drugs change from first-order elimination to zero-order elimination?

 3  What organs are involved in drug elimination?

七 学习资源、课外自主学习参考

同第八章。

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

14.Physiologic Factors Related to Drug Absorption

授课时间

200分钟

一 教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

 1  Define passive , active drug absorption, transcellular and paracellular drug absorption.

 2  Explain how Fisk's law of diffusion relates to passive drug absorption.

 3  Calculate the percent of drug nonionized and ionized for a weak acid or weak-base drug using the Henderson–Hasselbalch equation, and explain how this may affect drug absorption.

 4  Describe the anatomy and physiology of the GI tract and explain how stomach emptying time and GI transit time can alter the rate and extent of drug absorption.

 5  Explain the effect of food on gastrointestinal physiology and systemic drug absorption.

 6  Describe the various transporters and how they influence the pharmacokinetics of drug disposition in the GI tract

 7  Explain the pH-partition hypothesis and how gastrointestinal pH and the pKa of a drug may influence systemic drug absorption. Describe how drug absorption may be affected by a disease that causes changes in intestinal blood flow and/or motility.

 8  List the major factors that affect drug absorption from oral and non-oral routes of drug administration.

（二）技能（能力）目标：

Be familiar with the factors affecting absorption of drugs or pharmaceutical preparations after oral administration and strategies to improve its absorption.

二 授课内容（依据教学大纲）及时间分配

 1  Chapter objectives and main contents（5min）；

 2  Drug absorption and design of a drug product（10min）,Route of drug administration（20min）, Nature of cell membranes（15min）, Passage of drugs across cell membranes （40min）, Drug interactions in the gastrointestinal tract（10min）,

 3  Oral drug absorption and factors Affecting Drug Absorption in GI Tract （50min）

 4  Oral drug absorption during drug product development（5min）, Methods for studying factors that affect drug absorption（5min）, effect of disease states on drug absorption（20min）, miscellaneous routes of drug administration（15min）.

5  Discussion （5min）.

三 教学重点与难点

 1教学重点

 Understanding the mechanisms of drug absorption, the anatomy and physiology drug absorption organs, the physicochemical and physiological factors influencing drug absorption, important equations to describe the absorption.

 2 教学难点

Understand the relationship between anatomy & philology of GI tract and drug absorption mechanism, the principles of different drug absorption.

How to design drug product based on the drug absorption mechanism?

四 教学方法选择

多媒体教学：

广泛采用药物研究开发的案例，利用BCS分类法，探讨促进口服药物生物利用度的方法，掌握药物吸收原理的学习在新药研发及临床合理用药中的应用。

互动教学：

通过提问讨论，思考药物和不同药物剂型口服吸收的过程，影响因素，吸收快慢等。

五 更新或补充内容提要

无

六 复习思考题

1  What is an “absorption window”?

2  Why are some drugs orally absorbed better with food, whereas the oral absorption of other drugs are slowed or decreased by food?

3  What type of food is expected to have the greatest effect on gastrointestinal pH and gastrointestinal transit time?

4  Are drugs that are administered as an oral solution completely absorbed from the gastrointestinal tract?

5  What factors contribute to a delay in drug absorption?

6  What is the Primary Reason that protein drugs such as insulin are not given orally for systemic absorption?

7  Which region of the gastrointestinal tract is most populated by bacteria?  

What types of drugs might affect the gastrointestinal flora?

七 学习资源、课外自主学习参考

同第八章。

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

15.Biopharmaceutic Considerations in Drug Product Design

授课时间

100分钟

一 教学目标：含知识目标、技能（能力）目标

（一）知识目标：

 1  Describe the biopharmaceutic factors affecting drug design.

 2  Differentiate between the terms solubility and dissolution, drug absorption and bioavailability,

 3  Describe the various in vitro and in vivo tests commonly used to evaluate drug products.

 4  Define in vitro–in vivo correlation (IVIVC) and explain why a Level A correlation is the most important correlation for IVIVC

 5  Explain the biopharmaceutic classification system and how solubility, dissolution, and permeation apply to BCS classification.

（二）技能（能力）目标：结合实验课程目标

提高制剂设计时综合考虑生物药剂学&药物动力学因素的能力与方法。

二 授课内容（依据教学大纲）及时间分配

 1  Chapter objectives and main contents（5min）；

 2  Biopharmaceutic factors and rationale for drug product design（10min）,Rate-limiting steps in drug absorption（10min）, Physicochemical properties of the drug（10min）, Formulation factors affecting drug product performance（5min）；,

 3  Drug product performance in vitro（15min）: Dissolution and drug release testing（5min）, Compendial methods of dissolution（10min）, Dissolution profile comparisons（5min）, Problems of variable control in dissolution testing, performance of drug products: In vitro–in vivo correlation, drug product stability（10min）, Considerations in the design of a drug product （10min）；

4  Discussion （5min）

三 教学重点与难点

 1 教学重点

 Understanding the biopharmaceutic factors affecting drug design, the significance and method to estimate in vitro–in vivo correlation (IVIVC),the biopharmaceutic classification system and how solubility, dissolution, and permeation apply to BCS classification.

 2 教学难点

Understanding the biopharmaceutic factors affecting drug design and its rational application.

三 教学方法选择

多媒体教学：

结合国内外药物研究开发的案例，讲授生物药剂学理论在在新药研发中的应用。

互动教学：

通过提问讨论，思考药物的生物药剂学特征如何影响制剂产品的设计，进一步了解生物药剂学的重要性。

四 更新或补充内容提要

无

五 复习思考题

 1  If excipients do not have pharmacodynamic activity, how do excipients affect the performance of the drug product?

 2  What is meant by the rate-limiting step in drug bioavailability from a solid oral drug product?

 3  Drug absorption involves at least three distinct steps: dissolution, permeation, and disposition during transit in GI (an additional step of drug disposition in the body is involved as well for bioavailability). How are these processes validated in vitro when the in vivo requirement for drug bioavailability is waived?

 4  Why is it important to maintain sink conditions?

 5  What physical or chemical properties of a drug substance are important in designing a drug for (a) oral administration or (b) parenteral administration?

6  For a lipid-soluble drug that has very poor aqueous solubility, what strategies could be used to make this drug more bioavailable after oral administration?

六 学习资源、课外自主学习参考

同第八章。

课程名称

Biopharmaceutics and Pharmacokinetics

所属学科

药学

教材名称

《Applied Biopharmaceutics & Pharmacokinetics》第7版

授课年级

2017级药学全英文班

授课章节

16.Drug product performance in vivo: Bioavailability and Bioequivalence

授课时间

200分钟

一  教学目标：含知识目标、技能（能力）目标

（一） 知识目标：

 1  Define bioavailability, bioequivalence, and drug product performance.

 2  Explain why certain drugs and drug products have low bioavailability.

 3  Explain why first-pass effect as well as chemical instability of a drug can result in low relative bioavailability.

 4  Describe various methods for measuring bioavailability and the advantages and disadvantages of each.

（二） 技能（能力）目标：

 Master methods of bioavailability and bioequivalence evaluation.

二  授课内容（依据教学大纲）及时间分配

 1  Chapter objectives and main contents（5min）；

 2  Drug Product Performance（15min）, Purpose of Bioavailability and Bioequivalence Studies,（10min）,Relative and Absolute Bioavailability（20min）；50

 3  Methods for Assessing Bioavailability and Bioequivalence（10min）, In Vivo Measurement of Active Moiety or Moieties in Biological Fluids（20min）,Bioequivalence Studies Based on Pharmacodynamic End points—In Vivo Pharmacodynamic (PD) Comparison（10min），Bioequivalence Studies Based on Clinical Endpoints—Clinical Endpoint Study（10min）,50

 4  In Vitro Studies（10min）, Bioequivalence Studies Based on Multiple Endpoints（10min）, Design and Evaluation of Bioequivalence Studies（30 min）,

 5  The Biopharmaceutics Classification System (BCS)（10min）Clinical Significance of Bioequivalence Studies（10min）；

4  Discussion （30min）.

三  教学重点与难点

1  教学重点

（1）Understanding the difference between bioavailability and bioequivalence, and how these parameters influence drug product performance and development；

（2） In Vivo Measurement of Active Moiety or Moieties in Biological Fluids；

（3）Design and Evaluation of Bioequivalence Studies

2  教学难点

Design and measurement bioavailability and bioequivalence in vivo study.

四  教学方法选择

 1  多媒体教学：

结合国内外案例，讲授生物利用度和生物等效性研究的方法，增强学生对二个概念的充分理解。

 2  互动教学：

通过提问讨论，认识药物的生物利用度和生物等效性的差异及重要性，掌握设计、测定和计算相关参数的方法。

五  更新或补充内容提要

无

六  复习思考题

 1  What are the study protocol considerations for conducting a bioequivalence study?

 2  What is the reference listed drug (RLD), and how is the RLD selected?

 3  How is a bioavailability study of a new molecular entity conducted?

 4  Why does the value for relative bioavailability sometimes exceed 1.0, whereas the value for absolute bioavailability cannot exceed 1.0 ?

 5  Why are preclinical animal toxicology studies and clinical efficacy drug studies in human subjects not required by the FDA to approve a generic drug product as a therapeutic equivalent to the brand-name drug product?

 6  What do sequence, washout period, and period mean in a crossover bioavailability study?

 7  Why does the FDA require a food intervention (foodeffect) study for generic drug products before granting approval?

8  What type of bioequivalence studies are required for drugs that are not systemically absorbed or for those drugs in which the Cmax and AUC cannot be measured in the plasma?

六  学习资源、课外自主学习参考

同第八章。