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Biopharmaceutics
Читать книгу Biopharmaceutics - Группа авторов - Страница 1
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Страница 1
Table of Contents
List of Tables
List of Illustrations
Guide
Pages
Страница 7
Biopharmaceutics From Fundamentals to Industrial Practice
Страница 9
List of Contributors
Foreword
1 An Introduction to Biopharmaceutics
1.1 Introduction
1.2 History of Biopharmaceutics
1.3 Key Concepts and Definitions Used Within Biopharmaceutics
1.4 The Role of Biopharmaceutics in Drug Development
1.5 Conclusions
References
2 Basic Pharmacokinetics
2.1 Introduction
2.2 What is ‘Pharmacokinetics’?
2.3 Pharmacokinetic Profile
2.4 Bioavailability
2.5 Drug Distribution
Box 2.1
Drug Concentration in
blood
is not the same as the drug concentration in
plasma
!
Box 2.2 Why measure drug concentrations?
2.6 Volume of Distribution
Box 2.3
Total body water.
2.7 Elimination
2.7.1 Metabolism
2.7.2 Excretion
2.8 Elimination Half‐Life (
t
½
)
2.9 Elimination Rate Constant
Box 2.4
How long it will take for the drug to eliminate completely from the body?
2.9.1 Clearance
Box 2.5
The elimination rate constant, k and the elimination half‐life (t
½
)
2.10 Area Under the Curve (AUC)
2.11 Bioequivalence
2.12 Steady State
Box 2.6
How long it takes to get to the steady state?
Box 2.7
Therapeutic drug monitoring (TDM).
2.13 Compartmental Concepts in Pharmacokinetics
2.14 Concept of Linearity in Pharmacokinetics
2.15 Conclusions
Further Reading
3 Introduction to Biopharmaceutics Measures
3.1 Introduction
3.2 Solubility
3.3 Dissolution
3.4 Permeability
3.5 Absorptive Flux
3.6 Lipinsky's Rule of 5
3.6.1 Molecular Weight
3.6.2 Lipophilicity
3.6.3 Hydrogen Bond Donors/Acceptors
References
4 Solubility
4.1 Definition of Solubility
4.2 The Importance of Solubility in Biopharmaceutics
4.3 What Level of Solubility Is Required?
4.4 Solubility‐Limited Absorption
4.5 Methods to Assess Solubility
4.6 Brief Overview of Forces Involved in Solubility
4.6.1 van der Waals Interactions
4.6.2 Hydrogen Bonding
4.6.3 Ionic Interactions
4.7 Solid‐State Properties and Solubility
4.8 pH and Drug Solubility
4.9 Solvents
4.9.1 Biorelevant Solubility
4.9.2 Buffer System – Phosphate vs Bicarbonate
4.9.3 Solubilisation by Surfactants
4.9.4 Solubilisation During Digestion
4.9.5 Excipients and Solubility
4.10 Risk of Precipitation
4.11 Solubility and Link to Lipophilicity
4.12 Conclusions
References
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