Biopharmaceutics: From Fundamentals to Industrial Practice

Length: 320 pages
Edition: 1
Language: English
Publisher: Wiley
Publication Date: 2021-12-29
ISBN-10: 1119678285
ISBN-13: 9781119678281
Sales Rank: #6878234 (See Top 100 Books)

Explore the latest research in biopharmaceutics from leading contributors in the field

In Biopharmaceutics – From Fundamentals to Industrial Practice, distinguished Scientists from the UK’s Academy of Pharmaceutical Sciences Biopharmaceutica Focus Group deliver a comprehensive examination of the tools used within the field of biopharmaceutics and their applications to drug development. This edited volume is an indispensable tool for anyone seeking to better understand the field of biopharmaceutics as it rapidly develops and evolves.

Beginning with an expansive introduction to the basics of biopharmaceutics and the context that underpins the field, the included resources go on to discuss how biopharmaceutics are integrated into product development within the pharmaceutical industry. Explorations of how the regulatory aspects of biopharmaceutics function, as well as the impact of physiology and anatomy on the rate and extent of drug absorption, follow.

Readers will find insightful discussions of physiologically based modeling as a valuable asset in the biopharmaceutics toolkit and how to apply the principles of the field to special populations. The book goes on to discuss:

Thorough introductions to biopharmaceutics, basic pharmacokinetics, and biopharmaceutics measures
Comprehensive explorations of solubility, permeability, and dissolution
Practical discussions of the use of biopharmaceutics to inform candidate drug selection and optimization, as well as biopharmaceutics tools for rational formulation design
In-depth examinations of biopharmaceutics classification systems and regulatory biopharmaceutics, as well as regulatory biopharmaceutics and the impact of anatomy and physiology

Perfect for professionals working in the pharmaceutical and biopharmaceutical industries, Biopharmaceutics – From Fundamentals to Industrial Practice is an incisive and up-to-date resource on the practical, pharmaceutical applications of the field.

Cover
Table of Contents
Series Page
Title Page
Copyright Page
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
    2.6 Volume of Distribution
    2.7 Elimination
    2.8 Elimination Half‐Life (t½)
    2.9 Elimination Rate Constant
    2.10 Area Under the Curve (AUC)
    2.11 Bioequivalence
    2.12 Steady State
    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
    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
    4.7 Solid‐State Properties and Solubility
    4.8 pH and Drug Solubility
    4.9 Solvents
    4.10 Risk of Precipitation
    4.11 Solubility and Link to Lipophilicity
    4.12 Conclusions
    References
5 Permeability
    5.1 Introduction
    5.2 Enzymes, Gut Wall Metabolism, Tissue Permeability and Transporters
    5.3 Applications and Limitations of Characterisation and Predictive Tools for Permeability Assessment
    5.4 In Vivo Tools
    5.5 Conclusion
    References
6 Dissolution
    6.1 Introduction
    6.2 Purpose of Dissolution Testing
    6.3 History of Dissolution Testing
    6.4 Compendial (Pharmacopeial) Dissolution Apparatus
    6.5 Dissolution Media Selection
    6.6 Dissolution Agitation Rates
    6.7 Reporting Dissolution Data
    6.8 In Vitro In Vivo Relationships and Correlations (IVIVR/IVIVC)
    6.9 Evolution of Biorelevant Dissolution Testing
    6.10 Conclusions
    References
7 Biopharmaceutics to Inform Candidate Drug Selection and Optimisation
    7.1 Introduction
    7.2 Oral Product Design Considerations During Early Development
    7.3 Biopharmaceutics in Drug Discovery
    7.4 Biopharmaceutics Assessment
    7.5 Output of Biopharmaceutics Assessment
    7.6 Influence/Optimise/Design Properties to Inform Formulation Development
    7.7 Conclusion
    References
8 Biopharmaceutics Tools for Rational Formulation Design
    8.1 Introduction
    8.2 Formulation Development to Optimise Drug Bioavailability
    8.3 Traditional Formulation Strategies
    8.4 Decision Trees to Guide Formulation Development
    8.5 Computational Tools to Guide Formulation Strategies
    8.6 Decision‐Making for Optimising Enabling Formulations
    8.7 Decision Trees for Enabled Formulations
    8.8 System‐Based Formulation Strategies
    8.9 Biopharmaceutics Risk Assessment Roadmap (BioRAM)
    8.10 Conclusions
    References
9 Biopharmaceutic Classification System
    9.1 Description and History of the BCS
    9.2 BCS‐Based Criteria for Solubility, Dissolution and Permeability
    9.3 BCS‐Based Biowaivers
    9.4 Regulatory Development of BCS‐Based Biowaivers
    9.5 International Harmonisation of BCS‐Based Biowaiver Criteria – ICH M9
    9.6 BCS as a Development Tool
    9.7 Beyond the BCS
    9.8 Conclusions
    References
10 Regulatory Biopharmaceutics
    10.1 Introduction
    10.2 Clinical Bioequivalence Studies
    10.3 Design of Clinical Bioequivalence (BE) Studies
    10.4 Implication of Bioequivalence Metrics
    10.5 Bioequivalence Regulatory Guidelines
    10.6 Biowaivers
    10.7 Biopharmaceutics in Quality by Design
    10.8 Control of Drug Product and Clinically Relevant Specifications
    10.9 Establishing Clinically Relevant Dissolution Methods and Specifications
    10.10 Application of In Silico Physiologically Based Biopharmaceutics Modelling (PBBM) to Develop Clinically Relevant Specifications
    10.11 Additional Considerations for Establishing Dissolution Methods and Specifications
    10.12 Common Technical Document (CTD)
    10.13 Other Routes of Administration and Locally Acting Drug Products
    10.14 Conclusion
    References
11 Impact of Anatomy and Physiology
    11.1 Introduction
    11.2 Influence of GI Conditions on Pharmacokinetic Studies
    11.3 The Stomach
    11.4 Small Intestine
    11.5 The Colon/Large Intestine
    11.6 Conclusions
    References
12 Integrating Biopharmaceutics to Predict Oral Absorption Using PBPK Modelling
    12.1 Introduction
    12.2 Mechanistic Models
    12.3 Solubility Inputs
    12.4 Dissolution Inputs
    12.5 Permeability Inputs
    12.6 Incorporation of Modelling and Simulation into Drug Development
    12.7 Conclusions
    References
13 Special Populations
    13.1 Introduction
    13.2 Sex Differences in the Gastrointestinal Tract and Its Effect on Oral Drug Performance
    13.3 Ethnic Differences in the Gastrointestinal Tract
    13.4 Impact of Diet on Gastrointestinal Physiology
    13.5 Pregnancy and Its Effect on Gastrointestinal Physiology
    13.6 The Implication of Disease States on Gastrointestinal Physiology and Its Effect on Oral Drug Performance
    13.7 Diseases that Affect the Gastrointestinal Tract
    13.8 Infections in the Gastrointestinal Tract
    13.9 Systemic Diseases that Alter GI Physiology and Function
    13.10 Age‐related Influences on Gastrointestinal Tract Physiology and Function
    13.11 Conclusion
    References
14 Inhalation Biopharmaceutics
    14.1 Introduction
    14.2 Structure of the Lungs
    14.3 Molecules, Inhalation Devices, Formulations
    14.4 Inhaled Drug Delivery and Models for Studying Inhalation Biopharmaceutics
    14.5 Bioequivalence and an Inhalation Bioclassification System
    14.6 Conclusion
    References
15 Biopharmaceutics of Injectable Formulations
    15.1 Introduction
    15.2 Subcutaneous Physiology and Absorption Mechanisms
    15.3 Intramuscular Physiology and Absorption Mechanisms
    15.4 In Vitro Performance and IVIVC
    15.5 Bioequivalence of Injectable Formulations
    15.6 Summary
    References
16 Biopharmaceutics of Topical and Transdermal Formulations
    16.1 Introduction
    16.2 Skin Structure
    16.3 Active Pharmaceutical Ingredient Properties
    16.4 Topical and Transdermal Dosage Forms
    16.5 Measurement of In Vitro Drug Release
    16.6 Measurement of Skin Permeation
    16.7 Bioequivalence Testing of Topical/Transdermal Products
    16.8 Conclusions
    References
17 Impact of the Microbiome on Oral Biopharmaceutics
    17.1 Introduction
    17.2 Microbiome Distribution in the GI Tract
    17.3 Key Causes of Microbiome Variability
    17.4 Microbiome Influence on Key GI Parameters
    17.5 Enzymatic Degradation of Drugs by GI Microbiota
    17.6 Exploitation of the GI Microbiome for Drug Delivery
    17.7 Models of the GI Microbiome
    17.8 Conclusion
    References
Index
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