John Wiley & Sons Solid-State Properties of Pharmaceutical Materials Cover This book presents a detailed discussion of important solid-state properties of pharmaceutical mater.. Product #: 978-1-118-14530-2 Regular price: $188.79 $188.79 Auf Lager

Solid-State Properties of Pharmaceutical Materials

Byrn, Stephen R. / Zografi, George / Chen, Xiaoming (Sean)

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1. Auflage September 2017
432 Seiten, Hardcover
Wiley & Sons Ltd

ISBN: 978-1-118-14530-2
John Wiley & Sons

Kurzbeschreibung

This book presents a detailed discussion of important solid-state properties of pharmaceutical materials, as well as methods of solid-state analysis, such as X-Ray powder diffraction, microscopy, infrared spectroscopy, Raman spectroscopy, and solid state NMR. It also reviews important topics such as particle size/surface area, mechanical properties, and those physical and chemical transformations that impact solid-state stability. It discusses important applications of analytical methods of pharmaceutical solids in form selection, mixture analysis, solid dispersions, and nanotechnology.

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Presents a detailed discussion of important solid-state properties, methods, and applications of solid-state analysis
* Illustrates the various phases or forms that solids can assume and discussesvarious issues related to the relative stability of solid forms and tendencies to undergo transformation
* Covers key methods of solid state analysis including X-ray powder diffraction, thermal analysis, microscopy, spectroscopy, and solid state NMR
* Reviews critical physical attributes of pharmaceutical materials, mainly related to drug substances, including particle size/surface area, hygroscopicity, mechanical properties, solubility, and physical and chemical stability
* Showcases the application of solid state material science in rational selection of drug solid forms, analysis of various solid forms within drug substance and the drug product, and pharmaceutical product development
* Introduces appropriate manufacturing and control procedures using Quality by Design, and other strategies that lead to safe and effective products with a minimum of resources and time

Preface

Acknowledgments

Chapter 1: Solid State Properties and Pharmaceutical Development

1.1 Introduction

1.2 Solid State Forms

1.3 ICH Q6A Decision Trees

1.4 "Big Questions" for Drug Development

1.5 Accelerating Drug Development

1.6 Solid State Chemistry in Preformulation and Formulation

1.7 Learning before Doing and Quality by Design

1.8 Performance and Stability in Pharmaceutical Development

1.9 Moisture Uptake

1.10 Solid State Reactions

1.11 Noninteracting Formulations - Physical Characterizations

References

Chapter 2: Polymorphs

2.1 Introduction

2.2 How Are Polymorphs Formed?

2.3 Structural Aspect of Polymorphs

2.4 Physical, Chemical, and Mechanical Properties

2.5 Thermodynamic Stability of Polymorphs

2.6 Polymorph Cconversion

2.7 Control of Polymorphs

2.8 Polymorph Screening

2.9 Polymorph Prediction

References

Chapter 3: Solvates and Hhydrates

3.1 Introduction

3.2 Pharmaceutical Importance of Hydrates

3.3 Classification of Pharmaceutical Hydrates

3.4 Water Aactivity

3.5 Stoichiometric Hhydrates

3.6 Nonstoichiometric Hhydrates

3.7 Hydration/Dehydration

3.8 Preparation and Characterization of Hydrates and Solvates

References

Chapter 4: Pharmaceutical Salts

4.1 Introduction

4.2 Importance of Pharmaceutical Salts

4.3 Weak Acid, Weak Base, and Salt

4.4 pH-Solubility Profiles of Ionizable Compounds

4.5 Solubility, Dissolution and Bioavailability of Pharmaceutical Salts

4.6 Physical Stability of Pharmaceutical Salts

4.7 Strategies for S salt Sselection

References

Chapter 5: Pharmaceutical Co-crystals

5.1 Introduction

5.2 Co-crystals and Crystal Engineering

5.3 Co-crystals and Crystal Engineering

5.4 Co-crystals and Crystal Engineering

5.5 Solubility Phase Diagrams for Co-crystals

5.6 Preparation of Co-crystals

5.7 Dissolution and Bioavailability of Co-crystals

5.8 Comparison of Ppharmaceutical Ssalts and Cco-crystals

References

Chapter 6: Amorphous Solids

6.1 Introduction

6.2 The Formation of Amorphous Solids

6.3 Methods of Preparing Amorphous Solids

6.4 The Glass Transition Temperature

6.5 Structural Features of Amorphous Solids

6.6 Molecular Mobility

6.7 Mixtures of Amorphous Solids

6.8 References

Chapter 7: Crystal Mesophases and Nanocrystals

7.1 Introduction

7.2 Overview of Crystal Mesophases

7.3 Liquid Crystals

7.4 Conformationally Disordered (Condis) Crystals

7.5 Plastic Crystals

7.6 Nanocrystals

References

Chapter 8: X-ray Crystallography and Crystal Packing Analysis

8.1 Introduction

8.2 Crystals

8.3 Miller Indices and Crystal Faces

8.4 Determination of the Miller Indices of the Faces of a Crystal

8.5 Determination of Crystal Structure

References

Chapter 9: X-ray Crystallography and Crystal Packing Analysis X-ray Powder Diffraction

9.1 Introduction

9.2 X-ray Powder Diffraction of Crystalline Materials

9.3 Qualitative Analysis of Crystalline Materials

9.4 Phase Transformations

9.5 Quantitative Phase Analysis Using XRPD

9.6 Solving Crystal Structures Using Powder X-ray Diffraction

9.7 X-ray Diffraction of Amorphous and Crystal Mesophase Forms

9.8 Pair Distribution Function

9.9 X-ray Ddiffractometers

9.10 Variable Ttemperature XRPD

9.11 References

Chapter 10: Differential Scanning Calorimetry and Thermogravimetric Analysis

10.1 Introduction

10.2 The Basics of Differential Scanning Calorimetry

10.3 Thermal Transitions of Pharmaceutical Materials

10.4 DSC Instrumentation

10.54 Thermogravimetric Analysis

10.65 Operating a TGA Instrument

10.76 Evolved Gas Analysis

10.87 Applications of DSC and TGA

10.8 Optimization of the Freezing-Drying Cycle in Lyophilization

10.9 Determination of Chemical Purity of Organic Compounds

References

Chapter 11: Microscopy

11.1 Introduction

11.2 Light Microscopy

11.3 Polarized Light Microscopy

11.4 Thermal Microscopy

11.5 Functionality of the Light Microscope

11.6 Digital Microscope

11.7 Application of Light Microscopy to Pharmaceutical Materials

11.8 Scanning Electron Microscope

11.9 Environmental Scanning Electron Microscopy (ESEM)

11.10 Atomic Force Microscopy

References

Chapter 12: Vibrational Spectroscopy

12.1 Introduction

12.2 The Nature of Molecular Vibrations

12.3 Fourier Transformed Infrared Spectroscopy

12.4 Material Characterization by FT-IR Spectroscopy

12.5 FT-IR Instrumentation

12.6 Diffuse Reflectance FT-IR

12.7 Attenuated Total Reflectance FT-IR

12.8 FT-IR Microscopy

12.9 Near Infrared Spectroscopy

12.10 Raman Spectroscopy

12.11 Raman Instrumentation and Sampling

12.12 Raman Microscope

12.13 Terahertz Spectroscopy

12.14 Comparison of FT-IR, NIR, Raman, and Terahertz Spectroscopy

References

Chapter 13: Solid-State NMR Spectroscopy

13.1 Introduction

13.2 An Overview of Solid-State 13C CP/MAS NMR Spectroscopy

13.3 Solid State NMR Studies of Pharmaceuticals

13.4 Phase Identification in Dosage Forms

13.5 Other Basic Solid-State NMR Experiments Useful for Pharmaceu-tical Analysis

13.6 Determination of the Domain Structure of Amorphous Dispersions Using SSNMR

References

Chapter 14: Particle and Powder Analysis

14.1 Introduction

14.2 Particles in Pharmaceutical Systems

14.3 Particle Size and Shape

14.4 Particle Size Distribution

14.5 Dynamic Light Scattering

14.6 Zeta Potential

14.7 Laser Diffraction

14.8 Dynamic Image Analysis

14.9 Sieve Analysis

14.10 Bulk Properties of Pharmaceutical Particulates and Powder

14.11 Surface Area Measurement

References

Chapter 15: Hygroscopic Properties of Solids

15.1 Introduction

15.2 Water Vapor Sorption-Desorption

15.3 Water Vapor Sorption Isotherms, Relative Humidity and Water Activity

15.4 Measurement of Water Content and Water Vapor Sorption/Desorption Isotherms

15.5 Measurement of Water Vapor Sorption/Desorption Isotherms

15.56 Modes of Water Vapor Sorption

References

Chapter 16: Mechanical Properties of Pharmaceutical Materials

16.1 Introduction

16.2 Stress and Strain

16.3 Elasticity

16.4 Plasticity

16.5 Viscoelasticity

16.6 Brittleness

16.7 Hardness

16.8 Powder Compression

16.9 Powder Compression Models and Compressibility

16.10 Compactibility and Tensile Strength

16.11 Effect of Solid Form on Mechanical Properties

16.12 Effect of Moisture on Mechanical Properties

16.13 Methods for Testing Mechanical Properties

16.14 Nanoindention

References

Chapter 17: Solubility and Dissolution

17.1 Introduction

17.2 Principle Concepts Associated with Solubility

17.3 Prediction of Aqueous Drug Solubility

17.4 Solubility of Pharmaceutical Solid Forms

17.5 Solubility Determination Using the Shake Flask Method

17.6 High Throughput Screening of Solubility

17.7 Solubility Measurement of Metastable Forms

17.8 Kinetic Solubility Measurement

17.9 Solubility Determination of Drugs in Polymer Matrices

17.10 Dissolution Testing

17.11 Non-sink Dissolution Test

17.12 Intrinsic Dissolution Studies

References

Chapter 18: Physical Stability of Solids

18.1 Introduction

18.2 Underlying Basis for Physical Instability in Pharmaceutical Systems

18.3 Disorder in Crystals

18.4 Examples of the Role of Process-Induced Disorder in Solid-State Physical Instability in Pharmaceutical Systems

18.5 Considerations in Evaluating Solid-State Physical Stability

References

Chapter 19: Chemical Stability of Solids

19.1 Introduction

19.2 Examples of Chemical Reactivity in the Solid State

19.3 Some General Principles That Establish the Rate of Chemical Reactions in Solution

19.4 The Role of Crystal Defects in Solid-State Reactions

19.5 Chemical Reactivity in the Amorphous Solid State

19.6 Chemical Reactivity and Processed-Induced- -Disorder

19.7 The Effects of Residual Water on Solid-State Chemical Reactivity

19.8 Drug- Excipient Interactions

19.9 Summary

References

Chapter 20: Solid-State Properties of Proteins

20.1 Introduction

20.2 Solution Properties of Proteins

20.3 Amorphous Properties of Proteins

20.4 Crystalline Properties of Proteins

20.5 Local Molecular Motions and the Dynamical Transitional Temperature, Td

20.6 Solid-State Physical and Chemical Stability of Proteins

20.7 Cryoprotection and Lyoprotection

References

Chapter 21: Form Selection of Active Pharmaceutical Ingredients

21.1 Introduction

21.2 Form Selection

21.3 Amorphous Form Screening

21.4 Salt Selection

21.5 Co-crystal Screening

21.6 Polymorph Screening

21.7 Slurrying

21.8 High-throughput Screening

21.9 Crystallization in Cconfined Sspace

21.10 Non-solvent Based Polymorph Screening

21.11 Polymer Induced Heteronucleation

21.12 Physical Characterization

21.13 Thermodynamic Stability and Form Selection

References

Chapter 22: Mixture Analysis

22.1 Introduction

22.2 Limitations of Wet Chemistry

22.3 Pharmaceutical Analysis in the Solid State

22.4 Development and Validation of a Calibration Model

22.5 Measurement of Amorphous Content

22.6 Detection of the Degree of Crystallinity

22.7 Quantification of Mixtures of Polymorphs

22.8 Salt and Free Form Composition

22.9 Process Analytical Technology (PAT)

22.10 Physical and Chemical Attributes of a Process

22.11 Selection of Process Analyzers

References

Chapter 23: Product Development

23.1 Chemistry, Manufacture, and Control (CMC)

23.2 Preformulation

23.3 Drug Excipient Compatibility

23.4 Solid Dispersions

23.5 Abuse-Deterrent Dosage Forms

23.6 Drug Eluting Stents (DES)

23.7 Dry Powder Inhalers (DPI)

23.8 Lyophilization and Biopharmaceutical Products

References

Chapter 24: Quality by Design

24.1 Introduction

24.2 Quality by Design Wheel

24.3 Learning before Doing (LbD)

24.4 Risk Based Orientation

24.5 API Attributes and Process Design

24.6 Development and Design Space

24.7 Process Design - Crystallization

24.8 Phase Transformations during Wet Granulation

24.9 Dissolution Tests with an In-Vitro in-Vivo Correlation (IVIVC) for Quality by Design

24.10 Conclusion

References
Stephen R. Byrn, PhD is Charles B. Jordan Professor of Medicinal Chemistry in the School of Pharmacy, Purdue University. Dr. Byrn has founded and directed several programs at Purdue University including CAMP, the Center for AIDS Research, the Molecules to Market program, and Purdue's graduate programs in regulatory and quality compliance. Dr. Byrn has served as chair of the Pharmaceutical Sciences Advisory Committee to the FDA and Chair of the Drug Substances Technical Committee, Product Quality Research Initiative. Dr. Byrn is co-founder of SSCI, Inc. a cGMP research and information Company.

George Zografi, PhD is the Edward Kremers Professor Emeritus of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison. He was the recipient of the APhA Ebert Prize in 1984 and 2001, the AAPS Dale E. Wurster Award for Pharmaceutics in 1990 and its Distinguished Scientist Award in 1995, as well as the Volwiler Research Achievement Award of the American Association of Colleges of Pharmacy. Xiaoming Chen, PhD is currently the Director of Formulation Development in Antares Pharma Inc. Prior to that, he held various positions in pharmaceutical product development at Schering-Plough, OSI Pharmaceuticals, Astellas Pharma, and Shionogi Inc. He has published over a dozen of papers in peer-reviewed journals and is a co-inventor of four US patents.