Solid-State Materials in Pharmaceutical Chemistry - Byrn, Stephen R

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Auteur(s) : Byrn, Stephen R

Editeur : John Wiley & Sons

Langue : Anglais

Parution : 01/09/2025

Format : Moyen, de 350g à 1kg

Nombre de pages : 560.0

ISBN : 9781394254446

Résumé :

Biography of Authors xv

Preface xvii

Preface to the First Edition xvii

Acknowledgment xix

1 Solid-State Properties and Pharmaceutical Development 1

2 Polymorphs 27

3 Pseudopolymorphs: Hydrates and Solvates 49

4 Pharmaceutical Salts 65

5 Pharmaceutical Cocrystals 81

6 Amorphous Solids 97

7 Crystal Mesophases and Nanocrystals 121

8 X-Ray Crystallography and Crystal-Packing Analysis 131

9 X-Ray Powder Diffraction 139

10 Differential Scanning Calorimetry and Thermogravimetric Analysis 159

11 Microscopy 181

12 Vibrational Spectroscopy 203

13 Solid-State NMR Spectroscopy 227

14 Particle and Powder Analysis 247

15 Hygroscopic Properties of Solids 267

16 Mechanical Properties of Pharmaceutical Materials 287

17 Solubility and Dissolution 307

18 Physical Stability of Solids 329

19 Chemical Stability of Solids 349

20 Solid-State Properties of Proteins 375

21 Physical and Chemical Properties of RNA Therapeutics 389

22 Solid Form Selection of Active Pharmaceutical Ingredients 411

23 Final Stage Drug Substance Manufacturing and Control 431

24 Solid-State Mixture Analysis 455

25 Drug Product Development 479

26 Quality by Design 511

Index 527

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Biographie:

Stephen R. Byrn, PhD, Charles B. Jordan Professor of Medicinal Chemistry in the Department of Industrial and Molecular Pharmaceutics, Purdue University.

George Zografi, PhD, Edward Kremers Professor Emeritus of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison.

Xiaoming (Sean) Chen, PhD, works in the field of pharmaceutical product development and held various positions at Schering-Plough, OSI Pharmaceuticals, Astellas Pharma, Shionogi Inc, Antares Pharma, Arvinas, and Improved Pharma....

Sommaire:

Biography of Authors xv

Preface xvii

Preface to the First Edition xvii

Acknowledgment xix

1 Solid-State Properties and Pharmaceutical Development 1

1.1 Introduction 1

1.2 Solid-state Forms 1

1.3 Bulk and Surface Properties of Solids 6

1.4 ICH Q6A Decision Trees 7

1.5 Big Questions for Drug Development 8

1.6 Accelerating Drug Development 10

1.7 Solid-state Chemistry in Preformulation and Formulation 12

1.8 Solid-Lipid Nanoparticles 15

1.9 Learning Before Doing and Quality by Design 16

1.10 Performance and Stability in Pharmaceutical Development 19

1.11 Moisture Uptake 20

1.12 Solid-state Reactions 21

1.13 Noninteracting Formulations - Physical Characterizations 21

2 Polymorphs 27

2.1 Introduction 27

2.2 How Are Polymorphs Formed? 27

2.3 Structural Aspect of Polymorphs 29

2.3.1 Configurational Polymorphs 29

2.3.2 Conformational Polymorphs 30

2.4 Physical, Chemical, and Mechanical Properties 32

2.4.1 Solubility 33

2.4.2 Chemical Stability 34

2.4.3 Mechanical Properties 34

2.5 Thermodynamic Stability of Polymorphs 35

2.5.1 Monotropy and Enantiotropy 36

2.5.2 Burger and Ramberger's Rules 37

2.5.3 van't Hoff Plot 37

2.5.4 ??G?/temperature diagram 38

2.6 Polymorph Conversion 39

2.6.1 Solution-mediated Transformation 40

2.6.2 Solid-state Conversion 40

2.7 Control of Polymorphs 42

2.8 Polymorph Screening 43

2.9 Polymorph Prediction 44

3 Pseudopolymorphs: Hydrates and Solvates 49

3.1 Introduction 49

3.2 Pharmaceutical Importance of Hydrates 49

3.3 Classification of Pharmaceutical Hydrates 51

3.4 Water Activity 52

3.5 Stoichiometric Hydrates 53

3.6 Nonstoichiometric Hydrates 54

3.7 Emerging Interests in Organic Solvates 55

3.8 Isostructural Solvates 57

3.9 Dehydration and Desolvation 59

3.10 Preparation and Characterization of Hydrates and Solvates 61

4 Pharmaceutical Salts 65

4.1 Introduction 65

4.2 Importance of Pharmaceutical Salts 65

4.3 Weak Acid, Weak Base, and Salt 66

4.4 pH Solubility Profiles of Ionizable Compounds 69

4.5 Solubility, Dissolution, and Bioavailability of Pharmaceutical Salts 71

4.6 Physical Stability of Pharmaceutical Salts 75

4.7 Strategies for Salt Selection 76

5 Pharmaceutical Cocrystals 81

5.1 Introduction 81

5.2 Cocrystals and Crystal Engineering 81

5.3 Solubility Phase Diagrams for Cocrystals 83

5.4 Preparation of Cocrystals 85

5.5 Dissolution and Bioavailability of Cocrystals 88

5.6 Pharmaceutical Applications of Cocrystals 90

5.7 Comparison of Pharmaceutical Salts and Cocrystals 92

5.7.1 Formation 93

5.7.2 Preparation 93

5.7.3 Polymorphism and Pseudopolymorphism 93

5.7.4 Characterization 93

5.7.5 Stability 93

5.7.6 Formulation 94

5.7.7 Regulatory 94

6 Amorphous Solids 97

6.1 Introduction 97

6.2 The Formation of Amorphous Solids 98

6.3 Methods of Preparing Amorphous Solids 99

6.4 The Glass Transition Temperature 100

6.5 Structural Features of Amorphous Solids 103

6.6 Molecular Mobility 105

6.6.1 Overview of Molecular Mobility 105

6.6.2 Viscosity and Molecular Mobility 106

6.6.3 Relaxation Time 107

6.6.4 Fragility in Supercooled Liquids 108

6.6.5 Diffusive Relaxation Time in the Glassy State 110

6.6.6 Secondary Relaxations in Amorphous Solids 112

6.7 Mixtures of Amorphous Solid...