Solid State Development and Processing of Pharmaceutical Molecules - Michael Gruss

Sommaire:

Series Editors Preface xxi

Preface xxiii

1 Aspects for Developing and Processing Solid Forms 1
Michael Gruss

1.1 Aspects for Developing and Processing Solid Forms 1

1.1.1 Introduction 1

1.1.2 Education and Personal Background 1

1.1.3 Societal Impact - Fishing in ForeignWaters 4

1.1.3.1 Motivation 4

1.1.3.2 The Personal Dimension 5

1.1.3.3 Beyond the Impact on Individuals 6

1.1.3.4 Understanding the Market - Not an Easy Task 7

1.1.3.5 Benefits of an Interdisciplinary Mindset 9

1.1.4 The Basis for Mutual Understanding 9

1.1.5 Crystallization is a Separation, Not a Separated Process 11

1.1.6 Some Early Information About Solid-state Properties 13

1.1.7 Digitalization (Not Only) in the Laboratory 13

1.1.7.1 Prerequisites - Technology and People 13

1.1.7.2 Connect Data and the Right Information from Synthesis and Analysis 15

1.1.7.3 Contributions and Choices 17

1.1.7.4 Application of Digitalization 18

1.1.7.5 Fully Digitalized Infrastructure 20

1.1.8 Basic Terms and Concepts in theWorld of Solid State 21

1.1.8.1 Crystalline and Amorphous 21

1.1.8.2 Crystallization and Precipitation 23

1.1.8.3 Understanding the Phase Diagram - Analytical Characterization of the Solid-Liquid and Solid-Solid Systems 23

1.1.8.4 Polymorphism 24

1.1.8.5 Multi-component Compounds - Salt, Cocrystal, Solvate, and Hydrate 25

1.1.8.6 Solvates, Hydrates, Non-solvated Forms, or Ansolvates 26

1.1.8.7 Dispersed Primary Particles, Aggregates, and Agglomerates 29

1.1.8.8 Particle Size and Particle Size Distribution (PSD) 29

1.1.9 Investigating and Understanding the Polymorphic Landscape 29

1.1.10 Performing the Crystallization 31

1.1.11 Objectives for the Optimization of Crystallization Processes and Solid-State Properties 32

1.1.12 Implementation of In Silico and Simulation Techniques 32

1.1.13 Saving the Investment - Addressing Intellectual Property Rights 35

1.1.14 Concluding Remarks 36

List of Abbreviations 37

References 38

2 Determination of Current Knowledge 45
Andriy Kuzmov and Ronak Savla

2.1 Why is it Important to Search for Relevant Information Before Starting a Solid-State Project? 45

2.2 Where to Begin a Literature Search for a Solid-State Project? 47

2.2.1 Literature Search 48

2.2.1.1 Focusing Your Literature Search 49

2.2.2 Staying on Top of the Latest Publications 51

2.3 Patent Search 51

2.3.1 Types of Patent Reports 52

2.3.2 Understanding the Elements of Patents 53

2.3.3 Patent Classification 54

2.3.4 Patent Databases 56

2.3.4.1 Free Patent Databases 57

2.4 Other Useful Resources for Solid-State Projects 61

2.4.1 Cambridge Structural Database 61

2.4.2 Crystallography Open Database 62

List of Abbreviations 62

References 63

3 Systematic Screening and Investigation of Solid-State Landscapes 67
Ulrike Werthmann

3.1 Introduction 67

3.2 General Aspects of Solid-State Investigations in Early Drug Discovery Phase 68

3.3 Transition Phase from Late Stage Research to Early Stage Development 69

3.4 Solid-State Characteristics in Preclinical Formulations 70

3.5 API-crystallization Strategy in Candidate Profiling Phase 73

3.6 Selection Criteria of a Suitable Solid Form 77

3.7 Knowledge Management 79

3.8 Control of Solid Form Properties in Development 79

3.9 Exploratory Crystallization Experiments 80

List of Abbreviations 87

References 88<...