Disordered Pharmaceutical Materials E-Book

• Herausgeber: Wiley-VCH
• Kategorie: Wissenschaft und neue Technologien
• Sprache: Englisch

Seitenzahl: 1041

Veröffentlichungsjahr: 2016

Beschreibung

A one-stop resource for researchers, developers, and post graduate students in pharmaceutical science. This handbook and ready reference provides detailed, but not overloaded information -- presenting the topic without unnecessarily complex formalism.
As such, it gives a systematic and coherent overview of disordered materials for pharmaceutical applications, covering fundamental aspects, as well as preparation and characterization techniques for the target-oriented development of drug delivery systems based on disordered crystals and amorphous solids. Special attention is paid to examine the different facets and levels of disorder in their structural and dynamic aspects as well as the effect of disorder on dissolution and stability. Chapters on processing induced disorder and on patenting issues round off the book. As a result the book helps overcoming the challenges of using these materials in the pharmaceutical industry.
For pharmaceutical and medicinal chemists, materials scientists, clinical physicists, and pharmaceutical laboratories looking to make better and more potent pharmaceuticals.

Leseprobe

Table of Contents

Cover

Title Page

Copyright

List of Contributors

Chapter 1: Some Facets of Molecular Disorder in Crystalline and Amorphous Pharmaceuticals

1.1 The Crystal/Amorph Alternative

1.2 Characteristics of the Disorder in Glass Formers

Acknowledgments

References

Chapter 2: Influence of Disorder on Dissolution

2.1 Introduction

2.2 Approaches to Enhance Solubility

2.3 Measuring the Solubility Advantage of Amorphous Compounds

2.4 Solid Dispersions

2.5 Polymer Properties

2.6 Drug–Polymer Interactions

2.7 Polymer Concentration

2.8 Other Formulation Components

2.9 Formulation Variables

2.10 Reliable Measurement of Supersaturation

2.11 Conclusion

References

Chapter 3: Crystal Imperfections in Molecular Crystals: Physical and Chemical Consequences

3.1 Introduction

3.2 General Aspects of Defects in Crystals

3.3 Role of Imperfections in Reactivity and Stability – Chemistry in the Perfect and Imperfect Lattice

3.4 Role in Physical Processes

3.5 Concluding Remarks

References

Chapter 4: Observation and Characterization of Crystal Defects in Pharmaceutical Solids

4.1 Introduction

4.2 Techniques for Characterizing Defects within Crystals

4.3 Techniques for Characterizing Defects Emergent at Crystal Surfaces

4.4 Techniques for Quantifying Defect Densities within Crystals

4.5 The Complementarity of Techniques for Characterizing Defects

4.6 Summary and Outlook

Acknowledgment

References

Chapter 5: “Enantiomeric Disorder” Pharmaceutically Oriented

5.1 Introduction

5.2 Introduction and Lexicon of Specific Terms Used among Chiral Molecules and Chiral Molecular Associations

5.3 Restrictions in Symmetry Operations Inside Crystal Lattices with an Enantiomeric Excess Different from Zero

5.4 Impact of Chirality on Phase Diagrams and the Gibbs–Scott Phase Rule

5.5 Competitions between Solid Solutions (Impact of Polymorphism on Solid Solutions) Application: Preferential Enrichment

5.6 Disorder at Level 3 Multiepitaxy between Enantiomers

5.7 Conclusion and Perspectives

Acknowledgments

References

Chapter 6: Conformational Disorder and Atropisomerism in Pharmaceutical Compounds

6.1 Premise: Conformational Energy Barriers in Flexible Molecules

6.2 Conformational Topology and Crystallization of Chain Molecules

6.3 Conformational Polymorphism and Crystallization of Flexible Molecules

6.4 Conformational Flexibility of Ring Molecules: Carbohydrates

6.5 Hindered Conformational Isomerism: Atropisomerism

6.6 Conclusion

Acknowledgments

References

Chapter 7: Tautomerism in Drug Delivery

7.1 Broadband Dielectric Spectroscopy as a Powerful Tool for Investigating the Tautomerization Process in Condensed Materials

7.2 Tautomerization Kinetics of Supercooled Pharmaceuticals

Acknowledgment

References

Chapter 8: Disorders in Pharmaceutical Polymers

8.1 Polymers Architectures – Structural Disorders

8.2 Structural States and Phases Transitions

8.3 Dynamic Disorders

8.4 Blends of Polymer and Small Molecules

8.5 Effect of the Structural Properties of Pharmaceutical Polymers on Their Physical Behavior

8.6 Concluding Remarks

References

Chapter 9: Polymer Gels, Hydrogels, and Scaffolds – An Overview

9.1 Introduction

9.2 Gels and Hydrogels

9.3 Scaffolds

9.4 Conclusion

References

Chapter 10: Use of the Pair Distribution Function Analysis in the Context of Pharmaceutical Materials

10.1 Introduction

10.2 What Is the PDF?

10.3 How to Measure the PDF

10.4 Modeling of the PDF

10.5 Applications of PDF Analysis to Molecular and Pharmaceutical Compounds

10.6 Conclusion

Acknowledgments

References

Chapter 11: Application of Broadband Dielectric Spectroscopy to Study Molecular Mobility in Pharmaceutical Systems

11.1 Introduction to Broadband Dielectric Spectroscopy

11.2 Molecular Dynamics in Amorphous Pharmaceutical Systems

11.3 Molecular Mobility and Dielectric Response in Partially Ordered Pharmaceutical Systems

Acknowledgment

References

Chapter 12: Raman Spectroscopy in Disordered Molecular Compounds: Application to Pharmaceuticals

12.1 Introduction

12.2 Raman Spectroscopy

12.3 Analysis of Molecular Compounds by Raman Spectroscopy

12.4 Conclusion

References

Chapter 13: Study of Disordered Materials by Terahertz Spectroscopy

13.1 Introduction

13.2 Exploration of Terahertz Dynamics Prior to THz-TDS

13.3 Response of Supercooled Liquids and Glasses at Terahertz Frequencies

13.4 Terahertz Studies of Disordered Molecular Solids

13.5 Organic Glass-Forming Liquids

13.6 Characterization of Disordered Biological and Pharmaceutical Systems

13.7 Outlook

References

Chapter 14: Study of Disorder by Solid-State NMR Spectroscopy

14.1 Introduction

14.2 Basics of Solid-State NMR

14.3 Static Disorder

14.4 Dynamic Disorder

14.5 A Case Study

14.6 Final Remarks and Future Perspectives

References

Chapter 15: Processing-Induced Disorder in Pharmaceutical Materials

15.1 Introduction

15.2 Pharmaceutical Processing

15.3 Conclusion

References

Chapter 16: Patenting of Inventions Relating to Solid Forms, with Special Considerations on Disordered Forms

16.1 Patentability of Disordered Crystals

16.2 Patentability of Co-crystals

16.3 Patentability of Amorphous Forms

16.4 Patenting (Disordered) Nanocrystals

16.5 Conclusions

Index

End User License Agreement

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Guide

Cover

Table of Contents

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