Details

Disordered Pharmaceutical Materials

1. Aufl.

von: Marc Descamps
160,99 €
Verlag:	Wiley-VCH
Format:	EPUB
Veröffentl.:	28.03.2016
ISBN/EAN:	9783527652716
Sprache:	englisch
Anzahl Seiten:	544

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Beschreibungen

Titelbeschreibung

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.

Inhaltsverzeichnis

1 Some Facets of Molecular Disorder in Crystalline and Amorphous Pharmaceuticals 1 Marc Descamps and Jean-Francois Willart 1.1 The Crystal/Amorph Alternative 2 1.2 Characteristics of the Disorder in Glass Formers 28 Acknowledgments 51 References 51 2 Influence of Disorder on Dissolution 57 Khushboo Kothari and Raj Suryanarayanan 2.1 Introduction 57 2.2 Approaches to Enhance Solubility 59 2.3 Measuring the Solubility Advantage of Amorphous Compounds 64 2.4 Solid Dispersions 66 2.5 Polymer Properties 67 2.6 Drug?Polymer Interactions 70 2.7 Polymer Concentration 71 2.8 Other Formulation Components 73 2.9 Formulation Variables 74 2.10 Reliable Measurement of Supersaturation 75 2.11 Conclusion 76 References 77 3 Crystal Imperfections in Molecular Crystals: Physical and Chemical Consequences 85 William Jones and Mark D. Eddleston 3.1 Introduction 85 3.2 General Aspects of Defects in Crystals 87 3.3 Role of Imperfections in Reactivity and Stability ? Chemistry in the Perfect and Imperfect Lattice 92 3.4 Role in Physical Processes 96 3.5 Concluding Remarks 99 References 99 4 Observation and Characterization of Crystal Defects in Pharmaceutical Solids 103 Mark D. Eddleston andWilliam Jones 4.1 Introduction 103 4.2 Techniques for Characterizing Defects within Crystals 104 4.3 Techniques for Characterizing Defects Emergent at Crystal Surfaces 119 4.4 Techniques for Quantifying Defect Densities within Crystals 125 4.5 The Complementarity of Techniques for Characterizing Defects 126 4.6 Summary and Outlook 127 Acknowledgment 128 References 128 5 "Enantiomeric Disorder" Pharmaceutically Oriented 135 Gerard Coquerel and Rui Tamura 5.1 Introduction 135 5.2 Introduction and Lexicon of Specific Terms Used among Chiral Molecules and Chiral Molecular Associations 135 5.3 Restrictions in Symmetry Operations Inside Crystal Lattices with an Enantiomeric Excess Different from Zero 136 5.4 Impact of Chirality on Phase Diagrams and the Gibbs?Scott Phase Rule 137 5.5 Competitions between Solid Solutions (Impact of Polymorphism on Solid Solutions) Application: Preferential Enrichment 149 5.6 Disorder at Level 3 Multiepitaxy between Enantiomers 154 5.7 Conclusion and Perspectives 156 Acknowledgments 157 References 157 6 Conformational Disorder and Atropisomerism in Pharmaceutical Compounds 161 Attilio Cesaro, Barbara Bellich, Giovanna Giannini, and Alessandro Maiocchi 6.1 Premise: Conformational Energy Barriers in FlexibleMolecules 161 6.2 Conformational Topology and Crystallization of Chain Molecules 162 6.3 Conformational Polymorphism and Crystallization of Flexible Molecules 165 6.4 Conformational Flexibility of Ring Molecules: Carbohydrates 170 6.5 Hindered Conformational Isomerism: Atropisomerism 172 6.6 Conclusion 178 Acknowledgments 180 References 180 7 Tautomerism in Drug Delivery 183 Zaneta Wojnarowska and Marian Paluch 7.1 Broadband Dielectric Spectroscopy as a Powerful Tool for Investigating the Tautomerization Process in Condensed Materials 187 7.2 Tautomerization Kinetics of Supercooled Pharmaceuticals 190 Acknowledgment 197 References 198 8 Disorders in Pharmaceutical Polymers 201 Emeline Dudognon and Sheng Qi 8.1 Polymers Architectures - Structural Disorders 202 8.2 Structural States and Phases Transitions 205 8.3 Dynamic Disorders 213 8.4 Blends of Polymer and Small Molecules 221 8.5 Effect of the Structural Properties of Pharmaceutical Polymers on Their Physical Behavior 224 8.6 Concluding Remarks 234 References 235 9 Polymer Gels, Hydrogels, and Scaffolds ? An Overview 241 Madeleine Djabourov and Kawthar Bouchemal 9.1 Introduction 241 9.2 Gels and Hydrogels 243 9.3 Scaffolds 268 9.4 Conclusion 275 References 276 10 Use of the Pair Distribution Function Analysis in the Context of Pharmaceutical Materials 283 Pierre Bordet and PaulineMartinetto 10.1 Introduction 283 10.2 What Is the PDF? 284 10.3 How to Measure the PDF 288 10.4 Modeling of the PDF 290 10.5 Applications of PDF Analysis to Molecular and Pharmaceutical Compounds 292 10.6 Conclusion 297 Acknowledgments 298 References 298 11 Application of Broadband Dielectric Spectroscopy to Study Molecular Mobility in Pharmaceutical Systems 301 Katarzyna Grzybowska, Karolina Adrjanowicz, and Marian Paluch 11.1 Introduction to Broadband Dielectric Spectroscopy 301 11.2 Molecular Dynamics in Amorphous Pharmaceutical Systems 316 11.3 Molecular Mobility and Dielectric Response in Partially Ordered Pharmaceutical Systems 346 Acknowledgment 353 References 353 12 Raman Spectroscopy in Disordered Molecular Compounds: Application to Pharmaceuticals 361 Alain Hedoux 12.1 Introduction 361 12.2 Raman Spectroscopy 362 12.3 Analysis of Molecular Compounds by Raman Spectroscopy 370 12.4 Conclusion 388 References 388 XII Contents 13 Study of Disordered Materials by Terahertz Spectroscopy 393 Juraj Sibik and J. Axel Zeitler 13.1 Introduction 393 13.2 Exploration of Terahertz Dynamics Prior to THz-TDS 394 13.3 Response of Supercooled Liquids and Glasses at Terahertz Frequencies 397 13.4 Terahertz Studies of Disordered Molecular Solids 400 13.5 Organic Glass-Forming Liquids 404 13.6 Characterization of Disordered Biological and Pharmaceutical Systems 410 13.7 Outlook 416 References 418 14 Study of Disorder by Solid-State NMR Spectroscopy 427 Marco Geppi, Silvia Borsacchi, and Elisa Carignani 14.1 Introduction 427 14.2 Basics of Solid-State NMR 428 14.3 Static Disorder 433 14.4 Dynamic Disorder 448 14.5 A Case Study 458 14.6 Final Remarks and Future Perspectives 462 References 464 15 Processing-Induced Disorder in Pharmaceutical Materials 467 Sheng Qi 15.1 Introduction 467 15.2 Pharmaceutical Processing 468 15.3 Conclusion 484 References 485 16 Patenting of Inventions Relating to Solid Forms, with Special Considerations on Disordered Forms 491 Bertrand Gellie 16.1 Patentability of Disordered Crystals 493 16.2 Patentability of Co-crystals 496 16.3 Patentability of Amorphous Forms 500 16.4 Patenting (Disordered) Nanocrystals 509 16.5 Conclusions 511 Index 513

Autorenportrait

Marc Descamps is Professor for solid state physics and Head of the Technological Research Group "Therapeutic Materials" at the University of Lille, France. He is the author of more than 160 publications in international journals and he has collaborated with several large pharmaceutical companies. His research interests include: phase transitions in molecular materials, disordered crystals, molecular glasses and studies of the structural and dynamic properties of pharmaceutical solids by a variety of physicochemical techniques.