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Pharmaceutical Amorphous Solid Dispersions.

By: Contributor(s): Publisher: Somerset : John Wiley & Sons, Incorporated, 2015Copyright date: ©2015Edition: 1st edDescription: 1 online resource (505 pages)Content type:
  • text
Media type:
  • computer
Carrier type:
  • online resource
ISBN:
  • 9781118901380
Subject(s): Genre/Form: Additional physical formats: Print version:: Pharmaceutical Amorphous Solid DispersionsDDC classification:
  • 615.7
LOC classification:
  • RS192 -- .P437 2015eb
Online resources:
Contents:
Pharmaceutical Amorphous Solid Dispersions -- Contents -- Preface -- Contributors -- 1: Introduction to Amorphous Solid Dispersions -- 1.1 Introduction -- 1.2 Formation of the Amorphous State and the Glass Transition Temperature -- 1.3 Structure of Amorphous Solids -- 1.4 Molecular Mobility in Amorphous Solids -- 1.4.1 Secondary Johari-Goldstein β-Relaxation -- 1.5 Solid-State Crystallization from the Amorphous State -- 1.6 Supersaturation of API in Aqueous Media from the Amorphous State -- 1.7 Mixtures of Amorphous Solids -- 1.8 Formation and Properties of Amorphous Solid Dispersions -- 1.9 Solid-State Crystallization from Amorphous Dispersions -- 1.10 Dissolution and Supersaturation of API from Amorphous Solid Dispersions -- 1.11 Pharmaceutical Development of Amorphous Solid Dispersions -- References -- 2: Polymers and Surfactants -- 2.1 Polymers Commonly Used in Amorphous Solid Dispersions -- 2.1.1 Overview -- 2.1.2 Polymers -- 2.2 Surfactants Commonly Used in Solid Dispersions -- 2.2.1 Interfacial Properties -- 2.2.2 Self-Assembly -- 2.2.3 Applications of Surfactants -- 2.3 Synergies Between Surfactants and Polymers in Solid Dispersion Systems -- 2.3.1 The "Spring and Parachute" Model -- 2.3.2 Mechanistic Interactions Between Polymers and Surfactants -- 2.3.3 Examples of "Third-Generation" ASDs -- 2.4 Physical Properties of Materials and Considerations in Designing Solid Dispersions -- 2.4.1 Important Attributes -- 2.4.2 Preparation of Amorphous Solid Dispersions -- 2.4.3 Polymer Selection -- 2.4.4 Stability of Amorphous Solid Dispersions -- 2.4.5 Performance of ASDs -- References -- 3: Amorphous Solid Dispersion Screening -- 3.1 Introduction -- 3.2 Amorphous Dispersion Screening -- 3.2.1 API and Polymer Properties -- 3.2.2 Screening Considerations -- 3.2.3 Screening Methods -- 3.3 Amorphous Solid Dispersion Selection -- 3.3.1 Properties.
3.3.2 Selection Tools -- 3.4 Case Study -- 3.4.1 Miniaturized Studies -- 3.5 Conclusions -- References -- 4: Solid-State Characterization of Amorphous Dispersions -- 4.1 Introduction -- 4.2 Thermal Analysis Methods -- 4.3 Dielectric Relaxation Methods -- 4.4 Moisture Sorption Methods -- 4.5 Vibrational Spectroscopy and Microspectroscopy -- 4.6 Solid-State NMR Spectroscopy -- 4.7 Other Molecular Spectroscopic Methods -- 4.8 X-Ray Diffractometry -- 4.9 Microscopic and Surface Analysis Methods -- 4.10 Other Emerging Analytical Methods -- 4.11 Computational Models -- 4.12 Conclusions -- Acknowledgments -- References -- 5: Physical Stability and Crystallization Inhibition -- 5.1 Introduction -- 5.2 Theory of Crystallization in the Solid State -- 5.2.1 Nucleation Theory -- 5.2.2 Crystal Growth -- 5.2.3 Overall Kinetics of Crystallization -- 5.3 Factors Impacting the Crystallization Tendency of Active Pharmaceutical Compounds -- 5.3.1 Thermodynamic and Structural Considerations -- 5.3.2 Molecular Mobility -- 5.3.3 Impact of Preparation Method and Processing Steps -- 5.4 Role of Additives in Modifying Solid-State Crystallization -- 5.4.1 Miscibility -- 5.4.2 Impact of Polymers on Crystallization -- 5.5 Assessment of Physical Stability -- 5.5.1 Optical and Polarized Light Microscopy -- 5.5.2 X-Ray Diffraction -- 5.5.3 Solid-State Nuclear Magnetic Resonance Spectroscopy -- 5.5.4 Calorimetric Methods -- 5.5.5 Vibrational Spectroscopy -- 5.5.6 Second-Order Nonlinear Optical Imaging of Chiral Crystals -- 5.6 Crystallization in Aqueous Environments -- 5.6.1 Matrix Crystallization -- 5.6.2 Solution Crystallization -- 5.7 Summary and Outlook -- References -- 6: Solubility and Dissolution Considerations for Amorphous Solid Dispersions -- 6.1 Solubility and Dissolution: An Overview.
6.2 Differences Between Crystalline API, Amorphous Materials, and Amorphous Dispersions as it Pertains to Solubility and Dissolution -- 6.3 The Relationship of Polymer Properties with Solubility, Dissolution, and Supersaturation -- 6.3.1 The Impact of Polymer Properties on Dissolution, Solubility, and Supersaturation -- 6.4 Solubility and Dissolution Factors to Consider for Dispersions -- 6.4.1 Solubility -- 6.4.2 Dissolution -- 6.4.3 Characterization of Species Generated during Dissolution of Amorphous Solids and Their Impact on Performance -- 6.5 Solubility and Dissolution Measurements for Amorphous Dispersions: Summary, Conclusions, and Recommendations -- Acknowledgments -- References -- 7: Translational Development of Amorphous Dispersions -- 7.1 Introduction: Translational Drug Development -- 7.1.1 The Evolution of Early Development -- 7.1.2 How TDD Works -- 7.1.3 The Potency-Insolubility Conundrum and Telaprevir -- 7.2 Translational Development at the Discovery Stage -- 7.2.1 Absorption Modeling -- 7.2.2 Preparing and Characterizing an Amorphous Dispersion: Spray Drying and Glass Transition -- 7.2.3 Preparation and Characterization of SDD Suspension Formulations: Vehicle and Aqueous Stability -- 7.3 Translational Development After Discovery -- 7.3.1 Solid Form Development: Preparing Stable Dispersions -- 7.3.2 Manufacturability -- 7.3.3 Dosability -- 7.3.4 Storage Stability -- 7.4 Conclusions -- References -- 8: Preclinical and Clinical Studies -- 8.1 Introduction -- 8.2 In Vitro and Pharmaceutical Characterization -- 8.3 In Vivo Evaluation and Models -- 8.4 Clinical Assessments -- 8.5 Conclusions -- References -- 9: Spray Drying and Scale-Up -- 9.1 Introduction -- 9.2 Process Background and Physical Situation -- 9.3 Spray Drying Equipment -- 9.3.1 Spray Solution Preparation -- 9.3.2 Atomization -- 9.3.3 Drying -- 9.3.4 Product Collection.
9.3.5 Secondary Drying -- 9.4 Process Definition -- 9.4.1 Formulation Selection -- 9.4.2 Process Variables -- 9.5 Spray Drying Scale-Up -- 9.5.1 Scale-Up Considerations for Droplet Formation -- 9.5.2 Scale-Up Considerations for Droplet Drying Rate -- 9.5.3 Scale-Up Methodology -- 9.6 Conclusions -- References -- 10: Hot Melt Extrusion of Amorphous Solid Dispersions -- 10.1 Introduction -- 10.2 Materials Selection -- 10.2.1 Polymers -- 10.2.2 Plasticizers -- 10.2.3 Dissolution Adjuvants -- 10.2.4 Other Additives -- 10.2.5 General -- 10.3 Equipment Selection -- 10.3.1 Feeder -- 10.3.2 Extruder -- 10.3.3 Downstream Process -- 10.4 Process Design and Control -- 10.5 Amorphous Solid Dispersion Applications -- 10.5.1 HME Formulation Feasibility -- 10.5.2 HME Formulation Optimization -- 10.5.3 Maximizing Performance in the Finished Dosage Form -- 10.6 Summary -- References -- 11: Formulation Development of Amorphous Dispersions -- 11.1 Preparing Dispersions for Drug Products -- 11.1.1 Introduction -- 11.1.2 Creating an Amorphous Drug Substance -- 11.2 The Strategy of Quality by Design -- 11.3 Designing the Telaprevir Amorphous Dispersion Under QbD -- 11.3.1 Telaprevir and Its Process Development -- 11.3.2 Conceptual Approach to Telaprevir Process Design Space Development -- 11.3.3 Conceptual Approach to Defining Telaprevir Shelf Life -- 11.4 Concluding Remarks -- References -- 12: Scientific and Regulatory Considerations in Product Development -- 12.1 Introduction -- 12.2 Approval Process in the United States -- 12.3 The ICH -- 12.3.1 Module 1: Administrative Information and Prescribing Information -- 12.3.2 Module 2: Common Technical Document Summaries -- 12.3.3 Module 3: Quality -- 12.3.4 Module 4: Nonclinical Study Reports -- 12.3.5 Module 5: Clinical Study Reports -- 12.4 Quality-By-Design.
12.5 Development and Characterization of Amorphous Solid Dispersions -- 12.6 Conclusions -- References -- 13: Patenting Amorphous Solid Dispersions of Pharmaceuticals -- 13.1 Introduction -- 13.2 An Amorphous Solid Dispersion as a Patentable Invention -- 13.3 Considering Amorphous Solid Dispersions as Patentable Compositions of Matter -- 13.4 Claiming an Amorphous Solid Dispersion -- 13.4.1 Describing Amorphous Solid Dispersions in a Patent -- 13.5 Types of Patent Applications and Patent Examination -- 13.6 Conclusions -- References -- 14: Monographs on Polymers and Surfactants -- 14.1 Part I: Polymers -- 14.1.1 Notes -- 14.2 Part II. Surfactants -- 14.2.1 Notes -- References -- Appendix A -- Appendix B: Marketed Products -- Index -- End User License Agreement.
Summary: Providing a roadmap from early to late stages of drug development, this book overviews amorphous solid dispersion technology - a leading platform to deliver poorly water soluble drugs, a major hurdle in today's pharmaceutical industry.  Helps readers understand amorphous solid dispersions and apply techniques to particular pharmaceutical systems  Covers physical and chemical properties, screening, scale-up, formulation, drug product manufacture, intellectual property, and regulatory considerations  Has an appendix with structure and property information for polymers commonly used in drug development and with marketed drugs developed using the amorphous sold dispersion approach  Addresses global regulatory issues including USA regulations, ICH guidelines, and patent concerns around the world.
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Pharmaceutical Amorphous Solid Dispersions -- Contents -- Preface -- Contributors -- 1: Introduction to Amorphous Solid Dispersions -- 1.1 Introduction -- 1.2 Formation of the Amorphous State and the Glass Transition Temperature -- 1.3 Structure of Amorphous Solids -- 1.4 Molecular Mobility in Amorphous Solids -- 1.4.1 Secondary Johari-Goldstein β-Relaxation -- 1.5 Solid-State Crystallization from the Amorphous State -- 1.6 Supersaturation of API in Aqueous Media from the Amorphous State -- 1.7 Mixtures of Amorphous Solids -- 1.8 Formation and Properties of Amorphous Solid Dispersions -- 1.9 Solid-State Crystallization from Amorphous Dispersions -- 1.10 Dissolution and Supersaturation of API from Amorphous Solid Dispersions -- 1.11 Pharmaceutical Development of Amorphous Solid Dispersions -- References -- 2: Polymers and Surfactants -- 2.1 Polymers Commonly Used in Amorphous Solid Dispersions -- 2.1.1 Overview -- 2.1.2 Polymers -- 2.2 Surfactants Commonly Used in Solid Dispersions -- 2.2.1 Interfacial Properties -- 2.2.2 Self-Assembly -- 2.2.3 Applications of Surfactants -- 2.3 Synergies Between Surfactants and Polymers in Solid Dispersion Systems -- 2.3.1 The "Spring and Parachute" Model -- 2.3.2 Mechanistic Interactions Between Polymers and Surfactants -- 2.3.3 Examples of "Third-Generation" ASDs -- 2.4 Physical Properties of Materials and Considerations in Designing Solid Dispersions -- 2.4.1 Important Attributes -- 2.4.2 Preparation of Amorphous Solid Dispersions -- 2.4.3 Polymer Selection -- 2.4.4 Stability of Amorphous Solid Dispersions -- 2.4.5 Performance of ASDs -- References -- 3: Amorphous Solid Dispersion Screening -- 3.1 Introduction -- 3.2 Amorphous Dispersion Screening -- 3.2.1 API and Polymer Properties -- 3.2.2 Screening Considerations -- 3.2.3 Screening Methods -- 3.3 Amorphous Solid Dispersion Selection -- 3.3.1 Properties.

3.3.2 Selection Tools -- 3.4 Case Study -- 3.4.1 Miniaturized Studies -- 3.5 Conclusions -- References -- 4: Solid-State Characterization of Amorphous Dispersions -- 4.1 Introduction -- 4.2 Thermal Analysis Methods -- 4.3 Dielectric Relaxation Methods -- 4.4 Moisture Sorption Methods -- 4.5 Vibrational Spectroscopy and Microspectroscopy -- 4.6 Solid-State NMR Spectroscopy -- 4.7 Other Molecular Spectroscopic Methods -- 4.8 X-Ray Diffractometry -- 4.9 Microscopic and Surface Analysis Methods -- 4.10 Other Emerging Analytical Methods -- 4.11 Computational Models -- 4.12 Conclusions -- Acknowledgments -- References -- 5: Physical Stability and Crystallization Inhibition -- 5.1 Introduction -- 5.2 Theory of Crystallization in the Solid State -- 5.2.1 Nucleation Theory -- 5.2.2 Crystal Growth -- 5.2.3 Overall Kinetics of Crystallization -- 5.3 Factors Impacting the Crystallization Tendency of Active Pharmaceutical Compounds -- 5.3.1 Thermodynamic and Structural Considerations -- 5.3.2 Molecular Mobility -- 5.3.3 Impact of Preparation Method and Processing Steps -- 5.4 Role of Additives in Modifying Solid-State Crystallization -- 5.4.1 Miscibility -- 5.4.2 Impact of Polymers on Crystallization -- 5.5 Assessment of Physical Stability -- 5.5.1 Optical and Polarized Light Microscopy -- 5.5.2 X-Ray Diffraction -- 5.5.3 Solid-State Nuclear Magnetic Resonance Spectroscopy -- 5.5.4 Calorimetric Methods -- 5.5.5 Vibrational Spectroscopy -- 5.5.6 Second-Order Nonlinear Optical Imaging of Chiral Crystals -- 5.6 Crystallization in Aqueous Environments -- 5.6.1 Matrix Crystallization -- 5.6.2 Solution Crystallization -- 5.7 Summary and Outlook -- References -- 6: Solubility and Dissolution Considerations for Amorphous Solid Dispersions -- 6.1 Solubility and Dissolution: An Overview.

6.2 Differences Between Crystalline API, Amorphous Materials, and Amorphous Dispersions as it Pertains to Solubility and Dissolution -- 6.3 The Relationship of Polymer Properties with Solubility, Dissolution, and Supersaturation -- 6.3.1 The Impact of Polymer Properties on Dissolution, Solubility, and Supersaturation -- 6.4 Solubility and Dissolution Factors to Consider for Dispersions -- 6.4.1 Solubility -- 6.4.2 Dissolution -- 6.4.3 Characterization of Species Generated during Dissolution of Amorphous Solids and Their Impact on Performance -- 6.5 Solubility and Dissolution Measurements for Amorphous Dispersions: Summary, Conclusions, and Recommendations -- Acknowledgments -- References -- 7: Translational Development of Amorphous Dispersions -- 7.1 Introduction: Translational Drug Development -- 7.1.1 The Evolution of Early Development -- 7.1.2 How TDD Works -- 7.1.3 The Potency-Insolubility Conundrum and Telaprevir -- 7.2 Translational Development at the Discovery Stage -- 7.2.1 Absorption Modeling -- 7.2.2 Preparing and Characterizing an Amorphous Dispersion: Spray Drying and Glass Transition -- 7.2.3 Preparation and Characterization of SDD Suspension Formulations: Vehicle and Aqueous Stability -- 7.3 Translational Development After Discovery -- 7.3.1 Solid Form Development: Preparing Stable Dispersions -- 7.3.2 Manufacturability -- 7.3.3 Dosability -- 7.3.4 Storage Stability -- 7.4 Conclusions -- References -- 8: Preclinical and Clinical Studies -- 8.1 Introduction -- 8.2 In Vitro and Pharmaceutical Characterization -- 8.3 In Vivo Evaluation and Models -- 8.4 Clinical Assessments -- 8.5 Conclusions -- References -- 9: Spray Drying and Scale-Up -- 9.1 Introduction -- 9.2 Process Background and Physical Situation -- 9.3 Spray Drying Equipment -- 9.3.1 Spray Solution Preparation -- 9.3.2 Atomization -- 9.3.3 Drying -- 9.3.4 Product Collection.

9.3.5 Secondary Drying -- 9.4 Process Definition -- 9.4.1 Formulation Selection -- 9.4.2 Process Variables -- 9.5 Spray Drying Scale-Up -- 9.5.1 Scale-Up Considerations for Droplet Formation -- 9.5.2 Scale-Up Considerations for Droplet Drying Rate -- 9.5.3 Scale-Up Methodology -- 9.6 Conclusions -- References -- 10: Hot Melt Extrusion of Amorphous Solid Dispersions -- 10.1 Introduction -- 10.2 Materials Selection -- 10.2.1 Polymers -- 10.2.2 Plasticizers -- 10.2.3 Dissolution Adjuvants -- 10.2.4 Other Additives -- 10.2.5 General -- 10.3 Equipment Selection -- 10.3.1 Feeder -- 10.3.2 Extruder -- 10.3.3 Downstream Process -- 10.4 Process Design and Control -- 10.5 Amorphous Solid Dispersion Applications -- 10.5.1 HME Formulation Feasibility -- 10.5.2 HME Formulation Optimization -- 10.5.3 Maximizing Performance in the Finished Dosage Form -- 10.6 Summary -- References -- 11: Formulation Development of Amorphous Dispersions -- 11.1 Preparing Dispersions for Drug Products -- 11.1.1 Introduction -- 11.1.2 Creating an Amorphous Drug Substance -- 11.2 The Strategy of Quality by Design -- 11.3 Designing the Telaprevir Amorphous Dispersion Under QbD -- 11.3.1 Telaprevir and Its Process Development -- 11.3.2 Conceptual Approach to Telaprevir Process Design Space Development -- 11.3.3 Conceptual Approach to Defining Telaprevir Shelf Life -- 11.4 Concluding Remarks -- References -- 12: Scientific and Regulatory Considerations in Product Development -- 12.1 Introduction -- 12.2 Approval Process in the United States -- 12.3 The ICH -- 12.3.1 Module 1: Administrative Information and Prescribing Information -- 12.3.2 Module 2: Common Technical Document Summaries -- 12.3.3 Module 3: Quality -- 12.3.4 Module 4: Nonclinical Study Reports -- 12.3.5 Module 5: Clinical Study Reports -- 12.4 Quality-By-Design.

12.5 Development and Characterization of Amorphous Solid Dispersions -- 12.6 Conclusions -- References -- 13: Patenting Amorphous Solid Dispersions of Pharmaceuticals -- 13.1 Introduction -- 13.2 An Amorphous Solid Dispersion as a Patentable Invention -- 13.3 Considering Amorphous Solid Dispersions as Patentable Compositions of Matter -- 13.4 Claiming an Amorphous Solid Dispersion -- 13.4.1 Describing Amorphous Solid Dispersions in a Patent -- 13.5 Types of Patent Applications and Patent Examination -- 13.6 Conclusions -- References -- 14: Monographs on Polymers and Surfactants -- 14.1 Part I: Polymers -- 14.1.1 Notes -- 14.2 Part II. Surfactants -- 14.2.1 Notes -- References -- Appendix A -- Appendix B: Marketed Products -- Index -- End User License Agreement.

Providing a roadmap from early to late stages of drug development, this book overviews amorphous solid dispersion technology - a leading platform to deliver poorly water soluble drugs, a major hurdle in today's pharmaceutical industry.  Helps readers understand amorphous solid dispersions and apply techniques to particular pharmaceutical systems  Covers physical and chemical properties, screening, scale-up, formulation, drug product manufacture, intellectual property, and regulatory considerations  Has an appendix with structure and property information for polymers commonly used in drug development and with marketed drugs developed using the amorphous sold dispersion approach  Addresses global regulatory issues including USA regulations, ICH guidelines, and patent concerns around the world.

Description based on publisher supplied metadata and other sources.

Electronic reproduction. Ann Arbor, Michigan : ProQuest Ebook Central, 2019. Available via World Wide Web. Access may be limited to ProQuest Ebook Central affiliated libraries.

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