Pharmaceutical Amorphous Solid Dispersions

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 Contents

Contributors

Preface

Chapter 1: Introduction to Amorphous Solid Dispersions
George Zografi and Ann Newman

Chapter 2: Polymers and Surfactants
Padma Narayan, William W. Porter III, Meinolf Brackhagen, and Christopher Tucker

Chapter 3: Amorphous Solid Dispersion Screening
Ann Newman

Chapter 4: Solid state Characterization of Amorphous Dispersions
Frederick G. Vogt

Chapter 5: Physical Stability and Crystallization Inhibition
Lynne S. Taylor

Chapter 6: Solubility and Dissolution Considerations for Amorphous Solid Dispersions
Grace A. Ilevbare, Wei Xu, Christopher T. John, James Ormes, Jesse Kuiper, Allen C. Templeton, and Annette Bak

Chapter 7: Translational Development of Amorphous Dispersions
Patrick Connelly, Brian Patrick Quinn, Steve Johnston, Philip Bransford, Praveen Mudunuri, Andrey Peresypkin, Majed Fawaz, Setu Roday, Anuj Kuldipkumar, Hong-Ren Wang, Phillip Snyder, Jeff Katstra, Tapan Sanghvi, Bill Rowe, and Patricia Hurter

Chapter 8: Preclinical and Clinical Studies
Marcus E. Brewster, Geert Verreck, Jan Bevernage, Joachim Brouwers, Guy Van den Mooter, and Patrick Augustijns

Chapter 9: Spray-Drying and Scale-Up
Daniel E. Dobry, Dana M. Settell, and John M. Baumann

Chapter 10: Hot Melt Extrusion of Amorphous Solid Dispersions
Kieran Crowley and Andreas Gryczke

Chapter 11: Formulation Development of Amorphous Dispersions
Tapan Sanghvi, Jeff Katstra, Brian Patrick Quinn, Hayden Thomas, and Patricia Hurter

Chapter 12: Scientific and Regulatory Considerations in Product Development
Abhay Gupta, Ziyaur Rahmna, and Manssor A. Khan

Chapter 13: Chapter Patenting Amorphous Solid Dispersions of Pharmaceuticals
Jeffry A. Lindeman

Chapter 14: Monographs on Polymers and Surfactants
Xia Lu, Robert Wenslow, and Ann Newman

Appendix 1
Xia Lu, Robert Wenslow, and Ann Newman

Appendix 2: Marketed Products
Ann Newman Ann Newman is a pharmaceutical consultant with Seventh Street Development Group, where she provides consulting, training, and webcast services on solid-state pharmaceutics and pharmaceutical development. She is also an Adjunct Professor and Lecturer in the Department of Industrial and Physical Pharmacy at Purdue University. A senior pharmaceutical scientist with demonstrated scientific and leadership expertise in the pharmaceutical industry, Dr. Newman has over 25 years of large pharma and contract research experience.

A roadmap to enhance and maximize drug solubility and bioavailability

With an increasing number of poorly soluble or difficult to crystallize drugs entering development, new formulation strategies are required to achieve sufficient bioavailability. Amorphous solid dispersions are an option receiving increased attention in recent years, because they can improve dissolution rates and increase solubility characteristics of drug compounds.

This book highlights and discusses the advances in developing pharmaceutical amorphous solid dispersions. Chapters, written by contributing authors on the frontlines of R & D, provide a roadmap from early to late stages of drug development. They cover topics that include: physical and chemical properties, screening, scale-up, formulation, drug product manufacture, intellectual property, and regulatory considerations.

Pharmaceutical scientists using this book as a guide for formulating their drugs benefit from a number of features, including:

• A comprehensive overview of the amorphous solid dispersion technology, which is a leading technology platform to deliver poorly water soluble drugs – a major hurdle in today’s pharmaceutical industry

• How to apply amorphous solid dispersions techniques to particular pharmaceutical systems

• 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

• Global regulatory issues including USA regulations, ICH guidelines, and patent concerns around the world