Formulating Poorly Water Soluble Drugs

1. Front Matter

   Pages i-xiv

   PDF

2. Route-Specific Challenges in the Delivery of Poorly Water-Soluble Drugs

   • Zachary Warnken, Hugh D. C. Smyth, Robert O. Williams III

   Pages 1-39

3. Optimizing the Formulation of Poorly Water-Soluble Drugs

   • Daniel Ellenberger, Kevin P. O’Donnell, Robert O. Williams III

   Pages 41-120

4. Solid-State Techniques for Improving Solubility

   • Justin R. Hughey, Siyuan Huang, Robert O. Williams III

   Pages 121-163

5. Mechanical Particle-Size Reduction Techniques

   • Javier O. Morales, Alan B. Watts, Jason T. McConville

   Pages 165-213

6. Co-solvent and Complexation Systems

   • Soraya Hengsawas Surasarang, Robert O. Williams III

   Pages 215-256

7. Injectable Formulations of Poorly Water-Soluble Drugs

   • Youssef W. Naguib, Hannah L. O’Mary, Zhengrong Cui, Alan B. Watts

   Pages 257-293

8. Lipid-Based Formulations

   • Justin LaFountaine, Ping Gao, Robert O. Williams III

   Pages 295-327

9. Structured Development Approach for Amorphous Systems

   • Susanne Page, Reto Maurer, Nicole Wyttenbach

   Pages 329-382

10. Melt Extrusion

    • Abbe Haser, James C. DiNunzio, Charlie Martin, James W. McGinity, Feng Zhang

    Pages 383-435

11. Spray-Drying Technology

    • Dave A. Miller, Daniel Ellenberger, Marco Gil

    Pages 437-525

12. Pharmaceutical Cryogenic Technologies

    • Soraya Hengsawas Surasarang, Robert O. Williams III

    Pages 527-607

13. Precipitation Technologies for Nanoparticle Production

    • Julien Maincent, Robert O. Williams III

    Pages 609-689

14. Emerging Technologies to Increase the Bioavailability of Poorly Water-Soluble Drugs

    • Leena Kumari Prasad, Justin R. Hughey, James W. McGinity, Dave A. Miller, Robert O. Williams III

    Pages 691-740

15. Scientific and Regulatory Considerations for Development and Commercialization of Poorly Water-Soluble Drugs

    • Zedong Dong, Hasmukh Patel

    Pages 741-767

16. Back Matter

    Pages 769-779

    PDF

The objective of this volume is to consolidate within a single text the most current knowledge, practical methods, and regulatory considerations pertaining to formulations development with poorly water-soluble molecules. A pharmaceutical scientist’s approach toward solubility enhancement of a poorly water-soluble molecule typically includes detailed characterization of the compound’s physiochemical properties, solid-state modifications, advanced formulation design, non-conventional process technologies, advanced analytical characterization, and specialized product performance analysis techniques. The scientist must also be aware of the unique regulatory considerations pertaining to the non-conventional approaches often utilized for poorly water-soluble drugs. One faced with the challenge of developing a drug product from a poorly soluble compound must possess at minimum a working knowledge of each of the abovementioned facets and detailed knowledge of most. In light of the magnitude of the growing solubility problem to drug development, this is a significant burden especially when considering that knowledge in most of these areas is relatively new and continues to develop

• bioavailability
• lipophilic
• solubility
• dissolution
• formulation development
• nanoparticle processes
• amorphous systems
• drug delivery
• route-specific challenges

• Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, Austin, USA

  Robert O. Williams III, Alan B. Watts

• DisperSol Technologies, LLC, Georgetown, USA

  Dave A. Miller

Robert O. (Bill) Williams III, Ph.D. is the Johnson & Johnson Centennial Professor of Pharmaceutics at the College of Pharmacy, University of Texas at Austin. He earned a B.S. in Biology from Texas A&M University, a B.S. in Pharmacy from the University of Texas at Austin and Doctor of Philosophy in Pharmaceutics in 1986 from the University of Texas at Austin. Dr. Williams worked 9 years in the pharmaceutical industry in the United States and France before returning to the University of Texas at Austin. Dr Williams was elected a Fellow of the American Association of Pharmaceutical Scientists in 2006 and a Fellow of the American Institute of Medical and Biological Engineering in 2008. Dr. Williams is a member of numerous professional organizations, including American Association of Colleges of Pharmacy, and American Association of Pharmaceutical Scientists. Dr. Williams’ research interests include development of novel drug delivery systems for oral, pulmonary, nasal, injectable, buccal and topical applications, development of novel particle engineering technologies for low molecular weight drugs, peptides and proteins, and analytical technologies to characterize actives, excipients and polymers. He has published over 300 articles, abstracts and book chapters in the fields of pharmaceutical technology and drug delivery. In addition, Dr. Williams has co-edited one book. He is an inventor on numerous patents and patent applications. Dr. Williams is the Editor-in-Chief of the research journal AAPS PharmSciTech, and serves as a reviewer for International Journal of Pharmaceutics, Pharmaceutical Research, European Journal of Pharmaceutics and Biopharmaceutics, S.T.P. Pharma Sciences, Journal of Pharmaceutical Sciences, Pharmaceutical Development and Technology, Journal of Membrane Science, and Journal of Controlled Release.

Policies and ethics