Formulating Poorly Water Soluble Drugs

ISBN-13: 9783030887216 / Angielski / Miękka / 2023

Opis

The objective of this third edition 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 a minimum a working knowledge of each of the above mentioned 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.

Spis treści

Contents

1.      Route-Specific Challenges in the Delivery of Poorly Water-Soluble Drugs ……………….. Zachary Warnken, Hugh D.C. Smyth, and Robert O. Williams III

2.      Optimizing the Formulation of Poorly Water-Soluble Drugs………………………….. Xiangyu Ma, Daniel Ellenberger, Kevin P. O’Donnell, and Robert O. Williams III

3.      Solid-State Techniques for Improving Solubility ……………………………………….. Miguel O. Jara,  Justin R. Hughey, Siyuan Huang, and Robert O. Williams III

4.      Mechanical Particle-Size Reduction Techniques…………………………..……….…… Javier O. Morales, Alan B. Watts, and Jason T. McConville

5.      Co-solvent and Complexation Systems …………………………………………….... Junhuang Jiang and Robert O. Williams III

6.      Injectable Formulations of Poorly Water-Soluble Drugs ………………………….…... Hannah L. O’Mary and Zhengrong Cui,

7.      Lipid-Based Formulations…………………………………………………................... Daniel A. Davis Jr., Han-Hsuan Peng, and Robert O. Williams III

8.      Structured Development Approach for Amorphous Systems ……………………….... Susanne Page, Reto Maurer, Nicole Wyttenbach, and Felix Ditzinger

9.      Melt Extrusion………………………………………………………………………. Stephen A. Thompson, Daniel A. Davis Jr., James C. DiNunzio, Charlie Martin,
Robert O. Williams III, and Feng Zhang

10.  Spray-Drying Technology…………..………..………..………..……………………….. Dave A. Miller, Daniel Ellenberger, Tiago Porfirio, and Marco Gil

11.  Pharmaceutical Cryogenic Technologies ………………………………………….... Sawittree Sahakijpijarn, Chaeho Moon, and Robert O. Williams III

12.  Precipitation Technologies for Nanoparticle Production ……………………………. Tuangrat Praphawatvet and Robert O. Williams III

13.  Emerging Technologies to Increase the Bioavailability of Poorly Water-Soluble Drugs …
Daniel A. Davis Jr., Rishi Thakkar, Mohammed Maniruzzaman, Dave A. Miller, Robert O. Williams III

14.  Scientific and Regulatory Considerations for Development and Commercialization of Poorly Water-Soluble Drugs…………………………………………………………………. .Zedong Dong and Hasmukh Patel

O autorze

Robert O. (Bill) Williams is the Johnson & Johnson Centennial Chair and Professor of Pharmaceutics and the Division Head of Molecular Pharmaceutics and Drug Delivery 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 in 1995.  Dr Williams was elected Fellow of the American Association of Pharmaceutical Scientists in 2006,  Fellow of the American Institute of Medical and Biological Engineering in 2008 and Fellow of the National Academy of Inventors in 2019.  He was named the Inventor of the Year by the University of Texas at Austin in 2017.  Dr. Williams is a member of the American Association of Pharmaceutical Scientists (AAPS), as well as other professional societies including the American Association of Colleges of Pharmacy.  He is the co-founder of several pharmaceutical companies.  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 500 peer-reviewed research articles, reviews, abstracts and book chapters, and co-edited two books in the fields of pharmaceutical technology and drug delivery, including Formulating Poorly Water Soluble Drugs, Second Edition (aapspress and Springer). He is an inventor on over 45 patents and patent applications.  Dr. Williams served as Editor-in-Chief of the research journal Drug Development and Industrial Pharmacy from 2000 to 2014 and is the Editor-in-Chief of AAPS PharmSciTech since 2014.  He is on the Editorial Advisory Board of Journal of Drug Delivery Science and Technology and International Journal of Pharmaceutics and he serves as a reviewer for numerous other journals.

Daniel Alan Davis, Jr., Ph.D., Pharm.D.

Daniel Davis received his BS in Chemistry from the University of Texas at Austin in 2015 and PharmD from the University of Texas at Austin College of Pharmacy (UTCOP) in 2019, where he graduated with research honors and academic honors. His research contributions resulted in him receiving the prestigious College of Pharmacy’s Outstanding Research Award. Daniel completed his Ph.D. in 2021 as part of the PharmD/PhD Honor’s program in the Division of Molecular Pharmaceutics and Drug Delivery, and currently works as an associate principal scientist at DisperSol Technologies, LLC. Daniel has Authored six peer-reviewed publications, co-authored three peer-reviewed publications and eight published abstracts at international pharmaceutical conferences in the area of drug solubilization and amorphous solid dispersions, and he is an inventor on eight patents and patent applications. His research is focused on increasing the solubility of poorly water soluble drugs, specifically focused on innovation formulation designs for increased solubility. Much of this work uses KinetiSol processing, hot melt extrusion and selective laser sintering three-dimensional printing. Daniel received the B. Berard Matthews Endowed Scholarship, the Van Smith Endowed Presidential Scholarship, and the Undergraduate Research Fellowship from the University of Texas at Austin based on his research. Daniel serves as the social media editor for AAPS PharmSciTech and a peer reviewer for the International Journal of Pharmaceutics.

Dave A. Miller, Ph.D. is the Chief Scientific Officer at DisperSol Technologies. Prior to his current position, Dr. Miller served as Vice President of Research and Development at DisperSol Technologies for ten years. Before joining DisperSol, he was a Senior Principal Scientist at Hoffmann-La Roche. Dr. Miller specializes in formulation and processing technologies for improving oral bioavailability of insoluble small molecules. He has applied his expertise toward advancing numerous drug candidates through all stages of development from early discovery to line extension. Dr. Miller was an original inventor of the pharmaceutical applications of the KinetiSol technology and continues to be a primary innovative driver for application and expansion of the platform. He has published 45 research articles in peer-reviewed journals and authored 8 book chapters, and is co-editor of the First, Second, and Third Editions of the textbook, Formulating Poorly Water-Soluble Drugs. He is a co-inventor on numerous granted and pending patents world-wide. Dr. Miller holds a B.S. in Chemical Engineering and a Ph.D. in Pharmaceutics from the University of Texas at Austin.

Blurb

The objective of this third edition 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 a minimum a working knowledge of each of the above mentioned 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.

Highlights the most recent advancements reported in the literature on technologies to improve the dissolution and bioavailability of poorly water soluble drugs

Provides a comprehensive discussion of new technologies developed and recently over 40% updated new content

Essential read for scientists and researchers in pharmaceutical, chemical, and agricultural industries since over 80% of newly discovered drugs are poorly water soluble.