Properties and Formulation: From Theory to Real-World Application
Scientists have attributed more than 40 percent of the failures in new drug development to poor biopharmaceutical properties, particularly water insolubility. Issues surrounding water insolubility can postpone or completely derail important new drug development. Even the much-needed reformulation of currently marketed products can be significantly affected by these challenges. More recently it was reported that the percentage increased to 90% for the candidates of new chemical entities in the discovery stage and 75% for compounds under development.
In the most comprehensive resource on the topic, this third edition of Water-Insoluble Drug Formulation brings together a distinguished team of experts to provide the scientific background and step-by-step guidance needed to deal with solubility issues in drug development. Twenty-three chapters systematically describe the detailed discussion on solubility theories, solubility prediction models, the aspects of preformulation, biopharmaceutics, pharmacokinetics, regulatory, and discovery support of water-insoluble drugs to various techniques used in developing delivery systems for water-insoluble drugs. This book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies and featuring oral and parenteral applications. Highlighting the most current information and data available, this seminal volume reflects the significant progress that has been made in nearly all aspects of this field.
The aim of this book is to provide a handy reference for pharmaceutical scientists in the handling of formulation issues related to water-insoluble drugs. In addition, this book may be useful to pharmacy and chemistry undergraduate students and pharmaceutical and biopharmaceutical graduate students to enhance their knowledge in the techniques of drug solubilization and dissolution enhancement.
Chapter 1 Introduction
Rong (Ron) Liu
Chapter 2 Solubility Theory
Steven H. Neau
Chapter 3 Prediction of Solubility
Yisheng Chen, Xiaohong Qi, and Rong (Ron) Liu
Chapter 4 Preformulation Aspects of Insoluble Compounds
Wei-Qin (Tony) Tong and Hong Wen
Chapter 5 Water-Insoluble Drugs and Their Pharmacokinetic Behaviors
Honghui Zhou and Hao Zhu
Chapter 6 Regulatory Aspects of Dissolution for Low Solubility Drug Products
Pradeep Sathe, Robert A. Lionberger, Sau Lawrence Lee, Lawrence X. Yu, and Di (Doris) Zhang
Chapter 7 Formulation Strategies and Practice Used for Drug Candidates with Water-Insoluble Properties for Toxicology, Biology, and Pharmacology Studies in Discovery Support
Lian-Feng Huang, Jinquan Dong, and Shyam B. Karki
Chapter 8 Application of Complexation in Drug Development for Insoluble Compounds
Wei-Qin (Tony) Tong and Hong Wen
Chapter 9 Solubilization Using Cosolvent Approach
Jay S. Trivedi and Zhanguo Yue
Chapter 10 Emulsions, Microemulsions, and Lipid-Based Drug Delivery Systems for Drug Solubilization and Delivery·Part I: Parenteral Applications
John B. Cannon, Yi Shi, and Pramod Gupta
Chapter 11 Emulsions, Microemulsions, and Lipid-Based Drug Delivery Systems for Drug Solubilization and Delivery·Part II: Oral Applications
John B. Cannon and Michelle A. Long
Chapter 12 Micellization and Drug Solubility Enhancement
Rong (Ron) Liu, Rose-Marie Dannenfelser, Shoufeng Li, and Zhanguo Yue
Chapter 13 Polymeric Micelles in Water-Insoluble Drug Delivery
Rong (Ron) Liu, M. Laird Forrest, Glen S. Kwon, Xiaobing Xiong, and Zhihong (John) Zhang
Chapter 14 Liposomes in Solubilization
Rong (Ron) Liu, John B. Cannon, and Sophia Y.L. Paspal
Chapter 15 Pharmaceutical Salts
Steven H. Neau and Nikhil C. Loka
Chapter 16 Prodrugs for Improved Solubility in Water
Steven H. Neau, Nikhil C. Loka, and Kalyan K. Saripella
Chapter 17 Particle Size Reduction
Xiang (Lisa) Li, Zhanguo Yue, Robert W. Lee, James McShane, J. Michael Shaw, Ray W. Wood, and Dinesh B. Shenoy
Chapter 18 Development of Solid Dispersion for Poorly Water-Soluble Drugs
Madhav Vasanthavada, Simerdeep Singh Gupta, Wei-Qin (Tony) Tong, and Abu T.M. Serajuddin
Chapter 19 Alteration of the Solid State of the Drug Substances: Polymorphs, Solvates, and Amorphous Forms
Paul B. Myrdal, Stephen J. Franklin, and Michael J. Jozwiakowski
Chapter 20 Pharmaceutical Powder Technology·ICH Q8 and Building the Pyramid of Knowledge
Hans Leuenberger, Silvia Kocova El-Arini, and Gabriele Betz
Chapter 21 Soft Gelatin Capsules Development
S. Esmail Tabibi, Liangran Guo, and Shanker L. Gupta
Chapter 22 Oral Modified-Release Drug Delivery for Water-Insoluble Drugs
Shaoling Li, Nuo (Nolan) Wang, Rong (Ron) Liu, Zhanguo Yue, and Zhihong (John) Zhang
Chapter 23 Scalable Manufacturing of Water-Insoluble Drug Products
Nitin P. Pathak, Richard (Ruey-ching) Hwang, and Xiaohong Qi
Index
Biography
Ron Liu is CEO of AustarPharma, a pharmaceutical company based in Edison, New Jersey.
