Water-Insoluble Drug Formulation

Properties and Formulation: From Theory to Real-World ApplicationScientists 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) LiuChapter 2 Solubility Theory Steven H. NeauChapter 3 Prediction of Solubility Yisheng Chen, Xiaohong Qi, and Rong (Ron) LiuChapter 4 Preformulation Aspects of Insoluble CompoundsWei-Qin (Tony) Tong and Hong WenChapter 5 Water-Insoluble Drugs and Their Pharmacokinetic BehaviorsHonghui Zhou and Hao ZhuChapter 6 Regulatory Aspects of Dissolution for Low Solubility Drug ProductsPradeep Sathe, Robert A. Lionberger, Sau Lawrence Lee, Lawrence X. Yu, and Di (Doris) ZhangChapter 7 Formulation Strategies and Practice Used for Drug Candidates with Water-Insoluble Properties for Toxicology, Biology, and Pharmacology Studies in Discovery SupportLian-Feng Huang, Jinquan Dong, and Shyam B. KarkiChapter 8 Application of Complexation in Drug Development for Insoluble CompoundsWei-Qin (Tony) Tong and Hong WenChapter 9 Solubilization Using Cosolvent ApproachJay S. Trivedi and Zhanguo YueChapter 10 Emulsions, Microemulsions, and Lipid-Based Drug Delivery Systems for Drug Solubilization and Delivery·Part I: Parenteral ApplicationsJohn B. Cannon, Yi Shi, and Pramod GuptaChapter 11 Emulsions, Microemulsions, and Lipid-Based Drug Delivery Systems for Drug Solubilization and Delivery·Part II: Oral ApplicationsJohn B. Cannon and Michelle A. LongChapter 12 Micellization and Drug Solubility EnhancementRong (Ron) Liu, Rose-Marie Dannenfelser, Shoufeng Li, and Zhanguo YueChapter 13 Polymeric Micelles in Water-Insoluble Drug DeliveryRong (Ron) Liu, M. Laird Forrest, Glen S. Kwon, Xiaobing Xiong, and Zhihong (John) ZhangChapter 14 Liposomes in SolubilizationRong (Ron) Liu, John B. Cannon, and Sophia Y.L. PaspalChapter 15 Pharmaceutical SaltsSteven H. Neau and Nikhil C. LokaChapter 16 Prodrugs for Improved Solubility in WaterSteven H. Neau, Nikhil C. Loka, and Kalyan K. SaripellaChapter 17 Particle Size ReductionXiang (Lisa) Li, Zhanguo Yue, Robert W. Lee, James McShane, J. Michael Shaw, Ray W. Wood, and Dinesh B. ShenoyChapter 18 Development of Solid Dispersion for Poorly Water-Soluble DrugsMadhav Vasanthavada, Simerdeep Singh Gupta, Wei-Qin (Tony) Tong, and Abu T.M. SerajuddinChapter 19 Alteration of the Solid State of the Drug Substances: Polymorphs, Solvates, and Amorphous FormsPaul B. Myrdal, Stephen J. Franklin, and Michael J. JozwiakowskiChapter 20 Pharmaceutical Powder Technology·ICH Q8 and Building the Pyramid of Knowledge Hans Leuenberger, Silvia Kocova El-Arini, and Gabriele BetzChapter 21 Soft Gelatin Capsules DevelopmentS. Esmail Tabibi, Liangran Guo, and Shanker L. GuptaChapter 22 Oral Modified-Release Drug Delivery for Water-Insoluble DrugsShaoling Li, Nuo (Nolan) Wang, Rong (Ron) Liu, Zhanguo Yue, and Zhihong (John) ZhangChapter 23 Scalable Manufacturing of Water-Insoluble Drug ProductsNitin P. Pathak, Richard (Ruey-ching) Hwang, and Xiaohong QiIndex

Ron Liu is CEO of AustarPharma, a pharmaceutical company based in Edison, New Jersey.