3rd Edition

Water-Insoluble Drug Formulation

Edited By Ron Liu Copyright 2018
    756 Pages 212 B/W Illustrations
    by CRC Press

    756 Pages 212 B/W Illustrations
    by CRC Press

    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



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