ABSTRACT

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|5 pages

Introduction

ByRong (Ron) Liu

chapter 2|20 pages

Solubility Theory

BySteven H. Neau

chapter 3|37 pages

Prediction of Solubility

ByYisheng Chen, Xiaohong Qi, Rong (Ron) Liu

chapter 4|31 pages

Preformulation Aspects of Insoluble Compounds

ByWei-Qin (Tony) Tong, Hong Wen

chapter 5|15 pages

Water-Insoluble Drugs and Their Pharmacokinetic Behaviors

ByHonghui Zhou, Hao Zhu

chapter 6|12 pages

Regulatory Aspects of Dissolution for Low Solubility Drug Products

ByPradeep Sathe, Robert A. Lionberger, Sau Lawrence Lee, Lawrence X. Yu, Di (Doris) Zhang

chapter 8|27 pages

Application of Complexation in Drug Development for Insoluble Compounds

ByWei-Qin (Tony) Tong, Hong Wen

chapter 9|33 pages

Solubilization Using Cosolvent Approach

ByJay S. Trivedi, Zhanguo Yue

chapter 12|52 pages

Micellization and Drug Solubility Enhancement

ByRong (Ron) Liu, Rose-Marie Dannenfelser, Shoufeng Li, Zhanguo Yue

chapter 13|69 pages

Polymeric Micelles in Water-Insoluble Drug Delivery

ByRong (Ron) Liu, M. Laird Forrest, Glen S. Kwon, Xiaobing Xiong, Zhihong (John) Zhang

chapter 14|45 pages

Liposomes in Solubilization

ByRong (Ron) Liu, John B. Cannon, Sophia Y. L. Paspal

chapter 15|23 pages

Pharmaceutical Salts

BySteven H. Neau, Nikhil C. Loka

chapter 16|34 pages

Prodrugs for Improved Solubility in Water

BySteven H. Neau, Nikhil C. Loka, Kalyan K. Saripella

chapter 17|32 pages

Particle Size Reduction

ByRobert W. Lee, James McShane, J. Michael Shaw, Ray W. Wood, Dinesh B. Shenoy, Xiang (Lisa) Li, Zhanguo Yue

chapter 18|33 pages

Development of Solid Dispersion for Poorly Water-Soluble Drugs

ByMadhav Vasanthavada, Simerdeep Singh Gupta, Wei-Qin (Tony) Tong, Abu T. M. Serajuddin

chapter 19|38 pages

Alteration of the Solid State of the Drug Substances

Polymorphs, Solvates, and Amorphous Forms
ByPaul B. Myrdal, Stephen J. Franklin, Michael J. Jozwiakowski

chapter 20|32 pages

Pharmaceutical Powder Technology—ICH Q8 and Building the Pyramid of Knowledge

ByHans Leuenberger, Silvia Kocova El-Arini, Gabriele Betz

chapter 21|19 pages

Soft Gelatin Capsules Development

ByS. Esmail Tabibi, Shanker L. Gupta, Liangran Guo

chapter 22|32 pages

Oral Modified-Release Drug Delivery for Water-Insoluble Drugs

ByShaoling Li, Nuo (Nolan) Wang, Rong (Ron) Liu, Zhanguo Yue, Zhihong (John) Zhang, Wei (William) Li

chapter 23|26 pages

Scalable Manufacturing of Water-Insoluble Drug Products

ByNitin P. Pathak, Richard (Ruey-ching) Hwang, Xiaohong Qi