Water-Insoluble Drug Formulation

Front Cover
Ron Liu
CRC Press, Sep 30, 2000 - Medical - 672 pages
Delivering drugs in a water-insoluble formulation is a critical matter in therapeutic drug development. However, because a drug molecule has to be water soluble to be readily delivered to the cellular membrane while retaining its hydrophobic properties, issues surrounding water insolubility can postpone - or completely derail - important new drug development. Even much needed reformulation of currently marketed products can be significantly affected by these issues.

This book systematically describes the techniques used for water-insoluble formulations, providing step-by-step guidance as well as scientific background on drug and water properties and how they contribute to solubilization and dissolution. A world-class team of experts discusses how these issues are viewed - and solved - by key industry and R&D institutions.

This book provides 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.
 

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Contents

Introduction
1
Nonideal Solutions
11
Advantages and Disadvantages
20
Prediction of Solubility
25
Quantitative StructureSolubility Relationships
34
Group Contribution Method
54
References
60
iii
61
References
268
Classification of Copolymers
279
Factors Affecting Micellization and Solubilization
289
Biopharmaceutic Aspects 3 11
311
Pharmaceutical Applications
327
Acknowledgment
341
Liposomes In Solubilization
355
Types and Structures of Liposomes
365

Analytical Methods Development and Validation
66
Dissolution
77
Partition CoefficientDistribution Coefficient
84
Product Specific Aspects
90
Biopharmaceutical Aspects of WaterInsoluble
97
Applications of Complexation in the Formulation
111
Methods for Studying Complexation
117
Complexation by Cyclodextrins
126
Summary
135
Solubilization Using CoSolvent Approach
141
Stability Considerations
150
Commonly Used Cosolvents
158
Additional Literature
167
Emulsions and Microemulsions for Drug Solubilization
169
Drug Solubilization and Delivery Using Emulsions
178
Challenges with Emulsion Formulations for Drug Solubilization
194
Future Perspectives
203
Micellization and Drug Solubility Enhancement
213
Micellar Solubilization
231
Mixed Micelles
247
Other Micelles
260
Mechanisms and Strategies for Solubilization of Lipid Soluble
383
Pharmaceutical Applications
390
References
397
Pharmaceutical Salts
405
Prodrugs for Improved Aqueous Solubility
427
Particle Size Reduction
455
Particle Size Reduction Methods
473
Pharmaceutical Applications of SizeReduction Technology
480
References
488
Background
494
Mechanism of Dissolution Enhancement
500
Special Considerations for Polymorphs
546
The Utility of Amorphous Noncrystalline Forms
555
Strategy for WaterInsoluble Drug Formulation Using Metastable
561
Solubilization SystemsThe Impact of Percolation Theory
569
References
589
Applications
596
Soft Gelatin Capsules Development
609
Formulation Considerations
615
Control and Testing
630
Copyright

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