Handbook of Preformulation: Chemical, Biological, and Botanical Drugs

by Niazi; Sarfaraz K.

• ISBN13: 9780849371936
• ISBN10: 0849371937
• Edition: 1st
• Format: Hardcover
• Copyright: 2006-09-18
• Publisher: CRC Press

Summary

Preformulation studies are the physical, chemical, and biological studies needed to characterize a drug substance for enabling the proper design of a drug product, whereas the effectiveness of a drug product is determined during the formulation studies phase. Though the two disciplines overlap in practice, each is a significantly distinct phase of new drug development. Entirely focused on preformulation principles, this handbook provides detailed descriptions of preformulation methodologies, gives a state-of-the-art description of each technique, and lists the currently available tools useful in providing a comprehensive characterization of a new drug entity.

Author Biography

Sarfaraz K. Niazi is the Chief Executive Officer of Pharmaceutical Scientist, Inc., Deerfield, Illinois

Table of Contents

Preface	v
List of Appendices, Figures, Schemes, and Tables	xiii
1. Drug Discovery Trends	1	(32)
Introduction	1	(1)
Development Phases	2	(4)
Product Life Cycle	6	(5)
New Pathways to Discovery	11	(12)
References	23	(1)
Bibliography	23	(10)
2. Intellectual Property Considerations	33	(24)
Introduction	33	(1)
Patenting Strategies	33	(2)
Patenting Systems	35	(1)
What Is a Patent?	35	(1)
Patent Myths	36	(2)
What Is Not Patentable?	38	(1)
Patent Search	38	(6)
Components of a Patent Application	44	(5)
Understanding Claims	49	(6)
Food and Drug Administration	55	(1)
References	56	(1)
Bibliography	56	(1)
3. The Scope of Preformulation Studies	57	(30)
Introduction	57	(1)
Preformulation Testing Criteria	57	(1)
Regulatory Requirements	58	(7)
Testing Systems	65	(4)
Solid-State Characterization	69	(8)
Transport Across Biological Membranes	77	(2)
References	79	(1)
Bibliography	79	(8)
4. Dissociation, Partitioning, and Solubility	87	(54)
Introduction	87	(1)
The Ionization Principle	87	(11)
Quantitative Structure–Activity Relationships	98	(7)
Partitioning	105	(8)
Measurement Strategies	113	(9)
References	122	(1)
Bibliography	122	(9)
Appendix 1	131	(10)
5. Release, Dissolution, and Permeation	141	(56)
Introduction	141	(1)
Release	141	(6)
Assay Systems	147	(9)
The Biopharmaceutics Drug Classification Systems	156	(3)
References	159	(1)
Bibliography	159	(9)
Appendix	168	(29)
6. Solid-State Properties	197	(44)
Introduction	197	(1)
Crystal Morphology	197	(6)
Polymorphism	203	(4)
High-Throughput Crystal Screening	207	(3)
Solvates	210	(1)
Hydrates	210	(2)
Amorphous Forms	212	(1)
Hygroscopicity	212	(1)
Solubility	213	(5)
Study Methods	218	(13)
References	231	(1)
Bibliography	231	(10)
7. Dosage Form Considerations in Preformulation	241	(46)
Introduction	241	(1)
Solid Dosage Form Considerations	241	(21)
Solution Formulations	262	(1)
Emulsion Formulations	263	(8)
Freeze-Dried Formulations	271	(1)
Suspensions	272	(1)
Topical	273	(1)
Pulmonary Delivery	274	(1)
General Compatibility	275	(1)
References	275	(1)
Bibliography	276	(11)
8. Chemical Drug Substance Characterization	287	(42)
Introduction	287	(1)
Scheme of Characterization	288	(29)
Impurities	317	(5)
Good Manufacturing Practice	322	(4)
References	326	(1)
Bibliography	326	(3)
9. Characterization of Biopharmaceutical Drugs	329	(62)
Introduction	329	(4)
Preformulation Studies	333	(15)
Packaging and Materials	348	(37)
Physio-Chemical Characterization Tests	385	(2)
Design of Preformulation Studies	387	(1)
References	388	(1)
Bibliography	388	(3)
10. Characterization of Phytomedicines	391	(28)
Introduction	391	(1)
Regulatory Status	392	(1)
Characteristics of Phytomedicines	392	(7)
Efficacy and Safety	399	(1)
Regulatory Filing Procedure	400	(3)
Starting Material	403	(3)
Stability Testing	406	(4)
Bibliography	410	(9)
Glossary of Terms	419	(12)
Index	431