Developing Solid Oral Dosage Forms. Pharmaceutical Theory and Practice. Edition No. 2

Table of Contents

Part I: Theories and Techniques in the Characterization of Drug Substances and Excipients 1. Solubility of Pharmaceutical Solids 2. Crystalline and Amorphous Solids 3. Solid-State Characterization and Techniques 4. API Solid-Form Screening and Selection 5. Drug Stability and Degradation Studies 6. Excipient Compatibility and Functionality 7. Polymer Properties and Characterization 8. Interfacial Phenomena 9. Fundamental of Diffusion and Dissolution 10. Particle, Powder, and Compact Characterization

Part II: Biopharmaceutical and Pharmacokinetic Evaluations of Drug Molecules and Dosage Forms 11. Oral Absorption Basics: Pathways and Physicochemical and Biological Factors Affecting Absorption 12. Oral Drug Absorption: Evaluation and Prediction 13. Dissolution Testing of Solid Products 14. Bioavailability and Bioequivalence 15. Predictive Biopharmaceutics and Pharmacokinetics: Modeling and Simulation 16. In Vitro/In Vivo Correlations: Fundamentals, Development Considerations, and Applications

Part III: Design, Development and Scale-Up of Formulation and Manufacturing Process 17. Oral Formulations for Preclinical Studies: Principle, Design, and Development Considerations 18. Rational Design for Amorphous Solid Dispersions 19. Rational Design of Oral Modified-Release Drug Delivery Systems 20. Product and Process Development of Solid Oral Dosage Forms 21. Analytical Development and Validation for Solid Oral Dosage Forms 22. Statistical Design and Analysis of Long-Term Stability Studies for Drug Products 23. Packaging Selection for Solid Oral Dosage Forms 24. Clinical Supplies Manufacture: Strategy, GMP Considerations, and Cleaning Validation 25. Specification Setting and Manufacturing Process Control for Solid Oral Drug Products 26. Process Development, Optimization, and Scale-Up: Providing Reliable Powder Flow and Product Uniformity 27. Capsules Dosage Form: Formulation and Manufacturing Considerations 28. Design, Development, and Scale-Up of the High-Shear Wet Granulation Process 29. Process Development, Optimization, and Scale-Up: Fluid-Bed Granulation 30. Formulation, Process Development, and Scale-Up: Spray-Drying Amorphous Solid Dispersions for Insoluble Drugs 31. Process Development and Scale-Up: Twin-Screw Extrusion 32. Development, Scale-Up, and Optimization of Process Parameters: Roller Compaction Theory and Practice 33. Development, Optimization, and Scale-Up of Process Parameters: Tablet Compression 34. Development, Optimization, and Scale-Up of Process Parameters: Pan Coating 35. Development, Optimization, and Scale-Up of Process Parameters: Wurster Coating 36. Commercial Manufacturing and Product Quality 37. Emerging Technology for Modernizing Pharmaceutical Production: Continuous Manufacturing

Part IV: Regulatory Aspects of Product Development 38. Drug Product Approval in the United States and International Harmonization 39. Modern Pharmaceutical Regulations: Quality Assessment for Drug Substances 40. Modern Pharmaceutical Regulations: Quality Assessment for Drug Products

Authors

Yihong Qiu PhD, Senior Research Fellow, Oral Drug Products, Manufacturing Science and Technology, AbbVie Inc., North Chicago, IL, USA. Dr. Yihong Qiu is currently a Senior Research Fellow, Oral Drug Products, Science and Technology, AbbVie. His in-depth knowledge and extensive experience encompass various phases of product development, including preformulation, drug delivery technology, product/process design, biopharmaceutics/pharmacokinetics, formulation/process development, scale-up and optimization, manufacturing trouble-shooting, intellectual property and regulatory registration for NCE's, line-extension and marketed products. He also plays a key role in the product life cycle management, IP strategy, scientific and regulatory assessment of business opportunities. During his 25-year tenure with Abbott/AbbVie, his work has resulted in successful commercial IR and MR products, patented drug delivery technologies, IVIVC's and biowaivers approved by global regulatory agencies. Dr. Qiu's research interests include modified-release delivery systems, dissolution, bioavailability, IVIVC, drug delivery technology and science-based regulation. He is an elected fellow of the American Association of Pharmaceutical Scientists (AAPS), a member of 2010-2015 USP Expert Committee and a review committee member of Chang Jiang Scholars Program (2014-15). He has more than 50 publications in journals and books, 30 patents granted or pending, and numerous invited presentations. He is routinely invited to lecture at professional organizations and universities. Dr. Qiu received BS in Pharmacy, MS. in Pharmaceutics from China Pharmaceutical University, and Ph.D. in Pharmaceutics from The University of Iowa. Yisheng Chen Vice President, Novast Laboratories, Nantong, China. Dr. Yisheng Chen currently serves as Vice President of Product Development at Novast Laboratories, Ltd, leading the development of pharmaceutical products for global markets. Dr. Chen earned his Ph.D. degree in Pharmaceutics in 1994 from the University of Iowa. He then joined Burroughs Wellcome as a development scientist, and later Abbott Laboratories with increasing responsibilities where he was elected as an Associate Research Fellow, Volwiler Society. Dr. Chen also served as an expert member of both the Product Quality Research Institute (PQRI) and the USP Performance Testing Expert Panel, and as an adjunct professor at the Guangdong Pharmaceutical University. Dr. Chen has in-depth knowledge and extensive experience in various aspects of developing solid pharmaceutical products, ranging from formulation and process development, CMC documentation for regulatory filing, scale-up, and validation for commercialization. His expertise includes the quality by design (QbD) development of modified release (MR) products using traditional delivery technologies, and development of new delivery systems for MR products. Dr. Chen has extensive experience in the development and scale-up of beads coating process using Wurster coating technology for different types of products from lab to commercial scales. He has successfully led the development and secured the approval of more than 30 products approved in the US, EU, Japan and China, including new drug applications (NDAs) and high barrier branded abbreviated new drug applications (ANDAs). Dr. Chen also has the expertise in packaging protection of drug products. He developed a theoretical model for predicting moisture uptake by packaged products during storage. His theory provided the fundamental basis for the development of ASTM D7709 and the revision of USP general chapter < 671> on the standard methods for measuring the water vapor transmission rate (WVTR) of containers, as well as the scientific criteria of using MVTR/unit product to evaluate the performance of containers for product protection. Dr. Chen has published over 30 peer-reviewed articles, book chapters, and patents. He is a co-editor of "Developing Solid Oral Dosage Forms: Pharmaceutical Theory and Practice”. Dr. Chen is a frequent speaker at national and international conferences, and at major universities. Geoff G.Z. Zhang Senior Research Fellow, Drug Product Development, Abbvie, Inc., North Chicago, IL, USA. Dr. Geoff G. Z. Zhang is a Senior Research Follow at AbbVie Inc., an adjunct professor of the Department of Industrial and Physical Pharmacy at Purdue University, and a Fellow of the American Association of Pharmaceutical Scientists. He received his B.Sc. in Physical Chemistry from Fudan University, China, and Ph.D. in Pharmaceutics from the University of Minnesota, USA. He has contributed broadly to Physical Pharmacy, specifically in the areas of crystal engineering, polymorphism, characterization and crystallization of amorphous solids and amorphous solid dispersions, as well as delivery of poorly water soluble compounds. He has published over 70 peer-reviewed articles, reviews, and book chapters, given over 170 podium and poster presentations. During his 18-year tenure with Abbott/AbbVie, he has more than 120 granted patents and patent applications. He interacts and collaborates extensively with academic institutes and has mentored 40 graduate students on their thesis and summer research projects. He has received 2012 AAPS Pharmaceutical Research Meritorious Manuscript Award, and serves on the United State Pharmacopeia Physical Analysis Expert Committee. Lawrence Yu Deputy Director, Office of Pharmaceutical Quality,
Center for Drug Evaluation and Research,
US Food and Drug Administration,
Silver Spring, MD. Lawrence X. Yu, Ph.D., is the Deputy Director, Office of Pharmaceutical Quality, Food and Drug Administration, where he oversees new, generic, and biotechnology product quality review and inspection functions as well as the FDA CDER quality labs. He is also adjunct Professor of Pharmaceutical Engineering at the University of Michigan. Prior to joining the FDA, Dr. Yu had worked at Pfizer (Upjohn) and GlaxoWellcome for 8 years. Dr. Yu joined the FDA in 1999 and has served as Team Leader, Deputy Division Director, Division Director, Deputy Office Director, and Office Director. Dr. Yu's research interests have centered on the prediction of oral drug delivery and the development of pharmaceutical Quality by Design. His compartmental absorption and transit (CAT) model has laid the foundation for the commercial software, GastroPLUSTM and Simcyp®, which are being widely used in the pharmaceutical industry. Dr. Yu is a fellow and the past section Chair of the American Association of Pharmaceutical Scientists and an Associate Editor of the AAPS Journal. Dr. Yu has authored/co-authored over 140 papers, and presented over 100 abstracts, and given over 200 invited presentations. He is a co-editor of the books entitled "Biopharmaceutics Applications in Drug Development , "FDA Bioequivalence Standards , and "Developing Solid Oral Dosage Forms: Pharmaceutical Theory and Practice, 2nd Ed. Dr. Yu is the winner of numerous awards including AAiPS distinguished Scientist Award, AAPS Regulatory Science Achievement award, AIChE PD2M Drug Product QbD Achievement Award, Japan Naigai Foundation Distinguished Lectureship, China Beijing University IPEM graduation commencement address, Department of Health and Human Service Outstanding Leadership Award, FDA Commissioner's Special Citation, Outstanding Achievement, Group Recognition, and Team Excellence awards. Rao V. Mantri Executive Director, Drug Product Science & Technology, Bristol-Myers Squibb, New Brunswick, NJ, USA. Dr. Rao V. Mantri is currently working as Executive Director in Drug Product Science & Technology at Bristol-Myers Squibb Company. He received his B.Tech. in Chemical Engineering from Osmania University, India, M.S. in Chemical Engineering, M.S. in Pharmaceutical Chemistry and Ph.D. in Pharmaceutical Chemistry with honors from The University of Kansas, USA. Since joining BMS R&D in 2000, he has held positions of increasing responsibility in design, development and technology transfer of small molecules as well as biologics drug products. He has broad experience in formulation development, process engineering, materials science, analytical sciences, CMC regulatory filing strategy and leading multi-disciplinary CMC teams. His research interests include solubilization, drug delivery, materials science, drug-excipient interactions, drug stability, biopharmaceutics modeling, formulation development and process scale-up. He has 29 manuscripts, 8 patents and numerous invited talks and presentations. He also served on the 2010-2015 USP Excipients Expert Committee.