E13 – Physical Characterization and Analytical Test of Pharma Solids 1

Physical Characterization and Analytical Test of Pharmaceutical Solids I: 
Essential Knowledge

 One-Day Course E13-11, Sunday, November 17th, 8:30am – 5:00pm

 Dr. Steve R. Byrn, Purdue University, West Lafayette, IN
Dr. Xiaoming (Sean) Chen, Shionogi Inc., Florham Park, NJ

Physical characterization and methods of analysis of pharmaceutical solids are essential for drug research and development. Solid characteristics such as polymorphism, formation of hydrate and solvate, and crystallinity have profound impact on the quality attributes of drug substances and drug products such as solubility, dissolution, bioavailibility, processability, and stability. Characterization of those solid state properties is critical for selection and manufacture of desirable solid forms for development. This short course presents some essential knowledge for pharmaceutical solids. It also introduces methods of analysis of the solid state such as X-Ray powder diffraction, differential scanning calorimetry, thermogravimetric analysis, microscopy, infrared spectroscopy, Raman spectroscopy, and solid state NMR. Applications of those techniques in the final form selection of drug substances and mixture analysis of drug products are discussed.

This one-day course will benefit formulation scientists, process engineers, analysts, QA and QC managers, regulators, and researchers, who perform process development and manufacture of drug substances, develop formulations of drug products, conduct analytical testing and method development, set up stability programs, and evaluate stability data of drug substances and products.

1. Pharmaceutical Solids-Introduction
     * Polymorphs
     * Solvates and hydrates
     * Salt formation and co-crystal
     * Amorphous forms
2. Methods of Analysis
     * Crystal packing, unit cell, X-ray powder diffraction
     * Differential scanning calorimetry and thermo-gravimetric analysis
     * Microscopy
     * Infrared spectroscopy and Raman spectroscopy
     * Solid-state NMR

Dr. Stephen R. Byrn is Charles B. Jordan Professor of Medicinal Chemistry in the School of Pharmacy, Purdue University, West Lafayette, Indiana. He received his B.A. degree in Chemistry from DePauw University and his Ph .D. degree in Chemistry from the University of Illinois, Urbana. He did postdoctoral research at UCLA. His research focuses on solid state chemistry, polymorphism, stability, manufacturing science, quality by design, and medicinal chemistry. Dr. Byrn opened up the field of solid state chemistry of drugs with his research and books of that title (first edition, 1982, second edition, 2000). Dr. Byrn has founded and directed several programs at Purdue University including CAMP, the Center for AIDS Research, the Molecules to Market program, and Purdue’s graduate programs in regulatory and quality compliance. He is also one of the founders and a member of the executive committee of NIPTE (National Institute for Pharmaceutical Technology and Education). He continues to be involved in educating scientists in solid state chemistry, methods of analysis, and regulatory science. Dr. Byrn has served as chair of the Pharmaceutical Sciences Advisory Committee to the FDA and Chair of the Drug Substances Technical Committee, Product Quality Research Initiative. Dr. Byrn has extensive experience as a consultant in the pharmaceutical industry and currently serves as Purdue’s representative to the USP. Dr. Byrn is co-founder of SSCI, Inc. (Solid State Chemical Information) a cGMP research and information Company specializing in polymorphism, crystallization, analysis, problem solving and regulatory issues. SSCI, Inc. is now owned by Aptuit and Dr. Byrn serves as Head of the Aptuit Scientific Advisory Board. Dr. Byrn is also a technical founder of Andara now owned by Cyberkinetics, Inc. Andara specializes in devices and drugs for the treatment of spinal cord injury and CNS diseases.

Dr. Xiaoming (Sean) Chen received his Ph.D. in Industrial and Physical Pharmacy from Purdue University in 2000. He has worked as a project leader in discovery support and preformulation at Schering-Plough Research Institute for five years. He has contributed the nomination of five NCE for development and received one President Award, one Impact Award and three Excellence Awards from Schering-Plough Research Institute. He has also worked in Exploratory Formulation group of Schering-Plough for three years, leading formulation development of two important line extension projects. Dr. Chen has worked in OSI Pharmaceutical for more than three years in the area of formulation and process development for new cancer drugs. Currently, he is a Manager of Pharmaceutical Sciences in Shionogi Inc. Dr. Chen is an expert in physical characterization of solids, crystal form and salt selection, and controlled release formulation. He has published over a dozen of papers in peer-reviewed journals and is a co-inventor of three patents. Dr. Chen is a member of AAPS and has served in PDD award committee for two years.