With more than 70% of drug candidates classified as poorly soluble, there has been increasing interest in formulation technologies to enhance bioavailability for better absorption. Pre-formulation is a necessary step before formulation development which needs to be conducted as early as possible.
The goal of pre-formulation is to establish the physical, chemical, and mechanical properties of a drug substance that provides a roadmap and a guide for how to formulate the molecule into a fit-for-purpose formulation. The complexity of the fit-for-purpose formulations can range from simple (e.g. powder-in-bottle) to advanced (e.g. solubility-enhanced).
Pre-formulation can be divided into three parts:
- Know your molecule – thorough understanding of the physical, chemical, solid state and mechanical properties, solubility, dissolution rate, and stability
- Understand risks and mitigate key risks – assessment of molecule stability in both solution and solid state conditions (effect of pH, temperature, oxidation…) and compatibility with commonly used excipients
- Optimize your molecule – identification and selection of possible salts and screening for polymorphs
The physicochemical profile and the molecule’s position in the Developability Classification System (DCS) are used to design an advanced formulation screening model.
During this 60-minute webinar, industry experts will provide an in-depth review of pre-formulation techniques and discuss how these techniques can accelerate early phase development to animal PK and first-in-man studies.
Presented by
Michael J. Hageman, Ph.D.,
Former Executive Director of Discovery Pharmaceutics at Bristol-Myers Squibb
Dr. Hageman has over 30 years of experience within the pharmaceutical industry, including Upjohn, Pharmacia, Pfizer and for the last 11 years, Bristol-Myers Squibb. He has worked with Discovery organizations for the design and selection of developable molecules, both small drug-like molecules and larger protein biologics. Physicochemical property prediction and characterization, including preformulation and design of enabled formulations for enhanced bioavailability, were critical for successful progression of the drug candidates.
He obtained his BS in Pharmacy and PhD in Pharmaceutical Chemistry from the University of Kansas. He has been an adjunct professor at Purdue University, University of Kansas, and University of Utah, serving on 6 different thesis committees.
Dr. Hageman is an editor for the Journal of Pharmaceutical Sciences and chairs the Pharmaceutics Advisory Committee for PhRMA Foundation. He has also served as Chair of the Physical Pharmacy and Biopharmaceutics Section for AAPS and been involved in the organization of over 10 symposia at AAPS sponsored meetings.
He has nearly 50 publications, 12 patents/applications, over 70 invited presentations and over 65 meeting presentations. He has co-edited two books entitled Prodrugs: Challenges and Rewards and Optimizing the Drug-Like Properties of Leads in Drug Discovery.
Dr. Pingyun (P.Y.) Chen,
Director, Early Development at Catalent Pharma Solutions
Dr. Pingyun (P.Y.) Chen serves as the Director, Early Development at Catalent Pharma Solutions.
He began his pharmaceutical career as a Research Investigator in Pharmaceutical Development at GlaxoWellcome in 1999. After spending one year as a Principal Research Scientist at Eli Lilly in 2004, he returned to GlaxoSmithKline to co-lead the Solid Form Sciences team to provide global salt and polymorph screening and selection support for drug candidates from discovery through commercialization.
He joined Catalent Pharma Solutions as the Manager of the OptiformTM Technologies in 2010. Dr. Chen has given multiple presentations as an invited speaker in scientific conferences, co-authored over 40 publications and book chapters, and named as a co-inventor on multiple patents.
