8:25 Welcome Address And Chairperson’s Opening Remarks

Ron Liu, PhD MBA
President & Chief Executive Officer
AustarPharma

8:30 Opening Keynote Presentation: Thermodynamic Vs. Kinetic Stability: Knowing Which Is Which

• Understanding the distinction between thermodynamic and kinetic stability
• Exceeding the equilibrium solubility to give a supersaturated solution
• Measuring equilibrium solubility and metastable solubility within a substance
• Knowing accurately if and when the substance is metastable or undergoing a change
• Recognizing when equilibrium solubility is actually a consequence of kinetic solubility

Harry G. Brittain, PhD, FRSC
Institute Director
Center for Pharmaceutical Physics

9:15 Demonstration Of Bioavailability Enhancement Through The Use Of Biorise And Diffucaps Technologies Biorise®

• Displaying the production, stabilization and characterization of amorphous and nanocrystalline composites
• Preclinical demonstration of efficacy
• Clinical demonstration of efficacy Diffucaps®
• Discussing the production of bioavailability-enhanced extended release formulations using control of pH microenvironments
• Clinical demonstration of efficacy
• Mathematical modeling of pharmacodynamic response

Anthony Recupero, PhD
Senior Director, Business Development
Eurand

10:45 Nanocrystalline Drug-Polymer Solid Dispersions For Poorly Water-Soluble Drugs

• Nanocrystalline drug-polymer solid dispersion was formed by co-spray drying drug and Pluronic or PEGs
• Nanocrystalline solid dispersion showed improved in vitro dissolution rate and in vivo exposure
• Physical structure of the nanocrystalline solid dispersions was characterized by PXRD, DSC, AFM and TEM
• Mechanism led to the formation of nanocrystalline solid dispersion formation was investigated

Feng Qian, PhD
Senior Research Investigator
Bristol-Myers Squibb

11:30 Making Development Of An Insoluble Drug Candidate Possible By Using Solid Dispersions: A Case Study

• Displaying first in man studies of a highly insoluble compound with micronized drug substance in capsules
• Exposure was very low and there was no dose-proportionality at low doses.
• Evaluating multiple formulation strategies in a clinical study to obtain adequate bioavailability to proceed with further clinical trials
• Selecting for developing a solid dispersion with 20% drug load in HPMC
• Describes the polymer selection, physicochemical characterization, formulation development, stability results, and testing strategy for the solid dispersion product
• Understanding the challenges associated with commercial development

Satej Bhandarkar, PhD
Senior Manager, Analytical Sciences Department
Sanofi-Aventis U.S.

1:15 Pharmaceutical Co-Crystals: A Solubility Perspective

• Understanding the pharmaceutical co-crystal concept
• Utilizing pharmaceutical co-crystals to enhance solubility and dissolution of insoluble APIs
• Discussing mechanisms by which co-crystal solubility is enhanced
• Examining co-crystal structure-solubility relationships
• Identifying the PK impact
• Analyzing literature case studies

Naír Rodríguez-Hornedo, PhD
Associate Professor of Pharmaceutical Sciences, The College of Pharmacy
The University of Michigan

2:00 Amorphous Dispersion Approaches For Achieving Rapid Onset For Orally Administered Low-Solubility Compounds

• Outlining the need for increased solubility and rapid absorption
• Assessing the impact of enteric dispersions on absorption rate
• Developing rapidly dissolving amorphous formulations
• Pursuing formulation and process development for amorphous drugpolymer nanoparticles

David Lyon, PhD
Vice President, Physical and Biological Sciences
Bend Research, Inc.

3:30 Panel Discussion: How To Effectively Formulate Poorly Soluble Drugs

• Nanoparticles
• Amorphous forms
• Salt selection: Suitable salt properties for later stage development: stability, solubility, purity, etc.
• Polymorphs: Screening and characterization
• Cyclodextrins: Toxicology and pharmacokinetic properties and uses in development
• Assessing permeability and solubility

Jeffrey Skell, PhD
Director, DMPK
Genzyme Corp. Solubility and Discovery Techniques

4:15 The Role And Function Of Solubility Measurement From A Central Laboratory In Drug Discovery

• Summarizing of solubility methods and practices
• Evaluating kinetic vs thermodynamic solubility
• Comparing precipitation vs. aggregation aspects
• Understanding the relationship of solubility and in vitro biology and DMPK assays
• Discussing conclusions and recommendations

Yun Alelyunas, PhD
Principal, Scientist I, Head of Physical Properties Team
AstraZeneca

5:00 Implication Of BCS: Solubility And Permeability Class On Drug Formulation

• Examining the importance of tailoring your formulation platform based on BCS class
• Discussing the extension of BCS classification for formulation selection
• Evaluating pH-solubility profile and modified solubility criteria
• Comparing a Caco-2 in-vitro Permeability vs in-situ rat perfusion study
• Using BCS-based Formulation Decision Trees

M. Sherry Ku, PhD
Senior Director, Pharmaceutical Development
Pfizer, Inc.

5:45 Chairperson’s Closing Remarks And End Of Day One

6:30 Networking Dinner

Continue the networking experience by joining your colleagues for a dinner following the end of day one. Separate booking necessary. We hope you will join us!