8:45 Welcome Address And Chairperson’s Opening Remarks

9:00 Salt And Polymorph Selection Strategy Based On The Biopharmaceutical Classification System (BCS) For Early Pharmaceutical Development

• Providing an overview of Wyeth’s drug substance form selection process
• Conveying examples for the integration of form selection with toxicology (TOX) formulation development and pharmacokinetic (PK) assessment
• Outlining rationale for early solid-form selection
• Discussing pre-selection: First evaluation of a solid-state API
• Examining potential advantages with salt and polymorph form selection

M. Sherry Ku
PhD, Senior Director, Pharmaceutical Development
Wyeth Research

9:45 Sharing Best Practices For Polymorphism And Crystallinity Determination In Discovery

• Understanding and discussing discovery needs for Polymorphism and Crystallinity determination
• Surveying of a project's need for the determination
• Differing needs of discovery vs. development
• Examining observations in solubility determination relating to polymorphism
• Evaluating observation in preclinical toxicology studies relating to Crystallinity
• Summarizing potential techniques suitable for discovery phase

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

11:15 The Roles And Significances Of Materials Science And Engineering In Modern Drug Development

Discussing the concept of Materials Science Tetrahedron and its roles in guiding characterization and design of new products or materials

• Identifying the relationship between structure and mechanical properties of crystals
• Optimizing powder compaction properties of drugs by crystal engineering
• Engineering crystals by co-crystallization
• Fundamentals in powder compaction

Changquan Calvin Sun
PhD, Assistant Professor, Department of Pharmaceutics, College of Pharmacy
University of Minnesota

12:00 A Rational Approach towards Establishing Physical Quality Specifications for the API

• Discussing a rational approach to establishing physical quality parameters (particle size, particle shape, etc.) needed for a robust drug product manufacturing process
• Illustrating how this approach was implemented for real development projects through case study examples
• Examining conventional crystalline APIs as well as unusual solid forms (e.g., amorphous drug substance, solid dispersions)
• Discussing of the interplay between the limitations of the drug substance manufacturing process design space and drug product manufacturing requirements
• Displaying analytical approaches used to evaluate physical characteristics, including their strengths and their limitations
• Evaluating standard techniques: Laser diffraction for particle size measurement, X-ray tomography for studying API and excipient distribution in drug products

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

1:45 Materials Sciences And Particle Engineering: The Interface Between Drug Substance And Drug Product

Particle engineering is a cornerstone of a Pfizer technology strategy aimed at designing drug substance (DS) crystallization/isolation processes which maintain the traditional deliverables of yield, purity, process efficiency combined with a focus on controlling physical properties to create final DSs with rational properties for drug product (DP) design. The ultimate goal is to develop fully integrated DS and DP design to facilitate the progression of projects by either simplifying DP processing (e.g., direct compression vs wet granulation of tablets) or by enabling more sophisticated drug delivery systems (e.g., inhalation).

• Utilizing materials science capabilities to optimize the relationship between the drug substance form, its formation, and formulation
• Discussing particle engineering technologies (e.g. sonocrystallization) to control physical attributes of drug substances
• Evaluating high throughput and science of scale approaches to accelerate form and formulation selection
• Assessing the benefits of integrating of Drug Substance and Drug Product Design to facilitate development programs

Keith R. Horspool
PhD, Senior Director, Materials Science and Oral Products
Pfizer Inc

2:30 The Role Of XRPD In Accelerating Pharmaceutical Phase Identification And Selection

• Understanding the importance of rapid and early phase selection
• Identifying and analyzing new HT tools and techniques and useful phases of a drug substance, and reduce the risk of failure in drug development
• Detailing fast and economical methods for the identification and evaluation of crystalline phases of drug substances, including neutral API, salts, co-crystals, and hydrates, solvates and polymorphs
• Evaluating the merit of high throughput XRPD as one of the main analytical techniques used for rapid analysis of new pharmaceutical solid
• Discussing tools for managing the large volume of data that is generated

Michael McNevin
PhD, Senior Research Chemist
Merck Research Laboratories

3:45 The Continuing Evolution Of Solid-State NMR In Pharmaceutical Analysis

• Highlighting the role of solid-state NMR (SSNMR) as part of an integrated analytical strategy for chemical and pharmaceutical development
• Examining recent advances in the application of SSNMR, including investigations of weak solvates, solid solutions, inclusions, and other phenomena that can occur during API crystallization
• Illustrating the characterization of API and excipient phases in drug product and formulations, including low-dose products, with SSNMR and Raman spectroscopy
• Evaluating detailed structural analysis of polymorphs, salts and cocrystals, including crystal structure solution with SSNMR, powder x-ray diffraction, and computational methods
• Structural characterization of complex systems, including amorphous dispersions, variable hydrates and mixed co-crystal-salt phases

Fred Vogt
PhD, Manager, Analytical Sciences, Chemical Development
GlaxoSmithKline

4:30 The Appearance Of New Polymorph During The Development Work Preceding Process Lock

• Discussing optimization of crystallization procedure and range finding experiments
• Describing how a new form overwhelms the previously produced in various procedures, but very “slowly” travels from lab to lab
• Addressing the Challenge: In a limited time find conditions to restore production of thermodynamically stable form, and transfer these conditions to the pilot plant
• Reviewing alternative ways to obtain the stable form, which result in undesirable crystal habit

Elena Kostik
PhD, Principal Scientist
Synta Pharmaceuticals Inc

5:15 End Of Conference & Chairperson’s Closing Remarks