8:45 Welcome Address And Chairperson’s Opening Remarks

Harry G. Brittain
PhD, FRSC, Chief Executive Officer
Center for Pharmaceutical Physics

9:00 Opening Keynote Presentation: Understanding And Rationalizing Co-Crystal Discovery, Solubility And Selection

Co-Crystals offer the advantage of generating solid forms of active pharmaceutical ingredients (APIs) with other molecular components and produce materials with strikingly different and advantageous properties. Much of the research in this field has focused on the application of supramolecular chemistry concepts to the design of co-crystals while co-crystal formation and co-crystal structureproperty relationships are not well understood. Understanding how co-crystal solubility is affected by co-crystal components and solution chemistry is essential to (1) engineer co-crystals with customized solubility and (2) streamline co-crystal discovery and selection. This talk will present approaches that are valuable to predict co-crystalsolution phase behavior and guide co-crystal selection without the time and material consuming requirements of traditional methods.

• Identifying effective co-crystal synthesis by solution mediated processes
• Understanding why the same solvent can lead to no co-crystal or to co-crystal
• Discussing mechanisms by which co-crystal solubility is enhanced
• Examining co-crystal structure-solubility relationships
• Displaying thermodynamic indicators of co-crystal solubility and stability

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

9:45 Modulation Of The Solubility And Dissolution Rate Of Crystalline Substances: Effect Of Polymorphic/ Solvatomorphic Identity And Particle Size

• Outlining the structural aspects of polymorphism and solvatomorphism, and the resulting effects on the thermodynamic and kinetic properties of solids
• Discussing the most appropriate techniques for the study of organic crystalline polymorphism and solvatomorphism
• Summarizing of the theory relating particle size and dissolution rate of crystalline solids
• Examining methodology and tools, through the use of case studies, for evaluating the effect of solid-state characteristics on dissolution rate and solubility

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

11:15 Understanding When To Effectively Use Hydrates In Pharmaceutical Development

• Understanding the importance of hydrates in Pharmaceutical Development
• Discussing different types of hydrates
• Examining physical/chemical analysis of hydrates
• Estimating the relative stability among polymorphs and hydrates
• Processing issues with hydrates

Dedong Wu
PhD, Senior Scientist, Pharmaceutical and Analytical R&D
AstraZeneca

12:00 Polymorph Control And Crystal Engineering For Improvement Of API Mechanical Properties

• Discussing phase relationships of Polymorphs, solvates and hydrate
• Addressing solvent base morphology modifications
• Examining impurity base morphology modifications
• Identifying morphology modification and PSD control with in-line wet milling techniques and PAT technology

Richard Varsolona
Crystal Engineering Technology
Wyeth

1:45 Predicating Crystal Nucleation From The Amorphous State

• Understanding the physics of crystal nucleation
• Identifying sites for nucleus formation
• Determining the amorphous state most (or least) likely for recrystallization
• Relating crystallization to thermodynamic parameters such as Tg
• Comparing amorphous dispersions and solid solutions for amorphous form stabilization

Eric J. Munson
PhD, Professor, Department of Pharmaceutical Chemistry
University of Kansas

2:30 Practical Uses Of Amorphous API’s: Features And Stability

• Discussing and understanding where amorphous materials fit in drug development
• Evaluating the advantages and disadvantages of amorphous materials
• Weighing up the pros and cons of stabilization of amorphous solids in dispersions
• Identifying practical properties required for development
• Screening for solid dispersions – Uncovering novel tools and techniques
• Displaying case study examples of developing practical solid dispersions

Duk Soon Choi
PhD, Research Leader
Hoffmann La Roche

4:00 Interactive Roundtable Best Practice Discussions

After a jam-packed day of big picture keynotes, panel discussions, case studies, and presentations, the 8th Polymorphism & Crystallization Scientific Forum gives you the chance to meet and brainstorm with small groups of your peers during our interactive roundtable discussions. This is a great opportunity to make valuable contacts from your area of interest, and to deep-dive into the tricky details that you may missed in the course of the day’s sessions. MUST ATTEND!

Round Tables include:

• Identification and quantitation of forms
• Developing an Integrated approach to solid state development
• Chiral co-crystals
• Strategies for patenting co-crystals

** Delegates are encouraged to bring their own data or study results or submit them earlier to simon.curtis@iqpc.com

4:45 Salt Screening And Selection Of Pharmaceutical Salts

• Understanding the ability to prepare and isolate a salt form of a drug substance in its solid state, and the stability of that salt form
• Discussing ionic equilibria of acidic and basic substances
• Examining utility of salt-form ionic equilibria in the design of salt selection studies
• Understanding why the identification of a salt form of an API becomes essential if the characteristics of the free acid or free base are not found to be acceptable

Gregory Stephenson
PhD, Research Advisor, Preformulations
Eli Lilly & Company

5:30 Improvement Of Solid State Chemical Stability Through Form Selection

• Describing why solid state chemical stability has a significant impact on the quality, safety, and shelf life of drug substances and drug products
• Examining poor stability issues which could be due to molecular properties and/or solid state characteristics
• Improvingsolid state chemical stability by changing solid state characteristics such as crystal packing, Crystallinity, and hygroscopicity through selecting a different polymorph, salt form, or co-crystals
• Examining mechanisms of solid state chemical reactions
• Uncovering solid state characteristics and chemical stability
• Characterizing form selection and improvement of stability

Xiaoming (Sean) Chen
PhD, Drug Product Development & Manufacturing
OSI Pharmaceuticals, Inc.

6:15 Chairman’s Closing Remarks And End Of Day One