08.40 Pharma IQ Welcome And Chairperson’s Opening Address

Dr Susan Reutzel-Edens
Senior Research Advisor
Eli Lilly

Analysis of the Current Opportunities Within Crystallisation Development to Maximise Future Development Opportunities and In Turn Maximise Your ROI

08.50 Crystal Structure Prediction: New Opportunities In Pharmaceutical Development

The 2007 blind test on crystal structure prediction (CSP) has demonstrated that the crystal structures of small and rigid organic molecules have become predictable and the scope of applicability has continued to increase ever since. Today, CSP can be used for a significant portion of pharmaceutical molecules in order to confirm experimental results or to guide experimentalists to new crystal forms. The presentation will address:

• CSP using dispersion-corrected quantum calculations and tailormade force fields
• Validation studies: Blind tests, paracetamol and confidential work on industrial compounds
• Current scope of applicability and what is left to improve
• Complementarity between experimental and in silico polymorph screening
• Estimate of future performance based on past learning curves

Dr Marcus Neumann
Managing Director
Avant-garde Materials Simulation Deutschland GmbH

Discovering New Avenues of Development Within Polymorphism to Ensure Favourable Properties for Further Development

09.35 Ensuring Polymorphism Control - A Question Of Nucleation Or Growth?

• A review of the relative and competing roles of nucleation vs. crystal growth in polymorphic systems
• What is the true basis of an apparent solvent effect?
• What should I measure to compare nucleation rates of polymorphs?
• How do I compare growth rates?
• What this means for process control and design

Professor Roger Davey
Molecular Engineering
University of Manchester

10.50 Direct Nucleation Control Of Crystal Size Distribution And Polymorph Type

• Review of the issues associated with scale-up and prediction of nucleation and growth rates
• Implementation of direct nucleation control of crystal size distribution and polymorph type
• The benefits of using

Professor Chris Rielly
Head of Department of Chemical Engineering
University of Loughborough

11.35 The Role Of Co-Crystals In Solid-State Development – Discovering Opportunities Of Co-Crystals To Ensure The Most Favorable Properties For Further Development

Solid-state properties have a huge practical and commercial impact on active substances all the way from research to manufacture of the final product. The search for, and more importantly the selection of the optimal solid form (salt, co-crystal, polymorph) is closely linked to the intended application of the drug substance and to the final drug product. Good timing of solid-state development activities ranging from first screenings to crystallisation optimisation is becoming more and more important in view that CMC failures are one of the most important reasons for delays in drug development. An integrated approach to solid-state development is essential for successful development of a drug substance. In this presentation we will focus on:

• Strategies to synthesise and to select co-crystals with optimised properties
• Important structural and physicochemical parameters which are closely linked to the successful generation of such entities
• The importance of the understanding of phase diagrams for the design of successful co-crystal formation will be highlighted

Dr Rolf Hilfiker
Head of Department, Solid State Development, Vice President
Solvias

Industrial Applications of Polymorphic and Crystallisation Design

13.20 Kinetics Of Polymorphic Transformations: Understanding The Kinetics To Better Predict The Future Development Potential

• Discussion of the theory behind the kinetics of polymorphic transformations
• Seeding within polymorphic transformations
• Temperature control within polymorphic transformations and the impact on your development
• Dealing with impurities within polymorphs and the problems they pose for further development

Dr Simon Black
Principle Scientist
AstraZeneca

14.05 The Rational Design Of API Crystallisations Processes – An Industrial Perspective: Applying Theory To Industry

• The selection of the API phase for development
• Application of phase diagrams for crystal form control (with focus on managing enantiotropic polymorphs and solvates/hydrates)
• Particle size control toolkit
• Scale up from lab to pilot plant and beyond: Methods for assessing and mitigating the risks

Dr Aaron Cote
Scientific Director
Merck/MSD

15.20 API Particle Engineering To Enhance The Mechanical Properties And Dissolution Performance Of New Formulations

• Development of APIs for standardised drug product platforms using product development “Co-LABs”
• Design of API shape, size and form for optimal formulation using innovative approaches such as co-precipitation, spray drying and template crystallisation
• Case studies will be presented for dosage forms design with improved flow and dissolution performance using engineered APIs

Dr Subodh Deshmukh
Senior Director
Pfizer

16.05 Presentation From The Solid State Pharmaceutical Cluster For More Updates On This Talk, Please See Www.polyandcrys.com

Professor Brian Glennon
School of Chemical and Bioprocess Engineering
University College Dublin and Solid State Pharmaceutical Cluster

16.50 Ensuring Regulatory Compliance In Polymorph And Amorphous Form Selection:

A Regulatory Perspective

• Testing, selecting and controlling polymorphs
• Setting specifications for polymorphic forms
• Insight: How to ensure that the desired form is in the finished product
• Case studies regarding the influence of polymorphic forms on bioavailability behaviour

Dr Cornelia Nopitsch-Mai
Senior Quality Assessor
Bfarm

17.35 Exclusive Polymorphism And Crystallisation Poster Award Session*

Join this interactive session to look over and hear about the latest work from all the poster competition entrants. An exciting opportunity to explore the most cutting edge research, meet fellow scientists in the field and get involved with lively discussions. The session will be followed by a drinks reception where the poster session prize winner and runners up will be announced.

To enter or find out more please visit: www.polyandcrys.com

*The competition is limited to Pharmaceutical Manufacturers and Academics not providing solutions or services to others in the industry.

18:35 Chairpersons Summary And End Of Day One