08.50 Pharma IQ Welcome And Chairperson’s Opening Address

Professor Roger Davey
Molecular Engineering
University of Manchester

Product Control and Stabilisation to Ensure Success Within Future Development

09.00 Understand And Control The Product Form Issues Via QbD Approach

• What is QbD? And what are the opportunities within crystallisation?
• API crystal forms and their presence in drug products
• Basic crystal form physical characterisation techniques
• QbD and API crystal forms- Opportunities and challenges within
• QbD and the API crystal form development
• Control product crystal form system via physical characterisations

Dr Shawn Yin
Senior Research Investigator
Bristol Myers Squibb

09.45 New Ways Of Acquiring X-Ray Powder Diffraction Data To Complement Your Understanding Of A Compounds Solid State Behaviour

• The use of a Flow Thru Cell to identify metastable forms and to study solvent mediated transformations
• Variable temperature studies in a capillary tube and the advantagesof its use
• Ways of reducing air scatter for those all important studies of the amorphous state
• A walk up and use X-ray diffractometer, a solution for the busy physical properties laboratory

Dr Philip Lake
Principle Scientist
GSK

11.00 The Role Of Quantitative Phase Analysis In Drug Development

Solid state analysis has already become an integral part of everyday pharmaceutical development. Manufacturers always have to deal with the polymorphism of active pharmaceutical ingredients (API), at least as much to prove that polymorphism or possible solvate formation does not affect drug product’s performance. To avoid unexpected late stage failures, it is expedient to choose the thermodynamically most stable solid form for development. It is not advisable to develop polymorphic mixtures, legal consequences of polymorph patents or stability issues may necessitate that, however. Such a development primarily needs a suitable quantitative analytical method. The presentation aims to discuss some aspects of quantitative solid phase pharmaceutical analysis and its importance in API development.

• The importance of solid state characterisation of pharmaceuticals in connection with current regulation
• Possibilities and weaknesses of various techniques when applied to quantitative solid state analysis
• Case study I: Developing a polymorphic mixture
• Case study II: Developing a polymorph which is difficult to crystallise in a pure phase

Dr Zoltan Nemet
Drug Polymorphism Research Division
Gedeon Richter Plc.

11.45 The Application Of Process Analytical Technology To Crystallisation Development

• Quality by Design and the need for process understanding
• Role of PAT and the strength of combining techniques to understand complex phenomena
• Overview of PAT techniques for crystallization process characterization including turbidometric methods, ATR FTIR spectroscopy, flow-through slurry XRD and in-situ particle imaging
• Forward look and future challenges

Professor Kevin Roberts
Faculty of Engineering
University of Leeds

Strategic Tool Implementation: Successful Scale Up Approaches and Prospects for the Future

13.30 The Route To A Scalable Process – Nurturing Your Hits

Tailoring a screen to the physical chemical properties of an active pharmaceutical ingredient begins the process of identifying a scalable physical form.

• Thorough analysis of the material prepared ensures that scale up of false positives is minimised: Specific techniques will be discussed
• The first steps of moving from low milligrams to tens or hundreds of milligrams are often the most difficult due to the huge differences in environment from screen to flask: Difficulties and hints will be discussed
• Once the salt can be reproducibly prepared at tens of milligrams the next step is to develop a process to prepare high purity, crystalline material with a high yield. The crystallisation should be robust enough to “grow” to the crystallisation vessels of scale up labs and pilot plants

Dr Grahame Woollam
Senior Scientist
Novartis

14.15 Ensuring Correct Solid-State Form Selection: An Essential First Step In Drug Product Design

• Consideration of crystal form landscapes in final form selection:
• Salts, co-crystals and their polymorphs
• Structured approaches to solid form screening: Right sizing and right timing
• Designing drug products through solid form selection: Case studies
• Transforming molecules into medicines: Ensuring drug product performance

Dr Susan Reutzel-Edens
Senior Research Advisor
Eli Lilly

15.00 Discussion Of The Challenges Of Solid-State Characterisation In A GMP Environment

For more updates on this session, please see: www.polyandcrys.com

Dr Caitriona Cashell
PDC Physical Characterisation Lead, Pfizer
previously Wyeth Medica

16.15 Doing More With Less: Strategic Implementation Of Methods To Ensure The Most Appropriate Solid Form Is Chosen In An Efficient Manner

• Comparison of high through-put and manual methods used for polymorph screen
• The screen strategies could be case dependent
• Different methods should be used to minimise the “unexpected” polymorph
• Case studies of different forms that were identified from different methods
• Using a co crystal screen example to describe: How the initial screen can be used to evaluate the scalability?

Dr Zhibin Li
Senior Scientist
Boehringer-Ingelheim

17.00 Alternative Way Of Seeding Crystallisation: Self Assembled Layers As Defined Nucleation Templates

• Alternative way of seeding crystallisation by self assembled layers i.e. adsorbed molecular layer at gold single crystal surface
• Preparation and characterisation of self assembled layer on gold surface of drug molecule Entacapone
• Possibility of switching nucleation site from uncontrolled one to a designed surface toward more predictive nucleation
• Polymorph-specificity of self assembled layer templates and hydrodynamic influence on templated nucleation
• The future potential of seeding by self assembled layer and methodology for larger scale size processes

Dr Ana Kwokal
Research Scientist
Pliva

17.45 Panel Discussion: Mechanisms Of Polymorphic Transformations

• Understanding the mechanisms of polymorphic transformation
• Review of the developing models for polymorphic transformations
• An outlook to the future: How understanding polymorphic transformations will benefit crystallisation and pre-formulation

18.30 Chairpersons Summary And End Of Day One