Conference Day One: Monday 27th September 2010

08:00 Registration

08:50 Pharma IQ Welcome And Chairperson’s Opening Address

Characterisation of Co-Crystal Processes and Properties to Understand Co-Crystal Behaviour

09:00 Solid State NMR (SSNMR) Analysis Of Organic Co-Crystals And Complexes

  • Insights into the capabilities of SSNMR in providing detailed structural information and complexes from powdered samples
  • Exploring the intricacies of SSNMR: SSNMR can prove or disprove molecular association, observe structural features such as hydrogen bonding and intermolecular distances, and confirm the ionisation state of amines and carboxylic acids in the solid state
  • Utilising the advantages of SSNMR for the identification of pharmaceutical co-crystals, which are often produced initially by solvent drop grinding techniques that do not lend themselves to single crystal growth for X-ray diffraction studies

Dr Tran Pham
Principal Scientist
GlaxoSmithKline

09:45 2010 - Exploring The Structural Aspects Of Co-Crystallisation

Pharmorphix is one of Europe’s leading providers of solid-form research services to the international pharmaceutical and biotech industries. The ability to prepare co-crystals in significant quantities is one of the major challenges that still need to be overcome in order for this field to become an economically viable method of producing new drug products. Pharmorphix laboratories investigates how both traditional and new methodologies can be employed to overcome these problems.

Dr Christopher Frampton
Chief Scientific Officer
Pharmorphix

10:30 Networking Coffee Break

Optimisation of Co-Crystal Screening and Selection to Advance Co-Crystal Formulation and Development

11:00 Insights Into Accelerated Drug Development Using A Co-Crystal Screen Of Natural Products

  • Exploring the role of natural products in drug discovery
  • Analysis of the benefits and limitations of natural products as lead structures in oncology drug development
  • Co-Crystals in Industrial Practice: a look into case study AxP 107-11

Dr Michael-Robin Witt
Chief Technology Officer
Axcentua

11:45 Preparing And Accelerating Examination Of Co-Crystal Patents

The unique chemical nature of co-crystals and their beneficial pharmacological properties provide good arguments for their patentability. A robust co-crystal patent application must draw upon that unique chemical nature and beneficial pharmacological properties while at the same time marshal that information to form a legal document ready for rigorous examination. Co-crystal patent applications can also lend themselves well to expedited patent procedures such that the examination process may be shortened and the patent granted sooner. But, this takes planning.

Participants will learn about:

  • The “ins” and “outs” of co-crystal patent application preparation, including data to present and structuring co-crystal patent claims
  • The new expedited examination procedures at the US Patent and Trademark Office and how to take advantage of them
  • The patent prosecution highways existing between certain international patent offices and how to use them
  • The development of an overall strategy for obtaining meaningful patent protection

Dr Jeffrey Lindeman
J.A. Lindeman & Co. PLLC

12:30 Networking Lunch Break

14:00 Some Thermodynamics Underpinning The Selection Of A Co-Crystal For Development

  • How might a co-crystal be suitable for drug development when salts of weak bases generally are not?
  • Does enhanced drug solubility through co-crystal formation imply that the co-crystal is thermodynamically unstable in the solid state?
  • What thermodynamic considerations should be kept in mind when formulating a co-crystal?
  • How does thermodynamics inform the design of slurry experiments on co-crystals?

Dr Richard Schartman
Physical Chemist
Bristol Myers Squibb

Exploration of the Physical-Chemical Properties of Co-Crystals, How to Control them and in Turn, Generate Effective Co-Crystal Formulations

14:45 Is Co-Crystal True Solubility Within Reach?

The importance of pharmaceutical co-crystals lies in the ability to engineer properties such as solubility, dissolution, bioavailability and stability. A key question that arises with these materials is: what is the true solubility of the co-crystal, and how does it correlate with its components and its performance? Some co-crystals transform to API crystals in the presence of water and deliberate efforts are required to prevent this transformation, while others remain in the co-crystal phase.This talk will present approaches that are valuable to predict co-crystal-solution phase behaviour and guide co-crystal selection without the time and material consuming requirements of traditional methods.

Participants will learn about:

  • Measurement of co-crystal solubility and eutectic points
  • Thermodynamic indicators of co-crystal solubility and stability
  • Mechanisms by which co-crystal solubility is enhanced
  • Importance of phase purity on co-crystal properties
  • Approaches to prevent co-crystal conversions

Naír Rodríguez-Hornedo
Associate Professor, Dept. of Pharmaceutical Sciences
University of Michigan

15:30 Networking Coffee Break

16:00 Determining The Relative Energies Of Formation Of Co-Crystals: An Investigation Into The Strengths Of Intermolecular Packing Forces

  • Exploring how measured heat of formation values correlate to the packing of a series of co-crystals
  • Determining the relative contributions of Van der Waals versus hydrogen bond forces to the heat of formation
  • Comparing the heat of formation to the Gibbs free energy of formation and observed kinetics of crystallisation
  • Comparing measured heat of formation values to those predicted by molecular mechanics modeling and applying relative energy data effectively during co-crystal formation

Dr Mark Oliveira
Scientist III
Alkermes

16:45 Surfaces And Defects In Organic Solids – Factors Influencing Stability/Reactivity And Successfully Achieving Stability In Co-Crystal Systems

While single crystal X-ray diffraction tells us much about the average bulk structure of an organic crystal (single and multi-component) we also need to appreciate that stability will be affected by the nature of the exposed crystal surfaces as well as any crystalline imperfections present in the solid. The talk will review:

  • The use of Atomic Force Microscopy and Transmission Electron Microscopy for examining pharmaceutical solids including co-crystals and single component materials
  • Examination of various systems along with best practice strategies for sample preparation
  • Consideration of how surfaces and defects may influence observed stability/reactivity and how to tackle the challenges presented by this

Professor William Jones
Head of Materials Chemistry Group
University of Cambridge

IP Update: Insights into the Exact Data Required During the Patenting of Co-Crystal Inventions and Exploring How the Requirements Differ Between Co-Crystals and Salts

17:30 Peculiarities Of Co-Crystals Inventions: An IP Update From The European Patent Office

  • Peculiarities of co-crystals inventions from patent law point of view
  • Characterisation of a co-crystal in a claim
  • Is the distinction from salts a problem?
  • Typical objections of a EP Patent examiner
  • Impact of European Patent Office’s case law in particular G 02/08
  • Hint for drafting co-crystal patent application claims and description

Mr Bertrand Gellie
Director
The European Patent Office (EPO)

18:15 Chairperson’s Closing Remarks And Close Of Day One