Bo t h J a v e                                                         “A	great	mix	of	academic	and	industrial	representat...
Dear	Colleague,                                                                                                           ...
Pre-Conference Workshop Day: Monday 26th September 2011                                                                   ...
Conference Day One: Tuesday 27th September 2011        08:00 Registration and Welcome Coffee                              ...
Conference Day Two: Wednesday 28th September 2011         08:00 Registration and Welcome Coffee                           ...
Pharmaceutical                                                                                                            ...
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Pharmaceutical CoCrystals agenda

  1. 1. Bo t h J a v e “A great mix of academic and industrial representations. ok ul up 15 d s & y 2 to an The conference gave me a good perspective on where Pa 01 yb 1 co-crystal development is outside my own company” Merck y €Presents the 6th Annual 50Pharmaceutical 0 Main Conference: 27th - 28th September 2011Co-Crystals 2011 Workshop Day: 26th September 2011 cated C o-Lo phousOptimising Co-Crystal; Screening, Characterisation and Scale- Amo r l with aceuticaUp to Improve Drug Properties For Commercial Development m Phar ials 2011 r MateAmsterdam, The NetherlandsOptimise co-crystal formulation and development into Insights from Key Senior Speakersyour R&D strategy with key insights on how to: Including:• Achieve co-crystal scale-up with practical manufacturing processes Mike Zaworotko, Professor and Chairperson, of API’s, brand new case study led by Peter Karpinski, Novartis University of South Florida • Evaluate co-crystal behaviour and identify critical variables in Dr Nair Rodriguez-Hornedo, Associate order to improve solubility, stability and bioavailability, learn how Professor, Department of Pharmaceutical to engineer these properties with Nair Rodriuez-Horendo, University of Sciences, University of Michigan Michigan Jane Li, Senior Research Fellow, Boehringer Ingelheim• Ensure successful crystal engineering to utlise co-crystals effectively in early development, discussion led by Mike Zaworotko, Dr Peter Karpinski, Senior Principal Fellow, University of South Florida Novartis • Assess the practicalities of patenting amorphous and co-crystal Danius Macikenas, Scientific Fellow, Vertex forms to secure your development designs, best practice advice Dr Ir. J.H. Ter Horst, Professor, Delft University given by Emmeline Marttin, European Patent Office of Technology Anette Jensen, Principal Scientist, Lundbeck Nico Niemiejer, Senior Director, Johnson & Plus, Don’t Miss 3 Brand New Workshops: Johnson A. Demystifying the Scale Up of Pharmaceutical Co-Crystals Barbara Spong, Principal Scientist, Pfizer Insights from Grahame Woollam, Senior Scientist, Novartis B. Co-Crystal Characterisation to Support Systematic Design for Synthesis, Formulation Clare Rawlinson-Malone, Senior Research and Product Development Investigator, BMS with Dr. Nair Hornedo-Rodriguez, University of Michigan - David Good, Bristol-Myers-Squibb and Barbara Spong, Pfizer David Good, Principal Scientist, Bristol-Myers Squibb C. Exploring Co-Crystals as New Opportunities in API Development Emmeline Marttin, Examiner, Pure and Applied Organic Chemistry, European Patent OfficeHighlights for 2011 Dr Grahame Woollam, Senior Scientist, • New for 2011: The first ever co-crystals manufacture case study led by Peter Novartis Karpinski, Novartis • More case studies than ever before! Insights from 9 leading Pharma companies Sitaram Velaga, Profess or in Pharmaceutics, Luleä Tekniska University • Brand new ice breaker and problem solving sessions giving you everything from basic introductions to the latest cutting edge research to really address your conference needs Jason Gray, Commercial Manager, University of Bradford +44 (0)20 7368 9300 +44 (0)20 7368 9301
  2. 2. Dear Colleague, nference. 6th Annual Pharma ceutical Co-Crystal Co unity to welco me you to Pharma IQ’sI want to take this opport ce and fine-tune the e of their ability to enhan due to the e pharmac eutical industry becaus growing interest is partly n and Co-crystals are o f increasing interest to th gs that are otherwise difficult to develop. This bsorptio soluble dru consequently limited aaqueous s olubility of inherently in have inadequate solubility and ation of amorphous, scovered drug candidates state has been commonly employed in the formfact th at 40 to 70 % of newly di g the so lid enhancement by alterin several advantages in tha t:bioavailability. Solubility rugs. Co-crystals have polymorphic, a nd salt forms of d nough to form salts, ugs are acidic or basic e er of drug m olecules since not all dr r than empirical approa ches, and; (1) Th ey apply to a large numb rystal en gineering principles rathe r interactions in solution. an be designed using c al sensitivity to molecula (2) Their composition c d because of the co-cryst (3) Drug deliv ery can be fine-tune ritically important. development becomes c characterizati on for their selection and d their response to environmental discovered, meaningful g on their components an p in identifying As new co-crystals are erties can exist, dependin edict co-crystal behaviour is an important ste Co-crystals with a w ide range of prop s. The ability to pr . erature, pH, and additive nd formulate co-crystals conditions such as temp synthesis, and the right additives to stabilise a tal the conditions for co-crys at address effective strat egies, underlying on se ssions, and workshops th velopment as e presentations, discussi d engineering for rapid de This conference will includ pts for co-crystal discovery, characterisation an once theoretical and practical c pharmace utical products. cterisation and -crystal discovery, chara ur exp eriences and ideas on co in September to share yo your own approach. We invite you to join us rtunities to improve or oppo development, and look f ting you there. We look forward to mee Kind regards, edo, “This conferen Dr Naír Rodríguez-Horn aceutical Sciences ce is perfect” Associate Profes sor of Pharm Avantium Te University of Michigan chnologies Sponsorship and Exhibition Opportunities The Pharma IQ Pharmaceutical Co-Crystals conference is the only Co-Crystals focussed conference in the world and therefore the perfect platform for leading service providers to meet senior-level decision makers in the pharmaceutical/biopharmaceutical industry implementing Co-Crystal designs into R&D formulation strategies. Contact Pharma IQ to discuss how to position your company in front of our participants who are keen to learn more about today’s solutions to some of the common challenges faced by formulators. For more information on sponsorship and exhibition opportunities contact our Sponsorship team on +44 (0)20 7368 9300 or About Pharma IQ Who should attend? Become a member of Pharma IQ and receive complimentary Senior Vice President, Vice President, Executive Director, access to resources that will keep you at the forefront of industry Director, Associate Director, Head and Principals of: change. • Formulation You will receive access to our growing library of multi-media • Preformulation presentations from industry leaders, an email newsletter updating • Analytical you on new content that has been added, free aggregated news • Solid State feed from over 1000 global news sources tracking your industry • CMC and special member only discounts on events. • Drug Discovery Become a member here: Web: • API Development “A very good balance between academic and industrial work on co-crystal application in Pharma industry. Very “Very good at giving me an idea of the co-crystal valuable due to the highly comprehensive coverage of landscape in preparation, application and legal fields” co-crystal issues applied in the pharmaceutical industry” Team Leader - Physical Sciences, Almac Sciences Haris Trobradovic, Head of Preformulation, Bosnalijek d.d. +44 (0)20 7368 9300 +44 (0)20 7368 9301
  3. 3. Pre-Conference Workshop Day: Monday 26th September 2011 ing Includ ing10:30 – 13:30 WORKSHOP A 13:45 – 17:00 WORKSHOP B 17:15 – 20:15 WORKSHOP C rk Netwo s DrinkDemystifying the Scale Up of Pharmaceutical Co-Crystal Characterization to Support Systematic Exploring Co-Crystals as New OpportunitiesCo-Crystals Design for Synthesis, Formulation and Product in API Development Development How does a Co-Crystal Differ from a Salt? Co-crystals have proven valuable toward improving • Insights into the enhanced physicochemical properties A pharmaceutical co-crystal is a unique physical form physicochemical and biopharmaceutical drug properties afforded through implementation of the co-crystal composed of an Active Pharmaceutical Ingredient and as well as increasing the design space for drugs that formulation routeone or more additional components. The additional are difficult to crystallize. For the systematic design, • Understanding the approaches that can be component is known as a co-former, it may be a different screening, synthesis, and selection of effective implemented to prepare co-crystals efficientlyAPI molecule or a small molecule that is generally pharmaceutical co-crystals there is a need to apply • Analytical techniques for the structural regarded as safe. fundamental descriptions of their solution behavior and characterisation of co-crystals and for stability. As cocrystal screening methods have been distinguished co-crystals from mixtures ofCo-Crystals differ from salts in the following way: implemented in development programs, a gap has componentsWith a salt, a proton is transferred from the acidic to been identified in developing efficient characterization • Assessing the development potential of co-crystals the basic functionality of the crystallisation partner, methods that enable form selection, formulation, process and best practice strategies to help realise their as the pKa difference between the ionisable species development, and scale-up activities. commercial potentialis sufficiently large - with co-crystals no such proton This workshop will introduce fundamental considerations • Understanding the advantage of co-crystals in transfer takes place. for describing the thermodynamic stability and solubility generating new IP compared to traditional formulations of co-crystals and case studies that emphasize Sponsorship opportunity: for more informationWhat is the Benefit of a Co-Crystal Over a Salt? characterisation techniques relevant to solution phase contact or phone +44It has been estimated that approximately half of all API behavior, formulation, and material properties. (0)20 7368 9300that have been developed were ultimately progressed as salts; salt formation is considered an integral part of the Participants will learn about:development process. Co-crystals have the potential to • Meaningful indicators of co-crystal solubility and Media Partnersmodify the properties of both ionisable and non ionisable thermodynamic stability compounds. • How to measure eutectic points to describe co-crystal/ solution equilibria and their utility for constructing Recent studies showed how the position of the proton can phase diagrams and calculating solubility be delocalised i.e. mixed character of salt and co-crystal. • Important considerations for the design and scale- Furthermore, it has been shown that in some cases the up of crystallisation protocols ionisation state of the components may not affect the • How to evaluate the influence of excipients on co- physical properties of interest. crystal solubility and thermodynamic stability • Approaches for assessing the manufacturability Why is the Scale Up of Co-Crystals Considered to of co-crystals in oral solid dosage forms, such as be Challenging? materials characterisation tools (physical and With this in mind one can wade through the mechanical properties) and monitoring of physical mystical minefield of co-crystals and consider the stabilitymulticomponent systems as salts, and therefore prepare, process, profile and develop such chemical entities. 14:00 – 15:00 Dr Naír Hornedo-Rodriguez, Professor, University of MichiganWhat Participants will Learn: Naír Rodríguez-Hornedo is Associate Professor of Pharmaceutical Sciences at the University of• A case study will be discussed where co-crystals Michigan and was co-founder of the Pharmaceutical were prepared at increasing scales to 50g by a Engineering Program. Dr. Rodríguez has developed a seeded cooling crystallisation; then tested for stability, research program based on a molecular-mechanistic compatibility and therefore developability approach, founded on the premise that the concepts• The presentation will consider the design of co-crystal can be applied to: (i)ofdesign novel pharmaceutical materials with desirable supramolecular chemistry and crystal engineering screening through to the experiments which should be composition, structure and properties, and (ii) to understand crystallization performed to establish a robust crystallisation pathways and solid phase transformations that are important in controlling• If the favourable physical properties of a pharmaceutical processes and outcomes. In 2005 Dr. Rodríguez was awarded the Ebert Prize for the best article published in the Journal of multicomponent system allow selection for Pharmaceutical Sciences. Dr. Rodríguez has served on the FDA Advisory development, the position of a proton or indeed Committee for Pharmaceutical Sciences. She serves on the editorial the ionisation states of the chemical entities should be boards of the Journal of Pharmaceutical Sciences and the Encyclopedia of irrelevant Pharmaceutical Technology.Grahame Woollam, Senior Scientist, Novartis 15:00 – 16:00 David Good, Research Investigator,Grahame Woollam studied at The University of Liverpool obtaining a BSc Bristol-Myers-Squibbin Chemistry with Pharmacology and an MSc in Process Research & David is a research investigator for Bristol Myers-Squibb in New Brunswick, NJ. David has focused on the rationalDevelopment. Having gained an interest in polymorphism and crystallisation design of co-crystals and contributed toward methods toGrahame then worked as part of the Solid Form Sciences group at GSK measure and predict co-crystal solubility as part of hisStevenage for three years where he developed his expertise in this field. studies at the University of Michigan in Naír Rodríguez-Grahame is currently in his fourth year as a senior scientist in Chemical Hornedo’s laboratory. At BMS, David has continued& Pharmaceutical Profiling at Novartis Horsham where his work involves to pursue fundamental solution models to advancesynthesising and characterising physical forms of API in addition to .co-crystal characterization and formulation.preformulation. 16:00 – 16:30 Coffee BreakGrahame specialises in crystallisation and scale up with an avid interestin salt formation and cocrystallisation. His current projects focus on 16:30 – 17:30 Barbara Spong, Principal Scientist,gastrointestinal and respiratory disease areas, which generate molecules that Pfizerare inherently difficult to crystallise and formulate; engineering the physical Barbara Rodríguez Spong received her Bachelor ofform is often a prerequisite for their development. Science degree in Pharmacy from Rutgers University at New Brunswick, NJ (1998) and a Ph.D. in Pharmaceutics from the University of Michigan at Ann Arbor, MI (2005). The focus of her thesis was in solid state chemistry, studying the optimization of the pharmaceutical properties of poorly soluble drugs using alternate solid forms such as co-crystals and mesophases. She is currently a Principal Scientist at Pfizer, Inc in Pharmaceutical Development at Groton, CT responsible for solid dosage form design of Phase 3 and commercial drug products. +44 (0)20 7368 9300 +44 (0)20 7368 9301
  4. 4. Conference Day One: Tuesday 27th September 2011 08:00 Registration and Welcome Coffee 12:05 Ensuring Patenting Designs: Worst Case Scenarios & Best Practice ined Strategies Comb with n 08:50 Pharma IQ Welcome and Chairperson’s Opening Address sessio hous Discuss the importance of regulatory compliance when filing IP requests Amorp utical Dr Naír Hornedo-Rodriguez, Department of Pharmacy, University of Michigan, from Industry and regulatory perspectives ace Pharm Forum Ensuring Successful Co-Crystal Design with Effective Behavioural • Discuss the factors involved with ensuring a successful patenting request Materials Characterising Techniques • Learn best practice strategies 09:00 Opportunities and Challenges of Co-Crystal APIs in Pharmaceutical • Defining amorphous forms, what makes something amorphous and in Development patenting terms * Is a solid solution amorphous? ssion In recent years, co-crystals have emerged as alternative and promising * What about nano crystalline? Discu n sive o Sessi crystalline forms of APIs. Co-crystals are crystalline molecular complexes of a Exclu dy • Address the latest issues looking to the future of using amorphous or tu therapeutic agent and guest molecule(s), i.e. multi-component APIs. These C ase S co-crystal forms to reformulate existing drugs for new patenting claims crystalline solids offer attractive options for improving physicochemical properties of APIs to enhance and enable drug product development. Facillitated by: The challenges associated with developing co-crystals range from chemical Emmeline Marttin, Investigator, manufacturing in controlled crystallization to formulation development in Pure and Applied Organic Chemistry, EPO processing and stability. Similar to salts, co-crystals have propensity to Panelists: disproportionate, leading to decreased solubility. In addition, there are Nico Niemeijer, Senior Director, Johnson & Johnson potential risks of co-crystal physical stability in manufacturing and storage of Jason Gray, Commercial Manager, University of Bradford drug products. In this presentation, case studies are used to demonstrate strategies to overcome the challenges in developing co-crystal APIs. 12:30 Networking Lunch Break • General concepts of multi-component APIs and characteristics • Solubility behaviors of co-crystals/salts 13:30 Engineering Co-Crystal Solubility and Streamlining Co-Crystal Early Development or New F • Case study 1: Chemical manufacturing of co-crystal API: controlled crystallisation Understanding how co-crystal solubility is influenced by co-crystal • Case study 2: Formulation development of co-crystal API: stability challenges components and environmental conditions is essential to engineer 20 11 Dr Jane Li, Sr. Research Fellow, Boehringer Ingelheim Pharmaceuticals, US co-crystals with customised solubility and streamline co-crystal development. This talk will present: 09:45 Ensuring Successful Crystal Engineering of Multi-Component Solids • Meaningful characterisation methods to guide co-crystal and additive The emergence of pharmaceutical co-crystals has facilitated the generation of selection without the time and material consuming requirements of a wide range of new crystal forms of API’s with changed physicochemical traditional methods For New properties. • Key indicators of co-crystal solubility and thermodynamic stability It is therefore unsurprising that they have quickly become a fixture at the • Overcoming the barriers in co-crystal stability by fine-tuning co-crystal/ 2011 preformulation stage of drug development. However, this does not mean olution behaviour that crystal engineering can be readily applied to other classes of multi- • Critical analysis of co-crystal pHmax and co-crystal surfactant interactions to component solids such as simple salts and hydrates or that co-crystal highlight key issues on additive selection discovery is routine. This presentation will address several concepts from Dr Naír Rodriguez-Hornedo, Dept of Pharmaceutical Sciences, University of crystal engineering and participants will learn about the following: Michigan • What is a supramolecular synthon? Supramolecular synthons are key to rationalising the crystal structures of molecular solids and are therefore 14:15 Applying solubility models and eutectic measurements for efficient useful tools to make new compounds, especially co-crystals. The concept corcrystal characterization and development of supramolecular synthons will be explained and several case studies will Directly measuring the thermodynamic solubility of many cocrystals may be be detailed. difficult as their high solubility can lead to supersaturation and subsequent • Why are hydrates the nemesis of crystal engineering? Hydrates are ubiquitous phase transformations to less soluble forms. Characterizing cocrystal solution in solid-state chemistry and are frequently formed adventitiously. However, the phase behavior and solubility is essential to their utility and the design of nature of the water molecule means that it is promiscuous in terms of its screening, synthesis, and development strategies. This talk will present: supramolecular synthons and therefore highly challenging to a crystal engineer. • Efficient methods to characterize cocrystal solution phase behavior using • How to choose a co-crystal former library. Whereas carboxylic acids are eutectic points (i.e. isothermal invariant points) most typically used as cocrystal formers this does not mean that they are • Models for predicting the thermodynamic stability and solubility of cocrystals likely to work. Some new ideas about co-crystal former libraries will be • Strategies to evaluate the effect of additives on cocrystal stability and presented. solubility Mike Zaworotko, Professor, Department of Chemistry, University of David Good, Research Investigator, Bristol-Myers Squibb, US South Florida 15.00 Networking Coffee Break 10:30 Ice Breaker Session Conferences bring about the perfect opportunity to network with peers and 15:30 Technology Spotlight Session benchmark on solutions to key challenges. If you have the latest innovative technology or service in the market and would aker What are the take-home messages you hope to gain over the course of the Ic e Bre conference? like showcase your solution in front of senior industry figures and heads of sion Ses labs, then Pharma IQ’s Pharmaceutical Co-Crystals 2011 can provide you with What key challenges do you hope to overcome? the perfect opportunity. In a saturated market the pressure is on for everyone Formulate an outline of all the key issues you wish to be addressed during the to push compounds into the next stages of development ahead of the conference, discuss as a group and feedback to the conference chair. competition. The world’s only Co-Crystal conference offers you the unique At the end of day 2 results and concluding strategies will be assessed. chance to demonstrate your solution meets the challenge. Facilitated by Conference Chair For more information on sponsorship and exhibition opportunities 10:50 Networking Coffee Break contact sponsorship on +44 (0) 20 7368 9300 or Maximising Patent Opportunities with Novel Co-Crystal Designs 16:15 Choosing the Best Physicochemical Characterising Techniques; 11:20 Assessing the Practicalities of Patenting Amorphous and Co-Crystal Distinguishing Between Salts and Co-Crystals Forms to Secure Your Development Designs ined This panel will focus on the screening and physico-chemical PanelComb w h Securing a patenting request is vital to ensuring progression of formulation n n it designs when forming both co-crystal and amorphous forms to enhance characterisation of salts and co-crystals, including co-crystals Sessiosessio hous of carboxylic acids and polymorphism. An open discussion with your Amorp utical necessary drug properties or reformulate exisitng drugs to file new patent ce chance to ask the speakers questions and gain an understanding on some of P harma Forum requests. This interactive talk will expose you to the patenting application Materi als the basic and more advanced characterisation tools and features, including: process giving you the opportunity to raise questions, assess latest case • Using X-ray crystallography to understand co-crystal structures (hydrogen studies and ensure your IP applications when filing amorphous or co-crystal bonding, short intermolecular contacts) patent claims. • Interpretation of chemical and physical properties from the crystal structure • Preparing and presenting an amorphous patent claim • Implementing NMR solid-state analysis to understand co-crystal properties • Exploring the definition of amorphous and utilising this to form the right Facilitated by: Anette Jensen, Principal Scientist, Lundbeck patent claim, avoiding complications Panelists: Peter Karpinski, Sr Research Fellow, Novartis • Overcoming typical approval objections to patent applications and taking Dr Naír Rodriguez- Hornedo, Professor, University of Michigan steps to avoid complications Dr Jane Li, Senior Research Fellow, Boehringer Igelheim • Useful hints and tips for drafting a patent application claims form Emmeline Marttin, Investigator, Pure and Applied Organic Chemistry, EPO 17:00 Chairperson’s Closing Remarks and Close of Day One +44 (0)20 7368 9300 +44 (0)20 7368 9301
  5. 5. Conference Day Two: Wednesday 28th September 2011 08:00 Registration and Welcome Coffee 12:30 Networking Lunch Break 08:50 Pharma IQ Welcome and Chairperson’s Opening Address change 13:30 Technology Spotlight Session If you have the latest innovative technology or service in the market to assist Achieving Co-Crystal Scale-Up with Practical Manufacturing Processes with co-crystal scale-up and manufacture, and would like showcase your 09:00 From Mortar & Pestle to Plant: Achieving Successful Scale Up and solution in front of senior industry figures and heads of labs, then Pharma Manufacture of API Co-Crystals IQ’s Pharmaceutical Co-Crystals 2011 can provide you with the perfect Scale-up of API co-crystals is not a straightforward process due to the fact opportunity. In a saturated market the pressure is on for everyone to push OT E that hydrodynamics, mixing, and co-crystallisation kinetics scale up in a compounds into the next stages of development ahead of the competition. KEYN N nonlinear and dissimilar fashion. Scale-up itself should be seen in a The world’s only Co-Crystal conference offers you the unique chance to S ESSIO context of the entire process: the success at large scale is an effect of well- demonstrate your solution meets the challenge. For more information on sponsorship and exhibition opportunities contact designed experiments and thorough API co-crystal characterisation carried sponsorship on +44 (0) 20 7368 9300 or out at the bench scale. This talk includes: • Successful manufacture of API co-crystals in a correct polymorphic form 14.15 Interactive Roundtable Discussion; ‘Two Heads are Better Than One’ meeting prescribed specifications requires a thorough understanding of API This is your chance to discuss key topics and challenges in smaller groups. co-crystal properties and in-depth knowledge of co-crystallisation and Attendees will be able to share their own experiences and hear those of others, downstream processing unit operations, as well as significant scale up efforts exchange ideas and get clear answers to specific questions. So, in order to make the most of these interactive sessions, participants should come armed • Whenever practicable, for API manufacture, a seeded, cooling co- and ready to share their own experiences and have clear questions they need crystallisation is typically considered as the most desirable approach answers to.Either bring your questions with you on the day, or submit in • The supersaturation profile has a profound effect on the nucleation and advance to: growth processes and the resulting particle size distribution of co-crystalline • API and its control during co-crystallisation is necessary Choose from the following: In the four common batch co-crystallisation operations: cooling co- A) Overcoming Challenges with Co-crystal Disassociation Attendees will share their experiences and problem solving strategies in a crystallisation, reactive co-crystallisation, antisolvent co-crystallisation, and guided discussion on avoiding co-crystal disassociation. This roundtable will evaporative co-crystallisation - subsequent control of the co-crystal growth focus on the scientific application of methods and technologies used to chose stage may be realised by employing appropriate time-profiles for cooling the right co-former and prevent co-crystal disassociation rate, reagent addition rate, antisolvent addition rate, and evaporation rate, Facilitated by: Sitaram Velaga, Professor in Pharmaceutics, Luleä respectively Tekniska Universitet • Case study examples illustrate the progress that has been made in the pharmaceutical industry in the monitoring and control of co-crystallisation of APIs B) Implementing Co-Crystals into Your R&D Strategy Dr Peter Karpinski, Principal Research Fellow, Novartis Half the challenge with co-crystal implementation is convincing the powers above that pharmaceutical co-crystals are a viable option form for enhancing necessary drug properties. This roundtable will focus on strategies utilised to 09:45 Manufacturability and Physical Stability of Pharmaceutical Co-Crystals highlight the benefits of co-crystals as Solid Dosage Forms Facilitated by: Barbara Spong, Principal Scientist, Pfizer A series of co-crystals have been evaluated following milling, tableting, and aqueous film coating to monitor for process-induced changes C) Looking to Scale-Up; How to Achieve Production on a Manufacturing Scale Exc lusive Manufacturing co-crystals to scale is the current hot topic for industry and tudy (ie, co-crystal dissociation). The mechanical properties and tableting indices C ase S of co-crystal compacts were also determined relative to typical crystalline drug primary challenge for many developing co-crystal forms. This roundtable will substances and are presented for consideration in solid dosage form design. focus on the theoretical and practical tools behind designing and developing a co-crystal that can be produced on scale • Selection of pharmaceutical co-crystal forms with suitable physical and Facilitated by: Dr Grahame Woollam, Senior Scientist, Novartis chemical properties for drug product development • Examining the physical stability of co-crystals after mechanical processing D) Ensuring Co-Crystal Stability Throughout the Development Process • Identifying apparent trends in the mechanical properties of co-crystals Co-crystals are considered to be one of the favourable drug enhancement relative to typical crystalline drug substances forms due to the stability that can be optimised throughout development. This • Formulation and process development strategies for solid oral dosage forms roundtable will focus on maintaining stability whilst ensuring intrinsic solubility Barbara Spong, Principal Scientist, Pfizer and dissolution of co-crystal forms Facilitated by: Dr Nair Rodriguez-Hornedo, Associate Professor, Department of Pharmaceutical Sciences, University of Michigan 10:30 Networking Coffee Break 15.00 Networking Coffee Break 11.00 Successful Co-Crystal Engineering; Assessing Co-Crystallisation as a Separation Technology 15:30 Co-Crystals and Their Potential Application to the Drug Development Pipeline Over the last ten years there has been an increasing interest in the preparation This session will present how to exploit the thermodynamics of multi- of pharmaceutical co-crystals; typically to increase the dissolution rate and r ew Fo component chemical systems to come to new separation processes using ultimately bioavailability of an orally delivered drug. There will be a case study N multi-component solids such as co-crystals and organic salts. discussing such a multicomponent system, additionally and importantly 1 201 Since many pharmaceuticals are chiral, chiral separation techniques are however, this will cover the preparation of co-crystals of API for delivery by an important focus point for the pharmaceutical industry. A chiral separation by other routes; examples include inhalation and buccal cavity. To complement crystallisation often is complicated by the formation of a stable racemic the discovery and application of co-crystals, there will be a case study on the compound of the two enantiomers. The use of co-crystals in chiral separations scale up of co-crystals via seeded cooling crystallisation at 50 g; designed in will be discussed. just a few small steps from the original screening preparation method - for those who can not attend the workshop. It will be further shown that co-crystals facilitate In Situ Product Removal under To complete this presentation, there will be: conditions where crystallization of the pure component is not possible. • A case study revealing co-crystals prepared of model pharmaceutically active This presentation will cover: compounds at scale and tested as if completing a developability assessment • The co-crystal phase diagram of the physical forms • The various co-crystallisation methods • Including stress testing at temperature and humidity, milling, compression, • Co-crystallization in multicomponent systems excipient compatibility, solubility and dissolution. • Co-crystals to solve separation technology issues: In situ product removal Dr Grahame Woollam, Senior Scientist, Novartis & Chiral separations 16:15 Turning Your Design Approaches to Manufacturing Possibilities; Dr Joop H. ter Horst, Professor, Delft University of Technology Formulating the Right Structural Co-Crystal Designs Choosing the right co-formers and formulating the right co-crystal 11:45 Progress to Development Stages with Early Characterisation of the Right structural design can mean everything from developing an optimum Panel n Active Ingredient co-crystal to implementing designs to scale Sessio Taking your co-crystal from concept to delivery involves the optimisation of • Discuss the various methods of co-crystal screening and characterising many influencing factors, however the fundamental strategy to streamline co- available with our speaker panel and share your thoughts on the best • methods to take your compound from design conception right through to crystal formulation primarily starts with choosing the right active ingredient. product development This talk will cover: • Realise the potential of implementing co-crystals into development and • Adding value to co-crystal design by identifying the ‘right’ active ingredient the best practice measures of presenting and justifying design concepts to to advance into formulation phases secure development approval • Expediting time-to-market by understanding the screening methods available Facilitated by: Danius Macikenas, Scientific Fellow, Vertex to reduce time and cost spent on early stage characterisation Panellists: Dr Naír Hornedo-Rodriguez, University of Michigan • Understanding how effective early behavioural characterisation can influence Clare Rawlinson-Malone, Senior Research Investigator, Bristol Myers scale-up and manufacturing progression Squibb • Successfully utilising experimental models to find suitable solid co-crystal forms 17:00 Chairperson’s Closing Remarks and Close of Day Two Dainius Macikenas, Scientific Fellow, Vertex +44 (0)20 7368 9300 +44 (0)20 7368 9301
  6. 6. Pharmaceutical 5 WAYS TO REGISTER Co-Crystals 2011 Freephone: 0800 652 2363 or +44 (0)20 7368 9300 Fax: +44 (0)20 7368 9301 Main conference: Workshop Day: Location: 27th - 28th September 2011 26th September 2011 Amsterdam, The Netherlands Post: your booking form to IQPC Ltd. To speed registration, please provide the priority code located on the mailing label or in the box below. 129 Wilton Road, My registration code is PDFW London SW1V 1JZ Please contact our database manager on +44(0) 207 368 9300 or at quoting the registration code above to inform us of any changes or to remove your details. Online: Email: Join our LinkedIn group Team Discounts* IQPC recognises the value of learning in teams. Groups of 3 or more Pharmaceutical Co-Crystals 2011 booking at the same time from the same company receive a 10% discount. 5 or more receive a 15% discount. 7 receive a 20% discount. Only one discount available per person. PACKAGES Tick Book and pay by 15th July*** Book and pay by 12th August*** Standard Price Conference + 3 Workshops + Audio Recordings* €3,896+VAT €3,996+VAT €4,396+VAT Save €500 Save €400 Venue & Accommodation Conference + 2 Workshops + Audio Recordings** €3,347+VAT €3,447+VAT €3,747+VAT Save €400 Save €300 VENUE: TBC, Amsterdam, The Netherlands Conference + 1 Workshop + Audio Recordings** €2,798+VAT €2,898+VAT €3,098+VAT Save €300 Save €200 ACCOMMODATION: Overnight accommodation is not included in the registration fee. For updates on the venue and accommodation options, Conference + Audio Recordings* €2,249+VAT €2,449+VAT €2,449+VAT Save €200 please visit Roaming Pass (to Amorphous Pharma Materials) €199+VAT * Tick this box to opt out of full conference recordings (reducing price by €550) Free Online Resources ** Please select choice of workshop(s) A 6 B 6 C 6 *** To qualify for discounts, payments must be received by the early bird registration deadline. Early booking discounts are not valid inconjunction with any To claim a variety of articles, podcasts and other free resources please other offer. visit All above price are subject to Dutch VAT at 19%. VAT Registration # NL 807884728B01 Delegate Details Digital Conference On CD-ROM Please photocopy for each additional delegate A digital version of the conference proceedings, including all presentations, is available to buy. 6 Mr 6 Mrs 6 Miss 6 Ms 6 Dr 6 Other 6 I cannot attend the event, please send me the CD Rom priced at First Name Family Name £599 plus VAT Recent digital conferences available - £599 plus VAT each Job Title Tel No. 6 Preformulation and Formulation Summit - April 2011 Email 6 Lypholisation Europe - Jan 2011 6 Yes I would like to receive information about products and services via email 6 Pharmaceutical Co-Crystals 2010 Organisation 6 Amorphous Pharmaceutical Materials 2010 Nature of business 6 Please send me conference materials indicated above. Address 6 I have filled out credit card details below Postcode Country For further information Please call: 0207 368 9300 Telephone Fax or email: Approving Manager To search IQPC’s archived conference documentation Name of person completing form if different from delegate: visit: Signature I agree to IQPC’s cancellation, substitution and payment terms Special dietary requirements: 6 Vegetarian 6 Non-dairy 6 Other (please specify) Terms and Conditions Please indicate if you have already registered by Phone 6 Fax 6 Email 6 Web 6 Please read the information listed below as each booking is subject to IQPC Ltd standard terms and conditions. Return of this email will indicate that you accept these terms. Please note: if you have not received an acknowledgement before the conference, please call us to confirm your booking. Payment Terms: Upon completion and return of the registration form full payment is required no later than 5 business days from the date of invoice. Payment of invoices by means other than by credit card, or purchase order (UK Plc and UK government bodies only) will be subject to a €65 (plus VAT) per delegate processing fee. Payment must be received prior to the conference date. We reserve the right to refuse admission to the conference if payment Payment Method has not been received. IQPC Cancellation, Postponement and Substitution Policy: You may substitute delegates at any time by provid- Total price for your Organisation: (Add total of all individuals attending): ing reasonable advance notice to IQPC. For any cancellations received in writing not less than eight (8) days prior to the conference, you will receive a 90% Card Number: VISA 6 M/C 6 AMEX 6 credit to be used at another IQPC conference which must occur within one year from the date of issuance of such credit. An administration fee of 10% of the contract fee will be retained by IQPC for all permitted cancellations. No credit will be issued for any cancellations occurring within seven (7) days (inclusive) of the conference. 6666666666666666 In the event that IQPC cancels an event for any reason, you will receive a credit for 100% of the contract fee paid. You may use this credit for another IQPC event to be mutually agreed with IQPC, which must occur within one year Exp. Date: 6 6 6 6 Sec: 6 6 6 6 from the date of cancellation. In the event that IQPC postpones an event for any reason and the delegate is unable or unwilling to attend in on the rescheduled date, you will receive a credit for 100% of the contract fee paid. You may use this credit for another Conference code 11377.005 Name On Card: Signature: IQPC event to be mutually agreed with IQPC, which must occur within one year from the date of postponement. Except as specified above, no credits will be issued for cancellations. There are no refunds given under any circumstances. Billing Address (if different from below): IQPC is not responsible for any loss or damage as a result of a substitution, alteration or cancellation/postponement of an event. IQPC shall assume no liability whatsoever in the event this conference is cancelled, rescheduled or postponed due to a fortuitous event, Act of God, unforeseen occurrence or any other event that renders performance of this conference impracticable, illegal or impossible. For purposes of this clause, a fortuitous event shall include, City/County/Postcode Cheque enclosed for: € (Made payable to IQPC Ltd.) but not be limited to: war, fire, labour strike, extreme weather or other emergency. Please note that while speakers and topics were confirmed at the time of publishing, circumstances beyond the control of the organizers may necessitate substitutions, alterations or cancellations of the speakers and/or topics. By Direct Transfer: (Please quote 11377.005 with remittance advice) IQPC Bank details: HSBC Bank, 67 George As such, IQPC reserves the right to alter or modify the advertised speakers and/or topics if necessary without any liability to you whatsoever. Any substitutions or alterations will be updated on our web page as soon as possible. Street, Richmond, Surrey, TW9 1HG Sort Code: 40 05 15 Account No: 59090618 Discounts IBAN Code: GB98 MIDL 4005 1559 0906 18 Swift Code: MIDLGB22 All ‘Early Bird’ Discounts require payment at time of registration and before the cut-off date in order to receive any discount. Any discounts offered whether by IQPC (including team discounts) must also require payment at the time of registration. All discount offers cannot be combined with any other offer PAYMENT MUST BE RECEIVED PRIOR TO THE CONFERENCE 6 Please do not pass my information to any third party