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
50
Pharmaceutical
0
Main Conference:
27th - 28th September 2011
Co-Crystals 2011
Workshop Day:
26th September 2011
cated
C o-Lo phous
Optimising Co-Crystal; Screening, Characterisation and Scale- Amo
r l
with aceutica
Up to Improve Drug Properties For Commercial Development m
Phar ials 2011
r
Mate
Amsterdam, The Netherlands
Optimise co-crystal formulation and development into Insights from Key Senior Speakers
your 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 Office
Highlights 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
www.pharmacocrystals.com
+44 (0)20 7368 9300 +44 (0)20 7368 9301 enquire@iqpc.co.uk

2. Dear Colleague, nference.
6th Annual Pharma ceutical Co-Crystal Co
unity to welco me you to Pharma IQ’s
I 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 a
aqueous s olubility of inherently in have inadequate solubility and ation of amorphous,
scovered drug candidates state has been commonly employed in the form
fact 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 sponsorship@iqpc.co.uk
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: www.pharma-iq.com • 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 enquire@iqpc.co.uk

3. Pre-Conference Workshop Day: Monday 26th September 2011
ing
Includ ing
10:30 – 13:30 WORKSHOP A 13:45 – 17:00 WORKSHOP B 17:15 – 20:15 WORKSHOP C rk
Netwo s
Drink
Demystifying the Scale Up of Pharmaceutical Co-Crystal Characterization to Support Systematic Exploring Co-Crystals as New Opportunities
Co-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 route
one 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 efficiently
API 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 of
Co-Crystals differ from salts in the following way: implemented in development programs, a gap has components
With 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 potential
is 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 information
What is the Benefit of a Co-Crystal Over a Salt? characterisation techniques relevant to solution phase contact sponsorship@iqpc.co.uk or phone +44
It has been estimated that approximately half of all API behavior, formulation, and material properties. (0)20 7368 9300
that 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 Partners
modify 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 stability
multicomponent systems as salts, and therefore prepare,
process, profile and develop such chemical entities. 14:00 – 15:00 Dr Naír Hornedo-Rodriguez,
Professor, University of Michigan
What 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-Squibb
in 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 rational
Development. Having gained an interest in polymorphism and crystallisation
design of co-crystals and contributed toward methods to
Grahame then worked as part of the Solid Form Sciences group at GSK
measure and predict co-crystal solubility as part of his
Stevenage 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 advance
synthesising and characterising physical forms of API in addition to .co-crystal characterization and formulation.
preformulation.
16:00 – 16:30 Coffee Break
Grahame specialises in crystallisation and scale up with an avid interest
in 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 Pfizer
are inherently difficult to crystallise and formulate; engineering the physical Barbara Rodríguez Spong received her Bachelor of
form 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.
www.pharmacocrystals.com
+44 (0)20 7368 9300 +44 (0)20 7368 9301 enquire@iqpc.co.uk

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 sponsorship@iqpc.co.uk
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 Panel
Comb 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 Sessio
sessio 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 enquire@iqpc.co.uk

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 enquire@iqpc.co.uk
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: enquire@iqpc.co.uk
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 enquire@iqpc.co.uk

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 database@iqpc.co.uk quoting the registration
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Online: www.pharmacocrystals.com
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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 www.pharmacocrystals.com
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 www.pharmacocrystals.com
All above price are subject to Dutch VAT at 19%. VAT Registration # NL 807884728B01
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6 I cannot attend the event, please send me the CD Rom priced at
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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
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