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        4th
Improving                                                                                                March 29-31, 2010
                                                                                                         Philadelphia, PA

                                                                                                         Uncovering Novel Advances in


Solubility                                                                                   TM
                                                                                                         Enhancing Solubility, Amorphous
                                                                                                         Forms, Bioavailability & Lipid-
                                                                                                         Based Formulation of Drugs



Learn Best Practice Strategies on How to:

•   Make development of an insoluble drug candidate possible by using solid dispersions
•   Approach parenteral delivery of poorly soluble drugs
•   Utilize pharmaceutical co-crystals to enhance solubility and dissolution of insoluble APIs
•   Effectively understand the difference between thermodynamic vs. kinetic stability
•   Maximize exposure of water-insoluble drugs in toxicology evaluation and early
    formulation development
•   Enhance the bioavailability of poorly soluble compounds using lipid-based formulations


Conference Co-Chairs:
             Ron Liu, PhD MBA                                          Michael Pikal, PhD
             President & Chief Executive Officer                       Professor and Pfizer Distinguished
             AustarPharma                                              Chair, Pharmaceutical Technology,
                                                                       University of Connecticut

Speakers Include:
•
    Naír Rodríguez-Hornedo, PhD, Associate              •
                                                            Satej Bhandarkar, PhD, Senior Manager, Analytical Sciences
    Professor of Pharmaceutical Sciences, The College       Department, Sanofi-Aventis U.S.
    of Pharmacy, The University of Michigan             •
                                                            Jaymin Shah, PhD, Research Fellow, Parenteral Development
•   Harry G. Brittain, PhD, FRSC, Institute Director,       Centre of Emphasis, Pfizer, Inc.
    Center for Pharmaceutical Physics                   •   Yun Alelyunas, PhD, Principal, Scientist I, Head of Physical
•   René Holm, PhD, Head, Preformulation,                   Properties Team, AstraZeneca
    H. Lundbeck Denmark                                 •   Feng Qian, PhD, Senior Research Investigator, Bristol-Myers Squibb
•   M. Sherry Ku, PhD, Senior Director,                 •   Xiaoming (Sean) Chen, PhD, Drug Product Development & Manufacturing, OSI
    Pharmaceutical Development, Pfizer, Inc.                Pharmaceuticals, Inc.
•   Robin H. Bogner PhD, Associate Professor of         •   Vivian Bi, PhD, Associate Principle Scientist, Early Development, PAR&D,
    Pharmaceutics, School of Pharmacy,                      AstraZeneca
    University of Connecticut                           •   Yaling Wang, PhD, Research Fellow, Merck & Co.
                                                        •   Jeffrey Skell, PhD, Director, DMPK & Pharmaceutics, Drug and Biomaterial R & D, Genzyme Corporation


Sponsors:                                                                        Media Partners:
                                                                                                    Driving the Industry Forward   www.FuturePharmaUS.com




               1-800-882-8684 • www.improvingsolubility.com
Who will you meet at
             4th                                                                                                     the conference?



    Improving
                                                                                                                     Chief Scientific Officers, Vice
                                                                                                                     Presidents, Directors, Heads,
                                                                                                                     Scientists, Chemists, Research
                                                                                                                     Leaders/Fellows/Advisors, &
                                                                                                                     Managers specializing in:
                                                                                                                     •   Formulation




    Solubility
                                                                                                                     •   Pre-Formulation
                                                                                                           TM        •   Discovery R&D
                                                                                                                     •   Preclinical Development
                                                                                                                     •   Analytical Development
                                                                                                                     •   Drug Delivery
                                                                                                                     •   Drug Discovery
                                                                                                                     •   Medicinal Chemistry
                                                                                                                     •   Analytical Chemistry
     March 29-31, 2010 Philadelphia, PA                                                                              •   Chemical Development
                                                                                                                     •   Product Development
                                                                                                                     •   Toxicology
                                                                                                                     •   Pharmaceutics
         Dear Colleague,
                                                                                                                     •   Physiochemistry
         Improving drug solubility is one of                                                                         •   Chemical Engineering
                                             the biggest challenges for pharmac
         they are always looking for new strat                                     eutical companies as              •   Solid States
                                               egies to increase bioavailability of
                                                                                    new drugs.                       •   Process R&D
         Building on the success of last year
                                               ’s event, IQPC’s 4th Improving Solu
        back by popular demand. With an                                            bility conference is
                                              ever increasing number of poorly
        to market, pharmaceutical and biote                                      soluble drugs coming
        solutions to maximize the time-to-m
                                                 ch companies are looking for ways
                                                                                     to adopt novel             Sponsorship and
                                                 arket on their drug development pipe
        the latest solubility strategies and
                                             techniques to guarantee success in
                                                                                        lines. Discover         Exhibition Opportunities
        development pipelines.                                                    your drug
                                                                                                                Sponsorships and exhibits are excellent
                                                                                                                opportunities for your company to showcase
        You will hear over 18 in-depth sessi
                                                ons and case study examples inclu                               its products and services to high-level,
           • Nanocryst
                        alline drug-polymer solid dispersion                         ding:
                                                               s for poorly water-soluble drugs                 targeted decision-makers attending the 4th
           • The role
                       and function of solubility measure                                                       Improving Solubility conference. IQPC and
                                                          ment from a central laboratory in
             discovery                                                                         drug
                                                                                                                Pharma IQ help companies like yours achieve
          • Implicatio
                        n of BCS: Solubility and permeabi                                                       important sales, marketing and branding
          • Lipid-bas
                                                           lity class on drug formulation
                      ed drug delivery to effectively over                                                      objectives by setting aside a limited number of
                                                          come physical and biological barri
          • Oral lipid
                      -based formulations for the enhancem                                     ers
                                                                 ent of poorly soluble compound                 event sponsorships and exhibit spaces – all of
            delivery                                                                                            which are tailored to assist your organization
         • API cryst
                     al forms and their bioavailabilities                                                       in creating a platform to maximize its
         • Novel strat
                        egies for salt selection concerning                                                     exposure at the event and reach key decision
                                                              solubility enhancement, salt stability
           stabilization                                                                             and        makers in your field.

      Attend our pre-conference workshop                                                                        For more information on sponsoring or
                                             s which include “Biopharmaceutic
      the                                                                       al Considerations in            exhibiting at the 4th Improving Solubility
      Design of Oral Modified Release Drug                                                                      conference, please contact Mario Matulich
                                               Delivery Systems”, “Toxicology Form
      Development: Challenges and Solu                                               ulation                    at 212-885-2719 or sponsorship@iqpc.com.
                                         tions”, and “Enhancing Solubility
      Technology                                                             by Liposome
      For Water-Insoluble Drugs in Parentera
                                              l Application”, amongst other area
                                                                                  s.
     Additionally, benefit from industry                                                                           “Excellent networking and
                                         presentations from AstraZeneca, Merc
     Sanofi-Aventis, Bristol-Myers Squibb,
                                           Lundbeck, AustarPharma, and man
                                                                                 k, Novartis, Pfizer,              diverse sessions, good to
     pharmaceutical, biotech and acad
                                        emic experts. This conference prom
                                                                                y more                             have theoretical discourse.”
     networking and discussion-filled even                                  ises to be a
                                           t leaving you with new ideas and                                        - Dr. Jeff Skell, Director, DMPL and
     you maximize and enhance your drug                                        solutions to help                   Pharmaceutics, Genzyme
                                            -solubility boundaries.
     We look forward to seeing you in                                                                              “Very good! Great mix of
                                      Philadelphia in March!
     Best Regards,
                                                                                                                   details (technical) plus
                                                                              ghly                                 examples.”
                                                       P.S Don’t miss the hi
                                                                               ative                               - Dr. Debra Walker, Research Fellow,
                                                       interactive and inform s!                                   Merck & Co.
                                                                              hop
                                                       pre-conference works
     Simon Curtis
     Senior Conference Director, Pharma
                                                                             s.                                    “Great networking and
                                                        See page 3 for detail
                                        IQ
     Simon.curtis@iqpc.com                                                                                         discussion sessions.”
                                                                                                                   - Dr. Ly Phan, Senior Director,
                                                                                                                   Medicinal Chemistry, Enanta
                                                                                                                   Pharmaceuticals
2   1-800-882-8684 • www.improvingsolubility.com
Pre-Conference Workshops
    Monday, March 29, 2010
    A
                8:30 – 11:30 (Registration at 8:00)

                Challenges and Opportunities in Controlling Drug Substance Properties
    In order to control drug substance (DS) properties one has to select an optimal form       What will be covered:
    (specific polymorph or hydrate of free form, salt, or co-crystal) and be able to           • Why investigate the solid-state of your drug?

    consistently manufacture it with the same particle size (PS), particle size distribution   • Polymorphism

    (PSD), and crystal surface attributes.                                                     • Addressing polymorphism: Screening and characterization

                                                                                               • Crystallization of difficult-to-crystallize materials
    The use of automated and robotic systems in salt/co-crystal and polymorph                  • Selection of optimum solid form of drug substance
    screening, and in early crystallization development experimentation, facilitates DS        • Chiral material analysis
    form selection. Ultimate properties of DS are largely determined by the way the            • Drug substance specifications
    batch precipitation or crystallization processes are conducted and to obtain
    crystalline material of desired properties consistently, these processes must be           Benefits of attending:
    carefully controlled. This can be accomplished via in-situ seeding that simplifies the     • Understand best strategies for selecting an optimal form to control drug substance

    design and control of batch precipitation/crystallization and gives the results            • Weigh the pros and cons of different automated screening systems

    comparable with the conventional seeding approach. Continuous                              • Discover the benefits of in-situ seeding for batch design and control

    precipitation/crystallization removes the risk of batch-to-batch variability and ensures   • Display methods and techniques for reducing risk of batch-to-batch variability

    an optimal control of PS, PSD, and particle surface attributes.
                                                                                               Your Workshop Leader:
                                                                                               Peter Karpinski, PhD, US Leader of Salt & Polymorphism and Particle Engineering
                                                                                               Networks, Novartis Pharmaceuticals Corp



    B
                11:30 – 2:00 (Registration at 11:00) Lunch Included

                Biopharmaceutical Considerations in the Design of Oral Modified Release Drug Delivery Systems
    This workshop will highlight biopharmaceutical factors that must be considered in          •   Discussing issues related to insoluble drugs and or highly soluble drugs based on
    the design, evaluation and development of modified release dosage forms. It will               BCS system
    include hydrophilic matrices, osmotic pump and multi-unit delivery systems. The            •   Identifying drug release mechanisms and methodologies in connection with IVIVC
    influence of electrolyte concentration and polymer character, drug properties on the
                                                                                               Benefits of attending:
    textural and micro-environmental conditions within delivery systems relative to the        • Uncovering a series of fundamental considerations in oral modified release drug
    conditions of gastro-intestinal tract, drug release and absorption will be discussed.
                                                                                                 delivery systems
    Examples for each class of drug based on their BCS (Biopharmaceutical Classification       • Discovering many novel drug release mechanisms and methodologies applied in
    System) scheme will be presented and relative influence of formulation design,
                                                                                                 their evaluation
    transit time and GI physiology on absorption and bioavailability in the context of         • Specific case studies will be used to illustrate textural properties of delivery systems
    IVIVC will be discussed.
                                                                                                 relative to the GI environment
    What will be covered:
    • Displaying the influence of electrolyte concentration and polymer character
                                                                                               Your Workshop Leader: Reza Fassihi, Ph.D, AAPS Fellow, Professor of
    • Uncovering delivery system textural properties
                                                                                               Biopharmaceutics and Industrial Pharmacy, Temple University



    C
                2:30 – 5:00 (Registration at 2:00)

                Toxicology Formulation Development: Challenges and Solutions
    Toxicology formulation is an essential component of drug development to enable             •   Review on toxicology formulations in NDA filing of marketed drugs
    successful toxicology study of new drug candidate. The requirement for adequate            •   Novel formulation technologies to enhance exposure in toxicology species
    exposure at high doses to establish a safety window often imposes formulation
                                                                                               Benefits of attending:
    challenges to poorly soluble compounds. Novel formulation technologies and                 • Basic procedures and general considerations of toxicology formulation development
    excipients may be required to achieve the exposure target. However, a balance              • Learn safety of common and novel excipients
    between implementing novel formulation technologies and controlling the safety             • Broaden the knowledge of acceptable toxicology formulations
    risk of excipients needs to be considered.                                                 • Understand what a toxicologist needs from a toxicology formulation

    What will be covered:                                                                      • Learn novel formulation technologies that solve exposure limit of poorly soluble

    • Toxicology formulation development: basic procedures and general considerations            compounds
    • Excipient acceptance criteria in toxicology formulation

    • Toxicology formulation development from a toxicologist perspective
                                                                                               Your Workshop Leader: Chong-Hui Gu, PhD, Associate Director, Pharmaceutical
                                                                                               Development, Vertex Pharmaceuticals



    D
                5:30 – 8:00 (Registration at 5:00) Dinner Included

                Enhancing Solubility by Liposome Technology for Water-Insoluble Drugs in Parenteral Application
    Liposomes are unique as drug carriers in that they can encapsulate drugs with              •   Process consideration and manufacturing scalable batches
    widely varying polarities. Hydrophilic drugs can be entrapped in the aqueous spaces        •   Injectable liposomal formulation development for water-insoluble drugs – case
    while lipophilic drugs can be incorporated into the lipid membranes. Using a                   study of an latest FDA-approved product
    liposomal formulation can dramatically increase the apparent aqueous solubility of a
                                                                                               Benefits of attending:
    lipophilic drug, making possible delivery of a dose much higher than its water             • Understand the basic concepts of phospholipids, bilayer structures and liposomes
    solubility. A stable liposomal formulation entrapped water-insoluble drug is often         • Learn how to develop liposomal formulations based on bilayer structure and
    achievable without precipitation upon dilution. Scalable manufacturing of liposomes
                                                                                                 physicochemical properties of compounds
    is challenged, but process development and optimization can usually overcome               • Learn the process development of liposomes
    some scale-up issues. A case study of the latest FDA-approved marketed product             • Learn the aseptic process of liposomal formulations
    will be discussed during the session.                                                      • Understand what a formulator needs to know the key parameters in scalable

    What will be covered:                                                                        liposomal manufacturing
    • Basic procedures and general considerations of liposomal formulation                     • Learn how to take advantage of drug-delivery technologies to develop quality

      development                                                                                based improved products to the marketplace
    • Excipient acceptance criteria in liposomal formulation
                                                                                               Your Workshop Leader: Ron Liu, PhD MBA, President & Chief Executive Officer,
                                                                                               AustarPharma
3   1-800-882-8684 • www.improvingsolubility.com
Main Conference Day One
    Tuesday, March 30, 2010
    7:30    Registration and Coffee                                                        12:15   Networking Lunch
    8:25    Welcome Address and Chairperson’s Opening Remarks                              1:15    Pharmaceutical Co-Crystals: A Solubility Perspective
                   Ron Liu, PhD MBA                                                                • Understanding the pharmaceutical co-crystal concept
                   President & Chief Executive Officer                                             • Utilizing pharmaceutical co-crystals to enhance solubility and dissolution
                   AustarPharma                                                                      of insoluble APIs
                                                                                                   • Discussing mechanisms by which co-crystal solubility is enhanced

    8:30    Opening Keynote Presentation: Thermodynamic vs.                                        • Examining co-crystal structure-solubility relationships

            Kinetic Stability: Knowing Which is Which                                              • Identifying the PK impact

            • Understanding the distinction between thermodynamic and kinetic                      • Analyzing literature case studies

              stability                                                                            Naír Rodríguez-Hornedo, PhD, Associate Professor of Pharmaceutical
            • Exceeding the equilibrium solubility to give a supersaturated solution               Sciences, The College of Pharmacy, The University of Michigan
            • Measuring equilibrium solubility and metastable solubility within a

              substance                                                                    2:00    Amorphous Dispersion Approaches for Achieving
            • Knowing accurately if and when the substance is metastable or                        Rapid Onset for Orally Administered Low-Solubility
              undergoing a change                                                                  Compounds
            • Recognizing when equilibrium solubility is actually a consequence of                 • Outlining the need for increased solubility and rapid absorption
              kinetic solubility                                                                   • Assessing the impact of enteric dispersions on absorption rate
            Harry G. Brittain, PhD, FRSC, Institute Director, Center for                           • Developing rapidly dissolving amorphous formulations

            Pharmaceutical Physics                                                                 • Pursuing formulation and process development for amorphous drug-

                                                                                                     polymer nanoparticles
                Solid Dispersion in the Development Stage                                          David Lyon, PhD, Vice President, Physical and Biological Sciences, Bend
                                                                                                   Research, Inc.
    9:15    Demonstration of Bioavailability Enhancement
            Through the Use of Biorise and Diffucaps Technologies                          2:45    Afternoon Networking Break
            Biorise®
            • Displaying the production, stabilization and characterization of             3:30    Panel Discussion: How to Effectively Formulate Poorly
              amorphous and nanocrystalline composites                                             Soluble Drugs
            • Preclinical demonstration of efficacy                                                • Nanoparticles
            • Clinical demonstration of efficacy                                                   • Amorphous forms
            Diffucaps®                                                                             • Salt selection: Suitable salt properties for later stage development: stability,

            • Discussing the production of bioavailability-enhanced extended release                 solubility, purity, etc.
              formulations using control of pH microenvironments                                   •  Polymorphs: Screening and characterization
            • Clinical demonstration of efficacy                                                   • Cyclodextrins: Toxicology and pharmacokinetic properties and uses in

            • Mathematical modeling of pharmacodynamic response                                      development
            Troy Harmon, Vice President, Business Development, Eurand                              • Assessing permeability and solubility

                                                                                                   Jeffrey Skell, PhD, Director, DMPK, Genzyme Corp.
    10:00   Morning Networking Break
                                                                                                            Solubility and Discovery Techniques
    10:45   Nanocrystalline Drug-Polymer Solid Dispersions for
            Poorly Water-Soluble Drugs                                                     4:15    The Role and Function of Solubility Measurement from
            • Nanocrystalline drug-polymer solid dispersion was formed by co-spray                 a Central Laboratory in Drug Discovery
              drying drug and Pluronic or PEGs                                                     • Summarizing of solubility methods and practices
            • Nanocrystalline solid dispersion showed improved in vitro dissolution rate           • Evaluating kinetic vs thermodynamic solubility
              and in vivo exposure                                                                 • Comparing precipitation vs. aggregation aspects

            • Physical structure of the nanocrystalline solid dispersions was                      • Understanding the relationship of solubility and in vitro biology and DMPK

              characterized by PXRD, DSC, AFM and TEM                                                assays
            • Mechanism led to the formation of nanocrystalline solid dispersion                   • Discussing conclusions and recommendations

              formation was investigated                                                           Yun Alelyunas, PhD, Principal, Scientist I, Head of Physical Properties
            Feng Qian, PhD, Senior Research Investigator, Bristol-Myers Squibb                     Team, AstraZeneca

    11:30   Making Development of an Insoluble Drug Candidate                              5:00    Implication of BCS: Solubility and Permeability Class on
            Possible by Using Solid Dispersions: A Case Study                                      Drug Formulation
            • Displaying first in man studies of a highly insoluble compound with                  • Examining the importance of tailoring your formulation platform based
              micronized drug substance in capsules                                                  on BCS class
            • Exposure was very low and there was no dose-proportionality at low                   • Discussing the extension of BCS classification for formulation selection

              doses.                                                                               • Evaluating pH-solubility profile and modified solubility criteria

            • Evaluating multiple formulation strategies in a clinical study to obtain             • Comparing a Caco-2 in-vitro Permeability vs in-situ rat perfusion study

              adequate bioavailability to proceed with further clinical trials                     • Using BCS-based Formulation Decision Trees

            • Selecting for developing a solid dispersion with 20% drug load in HPMC               M. Sherry Ku, PhD, Senior Director, Pharmaceutical Development, Pfizer, Inc.
            • Describes the polymer selection, physicochemical characterization,

              formulation development, stability results, and testing strategy for the     5:45    Chairperson’s Closing Remarks and End of Day One
              solid dispersion product
            • Understanding the challenges associated with commercial development

            Satej Bhandarkar, PhD, Senior Manager, Analytical Sciences Department,
                                                                                           6:30    Networking Dinner
                                                                                                   Continue the networking experience by joining your colleagues for
            Sanofi-Aventis U.S.                                                                    a dinner following the end of day one. Separate booking necessary.
                                                                                                   We hope you will join us!


4   1-800-882-8684 • www.improvingsolubility.com
Main Conference Day Two
    Wednesday, March 31, 2010
    7:45    Registration and Coffee                                                                        • Understanding when to use lipid-based formulations - Compound suitability
                                                                                                             for lipid-based formulations
    8:25    Welcome Address and Chairperson’s Opening Remarks                                              • Recognizing how to suitably screen lipid-based formulations (formulation


                     Michael Pikal, PhD                                                                      screening flow & in vitro screening tests)
                                                                                                           • Displaying other unique challenges related to lipid-based formulations
                     Professor and Pfizer Distinguished Chair, Pharmaceutical Technology,
                     University of Connecticut                                                             Vivian Bi, PhD, Associate Principle Scientist, Early Development, PAR&D,
                                                                                                           AstraZeneca
    8:30    Opening Keynote: Strategies of Maximizing Exposure of
            Water-Insoluble Drugs in Toxicology Evaluation and Early                               12:15   Networking Luncheon
            Formulation Development
            Compounds optimized solely on the basis of receptor-based potency are usually                  Solubility Enhancement Techniques and Strategies
            hydrophobic and as a result, more than 40% of newly discovered drugs or NCEs
            are poorly water soluble or water-insoluble. In toxicological evaluation for water-    1:15    Approaches for Parenteral Delivery of Poorly Soluble
            insoluble drug candidates, maximizing the systemic exposure of these drug                      Drugs
            candidates is very critical, though the approach of solubilizing the drug in                   • Outlining the need for solubilization and limitations imposed by parenteral
            toxicological evaluation may not be relevant to the approach used for the final                  route of administration
                                                                                                           • Highlighting pre-formulation studies to determine the need and degree of
            finished product. This session will discuss some commonly and less commonly
            used solubilization techniques in the toxicological formations.                                  solubilization required
            • Approaches of maximizing exposure                                                            • Precedented approaches for solubilization and their limitations

                  • Solution                                                                               • Displaying novel solubilization approaches such as cyclodextrins, emulsions

                  • Liquid dispersions                                                                       and nanoparticles
                  • Solid dispersion/nanocrystal/amorphous                                                 Jaymin Shah, PhD, Research Fellow, Parenteral Development Centre of
                  • Suspension                                                                             Emphasis, Pfizer, Inc.
            • Categorize “conventional” and “non-conventional” approaches

                  • Accessibility/ convenience.- pH adjustment, micelles, lipid based and self-    2:00    Experiences with Captisol: Demonstrating Solubility
                    emulsifying systems, complexation, and co-solvents                                     Improvements, Formulability and Clinical Use
                  • Dissolution limited vs solubility limited – liposomes, polymeric micelles,             • Why not use Captisol?
                    emulsion/ microemulsion/ self-emulsifying systems, some micellar systems,              • Displaying case study examples of successful applications, challenges and
                    and complexation                                                                         limitations
                  • Low dose vs high dose: all the methods needed to try to increase                       • Understanding Captisol improvements

                                                                                                           • Discussing regulatory interactions
                    solubility
            • Vehicles to be considered; Interaction with membrane, toxicity/acceptability in              James D. Pipkin, PhD, Senior Director, New Product Development, CyDex
               humans, physical phenomena e.g., precipitation in GI fluid                                  Pharmaceuticals
            Ron Liu, PhD MBA, President & Chief Executive Officer, AustarPharma
                                                                                                   2:45    Afternoon Networking Break
                                 Lipid-Based Formulations
                                                                                                   3:15    Predicting Oral Absorption of Amorphous Compounds
    9:15    How to Enhance the Bioavailability of Poorly Soluble                                           That Precipitate in the GI Tract
            Compounds Using Lipid-Based Formulations                                                       • Ascertaining the factors that lead to precipitation of drugs in the
            • Design strategies for the successful development of lipid-based formulations                   gastrointestinal tract
                                                                                                           • Identifying assumptions necessary for relating in vitro dissolution to
              must give due consideration to the formulation’s digestibility and dispersibility
            • Discussing the mechanism by which these two important formulation                              bioavailability estimates
                                                                                                           • Provide simple expressions to predict bioavailability from in vitro
              considerations enhance absorption
            • Presenting cases studies that illustrate the importance of digestion and                       concentration vs. time curves
                                                                                                           • Estimating the bioavailability enhancement from the extent and duration of
              dispersion
            • Selecting a suitable oral liquid dosage form for delivery of lipid-based                       supersaturation
                                                                                                           • Discussing impact of precipitation on variations in bioavailability
              formulations- the use of softgels either with conventional gelatin-based shells
              or plant-based shells                                                                        Robin H. Bogner, PhD, Associate Professor of Pharmaceutics, School of
            Jeff Browne, PhD, Director, Technical Support, Business Development, Catalent                  Pharmacy, University of Connecticut
            Pharma Solutions
                                                                                                   4:00    API Crystal Forms and Their Bioavailabilities
    10:00   Morning Networking Break                                                                       • Screening API crystal forms
                                                                                                           • Understanding crystal forms and bioavailability
    10:45   Lipid-Based Drug Delivery to Effectively Overcome Physical                                     • Selecting a suitable API crystal form


            and Biological Barriers                                                                        • Controlling the desired API form in formulation and process development

            • Utilizing lipid-based formulations, solubilization approaches and self-emulsifying           Xiaoming (Sean) Chen, PhD, Senior Development Investigator, Drug Product
              solutions                                                                                    Development & Manufacturing, OSI Pharmaceuticals, Inc
            • Overcoming poor aqueous solubility and stability membrane permeability, drug

              efflux and bioavailability issues                                                    4:45    Novel Strategies for Salt Selection Concerning Solubility
            • Discussing biopharmaceutical considerations of lipid-based formulations seen                 Enhancement, Salt Stability and Stabilization
              from an industrial perspective                                                               • Discussing salt selection strategy and processes
            René Holm, PhD, Head, Preformulation, H. Lundbeck Denmark                                      • Areas of discussion will include:
                                                                                                                 • Feasibility analysis


    11:30   Oral Lipid-Based Formulations for the Enhancement of                                                 • Determination of salt stability


            Poorly-Soluble Compound Delivery                                                                     • Approaches to stabilize a salt

            •   Understanding the nature of lipid excipients and the lipid formulation                     Yaling Wang, Research Fellow, Merck & Co.
                classification system (LFCS)
            •   Discussing why lipid-based formulation is useful for bioavailability enhancement   5:30    Chairperson’s Closing Remarks & End of Conference

5   1-800-882-8684 • www.improvingsolubility.com
4th

          Improving Solubility                                                                                                               TM       March 29-31, 2010
                                                                                                                                                      Philadelphia, PA


    REGISTRATION CARD                            (Email this form to info@iqpc.com or fax to 646-378-6025)


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     ❑ Main Conference Only                           ❑ All-Access Pass                        ❑ Workshop(s) Only                                                    ❑ Networking Dinner
                                                                                               Choose Your Workshop(s): ❑A ❑B ❑C ❑D

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    About our Sponsors:
                                       Eurand is a specialty pharmaceutical                                             Catalent Pharma Solutions is a leading provider of advanced
                                       company that develops,                                                           dose form and packaging technologies as well as development,
                                       manufactures and commercializes                                                  manufacturing and packaging services for pharmaceutical,
    enhanced pharmaceutical and biopharmaceutical products based on its                              biotechnology and consumer health companies. Catalent applies its local market
    proprietary pharmaceutical technologies. Eurand has had six products                             expertise and technical creativity to advance treatments, change markets and
    approved by the FDA since 2001 and has a pipeline of product                                     enhance patient outcomes. Catalent’s proprietary drug delivery and packaging
    candidates in development for itself and its collaboration partners. The                         technologies enable customers to achieve their desired clinical and market outcomes,
    Company's technology platforms include bioavailability enhancement of                            and are used in many well-known products. With experience in more than 100
    poorly soluble drugs, custom release profiles, taste-masking, orally                             countries and a global facility network that spans five continents, Catalent is well
    disintegrating tablet (ODT) formulations, and drug conjugation.                                  positioned to serve you, wherever you do business Website: www.catalent.com
    Website: www.Eurand.com
                                                                                                                              Bend Research Inc. specializes in the invention,
                              CyDex Pharmaceuticals, Inc. is a specialty                                                      advancement, development, and commercialization of
                              pharmaceutical company focused on the                                                           pharmaceutical and health science technologies. We
                              development and commercialization of drugs                             develop drug-delivery solutions from a base of fundamental understanding,
    specifically designed to address limitations of current therapies in                             provide formulation and dosage-form assistance, and advance drug candidates all
    selected established markets. We have developed a portfolio of product                           the way to commercialization. We have a number of proprietary platform
    candidates utilizing our drug formulation technology using Captisol®                             technologies available for licensing, including our spray-dried dispersion (SDD)
    cyclodextrins. Captisol® cyclodextrins are a patent protected, specifically                      technology that increases the bioavailability of low-solubility compounds. At Bend
    modified family of cyclodextrins designed to improve solubility, stability,                      Research, we seek to develop strong alliances with companies that have
    bioavailability, safety and/or dosing of a number of active                                      challenging drug-delivery problems to solve. Please call Bruce Johnson at 541-382-
    pharmaceutical ingredients, or APIs. Website: www.cydexpharma.com                                4100 to learn more about our research, development, and GMP manufacturing
                                                                                                     capabilities. Website: www.bendresearch.com



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4th Improving Solubility

  • 1. Register by Jan. 29th and save up to $1,796. See page 6 for details. 4th Improving March 29-31, 2010 Philadelphia, PA Uncovering Novel Advances in Solubility TM Enhancing Solubility, Amorphous Forms, Bioavailability & Lipid- Based Formulation of Drugs Learn Best Practice Strategies on How to: • Make development of an insoluble drug candidate possible by using solid dispersions • Approach parenteral delivery of poorly soluble drugs • Utilize pharmaceutical co-crystals to enhance solubility and dissolution of insoluble APIs • Effectively understand the difference between thermodynamic vs. kinetic stability • Maximize exposure of water-insoluble drugs in toxicology evaluation and early formulation development • Enhance the bioavailability of poorly soluble compounds using lipid-based formulations Conference Co-Chairs: Ron Liu, PhD MBA Michael Pikal, PhD President & Chief Executive Officer Professor and Pfizer Distinguished AustarPharma Chair, Pharmaceutical Technology, University of Connecticut Speakers Include: • Naír Rodríguez-Hornedo, PhD, Associate • Satej Bhandarkar, PhD, Senior Manager, Analytical Sciences Professor of Pharmaceutical Sciences, The College Department, Sanofi-Aventis U.S. of Pharmacy, The University of Michigan • Jaymin Shah, PhD, Research Fellow, Parenteral Development • Harry G. Brittain, PhD, FRSC, Institute Director, Centre of Emphasis, Pfizer, Inc. Center for Pharmaceutical Physics • Yun Alelyunas, PhD, Principal, Scientist I, Head of Physical • René Holm, PhD, Head, Preformulation, Properties Team, AstraZeneca H. Lundbeck Denmark • Feng Qian, PhD, Senior Research Investigator, Bristol-Myers Squibb • M. Sherry Ku, PhD, Senior Director, • Xiaoming (Sean) Chen, PhD, Drug Product Development & Manufacturing, OSI Pharmaceutical Development, Pfizer, Inc. Pharmaceuticals, Inc. • Robin H. Bogner PhD, Associate Professor of • Vivian Bi, PhD, Associate Principle Scientist, Early Development, PAR&D, Pharmaceutics, School of Pharmacy, AstraZeneca University of Connecticut • Yaling Wang, PhD, Research Fellow, Merck & Co. • Jeffrey Skell, PhD, Director, DMPK & Pharmaceutics, Drug and Biomaterial R & D, Genzyme Corporation Sponsors: Media Partners: Driving the Industry Forward www.FuturePharmaUS.com 1-800-882-8684 • www.improvingsolubility.com
  • 2. Who will you meet at 4th the conference? Improving Chief Scientific Officers, Vice Presidents, Directors, Heads, Scientists, Chemists, Research Leaders/Fellows/Advisors, & Managers specializing in: • Formulation Solubility • Pre-Formulation TM • Discovery R&D • Preclinical Development • Analytical Development • Drug Delivery • Drug Discovery • Medicinal Chemistry • Analytical Chemistry March 29-31, 2010 Philadelphia, PA • Chemical Development • Product Development • Toxicology • Pharmaceutics Dear Colleague, • Physiochemistry Improving drug solubility is one of • Chemical Engineering the biggest challenges for pharmac they are always looking for new strat eutical companies as • Solid States egies to increase bioavailability of new drugs. • Process R&D Building on the success of last year ’s event, IQPC’s 4th Improving Solu back by popular demand. With an bility conference is ever increasing number of poorly to market, pharmaceutical and biote soluble drugs coming solutions to maximize the time-to-m ch companies are looking for ways to adopt novel Sponsorship and arket on their drug development pipe the latest solubility strategies and techniques to guarantee success in lines. Discover Exhibition Opportunities development pipelines. your drug Sponsorships and exhibits are excellent opportunities for your company to showcase You will hear over 18 in-depth sessi ons and case study examples inclu its products and services to high-level, • Nanocryst alline drug-polymer solid dispersion ding: s for poorly water-soluble drugs targeted decision-makers attending the 4th • The role and function of solubility measure Improving Solubility conference. IQPC and ment from a central laboratory in discovery drug Pharma IQ help companies like yours achieve • Implicatio n of BCS: Solubility and permeabi important sales, marketing and branding • Lipid-bas lity class on drug formulation ed drug delivery to effectively over objectives by setting aside a limited number of come physical and biological barri • Oral lipid -based formulations for the enhancem ers ent of poorly soluble compound event sponsorships and exhibit spaces – all of delivery which are tailored to assist your organization • API cryst al forms and their bioavailabilities in creating a platform to maximize its • Novel strat egies for salt selection concerning exposure at the event and reach key decision solubility enhancement, salt stability stabilization and makers in your field. Attend our pre-conference workshop For more information on sponsoring or s which include “Biopharmaceutic the al Considerations in exhibiting at the 4th Improving Solubility Design of Oral Modified Release Drug conference, please contact Mario Matulich Delivery Systems”, “Toxicology Form Development: Challenges and Solu ulation at 212-885-2719 or sponsorship@iqpc.com. tions”, and “Enhancing Solubility Technology by Liposome For Water-Insoluble Drugs in Parentera l Application”, amongst other area s. Additionally, benefit from industry “Excellent networking and presentations from AstraZeneca, Merc Sanofi-Aventis, Bristol-Myers Squibb, Lundbeck, AustarPharma, and man k, Novartis, Pfizer, diverse sessions, good to pharmaceutical, biotech and acad emic experts. This conference prom y more have theoretical discourse.” networking and discussion-filled even ises to be a t leaving you with new ideas and - Dr. Jeff Skell, Director, DMPL and you maximize and enhance your drug solutions to help Pharmaceutics, Genzyme -solubility boundaries. We look forward to seeing you in “Very good! Great mix of Philadelphia in March! Best Regards, details (technical) plus ghly examples.” P.S Don’t miss the hi ative - Dr. Debra Walker, Research Fellow, interactive and inform s! Merck & Co. hop pre-conference works Simon Curtis Senior Conference Director, Pharma s. “Great networking and See page 3 for detail IQ Simon.curtis@iqpc.com discussion sessions.” - Dr. Ly Phan, Senior Director, Medicinal Chemistry, Enanta Pharmaceuticals 2 1-800-882-8684 • www.improvingsolubility.com
  • 3. Pre-Conference Workshops Monday, March 29, 2010 A 8:30 – 11:30 (Registration at 8:00) Challenges and Opportunities in Controlling Drug Substance Properties In order to control drug substance (DS) properties one has to select an optimal form What will be covered: (specific polymorph or hydrate of free form, salt, or co-crystal) and be able to • Why investigate the solid-state of your drug? consistently manufacture it with the same particle size (PS), particle size distribution • Polymorphism (PSD), and crystal surface attributes. • Addressing polymorphism: Screening and characterization • Crystallization of difficult-to-crystallize materials The use of automated and robotic systems in salt/co-crystal and polymorph • Selection of optimum solid form of drug substance screening, and in early crystallization development experimentation, facilitates DS • Chiral material analysis form selection. Ultimate properties of DS are largely determined by the way the • Drug substance specifications batch precipitation or crystallization processes are conducted and to obtain crystalline material of desired properties consistently, these processes must be Benefits of attending: carefully controlled. This can be accomplished via in-situ seeding that simplifies the • Understand best strategies for selecting an optimal form to control drug substance design and control of batch precipitation/crystallization and gives the results • Weigh the pros and cons of different automated screening systems comparable with the conventional seeding approach. Continuous • Discover the benefits of in-situ seeding for batch design and control precipitation/crystallization removes the risk of batch-to-batch variability and ensures • Display methods and techniques for reducing risk of batch-to-batch variability an optimal control of PS, PSD, and particle surface attributes. Your Workshop Leader: Peter Karpinski, PhD, US Leader of Salt & Polymorphism and Particle Engineering Networks, Novartis Pharmaceuticals Corp B 11:30 – 2:00 (Registration at 11:00) Lunch Included Biopharmaceutical Considerations in the Design of Oral Modified Release Drug Delivery Systems This workshop will highlight biopharmaceutical factors that must be considered in • Discussing issues related to insoluble drugs and or highly soluble drugs based on the design, evaluation and development of modified release dosage forms. It will BCS system include hydrophilic matrices, osmotic pump and multi-unit delivery systems. The • Identifying drug release mechanisms and methodologies in connection with IVIVC influence of electrolyte concentration and polymer character, drug properties on the Benefits of attending: textural and micro-environmental conditions within delivery systems relative to the • Uncovering a series of fundamental considerations in oral modified release drug conditions of gastro-intestinal tract, drug release and absorption will be discussed. delivery systems Examples for each class of drug based on their BCS (Biopharmaceutical Classification • Discovering many novel drug release mechanisms and methodologies applied in System) scheme will be presented and relative influence of formulation design, their evaluation transit time and GI physiology on absorption and bioavailability in the context of • Specific case studies will be used to illustrate textural properties of delivery systems IVIVC will be discussed. relative to the GI environment What will be covered: • Displaying the influence of electrolyte concentration and polymer character Your Workshop Leader: Reza Fassihi, Ph.D, AAPS Fellow, Professor of • Uncovering delivery system textural properties Biopharmaceutics and Industrial Pharmacy, Temple University C 2:30 – 5:00 (Registration at 2:00) Toxicology Formulation Development: Challenges and Solutions Toxicology formulation is an essential component of drug development to enable • Review on toxicology formulations in NDA filing of marketed drugs successful toxicology study of new drug candidate. The requirement for adequate • Novel formulation technologies to enhance exposure in toxicology species exposure at high doses to establish a safety window often imposes formulation Benefits of attending: challenges to poorly soluble compounds. Novel formulation technologies and • Basic procedures and general considerations of toxicology formulation development excipients may be required to achieve the exposure target. However, a balance • Learn safety of common and novel excipients between implementing novel formulation technologies and controlling the safety • Broaden the knowledge of acceptable toxicology formulations risk of excipients needs to be considered. • Understand what a toxicologist needs from a toxicology formulation What will be covered: • Learn novel formulation technologies that solve exposure limit of poorly soluble • Toxicology formulation development: basic procedures and general considerations compounds • Excipient acceptance criteria in toxicology formulation • Toxicology formulation development from a toxicologist perspective Your Workshop Leader: Chong-Hui Gu, PhD, Associate Director, Pharmaceutical Development, Vertex Pharmaceuticals D 5:30 – 8:00 (Registration at 5:00) Dinner Included Enhancing Solubility by Liposome Technology for Water-Insoluble Drugs in Parenteral Application Liposomes are unique as drug carriers in that they can encapsulate drugs with • Process consideration and manufacturing scalable batches widely varying polarities. Hydrophilic drugs can be entrapped in the aqueous spaces • Injectable liposomal formulation development for water-insoluble drugs – case while lipophilic drugs can be incorporated into the lipid membranes. Using a study of an latest FDA-approved product liposomal formulation can dramatically increase the apparent aqueous solubility of a Benefits of attending: lipophilic drug, making possible delivery of a dose much higher than its water • Understand the basic concepts of phospholipids, bilayer structures and liposomes solubility. A stable liposomal formulation entrapped water-insoluble drug is often • Learn how to develop liposomal formulations based on bilayer structure and achievable without precipitation upon dilution. Scalable manufacturing of liposomes physicochemical properties of compounds is challenged, but process development and optimization can usually overcome • Learn the process development of liposomes some scale-up issues. A case study of the latest FDA-approved marketed product • Learn the aseptic process of liposomal formulations will be discussed during the session. • Understand what a formulator needs to know the key parameters in scalable What will be covered: liposomal manufacturing • Basic procedures and general considerations of liposomal formulation • Learn how to take advantage of drug-delivery technologies to develop quality development based improved products to the marketplace • Excipient acceptance criteria in liposomal formulation Your Workshop Leader: Ron Liu, PhD MBA, President & Chief Executive Officer, AustarPharma 3 1-800-882-8684 • www.improvingsolubility.com
  • 4. Main Conference Day One Tuesday, March 30, 2010 7:30 Registration and Coffee 12:15 Networking Lunch 8:25 Welcome Address and Chairperson’s Opening Remarks 1:15 Pharmaceutical Co-Crystals: A Solubility Perspective Ron Liu, PhD MBA • Understanding the pharmaceutical co-crystal concept President & Chief Executive Officer • Utilizing pharmaceutical co-crystals to enhance solubility and dissolution AustarPharma of insoluble APIs • Discussing mechanisms by which co-crystal solubility is enhanced 8:30 Opening Keynote Presentation: Thermodynamic vs. • Examining co-crystal structure-solubility relationships Kinetic Stability: Knowing Which is Which • Identifying the PK impact • Understanding the distinction between thermodynamic and kinetic • Analyzing literature case studies stability Naír Rodríguez-Hornedo, PhD, Associate Professor of Pharmaceutical • Exceeding the equilibrium solubility to give a supersaturated solution Sciences, The College of Pharmacy, The University of Michigan • Measuring equilibrium solubility and metastable solubility within a substance 2:00 Amorphous Dispersion Approaches for Achieving • Knowing accurately if and when the substance is metastable or Rapid Onset for Orally Administered Low-Solubility undergoing a change Compounds • Recognizing when equilibrium solubility is actually a consequence of • Outlining the need for increased solubility and rapid absorption kinetic solubility • Assessing the impact of enteric dispersions on absorption rate Harry G. Brittain, PhD, FRSC, Institute Director, Center for • Developing rapidly dissolving amorphous formulations Pharmaceutical Physics • Pursuing formulation and process development for amorphous drug- polymer nanoparticles Solid Dispersion in the Development Stage David Lyon, PhD, Vice President, Physical and Biological Sciences, Bend Research, Inc. 9:15 Demonstration of Bioavailability Enhancement Through the Use of Biorise and Diffucaps Technologies 2:45 Afternoon Networking Break Biorise® • Displaying the production, stabilization and characterization of 3:30 Panel Discussion: How to Effectively Formulate Poorly amorphous and nanocrystalline composites Soluble Drugs • Preclinical demonstration of efficacy • Nanoparticles • Clinical demonstration of efficacy • Amorphous forms Diffucaps® • Salt selection: Suitable salt properties for later stage development: stability, • Discussing the production of bioavailability-enhanced extended release solubility, purity, etc. formulations using control of pH microenvironments • Polymorphs: Screening and characterization • Clinical demonstration of efficacy • Cyclodextrins: Toxicology and pharmacokinetic properties and uses in • Mathematical modeling of pharmacodynamic response development Troy Harmon, Vice President, Business Development, Eurand • Assessing permeability and solubility Jeffrey Skell, PhD, Director, DMPK, Genzyme Corp. 10:00 Morning Networking Break Solubility and Discovery Techniques 10:45 Nanocrystalline Drug-Polymer Solid Dispersions for Poorly Water-Soluble Drugs 4:15 The Role and Function of Solubility Measurement from • Nanocrystalline drug-polymer solid dispersion was formed by co-spray a Central Laboratory in Drug Discovery drying drug and Pluronic or PEGs • Summarizing of solubility methods and practices • Nanocrystalline solid dispersion showed improved in vitro dissolution rate • Evaluating kinetic vs thermodynamic solubility and in vivo exposure • Comparing precipitation vs. aggregation aspects • Physical structure of the nanocrystalline solid dispersions was • Understanding the relationship of solubility and in vitro biology and DMPK characterized by PXRD, DSC, AFM and TEM assays • Mechanism led to the formation of nanocrystalline solid dispersion • Discussing conclusions and recommendations formation was investigated Yun Alelyunas, PhD, Principal, Scientist I, Head of Physical Properties Feng Qian, PhD, Senior Research Investigator, Bristol-Myers Squibb Team, AstraZeneca 11:30 Making Development of an Insoluble Drug Candidate 5:00 Implication of BCS: Solubility and Permeability Class on Possible by Using Solid Dispersions: A Case Study Drug Formulation • Displaying first in man studies of a highly insoluble compound with • Examining the importance of tailoring your formulation platform based micronized drug substance in capsules on BCS class • Exposure was very low and there was no dose-proportionality at low • Discussing the extension of BCS classification for formulation selection doses. • Evaluating pH-solubility profile and modified solubility criteria • Evaluating multiple formulation strategies in a clinical study to obtain • Comparing a Caco-2 in-vitro Permeability vs in-situ rat perfusion study adequate bioavailability to proceed with further clinical trials • Using BCS-based Formulation Decision Trees • Selecting for developing a solid dispersion with 20% drug load in HPMC M. Sherry Ku, PhD, Senior Director, Pharmaceutical Development, Pfizer, Inc. • Describes the polymer selection, physicochemical characterization, formulation development, stability results, and testing strategy for the 5:45 Chairperson’s Closing Remarks and End of Day One solid dispersion product • Understanding the challenges associated with commercial development Satej Bhandarkar, PhD, Senior Manager, Analytical Sciences Department, 6:30 Networking Dinner Continue the networking experience by joining your colleagues for Sanofi-Aventis U.S. a dinner following the end of day one. Separate booking necessary. We hope you will join us! 4 1-800-882-8684 • www.improvingsolubility.com
  • 5. Main Conference Day Two Wednesday, March 31, 2010 7:45 Registration and Coffee • Understanding when to use lipid-based formulations - Compound suitability for lipid-based formulations 8:25 Welcome Address and Chairperson’s Opening Remarks • Recognizing how to suitably screen lipid-based formulations (formulation Michael Pikal, PhD screening flow & in vitro screening tests) • Displaying other unique challenges related to lipid-based formulations Professor and Pfizer Distinguished Chair, Pharmaceutical Technology, University of Connecticut Vivian Bi, PhD, Associate Principle Scientist, Early Development, PAR&D, AstraZeneca 8:30 Opening Keynote: Strategies of Maximizing Exposure of Water-Insoluble Drugs in Toxicology Evaluation and Early 12:15 Networking Luncheon Formulation Development Compounds optimized solely on the basis of receptor-based potency are usually Solubility Enhancement Techniques and Strategies hydrophobic and as a result, more than 40% of newly discovered drugs or NCEs are poorly water soluble or water-insoluble. In toxicological evaluation for water- 1:15 Approaches for Parenteral Delivery of Poorly Soluble insoluble drug candidates, maximizing the systemic exposure of these drug Drugs candidates is very critical, though the approach of solubilizing the drug in • Outlining the need for solubilization and limitations imposed by parenteral toxicological evaluation may not be relevant to the approach used for the final route of administration • Highlighting pre-formulation studies to determine the need and degree of finished product. This session will discuss some commonly and less commonly used solubilization techniques in the toxicological formations. solubilization required • Approaches of maximizing exposure • Precedented approaches for solubilization and their limitations • Solution • Displaying novel solubilization approaches such as cyclodextrins, emulsions • Liquid dispersions and nanoparticles • Solid dispersion/nanocrystal/amorphous Jaymin Shah, PhD, Research Fellow, Parenteral Development Centre of • Suspension Emphasis, Pfizer, Inc. • Categorize “conventional” and “non-conventional” approaches • Accessibility/ convenience.- pH adjustment, micelles, lipid based and self- 2:00 Experiences with Captisol: Demonstrating Solubility emulsifying systems, complexation, and co-solvents Improvements, Formulability and Clinical Use • Dissolution limited vs solubility limited – liposomes, polymeric micelles, • Why not use Captisol? emulsion/ microemulsion/ self-emulsifying systems, some micellar systems, • Displaying case study examples of successful applications, challenges and and complexation limitations • Low dose vs high dose: all the methods needed to try to increase • Understanding Captisol improvements • Discussing regulatory interactions solubility • Vehicles to be considered; Interaction with membrane, toxicity/acceptability in James D. Pipkin, PhD, Senior Director, New Product Development, CyDex humans, physical phenomena e.g., precipitation in GI fluid Pharmaceuticals Ron Liu, PhD MBA, President & Chief Executive Officer, AustarPharma 2:45 Afternoon Networking Break Lipid-Based Formulations 3:15 Predicting Oral Absorption of Amorphous Compounds 9:15 How to Enhance the Bioavailability of Poorly Soluble That Precipitate in the GI Tract Compounds Using Lipid-Based Formulations • Ascertaining the factors that lead to precipitation of drugs in the • Design strategies for the successful development of lipid-based formulations gastrointestinal tract • Identifying assumptions necessary for relating in vitro dissolution to must give due consideration to the formulation’s digestibility and dispersibility • Discussing the mechanism by which these two important formulation bioavailability estimates • Provide simple expressions to predict bioavailability from in vitro considerations enhance absorption • Presenting cases studies that illustrate the importance of digestion and concentration vs. time curves • Estimating the bioavailability enhancement from the extent and duration of dispersion • Selecting a suitable oral liquid dosage form for delivery of lipid-based supersaturation • Discussing impact of precipitation on variations in bioavailability formulations- the use of softgels either with conventional gelatin-based shells or plant-based shells Robin H. Bogner, PhD, Associate Professor of Pharmaceutics, School of Jeff Browne, PhD, Director, Technical Support, Business Development, Catalent Pharmacy, University of Connecticut Pharma Solutions 4:00 API Crystal Forms and Their Bioavailabilities 10:00 Morning Networking Break • Screening API crystal forms • Understanding crystal forms and bioavailability 10:45 Lipid-Based Drug Delivery to Effectively Overcome Physical • Selecting a suitable API crystal form and Biological Barriers • Controlling the desired API form in formulation and process development • Utilizing lipid-based formulations, solubilization approaches and self-emulsifying Xiaoming (Sean) Chen, PhD, Senior Development Investigator, Drug Product solutions Development & Manufacturing, OSI Pharmaceuticals, Inc • Overcoming poor aqueous solubility and stability membrane permeability, drug efflux and bioavailability issues 4:45 Novel Strategies for Salt Selection Concerning Solubility • Discussing biopharmaceutical considerations of lipid-based formulations seen Enhancement, Salt Stability and Stabilization from an industrial perspective • Discussing salt selection strategy and processes René Holm, PhD, Head, Preformulation, H. Lundbeck Denmark • Areas of discussion will include: • Feasibility analysis 11:30 Oral Lipid-Based Formulations for the Enhancement of • Determination of salt stability Poorly-Soluble Compound Delivery • Approaches to stabilize a salt • Understanding the nature of lipid excipients and the lipid formulation Yaling Wang, Research Fellow, Merck & Co. classification system (LFCS) • Discussing why lipid-based formulation is useful for bioavailability enhancement 5:30 Chairperson’s Closing Remarks & End of Conference 5 1-800-882-8684 • www.improvingsolubility.com
  • 6. 4th Improving Solubility TM March 29-31, 2010 Philadelphia, PA REGISTRATION CARD (Email this form to info@iqpc.com or fax to 646-378-6025) YES! Please register me for ❑ Main Conference Only ❑ All-Access Pass ❑ Workshop(s) Only ❑ Networking Dinner Choose Your Workshop(s): ❑A ❑B ❑C ❑D Name ____________________________________________________________ Job Title _________________________________________________ Organization______________________________________________________ Approving Manager________________________________________ Address _____________________________________________ City________________________________________State__________Zip__________ Phone_____________________________________________E-mail____________________________________________________________________ ❑ Please keep me informed via email about this and other related events. ❑ Check enclosed for $_________ (Payable to IQPC) ❑ Charge my ❑ Amex ❑ Visa ❑Mastercard ❑ Diners Club Card #_______________________________Exp. Date___/___CVM Code_______ About our Sponsors: Eurand is a specialty pharmaceutical Catalent Pharma Solutions is a leading provider of advanced company that develops, dose form and packaging technologies as well as development, manufactures and commercializes manufacturing and packaging services for pharmaceutical, enhanced pharmaceutical and biopharmaceutical products based on its biotechnology and consumer health companies. Catalent applies its local market proprietary pharmaceutical technologies. Eurand has had six products expertise and technical creativity to advance treatments, change markets and approved by the FDA since 2001 and has a pipeline of product enhance patient outcomes. Catalent’s proprietary drug delivery and packaging candidates in development for itself and its collaboration partners. The technologies enable customers to achieve their desired clinical and market outcomes, Company's technology platforms include bioavailability enhancement of and are used in many well-known products. With experience in more than 100 poorly soluble drugs, custom release profiles, taste-masking, orally countries and a global facility network that spans five continents, Catalent is well disintegrating tablet (ODT) formulations, and drug conjugation. positioned to serve you, wherever you do business Website: www.catalent.com Website: www.Eurand.com Bend Research Inc. specializes in the invention, CyDex Pharmaceuticals, Inc. is a specialty advancement, development, and commercialization of pharmaceutical company focused on the pharmaceutical and health science technologies. We development and commercialization of drugs develop drug-delivery solutions from a base of fundamental understanding, specifically designed to address limitations of current therapies in provide formulation and dosage-form assistance, and advance drug candidates all selected established markets. We have developed a portfolio of product the way to commercialization. We have a number of proprietary platform candidates utilizing our drug formulation technology using Captisol® technologies available for licensing, including our spray-dried dispersion (SDD) cyclodextrins. Captisol® cyclodextrins are a patent protected, specifically technology that increases the bioavailability of low-solubility compounds. At Bend modified family of cyclodextrins designed to improve solubility, stability, Research, we seek to develop strong alliances with companies that have bioavailability, safety and/or dosing of a number of active challenging drug-delivery problems to solve. Please call Bruce Johnson at 541-382- pharmaceutical ingredients, or APIs. Website: www.cydexpharma.com 4100 to learn more about our research, development, and GMP manufacturing capabilities. Website: www.bendresearch.com Registration Information Special Discounts Available: A limited number of discounts are available Register & Pay By Register & Pay By Standard PRICING 1/29/2010 2/26/2010 Price for the non-profit sector, government organizations and academia. For more information, please contact customer service at 1-800-882-8684. Details for making payment via EFT or wire transfer: Conference Only $1,199 $1,599 $1,799 JPMorgan Chase - Penton Learning Systems LLC dba (save $600) (save $200) IQPC: 957-097239 ABA/Routing #: 021000021 All Access $2,199 $2,599 $2,799 Reference: Please include the name of the attendee(s) and the event (save $1,796) (save $1,396) (save $1,196) number: 10521.004 Payment Policy: Payment is due in full at the time of registration and Workshops $549 each $549 each $549 each includes lunches and refreshment. Your registration will not be confirmed until payment is received and may be subject to cancellation. Networking Dinner $99 $99 $99 For IQPC’s Cancellation, Postponement and Substitution Policy, please visit www.iqpc.com/cancellation Venue Information: Venue is to be announced. Please check the website at Please note multiple discounts cannot be combined. www.improvingsolubility.com for updates and announcements. A $99 processing charge will be assessed to all registrations not accompanied by credit card payment at the time of Special Dietary Needs: If you have a dietary restriction, please contact registration. Customer Service at 1-800-882-8684 to discuss your specific needs. MAKE CHECKS PAYABLE IN U.S. DOLLARS TO: IQPC ©2009 IQPC. All Rights Reserved. The format, design, content and * CT residents or people employed in the state of CT must add 6% sales tax. arrangement of this brochure constitute a trademark of IQPC. Unauthorized reproduction will be actionable under the Lanham Act and common law Team Discounts: For information on team discounts, please contact IQPC Customer Service at 1-800-882-8684. Only one principles. discount may be applied per registrant. 6 1-800-882-8684 • www.improvingsolubility.com