Improving Solubility 2010

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"Poorly soluble compounds represent about 60% of drugs in market and this number continues to increase. IQPC's 4th Annual Improving Solubility conference will provide you with new techniques to measure, predict and improve solubility. This can help turn your biggest challenge into your main success factor and competitive advantage!

Topics include: • Applying lipid based forumlations to address bioavailability issues • Overcoming physical instability • Using both solubility and permeability for predicting absorption • Highlighting new drug delivery technologies for improving bioavailability of poorly soluble drugs • Uncovering parenteral formulation of poorly water soluble drugs • Identifying the relationship between in-vitro data and how this would influence absorption • Discovering the right formulation for toxicology studies for poorly soluble compounds


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Improving Solubility 2010

  1. 1. Register by Feb. 26th and save up to $1,396! See page 7 for details. 4th Improving March 29-31, 2010 The Park Hyatt Philadelphia Philadelphia, PA Solubility TM Uncovering Novel Advances in 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 Professor • Navnit H. Shah, PhD, Distinguished Research Leader, of Pharmaceutical Sciences, The College of Pharmacy, Pharmaceutical R&D, Hoffmann-La Roche Inc. The University of Michigan • Manuel V. Sanchez, PhD, Research Advisor, • Harry G. Brittain, PhD, FRSC, Institute Director, Eli Lilly and Company Center for Pharmaceutical Physics • Narayan Variankaval, PhD, Research Fellow, • Ian Buxton, PhD, Director, Product Development, Merck Research Laboratories WW Pharmaceutical Development, GlaxoSmithKline • Robin H. Bogner PhD, Associate Professor of Pharmaceutics, • René Holm, PhD, Head, Preformulation, School of Pharmacy, University of Connecticut H. Lundbeck Denmark • Satej Bhandarkar, PhD, Senior Manager, Analytical Sciences Department, • Jeffrey Skell, PhD, Director, DMPK & Pharmaceutics, Sanofi-Aventis U.S. Drug and Biomaterial R & D, Genzyme Corporation • Yun Alelyunas, PhD, Principal, Scientist I, Head of Physical Properties Team, AstraZeneca • M. Sherry Ku, PhD, Senior Director, Pharmaceutical • Feng Qian, PhD, Senior Research Investigator, Bristol-Myers Squibb Development, Pfizer, Inc. Sponsors: Media Partners: Driving the Industry Forward www.FuturePharmaUS.com 1-800-882-8684 • www.improvingsolubility.com
  2. 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 The Park Hyatt Philadelphia • Chemical Development Philadelphia, PA • Product Development • Toxicology • Pharmaceutics • Physiochemistry • Chemical Engineering Dear Colleague, • Solid States Improving drug solubility is one of • Process R&D the biggest challenges for pharmac they are always looking for new strat eutical companies as egies to increase bioavailability of new drugs. Building on the success of last year ’s event, IQPC’s 4th Improving Solu Sponsorship and back by popular demand. With an bility conference is ever increasing number of poorly to market, pharmaceutical and biote soluble drugs coming ch companies are looking for ways Exhibition Opportunities solutions to maximize the time-to-m to adopt novel arket on their drug development pipe Sponsorships and exhibits are excellent the latest solubility strategies and lines. Discover techniques to guarantee success in opportunities for your company to showcase development pipelines. your drug its products and services to high-level, targeted decision-makers attending the 4th You will hear over 18 in-depth sessi ons and case study examples inclu Improving Solubility conference. IQPC and • Nanocryst alline drug-polymer solid dispersion ding: s for poorly water-soluble drugs Pharma IQ help companies like yours achieve • The role and function of solubility measure important sales, marketing and branding ment from a central laboratory in discovery drug objectives by setting aside a limited number of • Implicatio n of BCS: Solubility and permeabi event sponsorships and exhibit spaces – all of • Lipid-bas lity class on drug formulation ed drug delivery to effectively over which are tailored to assist your organization come physical and biological barri • Oral lipid -based formulations for the enhancem ers ent of poorly soluble compound in creating a platform to maximize its delivery exposure at the event and reach key decision • API cryst al forms and their bioavailabilities makers in your field. • Novel strat egies for salt selection concerning solubility enhancement, salt stability stabilization and For more information on sponsoring or exhibiting at the 4th Improving Solubility Attend our pre-conference workshop conference, please contact Mario Matulich s which include “Biopharmaceutic the Design of Oral Modified Release al Considerations in at 212-885-2719 or sponsorship@iqpc.com. Drug Delivery Systems”, “Toxicolo Development: Challenges and Solu gy Formulation tions”, and “Enhancing Solubility Technology For Water-Insoluble Drug by Liposome s in Parenteral Application”, amongst other areas. Additionally, benefit from industry presentations from AstraZeneca, Merc “Excellent networking and Sanofi-Aventis, Bristol-Myers Squibb, Lundbeck, AustarPharma, and man k, Novartis, Pfizer, diverse sessions, good to pharmaceutical, biotech and acad y more have theoretical discourse.” emic experts. This conference prom 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 Philadelphia in March! “Very good! Great mix of 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. 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. 4. Solubility Enhancement & Techniques Master Class Monday, March 29, 2010 11:25 Chairperson’s Opening Remarks 2: 30 Progresses and limitation in Characterization of Super Saturation Based Drug Delivery 11:30 Opening Keynote Presentation: How to • Overview of the analytical tools Effectively Formulate Poorly Soluble Drugs • Progress towards the characterization of supersaturated system • Nanoparticles • Spectroscopic methods and its limitations • Amorphous forms • Drug –polymer interaction tools to understand structural changes • Salt selection: suitable salt properties for later stage development: • Lesson for the future stability, solubility, purity Duk Soon Choi, PhD, Research Leader, Hoffmann La Roche • Polymorphs: screening and characterization • Cyclodextrins: toxicology and pharmacokinetic properties and uses 3:00 Approaches for Parenteral Delivery of Poorly in development Soluble Drugs • Assessing permeability and solubility • Outlining the need for solubilization and limitations imposed by parenteral Ian Buxton, PhD, Director, Product Development, WW route of administration Pharmaceutical Development, GlaxoSmithKline • Highlighting pre-formulation studies to determine the need and degree of solubilization required 12:10 Solid Dispersion in the Development Stage • Precedented approaches for solubilization and their limitations • Discussing the increased use of solid dispersions of drugs in • Displaying novel solubilization approaches such as cyclodextrins, emulsions polymers to enable the delivery of poorly soluble compounds and nanoparticles • Examining why the amorphous nature of these dispersions result in Jaymin Shah, PhD, Research Fellow, Parenteral Development Centre of many challenges associated with their production, stability, Emphasis, Pfizer, Inc. formulation into a dosage form and delivery • Understanding the thermodynamics, kinetics and dissolution 3:40 Afternoon Break performance of dispersions in the past 5-10 years • Highlighting some of these advances to provide a scientific 4:00 Parenteral Formulation Development and Non- perspective that can enable the successful design of solid ideal Solubility Behavior dispersions • Why Parenterals are important formulation option for Pharmaceutical Narayan Variankaval, PhD, Research Fellow, Merck Research Sector and growing in importance Laboratories • Review of solubility as it relates to Parenteral formulation drug discovery and development 12:50 Networking Luncheon • Non-ideal solubility behavior and its frequency • New solubility techniques to investigate and understand non-ideal 1:50 Design and Development of Super Saturation behavior Based Drug Delivery Manuel V. Sanchez, PhD, Research Advisor, Eli Lilly and Company* • Fundamentals of supersaturated system • Design consideration in development of supersaturated system 4: 40 Strategic Application of Early Formulation • Essentials for stabilization in solid state Screening in Drug Discovery • Maintaining super saturation during dissolution • Utility of solubilization approaches in early drug discovery • Impact of polymers , processes and down stream processing on • Selecting excipients and solubilization approaches in early drug discovery stability with case studies. • Novel high throughput formulation screening approach for application in Navnit H. Shah, PhD, Distinguished Research Leader, drug discovery Pharmaceutical R&D, Hoffmann-La Roche Inc. • Impact of enhanced formulations on early PK studies Suma Gopinathan, MSc, Associate Scientist and Head of Discovery Formulation, Lexicon Pharmaceuticals 5:20 End of Masterclass *Subject to final confirmation About the Venue The Park Hyatt Philadelphia 200 South Broad Street Philadelphia, PA 19102 Phone: (215) 893-1234 IQPC has secured a group rate for participants of The Park Hyatt Philadelphia. Please contact the hotel directly at (215) 893-1234 by March 8, 2010 to make sure you are eligible for this rate. Mention you are attending IQPC’s Improving Solubility for the group rate when making your reservation. 4 1-800-882-8684 • www.improvingsolubility.com
  5. 5. 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 Anthony Recupero, PhD, Senior Director, 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! 5 1-800-882-8684 • www.improvingsolubility.com
  6. 6. Main Conference Day Two Wednesday, March 31, 2010 7:45 Registration and Coffee 11:30 Oral Lipid-Based Formulations for the Enhancement of Poorly-Soluble Compound Delivery 8:25 Welcome Address and Chairperson’s Opening Remarks • Understanding the nature of lipid excipients and the lipid formulation Michael Pikal, PhD classification system (LFCS) Professor and Pfizer Distinguished Chair, Pharmaceutical Technology, • Discussing why lipid-based formulation is useful for bioavailability University of Connecticut enhancement • Understanding when to use lipid-based formulations - Compound suitability 8:30 Opening Keynote: Strategies of Maximizing Exposure of for lipid-based formulations Water-Insoluble Drugs in Toxicology Evaluation and Early • Recognizing how to suitably screen lipid-based formulations (formulation Formulation Development screening flow & in vitro screening tests) Compounds optimized solely on the basis of receptor-based potency are usually • Displaying other unique challenges related to lipid-based formulations hydrophobic and as a result, more than 40% of newly discovered drugs or NCEs Vivian Bi, PhD, Associate Principle Scientist, Early Development, PAR&D, are poorly water soluble or water-insoluble. In toxicological evaluation for water- AstraZeneca insoluble drug candidates, maximizing the systemic exposure of these drug candidates is very critical, though the approach of solubilizing the drug in 12:15 Networking Luncheon toxicological evaluation may not be relevant to the approach used for the final finished product. This session will discuss some commonly and less commonly Solubility Enhancement Techniques and Strategies used solubilization techniques in the toxicological formations. • Approaches of maximizing exposure 1:15 Panel Discussion: Patent Opportunities for • Solution Solubility Solutions: Amorphous Dispersions and • Liquid dispersions Co-crystals • Solid dispersion/nanocrystal/amorphous Courtney B. Meeker, Registered Patent Attorney, O'Brien Jones, PLLC • Suspension • Categorize “conventional” and “non-conventional” approaches 2:00 Experiences with Captisol: Demonstrating Solubility • Accessibility/ convenience.- pH adjustment, micelles, lipid based and self- Improvements, Formulability and Clinical Use emulsifying systems, complexation, and co-solvents • Why not use Captisol? • Dissolution limited vs solubility limited – liposomes, polymeric micelles, • Displaying case study examples of successful applications, challenges and emulsion/ microemulsion/ self-emulsifying systems, some micellar systems, limitations and complexation • Understanding Captisol improvements • Low dose vs high dose: all the methods needed to try to increase • Discussing regulatory interactions solubility James D. Pipkin, PhD, Senior Director, New Product Development, CyDex • Vehicles to be considered; Interaction with membrane, toxicity/acceptability in Pharmaceuticals humans, physical phenomena e.g., precipitation in GI fluid 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 That Precipitate in the GI Tract 9:15 How to Enhance the Bioavailability of Poorly Soluble • Ascertaining the factors that lead to precipitation of drugs in the Compounds Using Lipid-Based Formulations gastrointestinal tract • Design strategies for the successful development of lipid-based formulations • Identifying assumptions necessary for relating in vitro dissolution to must give due consideration to the formulation’s digestibility and dispersibility bioavailability estimates • Discussing the mechanism by which these two important formulation • Provide simple expressions to predict bioavailability from in vitro considerations enhance absorption concentration vs. time curves • Presenting cases studies that illustrate the importance of digestion and • Estimating the bioavailability enhancement from the extent and duration of dispersion supersaturation • Selecting a suitable oral liquid dosage form for delivery of lipid-based • Discussing impact of precipitation on variations in bioavailability formulations- the use of softgels either with conventional gelatin-based shells Robin H. Bogner, PhD, Associate Professor of Pharmaceutics, School of or plant-based shells Pharmacy, University of Connecticut Jeff Browne, PhD, Director, Technical Support, Business Development, Catalent Pharma Solutions 4:00 API Crystal Forms and Their Bioavailabilities • Screening API crystal forms 10:00 Morning Networking Break • Understanding crystal forms and bioavailability • Selecting a suitable API crystal form 10:45 Lipid-Based Drug Delivery to Effectively Overcome Physical • Controlling the desired API form in formulation and process development and Biological Barriers Xiaoming (Sean) Chen, PhD, Senior Development Investigator, Drug Product • Utilizing lipid-based formulations, solubilization approaches and self-emulsifying Development & Manufacturing, OSI Pharmaceuticals, Inc solutions • Overcoming poor aqueous solubility and stability membrane permeability, drug 4:45 Novel Strategies for Salt Selection Concerning Solubility efflux and bioavailability issues Enhancement, Salt Stability and Stabilization • Discussing biopharmaceutical considerations of lipid-based formulations seen • Discussing salt selection strategy and processes from an industrial perspective • Areas of discussion will include: René Holm, PhD, Head, Preformulation, H. Lundbeck Denmark • Feasibility analysis • Determination of salt stability • Approaches to stabilize a salt Yaling Wang, Research Fellow, Merck & Co. 5:30 Chairperson’s Closing Remarks & End of Conference 6 1-800-882-8684 • www.improvingsolubility.com
  7. 7. 4th Improving Solubility TM March 29-31, 2010 The Park Hyatt Philadelphia 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 ❑ Master Class ❑ 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 company that develops, O’Brien Jones, PLLC is an intellectual property firm located in Tysons manufactures and commercializes enhanced pharmaceutical Corner, Virginia, in the Washington, DC metropolitan area. With and biopharmaceutical products based on its proprietary degrees in biochemistry, chemistry, chemical engineering, electrical pharmaceutical technologies. Eurand has had six products approved by the FDA since 2001 and has a engineering, and mechanical engineering, we counsel clients in many different industries regarding a pipeline of product candidates in development for itself and its collaboration partners. The Company's diverse array of technologies. We offer a wide range of services, including: technology platforms include bioavailability enhancement of poorly soluble drugs, custom release profiles, • Domestic and international patent preparation and prosecution taste-masking, orally disintegrating tablet (ODT) formulations, and drug conjugation. Website: • Patent reissue and reexamination proceedings www.Eurand.com • Strategic patent portfolio management • Freedom-to-operate searches and reports CyDex Pharmaceuticals, Inc. is a specialty pharmaceutical company • Patentability, validity, enforceability, and infringement opinions focused on the development and commercialization of drugs specifically Website: www.obrienjones.com designed to address limitations of current therapies in selected established markets. We have developed a portfolio of product candidates utilizing our drug formulation technology Aptuit's SSCI division provides specialized services in the areas of solubility, using Captisol® cyclodextrins. Captisol® cyclodextrins are a patent protected, specifically modified family of dissolution, polymorphism, crystallization, solid-state problem solving and stability. cyclodextrins designed to improve solubility, stability, bioavailability, safety and/or dosing of a number of We focus on improving and protecting API, formulated product, and the active pharmaceutical ingredients, or APIs. Website: www.cydexpharma.com corresponding intellectual property for our customers. Working closely with our API business, as well as our formulation and preclinical technology services, we are able to use our solid-state expertise to add Catalent Pharma Solutions is a leading provider of advanced dose form and packaging technologies as value throughout the entire drug development process. Website: http://www.aptuit.com well as development, manufacturing and packaging services for pharmaceutical, biotechnology and consumer health companies. Catalent applies its local market ISP Pharmaceuticals is a global business providing products and services for drug synthesis, expertise and technical creativity to advance treatments, change markets and drug solubilization, excipients and coatings. Built on a foundation of science, our excipient enhance patient outcomes. Catalent’s proprietary drug delivery and packaging technologies enable portfolio includes Plasdone® binders and Polyplasdone® disintegrants. ISP offers contract customers to achieve their desired clinical and market outcomes, and are used in many well-known manufacturing services of APIs and intermediates. With expertise in material science, ISP products. With experience in more than 100 countries and a global facility network that spans five provides both ingredients and process technology services to improve drug solubility. We have expertise in continents, Catalent is well positioned to serve you, wherever you do business Website: www.catalent.com cGMP spray-dried solid dispersions for bioavailability enhancement and provide development, clinical supply and commercial manufacturing services. With experience working with more than 100 actives in Bend Research Inc. specializes in the invention, advancement, development, and commercialization of last 2 years, we can assist with your drug solubility challenges. Website: www.isppharmaceuticals.com pharmaceutical and health science technologies. We develop drug-delivery solutions from a base of fundamental understanding, provide formulation and dosage-form Croda Inc manufactures a variety of excipients using several technologies such as assistance, and advance drug candidates all the way to commercialization. molecular distillation, esterification, ethoxylation, and fractionation. In addition, Croda We have a number of proprietary platform technologies available for provides a line of Super Refined excipients produced using a proprietary process that licensing, including our spray-dried dispersion (SDD) technology that increases the bioavailability of low- removes polar and oxidative impurities, resulting in high-purity products that provide enhanced stability to solubility compounds. At Bend Research, we seek to develop strong alliances with companies that have the final dosage form. Website: www.croda.com/healthcare challenging drug-delivery problems to solve. Please call Bruce Johnson at 541-382-4100 to learn more about our research, development, and GMP manufacturing capabilities. Website: www.bendresearch.com Registration Information Register & Pay By Standard Team Discounts: For information on team discounts, please contact IQPC Customer PRICING 2/26/2010 Price Service at 1-800-882-8684. Only one discount may be applied per registrant. Special Discounts Available: A limited number of discounts are available for the Conference Only $1,599 $1,799 non-profit sector, government organizations and academia. For more information, (save $600) (save $200) please contact customer service at 1-800-882-8684. Details for making payment via EFT or wire transfer: All Access Pass: includes 2 day main conference and choice $2,599 $2,799 JPMorgan Chase - Penton Learning Systems LLC dba among workshops or Master Class** (save up to $1,396) (save up to $1,196) IQPC: 957-097239 ABA/Routing #: 021000021 Workshops $549 each $549 each Reference: Please include the name of the attendee(s) and the event number: 10521.004 Master Class $699 $699 Payment Policy: Payment is due in full at the time of registration and includes lunches and refreshment. Your registration will not be confirmed until payment is Networking Dinner** $99 $99 received and may be subject to cancellation. For IQPC’s Cancellation, Postponement and Substitution Policy, please visit Please note multiple discounts cannot be combined. **All-Access Pass does not include the Networking Dinner. www.iqpc.com/cancellation 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 Customer registration. 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 arrangement * CT residents or people employed in the state of CT must add 6% sales tax. of this brochure constitute a trademark of IQPC. Unauthorized reproduction will be actionable under the Lanham Act and common law principles. 7 1-800-882-8684 • www.improvingsolubility.com

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