IQPC's 4th Annual Improving Solubility conference provides new solutions to measure, predict and improve solubility, ultimately maximizing time-to-market. Topics include applying lipid based formulations, overcoming physical instability, new drug delivery technologies, identifying in-vitro absorption and discovering formulations for toxicology studies.
Call Girls Electronic City Just Call 7001305949 Top Class Call Girl Service A...
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