8:25 Welcome Address And Chairperson’s Opening Remarks

Michael Pikal, PhD
Professor and Pfizer Distinguished Chair, Pharmaceutical Technology
University of Connecticut

8:30 Opening Keynote: Strategies Of Maximizing Exposure Of Water-Insoluble Drugs In Toxicology Evaluation And Early Formulation Development

Compounds optimized solely on the basis of receptor-based potency are usually 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 waterinsoluble drug candidates, maximizing the systemic exposure of these drug candidates is very critical, though the approach of solubilizing the drug in toxicological evaluation may not be relevant to the approach used for the final finished product. This session will discuss some commonly and less commonly used solubilization techniques in the toxicological formations.

• Approaches of maximizing exposure
  • Solution
  • Liquid dispersions
  • Solid dispersion/nanocrystal/amorphous
  • Suspension
• Categorize “conventional” and “non-conventional” approaches
  • Accessibility/ convenience.- pH adjustment, micelles, lipid based and selfemulsifying systems, complexation, and co-solvents
  • Dissolution limited vs solubility limited – liposomes, polymeric micelles, emulsion/ microemulsion/ self-emulsifying systems, some micellar systems, and complexation
  • Low dose vs high dose: all the methods needed to try to increase solubility
• Vehicles to be considered; Interaction with membrane, toxicity/acceptability in humans, physical phenomena e.g., precipitation in GI fluid

Ron Liu, PhD MBA
President & Chief Executive Officer
AustarPharma

9:15 How To Enhance The Bioavailability Of Poorly Soluble Compounds Using Lipid-Based Formulations

• Design strategies for the successful development of lipid-based formulations must give due consideration to the formulation’s digestibility and dispersibility
• Discussing the mechanism by which these two important formulation considerations enhance absorption
• Presenting cases studies that illustrate the importance of digestion and dispersion
• Selecting a suitable oral liquid dosage form for delivery of lipid-based formulations- the use of softgels either with conventional gelatin-based shells or plant-based shells

Jeff Browne, PhD
Director, Technical Support, Business Development
Catalent Pharma Solutions

10:45 Lipid-Based Drug Delivery To Effectively Overcome Physical And Biological Barriers

• Utilizing lipid-based formulations, solubilization approaches and self-emulsifying solutions
• Overcoming poor aqueous solubility and stability membrane permeability, drug efflux and bioavailability issues
• Discussing biopharmaceutical considerations of lipid-based formulations seen from an industrial perspective

René Holm, PhD
Head, Preformulation
H. Lundbeck Denmark

11:30 Oral Lipid-Based Formulations For The Enhancement Of Poorly-Soluble Compound Delivery

• Understanding the nature of lipid excipients and the lipid formulation classification system (LFCS)
• Discussing why lipid-based formulation is useful for bioavailability enhancement
• Understanding when to use lipid-based formulations - Compound suitability for lipid-based formulations
• Recognizing how to suitably screen lipid-based formulations (formulation screening flow & in vitro screening tests)
• Displaying other unique challenges related to lipid-based formulations

Vivian Bi, PhD
Associate Principle Scientist, Early Development, PAR&D
AstraZeneca

Solubility Enhancement Techniques and Strategies

1:15 Patent Opportunities For Solubility Solutions: Amorphous Dispersions And Co-Crystals

• Pillars of Patenting Solid Forms: Obviousness and Novelty
• Challenges in Protecting Pharmaceutical Products
• Case Study of Stabilizing an Amorphous Form with a Dispersion – Protecting the Science with IP
• Co-Crystals v. Salts v. Polymorphs: IP Principles for Protection and Enforcement of Rights
• Differences Between Europe and the United States in Protecting Solutions to Solubility Problems

2:00 Experiences With Captisol: Demonstrating Solubility Improvements, Formulability And Clinical Use

• Why not use Captisol?
• Displaying case study examples of successful applications, challenges and limitations
• Understanding Captisol improvements
• Discussing regulatory interactions

James D. Pipkin, PhD
Senior Director, New Product Development
CyDex Pharmaceuticals

3:15 Predicting Oral Absorption Of Amorphous Compounds That Precipitate In The GI Tract

• Ascertaining the factors that lead to precipitation of drugs in the gastrointestinal tract
• Identifying assumptions necessary for relating in vitro dissolution to bioavailability estimates
• Provide simple expressions to predict bioavailability from in vitro concentration vs. time curves
• Estimating the bioavailability enhancement from the extent and duration of supersaturation
• Discussing impact of precipitation on variations in bioavailability

Robin H. Bogner, PhD
Associate Professor of Pharmaceutics, School of Pharmacy
University of Connecticut

4:00 API Crystal Forms And Their Bioavailabilities

• Screening API crystal forms
• Understanding crystal forms and bioavailability
• Selecting a suitable API crystal form
• Controlling the desired API form in formulation and process development

Xiaoming (Sean) Chen, PhD
Senior Development Investigator, Drug Product Development & Manufacturing, OSI Pharmaceuticals
Inc

4:45 Novel Strategies For Salt Selection Concerning Solubility Enhancement, Salt Stability And Stabilization

• Discussing salt selection strategy and processes
• Areas of discussion will include:
• 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