Conference Day One: 17th April 2012

09.00 Welcome and Opening Address

Predicting, Mitigating and Overcoming the Challenges of Poor Solubility to Ensure Optimum Stability and Bioavailability of Drug Candidates

09.10 Best Practice Approaches to Overcoming Poorly Soluble Drugs

Pharmaceutical pipelines of the 21st century are highly populated with poorly soluble drugs that create common hurdles across the industry such as poor bioavailability and low dissolution rates. Solubility sits at the forefront of the challenges faced by formulation and drug delivery scientists worldwide. This presentation addresses:

• The development of methods to overcome the challenges of poorly soluble compounds, highlighting the importance of understanding the behavior of the dose form
• The use of nano-particles to improve bioavailability, what other methods are also options?
• The use of solid dispersions in overcoming biopharmaceutical limitations
• Practical case studies demonstrating how poor solubility has been overcome

Marcus Brewster
Senior Research Fellow Head of Dept. Drug Delivery Research
Johnson and Johnson

09.50 Experimental Methods for Assessing Super Saturation of Ionisable Drugs

It is possible to take advantage of super saturation to get a far higher concentration of some drugs into solution than would be represented by the equilibrium solubility of the crystalline material. But what extent of super saturation can be achieved, and under what conditions? And what is the duration of super saturation, before the concentration falls to the equilibrium solubility value? Using our patented CheqSol measurement technology, we have made careful measurements of kinetic solubility, equilibrium solubility and the extent and duration of super saturation for 130 drugs. From studying this data, we have learned how to:

• Assess the likelihood that a compound will persist in solution at the higher concentration associated with amorphous-form solubility
• Measure the extent and duration of super saturation
• Identify compounds that are likely to respond successfully to solubility-enhancement approaches using polymers and other additives

These practical methods for studying compound properties in solution are a valuable adjunct to traditional formulation approaches and will be covered in this presentation

John Comer
Chief Scientific Officer
Sirius Analytical

11.00 Nano Systems for Poorly Soluble and Permeable Compounds

This presentation will assess and answer the following questions:

• Why explore different delivery systems? For better medicines/therapeutics, the delivery system is as important as the drug.
• Why nano? Nano systems can be route independent making new indications possible.
• What to deliver? One size doesn't fit all.

Professor M.N.V Ravi Kumar
Professor of Drug Delivery
University of Strathclyde

11.40 Utility of Salts in Enabling Development of Poorly Soluble APIs

• Providing a background to the use of salts
• Assessing salt screening and selection and the influence of salts on physicochemical properties
• What is the relationship between salt/ polymorph/ solvate and what are typical basic salts?
• Exploring the need for stronger counter ions
• Highlighting the advantages and disadvantages of using salts and drawing conclusions

David Elder
Director of Product Development
GlaxoSmithKline

12.20 PANEL DISCUSSION: Exploring Best Practice Methods and Novel Approaches for Overcoming the Challenges of Poor Solubility and Stability

In this interactive session, hear from your peers and pose questions to an expert panellist team to gather and share ideas for improving bioavailability through ensuring solubility and stability.

14.00 Developing Super Saturation Based Formulations

• Assessing super saturation as a novel formulation technology to ensure the development of dosage forms with desirable biopharmaceutical properties
• Using super saturating drug delivery systems to improve oral bioavailability
• What are the benefits and limitations of a super saturation based formulation?

Rene Holm
Head of Preformulation
Lundbeck

14.40 Overcoming Poor Solubility Through Formulation with Mesoporous Silica Materials

• How do mesoporous silica materials enhance solubility?
• In vitro assessment of mesoporous silica-based formulations
• Case studies demonstrating how solubility-limited bioavailability has been overcome using mesoporous silica materials
• Proof of concept in humans

Michiel Van Speybroeck
Director, Research and Development
Formac Pharmaceuticals

15.50 Quality by Design: Ambitions and Realities

• How to build Quality by Design into each stage of drug development
• Analysing NIR as a spectroscopic tool, but what other models are out there?
• Developing effective risk management strategies to plan and prioritise experimental work
• Highlighting the subtle differences between, and the implications of, European and American regulation for QbD practices

Wim Oostra
Department Head
Merck

16.30 Continuous Manufacturing in Pharma: Technologies, Opportunities, Challenges, Trends & Drivers for Continuous Processing

• Considerations for formulation and pharmaceutical development within the continuous manufacturing paradigm
• Smoothening the interface between product - and process- development and between R&D and commercial manufacture
• Benefit of Continuous. Manufacturing Technologies within R&D - shortening development timelines with continuous manufacturing (CM) of pharmaceutical development material
• QC and regulatory aspects and meeting regulatory initiatives for QbD

Dr. Norbert Rasenack
Team Leader Continuous Manufacturing Downstream, Contin.Manuf Unit within Global R&D
Novartis Pharma

17.10 Chairperson’s Closing Remarks and End of Day One