Conference Day One: Tuesday 24th, June 2008

09.00 Welcome From Pharma IQ And Chairperson’s Opening Remarks

09.10 Application Of Solid Dispersion And Nanoparticulate Formulation Technologies For Poorly Soluble Drug Candidates

• Identification of solid dispersions and nanoparticulate formulations as technologies to overcome poor solubility and bioavailability issues
• The importance of elucidating the background to these approaches with respect to the increasing numbers of products appearing in the market
• Discussion of former hurdles and current improvements of understanding, selecting and applying technologies successfully to new molecules
• Case study discussion illustrating a solvent based process for making solid dispersions, illustrating current achievements in this field

Dr Carsten Timpe
Fellow
Novartis

09.55 RightSize™ Particle Manufacture From Discovery To Production; A Robust, One Step Manufacturing Process For:

• Solid dispersions
• Particle size control down to nm range
• Pure crystals of predetermined polymorph
• Good crystallographic properties

Dr Per Andersson
CEO
XSPAY

10.45 Solubility Modeling Aspects for Drug Development

Drug solubility in different solvents is a very important consideration at multiple stages of the drug development process, such as formulation, chemical process development and solid form screening. The following aspects of solubility modeling are covered in the present study: QSPR model for b-Cyclodextrin complexation free energy; clustering of solvents to get a diverse subset for accelerated crystallization and solubility screening, as well as relative solubility of crystalline polymorphs. Two independent models of b-Cyclodextrin complexation energy are considered: a simple PLS model based on several s-moment (COSMOTherm) descriptors, and a Cubist recursive partitioning model based on a larger set of traditional 2D descriptors. Clustering of a set of about 70 typical organic solvents is performed based solely on the s-moments descriptors. An approach is suggested for polymorph solubility prediction in different solvents, which combines the COSMOTherm solvation free energy calculations with a modified approximation to the polymorphs free energies of fusion.

Yuriy Abramov
Principal Scientist
Pfizer

11.30 Solubility As A Determinant Of Form Selection

In recent years, drug candidate compounds tend to become more lipophilic and less soluble and this can limit their bioavailability. The need to achieve acceptably high solubilities and dissolution rates can play a major part in solid form selection and may favor the development of forms other than the conventional crystalline free bases and salts, in particular amorphous and co-crystal forms. Examples of the improved properties obtainable in this way will be presented. Amorphous APIs are often dispersed in polymer matrices to increase their glass transition temperatures and minimise the probability of degradation or crystallisation. An example of a dispersion screen to identify the most suitable dispersant and conditions for preparing the dispersion will be given. Subjects:

• Solubility and dissolution rate as criteria for form selection
• Stabilisation of amorphous products in solid dispersions

Dr Edwin Aret
Scientist
Avantium

13.45 Developing Early Formulation In Vivo Studies

• Strategy and techniques of early formulation development for animal studies
• In silico and in vitro techniques for early formulation evaluation
• Case study examples
• How to get the most out of in vivo results of early formulation

Dr Chong-Hui Gu
Associate Director
Vertex Pharmaceuticals

14.30 Formulations For In Vivo Studies In Discovery And Preclinical Development

• Solubility: crucial property for formulation and absorption
• Physiological and anatomical characteristics of animal models to be considered
• Test formulations for intravenous administration
• Test formulations for oral administration and biopharmaceutical characterisation

Dr Stephan Buchmann
Head of Preformulation and Preclinical Galenics
Actelion Pharmaceutical

15.45 Dose, Dissolution Rate And Solubility: Impact Or Oral Bioavailability

• Understanding GI physiology
• "In vivo" solubility
• Does it make sense to draw correlation between in vitro dissolution and in vivo absorption?

Dr Sesha Neervannan
Vice President, Pharmaceutical Development
ALLERGAN

16.30 Formulations For Toxicology Studies: Current Challenges And Future Prospects

• Which formulations, what governs the choice?
• How early should we consider the various possibilities?
  • Earlier link
  • Link to discovery PK
• Recent case studies, solutions vs suspensions vs new vehicles

Dr Claire Mackie Director Discovery Adme/tox. Johnson and Johnson

Dr Marcus Brewster Distinguished Research Fellow, Pharmaceutical Research Johnson and Johnson

Dr Ann Lampo Senior Director, Early Development Toxicology Johnson and Johnson

17.15 Roundtable Discussion: Looking At The Future Of Various Markets:

• Nanosuspension in improving solubility
• Solid dispersion in solubility
• Invitro and Invivo studies in improving solubility

17.45 Closing Remarks And Networking Drinks Reception

[ Register Now] · [ Next: Conference Day Two: Wednesday 25th, June 2008 ]