7th Annual Improving Solubility Conference

8:00 AM Registration & Morning Coffee

8:20 AM Chairperson’s Welcome & Opening Remarks

8:30 AM KEYNOTE: Introducing Levitation Technology for the Production of Amorphous Drugs

C.J. Benmore , Physicist, Argonne National Laboratory

The pharmaceutical industry is all too familiar with the challenges of the amorphous state. Scientists at the U.S. Department of Energy’s (DOE) Argonne National Laboratory have discovered a way to use sound waves to levitate individual droplets of solutions containing different pharmaceuticals.

How this technique was discovered and how it works
Powerful analytical tool for understanding the conditions that make for the best amorphous preparation
The Implications: How this could lead to the development of drugs with higher bioavailability

C.J. Benmore
Physicist
Argonne National Laboratory

9:15 AM Developing Super Saturation Based Formulations

Rene Holm , Head, Preformulation, H. Lundbeck

Super saturated formulations systems are currently under extended evaluation by a number of companies and academic groups as a new formulation system for low soluble compounds. And the term, as well as being under intense scrutiny, is being used in several different relations. These different types of supersaturations will be touched upon and, some of the frequently used crystallization inhibitors will be be discussed along with new developments within oversaturated lipid based formulations systems, such as:

Lipid-based formulations
Rapidly dissolving solid forms
Solid dispersions, prodrugs, co-crystals, and nanoformulations

Rene Holm
Head, Preformulation
H. Lundbeck

10:00 AM Morning Networking Break

10:30 AM Computational Approaches to Guide Solubility Improvement of Pharmaceuticals

Yuriy Abramov , Sr. Principle Scientist, Pfizer

Computational Chemistry is fundamental to bridging the scientific and cultural gap between R&D discovery and R&D development. Computational methods have traditionally focused on small, rigid molecules to guide experimental research, and to measure properties such as solubility. However, there has been advancement of computational approaches that can be applied to pharmaceutically relevant molecules. This unique study covers:

Thermodynamic cycle calculations to guide solubility improvement strategies
Rational co-former or solvent selections for co-crystallization or desolvation
Modeling of Cyclodextrins complexation free energies
Prediction of relative polymorph solubilities

Yuriy Abramov
Sr. Principle Scientist
Pfizer

11:15 AM Reducing Development Timelines and Cost of Lipid-Based Drug Delivery: The Lipidex® Experience

Eduardo Jule , Global R&D, Capsugel

Overview of innovative means of controlling outcomes through lipidbased technology.

Evaluation of the choice of appropriate lipid excipients (oils,surfactants, cosurfactants, cosolvents) Based on API
biopharmaceutical properties
Discussing the means of optimizing lipid excipient blends to meet the desired target dose
Demonstrating phase diagrams, rationale and selection – the Lipidex® database
Assessing technology to select the optimal lipid formulation based on in vitro evaluation (dispersion, digestion)
Examining technology impact on scale up and manufacturing (capsule compatibility, process parameters)

Eduardo Jule
Global R&D
Capsugel

12:00 PM Networking Lunch

1:00 PM Toxicology Formulation Strategies and Enabled Formulation Development

Mengwei Hu , Development Fellow, Merck

Toxicology formulation is an essential component of drug development for any new drug candidate. Poorly soluble compounds are less likely to remain stable during the formulation process, especially as novel formulation technologies and excipients may be required to achieve the exposure target. Finding the “sweet spot” between implementing novel formulation technologies and controlling the safety risk of excipients needs to be considered. This session explores:

Strategies for formulation screening and selection
Excipient considerations
Enabled formulations development and case studies

Mengwei Hu
Development Fellow
Merck

1:45 PM Absorption Risk Assessment and Feedback Paradigm in Early Discovery Support

Shobha Bhattachar , Sr. Research Scientist, Eli Lilly & Company

It is a well known fact that poorly soluble compounds pose significant challenges in development. Despite the wide variety of technologies available today, enablement of poorly soluble compounds come with many challenges, especially as the doses increase beyond a certain optimum value. It is essential, therefore, that Preformulation scientists on discovery teams assess absorption risks in a stage appropriate manner and provide continuous feedback to the teams in order to influence the selection of appropriate compounds for development.

Novel approaches that have successfully been used to make these assessments will be discussed
Illustrative case studies

Shobha Bhattachar
Sr. Research Scientist
Eli Lilly & Company

2:30 PM Afternoon Refreshment & Networking Break

3:00 PM Experimental Methods for Investigating & Modifying Supersaturation and Precipitation Behavior of Poorly Soluble Drugs

Jon Mole , Executive Vice President, Sirius Analytical Inc

Solubility measurement using titration with mass and charge balance analysis to determine concentration in the presence of precipitate
Using solid dispersions to enhance solubility and supersaturation
Applying this knowledge in small-scale dissolution studies with solubility enhancement and simulated absorption
Surface Dissolution Imaging and real-time particle size & shape measurement to enhance mechanistic understanding of solubility & dissolution

Jon Mole
Executive Vice President
Sirius Analytical Inc

3:45 PM Amorphous Solid Dispersions: toward a predictable science

Marshall Crew , President/Co-Founder, Agere Pharmaceuticals

Amorphous solid dispersions were first introduced to the industry over 40 years ago and since that time a tremendous amount of research has been conducted to understand the science of the solid and solution state. However, formulation development still remains largely an empirically-driven process. Therefore, there is a need to make the formulation process a rigorous, predictable science. Specifically, such an approach must be centered on the API and excipient molecular and bulk properties. This information would ideally be sufficient to predict the optimal combination of:

Excipient type and API loading
Manufacturing conditions
Performance enhancement
Physical and chemical stability

Marshall Crew
President/Co-Founder
Agere Pharmaceuticals

4:30 PM Rational Formulation Design Guided by Biopharmaceutics Modeling and Automated Formulation Screening

Chong-Hui Gu , Director, Agios Pharmaceuticals

Designing formulations to be as efficacious as possible is on the top of mind for any pharmaceutical scientist. Biopharmaceutics modeling is considered as an important early step to assessing biologically relevant solubility characteristics and an initial step toward choosing dosage form design and formulation options. This session will explain:

Examining why to tailor your formulation platform based on BCS class
Discussing the extension of BCS classification for formulation selection
Evaluating pH-solubility profile and modified solubility criteria
Invaluable screening techniques as well as the newest automation

Chong-Hui Gu
Director
Agios Pharmaceuticals

5:00 PM Strategies to Overcome Drug Solubility Challenges Utilizing Advances in Gelatin and OptiShellTM Soft Capsule Technologies

Norman Stroud , Director of Technology Development, Catalent Pharma Solutions

Overview of soft capsule technologies - conventional gelatin-based capsule shells and OptiShellTM
The advantages of using softgels for the encapsulation of drugs solubilized in hydrophilic vehicles
Recent developments and opportunities to overcome solubility challenges using polysaccharide-based soft capsule shells
Lipid-based fill formulations - SEDDS and SMEDDS

Norman Stroud
Director of Technology Development
Catalent Pharma Solutions

5:45 PM Application of Nanosuspension to Improve the Bioavailability and Permeability of Poorly Soluble Drugs

Indrajit Ghosh , Principal Scientist/Project leader, Pharmaceutical Development Technology, Novartis

The selection of proper special drug delivery approach in order is essential to increase the exposure of poorly soluble drugs. Exploring the potential of nanosuspension formulation for different dosage forms is crucial to reviewing whether or not this technique would increase the bioavailability of your products. This session covers the challenges and solutions during the formulation design of nanosuspension systems, as well as:

Identification of critical process parameters to prepare stable nanosuspension by top down approach
Importance of appropriate nanoparticle size on oral drug absorption
Case studies to demonstrate the permeability enhancement of poorly soluble drug through the human skin

Indrajit Ghosh
Principal Scientist/Project leader, Pharmaceutical Development Technology
Novartis