8:30 - 11:30 Workshop A: Challenges and Opportunities in Controlling Drug Substance Properties

(Registration at 8:00)

In order to control drug substance (DS) properties one has to select an optimal form (specific polymorph or hydrate of free form, salt, or co-crystal) and be able to consistently manufacture it with the same particle size (PS), particle size distribution (PSD), and crystal surface attributes.

The use of automated and robotic systems in salt/co-crystal and polymorph screening, and in early crystallization development experimentation, facilitates DS form selection. Ultimate properties of DS are largely determined by the way the batch precipitation or crystallization processes are conducted and to obtain crystalline material of desired properties consistently, these processes must be carefully controlled. This can be accomplished via in-situ seeding that simplifies the design and control of batch precipitation/crystallization and gives the results comparable with the conventional seeding approach. Continuous precipitation/crystallization removes the risk of batch-to-batch variability and ensures an optimal control of PS, PSD, and particle surface attributes.

What will be covered:

• Why investigate the solid-state of your drug?
• Polymorphism
• Addressing polymorphism: Screening and characterization
• Crystallization of difficult-to-crystallize materials
• Selection of optimum solid form of drug substance
• Chiral material analysis
• Drug substance specifications

Benefits of attending:

• Understand best strategies for selecting an optimal form to control drug substance
• Weigh the pros and cons of different automated screening systems
• Discover the benefits of in-situ seeding for batch design and control
• Display methods and techniques for reducing risk of batch-to-batch variability

Your Workshop Leader:

Peter Karpinski
PhD, US Leader of Salt & Polymorphism and Particle Engineering Networks
Novartis Pharmaceuticals Corp

11:30 - 2:00 Workshop B: Biopharmaceutical Considerations in the Design of Oral Modified Release Drug Delivery Systems

(Registration at 11:00) Lunch Included

This workshop will highlight biopharmaceutical factors that must be considered in the design, evaluation and development of modified release dosage forms. It will include hydrophilic matrices, osmotic pump and multi-unit delivery systems. The influence of electrolyte concentration and polymer character, drug properties on the textural and micro-environmental conditions within delivery systems relative to the conditions of gastro-intestinal tract, drug release and absorption will be discussed. Examples for each class of drug based on their BCS (Biopharmaceutical Classification System) scheme will be presented and relative influence of formulation design, transit time and GI physiology on absorption and bioavailability in the context of IVIVC will be discussed.

What will be covered:

• Displaying the influence of electrolyte concentration and polymer character
• Uncovering delivery system textural properties
• Discussing issues related to insoluble drugs and or highly soluble drugs based on BCS system
• Identifying drug release mechanisms and methodologies in connection with IVIVC

Benefits of attending:

• Uncovering a series of fundamental considerations in oral modified release drug delivery systems
• Discovering many novel drug release mechanisms and methodologies applied in their evaluation
• Specific case studies will be used to illustrate textural properties of delivery systems relative to the GI environment

Your Workshop Leader:

Reza Fassihi
Ph.D, AAPS Fellow, Professor of Biopharmaceutics and Industrial Pharmacy
Temple University

2:30 - 5:00 Workshop C: Toxicology Formulation Development: Challenges and Solutions

(Registration at 2:00)

Toxicology formulation is an essential component of drug development to enable successful toxicology study of new drug candidate. The requirement for adequate exposure at high doses to establish a safety window often imposes formulation challenges to poorly soluble compounds. Novel formulation technologies and excipients may be required to achieve the exposure target. However, a balance between implementing novel formulation technologies and controlling the safety risk of excipients needs to be considered.

What will be covered:

• Toxicology formulation development: basic procedures and general considerations
• Excipient acceptance criteria in toxicology formulation
• Toxicology formulation development from a toxicologist perspective
• Review on toxicology formulations in NDA filing of marketed drugs
• Novel formulation technologies to enhance exposure in toxicology species

Benefits of attending:

• Basic procedures and general considerations of toxicology formulation development
• Learn safety of common and novel excipients
• Broaden the knowledge of acceptable toxicology formulations
• Understand what a toxicologist needs from a toxicology formulation
• Learn novel formulation technologies that solve exposure limit of poorly soluble compounds

Your Workshop Leader:

Chong-Hui Gu
PhD, Associate Director, Pharmaceutical Development
Vertex Pharmaceuticals

5:30 - 8:00 Workshop D: Enhancing Solubility by Liposome Technology for Water-Insoluble Drugs in Parenteral Application

(Registration at 5:00) Dinner Included

Liposomes are unique as drug carriers in that they can encapsulate drugs with widely varying polarities. Hydrophilic drugs can be entrapped in the aqueous spaces while lipophilic drugs can be incorporated into the lipid membranes. Using a liposomal formulation can dramatically increase the apparent aqueous solubility of a lipophilic drug, making possible delivery of a dose much higher than its water solubility. A stable liposomal formulation entrapped water-insoluble drug is often achievable without precipitation upon dilution. Scalable manufacturing of liposomes is challenged, but process development and optimization can usually overcome some scale-up issues. A case study of the latest FDA-approved marketed product will be discussed during the session.

What will be covered:

• Basic procedures and general considerations of liposomal formulation development
• Excipient acceptance criteria in liposomal formulation
• Process consideration and manufacturing scalable batches
• Injectable liposomal formulation development for water-insoluble drugs – case study of an latest FDA-approved product

Benefits of attending:

• Understand the basic concepts of phospholipids, bilayer structures and liposomes
• Learn how to develop liposomal formulations based on bilayer structure and physicochemical properties of compounds
• Learn the process development of liposomes
• Learn the aseptic process of liposomal formulations
• Understand what a formulator needs to know the key parameters in scalable liposomal manufacturing
• Learn how to take advantage of drug-delivery technologies to develop quality based improved products to the marketplace

Your Workshop Leader:

Ron Liu
PhD MBA, President & Chief Executive Officer
AustarPharma