Tuesday, November 18
5:00 - 6:00 pm Early Registration
Wednesday, November 19
7:30 am Registration and Morning Coffee
Separation at Scale: Chromatography and Crystallization
(Shared session with Mastering Process Chemistry Conference)
8:30 Chairperson’s Remarks
Orn Almarsson, Ph.D., Vice President of Pharmaceutical Chemistry, Alkermes Inc.
8:35 Supercritical Fluid Chromatography (SFC) as an Isolation Tool for By-Product and Impurity Identification
Todd Zelesky, Scientist, Development Analytical Department, Pfizer Inc.
As a drug moves successfully through the development stages of the pipeline it becomes increasingly important to identify drug related impurities. By-product structural information can be instrumental to the process chemists in moving forward with key reaction optimization decisions. Supercritical Fluid Chromatography (SFC) is an isolation and purification tool that allows for targeted impurities to be isolated quickly. SFC has many notable advantages over HPLC for the isolation of reaction impurities, including cost effectiveness and speed.
9:05 Case Studies of Analytical Challenges in API Process Research & Development
Yong Chen, Ph.D., Research Investigator, Process Analytical Chemistry, Process R&D, Global Pharmaceutical R&D, Abbott Laboratories
Analytical strategies for the investigation and control of process-related impurities during the development of scaled-up API processes will be discussed. Emphasis will be focused on orthogonal method development and innovative chromatographic approaches coupled with modern detection technologies. Case studies will demonstrate efficient approaches toward understanding and tracking the origin, fate, and rejection of critical impurities in the entire scale-up processes.
9:40 Networking Coffee Break, Poster and Exhibit Viewing
10:15 Pharmaceutical Co-Crystals: History and Relevance to Drug Development
Orn Almarsson, Ph.D., Vice President of Pharmaceutical Chemistry, Alkermes Inc.
The aim of this presentation will be to provide perspective on the recent development of the field of pharmaceutical co-crystals. Prior to 2002, this field was dormant, with a few examples of pharmaceutically relevant co-crystals scattered in the literature. A surge of interest ensued in 2002, spurred in part by productivity concerns and demand for innovation in pharmaceutical R&D. Areas of impact of pharmaceutical co-crystal technology will be discussed, including tailoring materials for improved product performance, processing and separations.
10:45 Scaling-Up Co-Crystal Crystallizations
Renato Chiarella, Ph.D., Scientist, Formulation Development, Johnson & Johnson Pharmaceutical Research and Development
11:15 Close of Session
11:15 Luncheon Technology Workshop (Sponsorships Available) or Lunch on Your Own
1:00 pm Comments by Session Chairperson
Opening Presentation
1:15 Protecting Your Drug Formulation in the Changing Patent Landscape
Janet B. Linn, J.D., L.L.M. in Trade Regulation, Eckert Seamans
As the result of an active Supreme Court and Congress, long standing principles of patent law are in flux. This presentation will summarize the effect of recent court decisions and proposed legislation and regulations on patent procurement and enforcement. The changing landscape needs to be considered to insure the best protection for intellectual property going forward.
Crystallization
1:45 Thermodynamic Approach to Crystal-Form Selection: A Case Study
Roxana F. Schlam, Ph.D., Solid-State Chemistry, ARD, Bristol-Myers Squibb
The selection of a crystalline form for development can be very challenging due to the number and/or nature of the forms emerging at the screening stage. The primary purpose of this presentation is to serve as a reference for projects that may encounter similar challenges. The focus points that will be detailed in the presentation are: (a) implications of using kinetic vs. thermodynamic data, (b) assessment of risks involved in “making forms” in the dryer, (c) use of thermodynamic information of the crystal systems for robust process design, and (d) characterization of solvates.
2:15 PAT for Product Quality and Batch-to-Batch Consistency in API Crystallization
Reginald Tan, Ph.D., Principal Scientist and Program Manager, Crystallization and Particle Science Group, Institute of Chemical and Engineering Sciences-Singapore
Crystallization is the most important unit operation for the separation and purification of chemicals in the pharmaceutical industries. Crystallization processes in pharmaceutical active ingredient manufacturing have been traditionally a recipe-based operations, offering little scope for dynamic process control and improvement. With the change in regulatory climate from Quality-by-Testing (QbT) to Quality-by-Design (QbD) and with the advent of the Process Analytical Technology (PAT) initiative, it is timely to examine the impact of such quality-based emphasis on crystallization control. In this presentation, we will discuss the use of PAT for control of crystallization. Case studies will be presented to demonstrate the new control strategies employing ATR-FTIR and FBRM in achieving the desired particle size distribution and batch-to-batch consistency in cooling and anti-solvent crystallization processes.
2:45 Networking Refreshment Break, Poster and Exhibit Viewing
3:30 Controlling Crystal Properties for Formulation
Helen P. Jones, Ph.D., Crystallization Specialist, AstraZeneca Process Engineering
The aim of crystallization process design is to develop robust processes to deliver crystalline material with consistent particle properties for formulation. Here a methodology for design of robust crystallization processes will be described. The effects of seeding, temperature cycling and pharmaceutically acceptable additives on particle size and morphology will be considered.
4:00 Crystal Engineering of Pharmaceutical Co-Crystals
Michael Zawarotco, Ph.D., Professor and Chair, Chemistry Department, University of South Florida
The range of crystal forms available for a given API has traditionally been limited to salts, polymorphs and hydrates/solvates. The field of crystal engineering focuses upon self-assembly of existing molecules or ions and it has evolved in such a manner that a wide range of new compounds can be generated using rational design strategies. APIs are particularly amenable to crystal engineering studies as exemplified by an emerging class of crystal forms that have been termed pharmaceutical co-crystals, i.e. co-crystals involving an API and a stoichiometric amount of a pharmaceutically acceptable co-crystal former. This presentation will address the history, design, preparation and properties of pharmaceutical co-crystals.
4:30 Closing Comments
4:45 Networking Reception in the Exhibit Hall
5:45 Close of Day