Institute for International Research

Case Study: Application of IVIVC and BCS for Optimum Formulation Development

Recent years have seen large advancements of increasing focus on bio-relevant dissolution and in vitro-in vivo correlation (IVIVC) with the hope to aid formulation development.This presentation focuses on applications of IVIVC and Biopharmaceutics Classification System (BCS) in an attempt to powering the feasibility of developing optimum oral pharmaceutical products. Conventional and non-conventional dissolution methods and correlation of each method with in vivo results in conjunction with the BCS status of evaluated compounds will be addressed.

Dongzhou J. Liu, PhD, MS, MBA, Assistant Director, GLAXOSMITHKLINE

Case Study: Development of a Biorelevant In Vitro Dissolution Method Using USP Apparatus IV to Predict In Vivo Release Profile and Establish IVIVC

Dissolution testing plays many important roles throughout drug product development. However, traditional dissolution tests emphasize heavily on its QC role to get the complete drug release. The purpose of this study is to develop a bio-relevant dissolution method to predict the in-vivo drug release to guide the formulation development/selection for the clinical studies and to better design the clinical trials.

• Bio-relevant dissolution method using USP IV
• Rate vs. accumulative dissolution profile
• Prediction of in-vivo drug release rank order
• Prediction of food effect
• Guide formulation development
• Potential direct IVIVC without data deconvolution

Use and Importance of Dissolution in Generic Development Including IVIVC

Dissolution of a solid dosage form constitutes one of the primary tests to select a formulation with significant clinical relevance and to compare between different formulations. Dissolution is not only used as a quality control test to release batches on the market but also as a tool for development and validation of the formulation and a criteria of in vivo performance thanks to IVIVC. In generic development, dissolution tests can play a key role in improving the selection of API, identifying the critical process parameters which influence the formulation behavior and increasing the quality of the development thanks to IVIVC. This presentation will discuss how dissolution can be used to select between different active pharmaceutical ingredients (Examples of API dissolution testing using Apparent Dissolution techniques and USP Apparatus 4 – Flow Through Dissolution will be presented.), the possibility to develop IVIVC for generic and how to use dissolution to de-risk bioequivalence.

Eric Beyssac, PhD, Faculty of Pharmacy, ERT CIDAM, Universite d'Auvergne, Clermont-Ferrand, France

Provided by

Quality by Design: Understanding the Correlation between Drug Dissolution Behavior and Key Formulation Parameters

One challenge faced by many analytical scientists is how to develop and improve the dissolution method as the formulation evolves throughout the development phases. This presentation provides a case study about how to utilize alternative analytical technologies to the fundamental understanding of correlating drug dissolution behavior with key formulation parameters.

• Challenges faced by analytical scientists during parallel formulation development and dissolution method development
• Application of FBRM (Focused Beam Reflectance Measurement) to understand the impact of key formulation parameters on drug dissolution behavior
• Application of USP IV apparatus (flow-through-cell) to understand the impact of key formulation parameters on drug dissolution behavior
• Considerations of developing a "biorelevant" dissolution method

Interactive Panel Discussion: Dissolution Testing and Specification Setting: Where Does Dissolution Testing Add Value?

This interactive panel discussion explores how you can use dissolution testing to add value to your product development process. Hear best practices and key strategies directly from the industry on how to best implement value and give your data meaning. This session will also discuss how to best set your dissolution specification for optimum results.

Panel:

David Fortunato, Scientist, JOHNSON & JOHNSON PRD, LLC.

Jianmei Kochling, Group Leader, VERTEX PHARMACEUTICALS

Dongzhou J. Liu, PhD, MS, MBA, Assistant Director, GLAXOSMITHKLINE

Larry Stevens, Senior Research Scientist III, ALCON RESEARCH, LTD

Flow Through Dissolution Testing for Low Dose Products

USP Apparatus 4 or the flow through dissolution system has been employed for many years in the testing of different dosage forms such as tablets and capsules. However, recent formulations and drug delivery technologies developed by industry have required a newer approach to dissolution testing. The purpose of this presentation is to discuss the applications with case studies for low dose products.

Samir Haddouchi, Lab & Project Manager, SPS PHARMA SERVICES Educational Grant Provided by

Maximizing Productivity through Automation

Automation can significantly impact your dissolution testing process. During this session you will learn about the latest technology and how it can be implemented to save your company time and money. Strategies for utilizing automation for potential resource savings will be discussed.

• The State of Automation in Pharmaceuticals
• Selecting the Appropriate Technology
• Changing from Manual to Automated Methods
• Case Studies in Automation Implementation
• The Future of Automation in Pharmaceuticals

Accelerating Formulation Development with Fiber Optic Dissolution

Fiber optic dissolution has become increasingly popular in the last 5 years due to time savings attained when evaluating the dissolution rates of dosage forms. The real advantage lies with the expeditious processing and reporting of results seconds after the run is finished. This allows the analyst to screen several different formulations with the only rate-limiting step being the dissolution run. Another advantage of fiber optic dissolution is the nearly unlimited sampling rate without any loss of media. Hear two case studies detailing the advantages of fiber optic dissolution in formulation development from Novartis Pharmaceuticals and Pfizer.

• What are the advantages to using fiber optic dissolution?
• How can accurate data be generated in real time?
• How can methods be developed/validated?
• How can this technology be applied to support formulation screening?
• Case studies of the application of the system will be presented

Kevin C. Bynum, Fellow, NOVARTIS PHARMACEUTICAL

Andrew Blanchard, Global R&D, PFIZER