-
Advances in Modeling and Simulation of Drug Absorption to Support Oral Formulation Development*
Wednesday, November 14
2:00 pm – 4:30 pm
Symposium
ACPE #073-999-07-567-L04
The role of development scientists working in Drug Discovery programs has significantly increased in discovering “developable” compounds. Despite these efforts, a significant number of new chemical entities continue to have absorption limitations. Some of the root causes of absorption problems are poor solubility, slow dissolution rate, short absorption window, poor permeability, food effects and pH-dependencies. In certain instances wherein a controlled or modified drug release is desirable, identification of in vivo properties of the drug such as absorption “window” and rate of absorption are important. As the NCE is progressed along to development groups, clinical formulation development has to accommodate these molecules along with an assurance of optimal delivery including adequate and consistent drug exposure in clinical trials. It is important to identify the root causes of sub-optimal absorption properties before embarking on costly and resource-intense formulation efforts and clinical trials. Herein the modeling and simulation of drug absorption has a great potential to form a rational basis of decision making during formulation development. It can guide the process towards a more focused formulation evaluation. This symposium will address recent advances in absorption modeling and simulation. An overview on how to delineate various absorption limitations using modeling approaches will be discussed. Followed by the general concept of absorption modeling, specific case studies where modeling and simulation has aided in rational formulation development will be presented. Some of the case studies will focus on a) setting API particle size specifications using dissolution/absorption models; b) pH-dependent absorption of ionizable compounds; and c) feasibility assessment of controlled release formulation. A special topic will be the effect of food, which can mechanistically be seen as a sum of several underlying effects. Emphasis is not only given to success stories but also the weaknesses and drawbacks of commercial and in-house modeling approaches.
Moderators
Venkatramana M. Rao, Ph.D.
Bristol-Myers Squibb Company
Martin Kuentz, Ph.D.
University of Applied Sciences
General Overview: Delineating Factors Limiting Oral Absorption
Lawrence X. Yu, Ph.D.
U.S. Food and Drug Administration
Can Dissolution/Absorption Models be Used to Set API Particle Size Specifications?
Venkatramana M. Rao, Ph.D.
Bristol-Myers Squibb Company
Drug Absorption Modeling as a Tool to Define the Strategy in Clinical Formulation Development
Martin Kuentz, Ph.D.
University of Applied Sciences
Predicting Pharmacokinetics of Drugs Using Physiologically Based Modelling – Application to Food Effects and Modified Release
Neil Parrott, Ph.D.
Hoffmann-La Roche, Inc.
*Session tentatively scheduled to be recorded.
Back to Top