Understanding the effect of API properties on bioavailability through absorption modeling.
Selection of API phase is one of the first decision points in the formulation development process. Subsequent to phase selection, the focus shifts to the API physical properties such as particle size. Oftentimes, such properties are closely monitored throughout the drug development, as they can have a direct impact on the formulation bioperformance. The purpose of this mini-review was to describe the potential for application of absorption modeling in understanding the effect of API properties on bioavailability. Examples are provided to demonstrate how absorption modeling can be applied both early on to set the formulation strategy as well as during the development process to help with setting of specifications around the API. Limitations of the existing models and areas of possible expansion of such tools are also discussed.
Kesisoglou
Filippos
F
Department of Pharmaceutical Research, Merck Research Laboratories, Merck & Co., Inc., WP75B-210, 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486-0004, USA. filippos_kesisoglou@merck.com
Wu
Yunhui
Y
D000042:Absorption / Q000502:physiology*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003198:Computer Simulation; D004355:Drug Stability; D005772:Gastrointestinal Transit; D006801:Humans; D007700:Kinetics; D008954:Models, Biological; D008962:Models, Theoretical; D010316:Particle Size; D012995:Solubility