Abstract
Compound solubility and permeability play an important role in oral absorption of drug candidates and ultimately their Biopharmaceutics Classification System (BCS) classification. BCS classification of drug candidates can influence the drug development path, specifically around formulation development, and the potential route used for drug administration. The in situ single pass perfused rat intestinal model has been shown to be highly predictive of human absorption of marketed drugs and thus, it is a useful tool for assessing the intestinal permeability of drug candidates during early stages of drug development. With the perfused rat intestinal model, the permeability of drug candidates is calculated using a macroscopic mass balance approach and a complete radial mixing model. This model is an effective approach used for selecting drug candidates with a desired BCS classification, which ultimately could improve the success rate in the selection of new chemical entities for eventual clinical use.
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Acknowledgements
The views expressed here are solely those of the author and do not reflect the opinions of Janssen Research & Development, LLC.
The authors would like to thank Shannon Dallas and Dennis Kalamaridis for reviewing the chapter.
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Markowska, M., Kao, L.M. (2014). In Situ Single Pass Perfused Rat Intestinal Model. In: Caldwell, G., Yan, Z. (eds) Optimization in Drug Discovery. Methods in Pharmacology and Toxicology. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-742-6_5
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DOI: https://doi.org/10.1007/978-1-62703-742-6_5
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