Articles with "efflux ratio" as a keyword



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Simplified Method to Determine the Efflux Ratio on P-Glycoprotein Substrates Using Three-Compartment Model Analysis for Caco-2 Cell Assay Data

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Published in 2019 at "Pharmaceutical Research"

DOI: 10.1007/s11095-019-2729-x

Abstract: Multiple time-point sampling is required in transcellular transport studies to accurately calculate the appropriate efflux ratio (ER). Our study sought to develop a simplified method to determine the ER in Caco-2 cells. The equation for… read more here.

Keywords: three compartment; point; efflux ratio; compartment model ... See more keywords
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Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics.

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Published in 2020 at "Journal of pharmaceutical sciences"

DOI: 10.1016/j.xphs.2020.06.013

Abstract: Receptor Interacting Protein 2 (RIP2) kinase inhibitors have been reported for therapeutic opportunities in inflammatory bowel diseases such as Ulcerative Colitis and Crohn's disease. During lead optimization, team identified 4-aminoquinoline series and several compounds from… read more here.

Keywords: permeability high; high glycoprotein; efflux ratio; glycoprotein efflux ... See more keywords