Figure 2 Permeability of 10 compounds in 5 independent experiments. Results demonstrate the high reproducibility of the 3-day Caco-2 culture for the evaluation of permeability. These 10 compounds are chosen from a list of compounds recommended for the validation of Caco-2 permeability assay by the U.S. Food and Drug Administration.

doi:10.1201/9780203910696-67

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Figure 2 Permeability of 10 compounds in 5 independent experiments. Results demonstrate the high reproducibility of the 3-day Caco-2 culture for the evaluation of permeability. These 10 compounds are chosen from a list of compounds recommended for the validation of Caco-2 permeability assay by the U.S. Food and Drug Administration.

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ABSTRACT

Orally delivered drugs are firstly subjected to metabolism in the intestinal mucosa, which is now known to contain a high concentration of the 3A4 isoform of cytochrome P450. The metabolites plus the parent molecules that enter the systemic circulation are then further subjected to metabolism in the liver. The parent drug and its metabolites are then subjected to elimination either into feces via bile excretion in the liver, or into urine via the kidneys. In the kidney, further metabolism may occur. Drug metabolism is critical to three important drug properties: metabolic stability, toxicity, and drug-drug interaction.