Compound Fa(%) Fa types Literature references Remarks Ganciclovir 3 Low [176]   Melagatran 5 Low In-house   Enalaprilat 10 Low [177]   Sulphasalazine 12 Low [178] Drain substrate Acyclovir 17 Low [128,180]   Chlorothiazide 25 Middle [178,180] Dose-dependent F;saturated abs Mannitol 26 Middle [178,181]   Atenolol 56 Middle [178,182]   Zomig 60 Middle In-house   Ranitidine 61 Middle [183] The Fa value is calculated from Fa=F/(1-CLH/QH); With transport protein interaction Digoxin 81 High [184] Static urinary excretion data, Fa values can be calculated from the oral and intravenous injection ;P-gp substrate Methotrexate 82 High [185] Static urinary excretion data, Fa values can be calculated from the oral and intravenous injection; a decrease in absorption at high doses Quinidine 90 High [186] The Fa value is calculated from Fa=F/(1-CLH/QH); P-gp/MRP inhibitor/substrate Antipyrine 100 High [187]   Caffeine 100 High [188]   Metoprolol 100 High [178,189]   probenecid 100 High [190] MRP inhibitor/substrate Propranolol 100 High [191]   Testerone 100 High [192]   Theophylline 100 High [193]   Verapamil 100 High [194] P-gp/MRP substrate inhibitor D-glucose 100 High   Glucose transport protein Glycine-proline 100 High   Dipeptide transport protein L-leucine 100 High   Amino acid transport protein L-phenylalanine 100 High   Amino acid transport protein

Table 2: It shows the establishment of the human oral absorption (Fa) and labelled compound permeability relationship in Caco-2 cell monolayers.

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