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50 values of thrombin and trypsin inhibition and Caco-2 permeability values described in this paper were determined using the procedures indicated in reference 3
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50 values of thrombin and trypsin inhibition and Caco-2 permeability values described in this paper were determined using the procedures indicated in reference 3.
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7. Compounds 1 were characterised by NMR, MS, IC and HPLC.
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The oral bioavailability of compound 1c (racemate) in dogs was studied in Beagle dogs (weighing approximately 20 kg) which were given compound 1c at a dose of 10 mg/kg in 5% Gummi arabicum orally (n = 2) or in PEG 400/saline = 1/1 intravenously (n = 1). Plasma samples were collected and the concentrations of compound 1c were determined using HPLC. The enantiomeric ratio of 1c in the plasma samples was not determined. The individual oral bioavailability in these dogs was 31% and 41%
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8. The oral bioavailability of compound 1c (racemate) in dogs was studied in Beagle dogs (weighing approximately 20 kg) which were given compound 1c at a dose of 10 mg/kg in 5% Gummi arabicum orally (n = 2) or in PEG 400/saline = 1/1 intravenously (n = 1). Plasma samples were collected and the concentrations of compound 1c were determined using HPLC. The enantiomeric ratio of 1c in the plasma samples was not determined. The individual oral bioavailability in these dogs was 31% and 41%.
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