Pharmacokinetics of an Antiallergic Agent, 1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole Difumarate (KG-2413) after Oral Administration : Interspecies Differences in Rats, Guinea Pigs and Dogs

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The pharmacokinetics of an antiallergic agent, 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole difumarate (KG-2413) after oral administration were studied in rats, guinea pigs and dogs. Maximum plasma level (C_<max>) appeared at 23,32 and 51 min after dosing in rats, guinea pigs and dogs, respectively. Plasma half-lives of the terminal phase were comparable to those after intravenous administration in each animal species. Pronounced interspecies differences were observed in the C_<max>/dose and area under the plasma concentration-time curve (AUC)/dose, namely, these values were high in guinea pigs and low in rats and dogs. The extents of bioavailability were 0.036 in rats (20 mg/kg), 0.50 in guinea pigs (2 mg/kg) and 0.052 in dogs (2 mg/kg). These variations in the pharmacokinetic parameters in the animals were assumed to be mostly due to the species difference in the hepatic intrinsic clearance.
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