STUDIES ON METABOLIC FATE OF A NEW ANTIALLERGIC AGENT, AZELASTINE (4-(p-CHLOROBENZYL)-2-[N-METHYLPERHYDROAZEPINYL-(4)]-1-(2H)-PHTHALAZINONE HYDROCHLORIDE)

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Abstract
The metabolic fate of a new antiallergic agent, azelastine (4-(p-chlorobenzyl)-2-[N-methylperhydroazepinyl-(4)]-1-(2H)-phthalazinone hydrochloride) in rats and guinea pigs was investigated using its 14C-labeled compound. The blood level of radioactivity reached the maximum at 1-1.5 h after oral administration, indicating the rapid absorption of the drug from the gastrointestinal tract. A high concentration of radioactivity was detected in the lung of both species after oral or i.v. administration. The major pathway of excretion of radioactivity was by way of feces, in both species. The radioactivity excreted in feces was due to that which was excreted in bile and exsorbed into the gastrointestinal tract. When the drug was given to pregnant rats, the concentration of radioactivity in the fetus was significantly lower than those in the placenta and uterus, indicating the limited placental transfer of the drug. The successive oral administration of the drug in lower doses exerted no effect on the activity of microsomal drug-metabolizing enzymes of the rat liver; in higher doses, it had a slight effect.

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