Metabolic Fate of d-cis-3-Acetoxy-5-[2-(dimethylamino) ethyl]-2,3-dihydro-2-(p-methoxyphenyl)-1,5-benzothiazepin-4 (5H)-one Hydrochloride (CRD-401)

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Absorption, excretion and metabolism of d-cis-3-acetoxy-5-[2-(dimethylamino) ethyl]-2,3-dihydro-2-(p-methoxyphenyl)-1,5-benzothiazepin-4 (5H)-one hydrochloride (CRD-401) were studied in rats. CRD-401 was found to be absorbed rapidly and almost completely from the digestive tract, the half-life for absorption being 26 min. More than 90% of the radioactivity after oral administration of ^<14>C-CRD-401 was recovered from the feces and urine within 72 hours. The feces is the major excretory route since approximately 60% of the total radioactivity recovered appeared in the 72 hour feces and 65% of the administrated radioactivity was excreted in the 24 hour bile. CRD-401 was extensively metabolized by rat since only 0.1% of the drug was recovered unchanged in the 24 hour urine and bile. Metabolic pathways of CRD-401 consisted of deacetylation, N-demethylation, O-demethylation, hydroxylation and N-oxidation. Major metabolites in urine and bile were deacetyl-O-demethyl-CRD-401,deacetyl-N, O-demethyl-CRD-401,and deacetyl-N, O-demetyl-methoxyl-CRD-401. The presence of N-oxide analogs of CRD-401 as minor metabolites was demonstrated in urine but not in bile.
公益社団法人日本薬学会の論文
1971-08-25