新抗炎症薬N-(3-Chloro-2-methylphenyl)anthranilic Acid(GEA 6414)の代謝に関する研究(第1報)ヒト, イヌ, ウサギおよびラットの尿中代謝物

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After the oral administration of N-(3-chloro-2-methylphenyl) anthranilic acid (GEA-6414), the urinary metabolites were examined in human, dogs, rabbits and rats. Two kinds of metabolites, M-I and M-II, besides GEA 6414 were detected from the human urine by TLC and GLC. M-I and M-II were identified as N-(3-chloro-2-hydroxymethylphenyl) anthranilic acid and N-(3-chloro-4-hydroxy-2-methylphenyl) anthranilic acid, respectively. The glucuronides of M-I and M-II were estimated as major metabolites of GEA6414 in the human urine. M-I was also excreted along with its glucuronide in the urine from rabbits and rats. M-II was detected only in the urine from human and rats, but its glucuronide was excreted in the urine from human, rabbits and rats. M-II sulfate was detected only in the rat urine as a major metabolite. In the rabbit urine 64% of dosed GEA 6414 were excreted as its glycine conjugate. A little amount of GEA 6414 and its glucuronide were detected in the dog urine.
社団法人日本薬学会の論文
1981-03-25