カブリロ-およびニコチノヒドロキサム酸の生体内分布, 排泄および代謝

概要

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Hydroxamic acid has been known to inhibit urease activity of gastrointestinal tract and decrease the level of blood ammonia. Using caprylo-and nicotinohydroxamic acid-[carbonyl-^<14>C] which are potent inhibitors of urease activity, distribution, metabolism and excretion of the compounds were studied after their oral administration to rats and guinea pigs. Caprylohydroxamic acid was rapidly hydrolyzed by liver homogenate to caprylic acid and hydroxylamine, and hydroxamic acid was not detected in any tissues except in gastrointestinal tract 2 hr after its administration. Radioactivity derived from hydroxamic acid was found in the liver and heart in considerable amounts, but most of total radioactivity was axcreted by expiration as CO_2 and several percentage was excreted in urine within 24 hr. Nicotinohydroxamic acid was slowly decomposed by liver homogenate and a small amount of hydroxamic acid remained in the tissues 2 hr after its administration. Radioactivity derived from hydroxamic acid was observed considerably in the liver and kidney, and widely distributed in other tissues. Half of total radioactivity was excreted in urine and a few percentage as CO_2 within 24 hr. A part of the radioactivity was retained in the body and excreted gradually only in urine. Pattern of metabolites of nicotinohydroxamic acid in urine was similar to those of nicotinamide already reported.
公益社団法人日本薬学会の論文
1973-12-25