Article date: October 1984
By: CO Meese, C Fischer, U Klotz, in Volume 18, Issue 4, pages 612-615
In two healthy male subjects the disposition of deuterated N‐(2H3) acetyl‐5‐aminosalicylic acid (d3‐ac‐5‐AS) was investigated after a single rectal dose of 500 mg d3‐ac‐5‐AS. Urine and plasma were analysed by h.p.l.c. and gas chromatography mass‐spectrometry. Peak concentrations of around 0.5 microgram/ml occurred within 6 h and plasma concentrations declined thereafter with a half‐life (t1/2) of about 6 h which was confirmed by urinary excretion data. Renal clearance of d3‐ac‐5‐AS ranged between 200 and 300 ml/min and only 4.4‐ 11.2% of the dose could be recovered in the 48 h urine. Since no undeuterated ac‐5‐AS could be detected in any of the plasma and urine samples an irreversible acetylation of 5‐AS is assumed in man.
DOI: 10.1111/j.1365-2125.1984.tb02513.x
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