Xenobiotica. 1978 Aug;8(8):461-74. doi: 10.3109/00498257809056148.

The fate of saccharin impurities: the excretion and metabolism of toluene-2-sulphonamide in man and rat.

Xenobiotica; the fate of foreign compounds in biological systems

A G Renwick, L M Ball, D L Corina, R T Williams

PMID: 695690 DOI: 10.3109/00498257809056148

Abstract

Oral doses (20 mg/kg) of [Me-14C]toluene-2-sulphonamide were rapidly eliminated by rats (92% of dose in 24 h). Most of the 14C (88%) was recovered in the urine within 7 days with litte (5%) in the faeces. Larger oral doses (125 and 200 mg/kg) were eliminated more slowly (70 and 43% respectively in 24 h) but the overall distribution of 14C between urine and faeces was unchanged. 2. Low oral doses (0.2--0.4 mg/kg) of [Me-14C]toluene-2-sulphonamide were excreted more slowly in man than in the rat, with about 50% recovered in the urine in 24 h and 80% in 48 h. Negligible 14C (less than 1%) appeared in the faeces. 3. The main metabolites of toluene-2-sulphonamide were 2-sulphamoylbenzyl alcohol and its sulphate and glucuronic acid conjugates (80% of the 14C in the urine of rats and 35% in man) and saccharin (35% in man and 3% in the rat). Other metabolities found in the urine were 2-sulphamoylbenzoic acid (2% in the rat and 4% in man) and N-acetyltoluene-2-sulphonamide (6% in rat and 2% in man) together with unchanged compound (5% in rat and 3% in man).

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Substances

• Sulfonamides
• Toluene
• Saccharin

MeSH terms

• Animals
• Biotransformation
• Chromatography
• Feces / analysis
• Female
• Humans
• Male
• Mass Spectrometry
• Rats
• Saccharin*
• Spectrophotometry
• Sulfonamides / metabolism
• Sulfonamides / urine
• Toluene / analogs & derivatives
• Toluene / metabolism
• Toluene / urine

Publication Types

• Journal Article

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