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14C-saccharin was administered by gastric tube to 8 adult rhesus monkeys. The compound appeared promptly in the blood and reached a maximum value 1 to 2 hr after administration. Plasma levels and plasma clearance during the first 6 hr and urinary and fecal excretion over 96 hr were found to be independent of total dosage over a range of 0.04 to 10 mg/kg. Urinary excretion as a percentage of administered dose was approximately 91% in 24 hr, 97% in 48 hr, 98% in 72 hr and more than 98% in 96 hr. Total fecal excretion over 96 hr was approximately 1% of the administered dose. Thin-layer chromatographic analysis of urines confirmed the presence of 2 hydrolytic products in small amounts. Residual tissue levels in liver, spleen, kidneys, and skeletal muscle 96 hr after administration amounted to less than 0.1% of the administered dose.
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Pitkin et al. (1971) studied this question.
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