A Preliminary Report on the Pharmacokinetics of Saccharin in Man: Single Oral Dose Administration

: The pharmacokinetics of saccharin were studied in two human subjects. One male and one female subject ingested a single 100 mg oral dose of saccharin. Absorption was fast and the elimination half-lives were 1.2 and 6.6 hours for the male and female subject, respectively. Approximately 85% of the oral dose was recovered in the urine as intact saccharin and renal clearance approximated renal plasma flow when corrected for the unbound fraction of saccharin in plasma. Saccharin elimination appears to be related to previous saccharin ingestion, suggesting a high-retention compartment.