Sucralose metabolism and pharmacokinetics in man.
The metabolic and pharmacokinetic profile of sucralose was studied in human volunteers. Following a single oral dose of (14)C-sucralose (1mg/kg, 100 microCi) to eight male subjects, a mean of 14.5% (range 8.9 to 21.8%) of the radioactivity was excreted in urine and 78.3% (range 69.4 to 89.6%) in the faeces, within 5 days. The total recovery of radioactivity averaged 92.8%. Plasma concentrations of radioactivity were maximal at about 2 hours after dosing. The mean residence time (MRT) for sucralose was 18.8hr, while the effective half-life for the decline of plasma radioactivity was 13hr. Two volunteers given a higher oral dose (10mg/kg, 22.7 microCi) excreted a mean of 11.2% (9.6 and 12.7%) of the radioactivity in urine, and 85.5% (84.1 and 86.8%) in faeces over 5 days. The total recovery of radioactivity was 96.7%. The radiolabelled material present in faeces was essentially unchanged sucralose. Sucralose was the principal component in the urine together with two more polar components which accounted for only 2.6% of the administered dose (range 1.5 to 5.1% of dose); both metabolites possessed characteristics of glucuronide conjugates of sucralose.
Roberts
A
A
University of Southampton, Bassett Crescent East, Southampton SO9 3TU, UK.
Renwick
A G
AG
Sims
J
J
Snodin
D J
DJ
D000328:Adult; D019540:Area Under Curve; D002250:Carbon Radioisotopes / Q000097:blood / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D002852:Chromatography, Ion Exchange; D002855:Chromatography, Thin Layer; D005243:Feces / Q000737:chemistry; D005503:Food Additives / Q000493:pharmacokinetics; D008401:Gas Chromatography-Mass Spectrometry; D006207:Half-Life; D006801:Humans; D016018:Least-Squares Analysis; D008297:Male; D008875:Middle Aged; D008954:Models, Biological; D012588:Scintillation Counting; D013395:Sucrose / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000652:urine; D013549:Sweetening Agents / Q000493:pharmacokinetics*
D002250:Carbon Radioisotopes; D005503:Food Additives; D013549:Sweetening Agents; D013395:Sucrose; C026285:trichlorosucrose