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Sucralose metabolism and pharmacokinetics in man

2000; Elsevier BV; Volume: 38; Linguagem: Inglês

10.1016/s0278-6915(00)00026-0

1873-6351

Ashley Roberts, A. G. Renwick, James W. Sims, David J. Snodin,

Glycosylation and Glycoproteins Research

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.