Sucralose
Sucralose, a sweetener. A chlorinated disaccharide (4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose) in which three hydroxyls of sucrose are… Oral half-life 13 h.
A chlorinated disaccharide (4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose) in which three hydroxyls of sucrose are replaced by chlorine, blocking enzymatic hydrolysis by intestinal sucrase-isomaltase and salivary/pancreatic amylase. It binds the sweet-taste receptor (TAS1R2/TAS1R3 heterodimer) on lingual and enteroendocrine cells with ~600x the potency of sucrose, evoking sweetness without providing metabolizable carbohydrate or a meaningful glycemic/insulinemic response. The chlorination renders it metabolically inert: roughly 85% passes unabsorbed and is excreted in faeces, while the ~15% absorbed (partly via passive diffusion) is not catabolized and is cleared unchanged in urine, with a minor fraction (~2% of dose) as glucuronide conjugates. It is heat-stable, non-cariogenic, and contributes negligible calories.
E955; intensely sweet (~600x sucrose), non-nutritive and non-glycemic. FDA-approved general-purpose sweetener with ADI 5 mg/kg/day (EFSA 15 mg/kg/day, JECFA 15 mg/kg/day); generally well tolerated, though high intakes can cause GI/laxative effects and its safety/microbiome and thermal-degradation profiles remain debated. PK (Roberts 2000, n=8): only ~14.5% of an oral dose is absorbed (F≈0.145, recovered unchanged in urine) with an effective plasma t½ ~13 h (Tmax ~2 h); the remainder is excreted unchanged in faeces. PK: THE RECORD IS NOT MEASURING SUCRALOSE, AND THE SCHEMA HAS AN ENUM MEMBER FOR EXACTLY THAT. Its citation states "the effective half-life for the decline of plasma RADIOACTIVITY was 13hr" — total drug-related material, not the parent — and the analyte field was unset, so every surface presented it as a sucralose half-life. Declared. THE BIOAVAILABILITY IS ALSO A RECOVERY RATHER THAN A MEASUREMENT: "a mean of 14.5% (range 8.9 to 21.8%) of the radioactivity was excreted in urine and 78.3% ... in the faeces". For this compound the substitution is defensible — the faecal fraction is unabsorbed parent, "essentially unchanged sucralose" in that abstract own words — but it is defensible HERE and not in general, and about a sixth of the urinary figure is glucuronide rather than sucralose, so the parent-referenced value would be nearer 0.12. The catalogue still has no field for fractional absorption as distinct from bioavailability, which is the same schema gap the mineral pass logged. NO VOLUME IS AUTHORED AND NONE IS PUBLISHED: the paper reports a mean residence time of 18.8 h and no volume or clearance, so the curve renders against the solver default and that gap is recorded rather than filled.
Pharmacokinetics
- Oral — t½ 13 h · F 14%
Sources: PMID:10882816