Category: sweetener
Aliases: E954, Sweet'N Low, Benzosulfimide, o-Sulfobenzoic acid imide, Sodium saccharin, 1,2-Benzisothiazol-3(2H)-one 1,1-dioxide, Saccharine, Benzoic sulfimide
Saccharin (C7H5NO3S, free acid) is a high-intensity non-nutritive sweetener roughly 300-400x sweeter than sucrose, with a characteristic bitter-metallic aftertaste at higher concentrations. It activates the sweet taste receptor, the T1R2/T1R3 heterodimer expressed on lingual taste cells, with the anionic sulfonyl-imide head group driving receptor binding; at high concentrations it also weakly antagonises the receptor, contributing to off-taste. It is essentially non-caloric and does not raise blood glucose or stimulate appreciable insulin release. In the body it is biologically inert: absorbed from the gut, not metabolised, not glucuronidated, and excreted unchanged via renal tubular secretion. Marketed as sodium or calcium salts for solubility. Approved as food additive E954; the rodent bladder-tumour signal was shown to be a male-rat-specific mechanism not relevant to humans, and it was delisted as a carcinogen.
PO: 1.17h
E954; non-nutritive sweetener ~300-400x sweeter than sucrose; JECFA ADI 0-5 mg/kg bw/day (as saccharin). Once flagged for rat bladder tumours but removed from US carcinogen lists in 2000 (mechanism not human-relevant); GRAS/approved in US, EU, and globally. PK (Sweatman 1981): oral fraction absorbed ~0.85; elimination t½ ~70 min (1.17 h, from the IV phase). Oral plasma curves are complex/variable, so ka and Vd are left to solver defaults.