Saccharin
Saccharin, a sweetener. Saccharin (C7H5NO3S, free acid) is a high-intensity non-nutritive sweetener roughly 300-400x sweeter than sucrose, with… Oral half-life 1.2 h.
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.
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. PK: EVERY STORED NUMBER IS VERBATIM AND EACH ONE IS A DIFFERENT KIND OF QUANTITY THAN THE FIELD IT SITS IN. The half-life is "a two-compartment open model with a terminal half-life of 70 min" — a TERMINAL half-life from an INTRAVENOUS fit, stored on an oral route, which is the class-12 pairing and the class-8 route mismatch at once. The bioavailability is "The fraction absorbed was about 0.85", which is fractional ABSORPTION and not bioavailability; for saccharin the two coincide, because the same abstract says the compound is recovered quantitatively in urine with high renal clearance and no metabolism, so there is no first pass for them to differ across. THAT COINCIDENCE IS THE POINT: raloxifene carries the identical sentence shape, and storing its fraction absorbed as bioavailability would have been a fifty-fold error. NO VOLUME IS PUBLISHED — the abstract says only that "Renal clearance was high" — so the curve renders against the solver default, and this record note previously presented that as a choice ("ka and Vd are left to solver defaults") rather than as the gap it is. AND THE ABSTRACT WARNS AGAINST THE ORAL MODEL IN ITS OWN WORDS: "After oral administration (2 g) more complex and variable plasma concentration-time curves were obtained".
Pharmacokinetics
- Oral — t½ 1.2 h · F 85%
Sources: PMID:7303723