Oral semaglutide: difference between revisions
Diff·revision 4 → 5·07:31, 12 Oct 2024
Difference between revision 4 and revision 5 of Oral semaglutide. 5 lines changed; the page grew by 408 bytes.
| Revision 4 — 00:07, 23 Sep 2024 Ref_Desk_Ron (talk) add the discontinued indication with its date 2,129 bytes ±0 | Revision 5 — 07:31, 12 Oct 2024 LiraLotte (talk) give the INN alongside the trade name at first mention 2,537 bytes +408 | ||
|---|---|---|---|
| 11 | Peptides are not orally bioavailable: gastric acid and proteases degrade them, and the intestinal epithelium excludes molecules of that size. SNAC addresses both by buffering the local gastric pH and transiently increasing local permeability, allowing absorption across the gastric mucosa itself rather than in the intestine.{{r|buckley2018}} | 11 | Peptides are not orally bioavailable: gastric acid and proteases degrade them, and the intestinal epithelium excludes molecules of that size. SNAC addresses both by buffering the local gastric pH and transiently increasing local permeability, allowing absorption across the gastric mucosa itself rather than in the intestine.{{r|buckley2018}} |
| 12 | 12 | ||
| + | 13 | The resulting bioavailability is roughly 0.4–1%, which is why the oral dose is an order of magnitude larger than the injected one in milligram terms. It is also critically dependent on dosing conditions.{{r|buckley2018}} | |
| + | 14 | ||
| 13 | == The absorption mechanism == | 15 | == The absorption mechanism == |
| 14 | SNAC acts locally and transiently. It raises pH in the immediate vicinity of the dissolving tablet, protecting the peptide from pepsin, and promotes transcellular absorption across the gastric epithelium. The effect is confined to the region around the tablet and to the period during which it dissolves.{{r|buckley2018}} | 16 | SNAC acts locally and transiently. It raises pH in the immediate vicinity of the dissolving tablet, protecting the peptide from pepsin, and promotes transcellular absorption across the gastric epithelium. The effect is confined to the region around the tablet and to the period during which it dissolves.{{r|buckley2018}} |
| ⋮ | ⋮ | ||
| 16 | Because absorption occurs at the tablet's location, anything that moves the tablet or dilutes the local environment reduces exposure. This is why the dosing conditions — fasting, no more than 120 mL of water, and a further 30 minutes without food, drink or other oral medicines — are part of the product rather than advice.{{r|knudsen2019}} | 18 | Because absorption occurs at the tablet's location, anything that moves the tablet or dilutes the local environment reduces exposure. This is why the dosing conditions — fasting, no more than 120 mL of water, and a further 30 minutes without food, drink or other oral medicines — are part of the product rather than advice.{{r|knudsen2019}} |
| 17 | 19 | ||
| + | 20 | Deviations change exposure severalfold, and between-individual variability is correspondingly larger than for the injected formulation.{{r|buckley2018}} | |
| + | 21 | ||
| 18 | == References == | 22 | == References == |
| 19 | {{reflist}} | 23 | {{reflist}} |
| ⋮ | ⋮ | ||
| 24 | [[Category:GLP-1 receptor agonists]] | 28 | [[Category:GLP-1 receptor agonists]] |
| 25 | [[Category:Peptide drugs]] | 29 | [[Category:Peptide drugs]] |
| + | 30 | [[Category:Pharmacokinetics]] | |
| 26 | 31 |