Oral Dosing of GLP-1 Compounds
The present invention relates to improved uses of GLP-1 peptides in oral therapy.
1 . A solid composition comprising a GLP-1 peptide and an enhancer,
wherein
a) said peptide has a plasma half-life in humans of at least 60 hours;
b) said composition is administered orally at least 3 times; and
c) said composition is administered such that the ratio between the plasma half-life in days in humans of said peptide and the dosing interval in days of said composition is more than 2:1.
2 . The composition according to claim 1 , wherein said composition is administered every second day or more frequently.
3 . The composition according to claim 2 , wherein said composition is administered once daily.
4 . The composition according to claim 1 , wherein said composition is in the form of a tablet.
5 . The composition according to claim 1 , wherein said composition is administered at least 5 times.
6 . The composition according to claim 1 , wherein said enhancer is a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, such as SNAC.
7 . The composition according to claim 6 , wherein the amount of SNAC is 100-500 mg SNAC.
8 . The composition according to claim 1 , wherein said enhancer is a salt of capric acid, such as sodium caprate.
9 . The composition according to claim 1 , wherein said peptide has plasma half-life in humans of at least 72 hours.
10 . The composition according to claim 1 , wherein said peptide is administered in an amount of 0.01-100 mg.
11 . The composition according to claim 7 , wherein said composition comprises 1-100 mg GLP-1 peptide.
12 . The composition according to claim 11 , wherein said peptide is semaglutide or N ε26 {2-[2-(2-{2-[2-(2-{(S)-4-Carboxy-4-[10-(4-carboxy-phenoxy)decanoylamino]butyrylamino}ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}, N ε37 -{2-[2-(2-{2-[2-(2-{(S)-4-carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)-ethoxy]acetylamino}ethoxy)ethoxy]acetyl}-[Aib 8 ,Arg 34 ,Lys 37 ]GLP-1(7-37)-OH.
13 . The composition according to claim 12 , wherein said composition comprises 2-60 mg semaglutide and 200-400 mg SNAC.
14 . The composition according to claim 1 , wherein said composition further comprises one or more pharmaceutically acceptable excipients.
15 . (canceled)
16 . A method for treating diabetes and/or obesity in a subject in need of such treatment, said method comprising administering to said subject a therapeutically effective amount of a composition according to claim 1 .
17 . The composition according to claim 6 , wherein the amount of SNAC is 50-90%(w/w) of said composition.
18 . The composition according to claim 17 , wherein said composition comprises 1-100 mg GLP-1 peptide.
19 . The composition according to claim 18 , wherein said peptide is semaglutide or N ε26 {2-[2-(2-{2-[2-(2-{(S)-4-Carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)-ethoxy]acetylamino}ethoxy)ethoxy]acetyl}, N ε37 -{2-[2-(2-{2-[2-(2-{(S)-4-carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}-[Aib 8 ,Arg 34 ,Lys 37 ]GLP-1(7-37)-OH.
20 . The composition according to claim 19 , wherein said composition comprises 2-60 mg semaglutide.