Solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl) amino) caprylic acid
The present invention relates to solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and their use in medicine.
1. A solid composition for oral administration comprising a GLP-1 agonist, a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, magnesium stearate, povidone, and microcrystalline cellulose,
wherein the GLP-1 agonist is semaglutide,
wherein the composition comprises at least 60% (w/w) of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.
2. The composition according to claim 1 , wherein the composition comprises 0.1-10% (w/w) of the magnesium stearate, 0.1-10% (w/w) of the povidone, and 5-40% (w/w) of the microcrystalline cellulose; and wherein the sum of the magnesium stearate, the povidone, and the microcrystalline cellulose is no more than 40% (w/w) of the composition.
3. The composition according to claim 2 , wherein the composition comprises 0.5-5% (w/w) of the magnesium stearate.
4. The composition according to claim 3 , wherein the composition comprises 1-3.5% (w/w) of the magnesium stearate.
5. The composition according to claim 4 , wherein the composition comprises 1% (w/w) of the magnesium stearate.
6. The composition according to claim 2 , wherein the composition comprises 0.2-4% (w/w) of the povidone.
7. The composition according to claim 6 , wherein the composition comprises 0.5-3% (w/w) of the povidone.
8. The composition according to claim 7 , wherein the composition comprises 1% (w/w) or 2% (w/w) of the povidone.
9. The composition according to claim 2 , wherein the composition comprises 10-30% (w/w) of the microcrystalline cellulose.
10. The composition according to claim 9 , wherein the composition comprises 5-25% (w/w) of the microcrystalline cellulose.
11. The composition according to claim 10 , wherein the composition comprises a percentage (w/w) of the microcrystalline cellulose selected from the group consisting of 10.9% (w/w), 18% (w/w), 19.5% (w/w), and 20.5% (w/w).
12. A solid composition for oral administration comprising a semaglutide, a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, a lubricant, a binder, and a filler,
wherein the composition comprises at least 60% (w/w) of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid,
wherein the composition comprises 1-3.5% (w/w) of the magnesium stearate,
wherein the composition comprises 0.5-3% (w/w) of the povidone, and
wherein the composition comprises 5-25% (w/w) of the microcrystalline cellulose.
13. The composition according to claim 12 , wherein the composition comprises 2% (w/w) of the povidone.
14. The composition according to claim 12 , wherein the composition comprises at least 70% (w/w) of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.
15. The composition according to claim 14 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC).
16. The composition according to claim 15 , wherein the composition comprises 2% (w/w) of the povidone.
17. A solid composition for oral administration comprising semaglutide, N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC), a lubricant, a binder, and a filler,
wherein the composition comprises 300 mg of SNAC,
wherein the composition comprises 1-3.5% (w/w) of the magnesium stearate,
wherein the composition comprises 0.5-3% (w/w) of the povidone, and
wherein the composition comprises 5-25% (w/w) of the microcrystalline cellulose.
18. The composition according to claim 17 , wherein the composition comprises 2% (w/w) of the povidone.