Compositions of GLP-1 peptides and preparation thereof
The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.
1. A solid dosage pharmaceutical composition comprising (1) a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (salt of NAC) and (2) a granule;
wherein the granule comprises semaglutide, a binder, a filler, and no salt of NAC;
wherein the filler is at least 15% (w/w) of the granule; and
wherein the binder is less than 40% (w/w) of the granule.
2. The composition according to claim 1 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC).
3. The composition according to claim 1 , wherein the filler is microcrystalline cellulose.
4. The composition according to claim 1 , wherein the filler is 50-75% (w/w) of the granule.
5. The composition according to claim 4 , wherein the filler is microcrystalline cellulose.
6. The composition according to claim 1 , wherein the binder is povidone.
7. The composition according to claim 1 , wherein the binder is 15-25% (w/w) of the granule.
8. The composition according to claim 7 , wherein the binder is povidone.
9. The composition according to claim 1 , further comprising a lubricant that is not in the granule.
10. The composition according to claim 9 , wherein the lubricant is magnesium stearate.
11. The composition according to claim 1 , wherein the weight of the composition is in the range of 150 mg to 1000 mg.
12. The composition according to claim 11 , wherein the weight of the composition is in the range of 300 mg to 600 mg.
13. The composition according to claim 12 , wherein the weight of the composition is in the range of 350 mg to 450 g.
14. The composition according to claim 1 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC), the filler is microcrystalline cellulose, and the binder is povidone.
15. The composition according to claim 1 , wherein the filler is 50-75% (w/w) of the granule, and wherein the binder is 15-25% (w/w) of the granule.
16. The composition according to claim 15 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC), the filler is microcrystalline cellulose, and the binder is povidone.
17. The composition according to claim 14 , further comprising magnesium stearate that is not in the granule.
18. The composition according to claim 15 , further comprising magnesium stearate that is not in the granule.
19. The composition according to claim 16 , further comprising magnesium stearate that is not in the granule.
20. The composition according to claim 14 , wherein the weight of the composition is in the range of 300 mg to 600 mg.
21. The composition according to claim 15 , wherein the weight of the composition is in the range of 300 mg to 600 mg.
22. The composition according to claim 16 , wherein the weight of the composition is in the range of 300 mg to 600 mg.
23. The composition according to claim 1 , wherein the composition comprises at least 60% (w/w) of the salt of NAC.
24. The composition according to claim 23 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC).
25. The composition according to claim 23 , wherein the composition comprises at least 70% (w/w) of the salt of NAC.
26. The composition according to claim 25 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC).
27. The composition according to claim 16 , wherein the composition comprises at least 60% (w/w) of the SNAC.
28. The composition according to claim 27 , wherein the composition comprises at least 70% (w/w) of the SNAC.