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) semaglutide and (2) a granule;
wherein the granule comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (salt of NAC), a lubricant, and no semaglutide;
wherein the salt of NAC is at least 75% (w/w) of the granule; and
wherein the lubricant is less than 10% (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 salt of NAC is 80-86% (w/w) of the granule.
4. The composition according to claim 3 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC).
5. The composition according to claim 1 , wherein the lubricant is magnesium stearate.
6. The composition according to claim 1 , wherein the lubricant is 1-3% (w/w) of the granule.
7. The composition according to claim 6 , wherein the lubricant is magnesium stearate.
8. The composition according to claim 1 , wherein the granule further comprises a filler.
9. The composition according to claim 8 , wherein the filler is microcrystalline cellulose.
10. The composition according to claim 8 , wherein the microcrystalline cellulose is 10-20% (w/w) of the granule.
11. The composition according to claim 8 , wherein the microcrystalline cellulose is less than 20% (w/w) of the granule.
12. The composition according to claim 11 , wherein the microcrystalline cellulose is 14-17% (w/w) of the granule.
13. The composition according to claim 1 , wherein the weight of the composition is in the range of 150 mg to 1000 mg.
14. The composition according to claim 13 , wherein the weight of the composition is in the range of 300 mg to 600 mg.
15. The composition according to claim 14 , wherein the weight of the composition is in the range of 350 mg to 450 g.
16. The composition according to claim 1 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC), and wherein the lubricant is magnesium stearate.
17. The composition according to claim 16 , wherein the salt of NAC is 80-86% (w/w) of the granule, and wherein the lubricant is 1-3% (w/w) of the granule.
18. The composition according to claim 17 , wherein the granule further comprises a filler, wherein the filler is microcrystalline cellulose, and wherein the microcrystalline cellulose is 10-20% (w/w) of the granule.
19. The composition according to claim 18 , wherein the microcrystalline cellulose is 14-17% (w/w) of the granule.
20. The composition according to claim 17 , wherein the granule further comprises a filler, wherein the filler is microcrystalline cellulose, and wherein the microcrystalline cellulose is less than 20% (w/w) of the granule.
21. The composition according to claim 1 , wherein the composition comprises at least 60% (w/w) of the salt of NAC.
22. The composition according to claim 21 , wherein the salt of NAC is sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC).
23. The composition according to claim 21 , wherein the composition comprises at least 70% (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 16 , wherein the composition comprises at least 60% (w/w) of the SNAC.
26. The composition according to claim 25 , wherein the composition comprises at least 70% (w/w) of the SNAC.