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:
(a) a first type of granules comprising at least 75% (w/w) of sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC) and less than 10% (w/w) of a lubricant; and
(b) a second type of granules comprising semaglutide, at least 15% (w/w) of a filler, and less than 40% (w/w) of a binder.
2. The composition according to claim 1 , wherein the lubricant is magnesium stearate.
3. The composition according to claim 1 , wherein the lubricant is 1-3% (w/w) of the first granule.
4. The composition according to claim 3 , wherein the lubricant is magnesium stearate.
5. The composition according to claim 1 , wherein the filler is microcrystalline cellulose.
6. The composition according to claim 1 , wherein the filler is 50-75% (w/w) of the second granule.
7. The composition according to claim 6 , wherein the filler is microcrystalline cellulose.
8. The composition according to claim 1 , wherein the binder is povidone.
9. The composition according to claim 1 , wherein the binder is 15-25% (w/w) of the second granule.
10. The composition according to claim 9 , wherein the binder is povidone.
11. The composition according to claim 1 , further comprising a filler in the first granule.
12. The composition according to claim 11 , wherein the filler is microcrystalline cellulose.
13. The composition according to claim 11 , wherein the filler is less than 20% (w/w) of the first granule.
14. The composition according to claim 13 , wherein the filler is microcrystalline cellulose.
15. The composition according to claim 11 , wherein the filler is 10-20% (w/w) of the first granule.
16. The composition according to claim 15 , wherein the filler is microcrystalline cellulose.
17. The composition according to claim 14 , wherein the filler is 14-17% (w/w) of the granule.
18. The composition according to claim 17 , wherein the filler is microcrystalline cellulose.
19. The composition according to claim 1 , wherein the weight of the composition is in the range of 150 mg to 1000 mg.
20. The composition according to claim 1 , wherein the lubricant is magnesium stearate, the filler is microcrystalline cellulose, and the binder is povidone.
21. The composition according to claim 1 , wherein the SNAC is 80-86% (w/w) of the first granule, the lubricant is 1-3% (w/w) of the first granule, the filler is 50-75% (w/w) of the second granule, and the binder is 15-25% (w/w) of the second granule.
22. The composition according to claim 21 , wherein the lubricant is magnesium stearate, the filler is microcrystalline cellulose, and the binder is povidone.
23. The composition according to claim 1 , further comprising lubricant outside the first type of granules and second type of granules.
24. The composition according to claim 23 , wherein the lubricant is magnesium stearate.
25. The composition according to claim 22 , further comprising magnesium stearate outside the first type of granules and second type of granules.
26. The composition according to claim 25 , wherein the magnesium stearate outside the first type of granules and the second type of granules is in an amount of 2 mg.
27. The composition according to claim 1 , 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.
29. The composition according to claim 22 , wherein the composition comprises at least 60% (w/w) of the SNAC.
30. The composition according to claim 29 , wherein the composition comprises at least 70% (w/w) of the SNAC.