Compositions containing an acid-neutralizing polymer for oral administration of glucagon-like peptide-1 and its analogues

Claims

1. A pharmaceutical composition comprising a therapeutically active agent, an absorption enhancer, and a polymer containing a plurality of alkaline groups, wherein the concentration of said polymer in the composition is at least 10 wt.% of the total weight of the composition, and said absorption enhancer is a substituted or unsubstituted fatty acid or a salt thereof, wherein said therapeutically active agent is a polypeptide selected from glucagon-like peptide-1 and a glucagon-like peptide-1 receptor agonist.

2. The composition according to claim 1, wherein at least a portion of said alkaline groups are carboxylate groups.

3. The composition according to claim 2, wherein at least a portion of said carboxylate groups are in the form of a pharmaceutically acceptable salt.

4. The composition according to claim 1, wherein said absorption enhancer comprises NAC or a salt thereof.

5. The composition according to claim 1, wherein the concentration of said absorption enhancer is at least 50% by weight of the total weight of the composition.

6. The composition according to claim 1, wherein the concentration of said polymer is at least 20% by weight of the total weight of the composition.

7. The composition according to claim 1, wherein the total concentration of said absorption enhancer and said polymer is at least 80% by weight of the total weight of the composition.

8. The composition according to claim 1, wherein the concentration of said alkaline groups in the composition is at least 0.1 millimoles per gram.

9. The composition according to claim 1, wherein said polymer is a cross-linked polymer.

10. The composition according to claim 1, any one of claims 1-12, wherein said polymer comprises a polysaccharide.

11. The composition according to claim 1, wherein said polymer is characterized by a pKa value in the range from 1.2 to 7.

5.

12. The composition according to any one of claims 1-11, wherein said glucagon-like peptide-1 receptor agonist is exenatide and / or lixisenatide, or is selected from liraglutide, semaglutide, taspoglutide, exenatide, lixisenatide, dapiglutide and tirzepatide.

13. The composition according to any one of paragraphs 1-11, presented in the form of a single dosage form.

14. The composition according to claim 13, wherein the amount of said alkaline groups in a single dosage form is at least 0.03 millimoles.

15. The use of a composition according to any one of claims 1 to 14, for the treatment of a condition treatable with said therapeutically active agent, wherein said treatment comprises oral administration of the composition.