Claims for Patent: 11,834,521
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Summary for Patent: 11,834,521
| Title: | Ultra-pure agonists of guanylate cyclase C, method of making and using same |
| Abstract: | The invention provides processes of purifying a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-251 described herein. The processes include a solvent exchange step before a freeze-drying (lyophilization) step. |
| Inventor(s): | Kunwar Shailubhai, Stephen Comiskey, Rong Feng, Juncai BAI, Ruoping ZHANG, Jun Jia, Junfeng Zhou, Qiao Zhao, Guoqing Zhang |
| Assignee: | AMBIOPHARM Inc, Bausch Health Ireland Ltd |
| Application Number: | US18/193,144 |
| Patent Claims: |
1. An oral formulation comprising a purified peptide comprising the Guanylate Cyclase-C(GCC) agonist of amino acid sequence of SEQ ID NO: 1, characterized in that the purified peptide has: a) a bulk density of not greater than 0.1 g/mL; b) less than 0.25% alpha-Asp-9-plecanatide relative to the weight of the purified peptide; and c) less than 2% by weight of topoisomers relative to the weight of the purified peptide. 2. The oral formulation of claim 1, comprising less than 0.5% by weight of topoisomers relative to the weight of the purified peptide. 3. The oral formulation of claim 1, wherein the formulation further comprises at least one pharmaceutically acceptable excipient, wherein the at least one pharmaceutically acceptable excipient comprises magnesium stearate. 4. The oral formulation of claim 1, comprising 0.01 mg to 10 mg of the purified peptide. 5. The oral formulation of claim 1, comprising 0.1 mg to 5 mg of the purified peptide. 6. The oral formulation of claim 1, comprising 3 mg of the purified peptide. 7. The oral formulation of claim 1, wherein the purified peptide has a bulk density of 0.03 to 0.1 g/mL. 8. The oral formulation of claim 1, comprising 0.1% to 0.5% by weight of topoisomers relative to the weight of the purified peptide. 9. The oral formulation of claim 1, comprising 0.15% to 0.25% by weight of alpha-Asp-9-plecanatide relative to the weight of the purified peptide. 10. An oral formulation comprising: (i) a purified peptide comprising the Guanylate Cyclase-C(GCC) agonist of amino acid sequence of SEQ ID NO: 1, characterized in that the purified peptide has: a) a bulk density of not greater than 0.1 g/mL; b) less than 0.25% alpha-Asp-9-plecanatide relative to the weight of the purified peptide; and c) less than 2% by weight of topoisomers relative to the weight of the purified peptide; and (ii) at least one pharmaceutically acceptable excipient, wherein the at least one pharmaceutically acceptable excipient comprises microcrystalline cellulose. 11. The oral formulation of claim 10, comprising 0.01 mg to 10 mg of the purified peptide. 12. The oral formulation of claim 10, comprising 0.1 mg to 5 mg of the purified peptide. 13. The oral formulation of claim 10, comprising 3 mg of the purified peptide. 14. The oral formulation of claim 10, wherein the at least one pharmaceutically acceptable excipient further comprises magnesium stearate. 15. The oral formulation of claim 10, wherein the purified peptide has a bulk density of 0.03 to 0.1 g/mL. 16. The oral formulation of claim 10, comprising 0.1 to 0.5% by weight of topoisomers relative to the weight of the purified peptide. 17. The oral formulation of claim 10, comprising 0.15 to 0.25% by weight of alpha-Asp-9-plecanatide relative to the weight of the purified peptide. |
