Dry-powder peptide medicament
Disclosed is a dry-powder peptide medicament with a non-typical concentration of carbohydrate excipient, as well as said medicament for use in treatment or prevention of a disease or condition, as well as methods for manufacturing said medicament.
1. A method for manufacturing a dry-powder medicament, comprising the steps of:
providing a cyclized peptide as an active agent, wherein the peptide consists of 7-17 amino acids and comprises the hexamer TPEGAE (SEQ ID NO: 2), wherein the peptide is cyclic, and wherein the peptide does not exhibit TNF-receptor-binding activity;
dissolving or diluting the active agent, optionally together with a carbohydrate, in a solvent, wherein the solvent consists of water, thereby yielding a solution with a carbohydrate content of total solids in solution of less than 5% (w/w); and
removing the solvent from said solution by spray drying, spray-freeze-drying, supercritical fluid precipitation, air-jet milling, lyophilisation or rotary evaporation to obtain the dry-powder medicament.
2. The method according to claim 1 , wherein the solution has a sugar content of total solids in solution of less than 5% and a sugar alcohol content of total solids in solution of less than 5% (w/w).
3. The method according to claim 1 , wherein the solvent is removed by spray drying and the inlet temperature of the spray dryer is between 50-110° C. and the outlet temperature of the spray dryer is between 20-80° C.
4. The method according to claim 1 , wherein the carbohydrate content of total solids in solution is less than 1% (w/w).
5. The method according to claim 1 , wherein the carbohydrate content of total solids in solution is less than 0.1% (w/w).
6. The method according to claim 1 , wherein the carbohydrate content of total solids in solution is less than 0.01% (w/w).
7. The method according to claim 1 , wherein the total solids concentration before removal of the solvent is between 2-4% (w/v).
8. The method according to claim 3 , wherein the solvent is removed by spray drying and the inlet temperature of the spray dryer is between 70-90° C.
9. The method according to claim 3 , wherein the solvent is removed by spray drying and the inlet temperature of the spray dryer is between 75-85° C.
10. The method according to claim 3 , wherein the solvent is removed by spray drying and the outlet temperature of the spray dryer is between 40-60° C.
11. The method according to claim 3 , wherein the solvent is removed by spray drying and the outlet temperature of the spray dryer is between 45-55° C.
12. The method according to claim 1 , wherein the total solids concentration before removal of the solvent is between 1-10% (w/v).
13. The method according to claim 1 , wherein the medicament does not contain any excipient.
14. The method according to claim 1 , wherein the medicament consists essentially of the peptide.
15. The method according to claim 14 , wherein the peptide comprises the amino acid sequence CGQRETPEGAEAKPWYC (SEQ ID NO: 1).
16. The method according to claim 1 , wherein the peptide comprises the amino acid sequence CGQRETPEGAEAKPWYC (SEQ ID NO: 1).
17. The method according to claim 1 , wherein the medicament consists of powder particles of a mean diameter of 0.5 to 10 micrometers.
18. The method according to claim 17 , wherein the medicament consists of powder particles of a mean diameter of 1 to 5 micrometers.
19. The method according to claim 18 , wherein the medicament consists of powder particles of a mean diameter of 1 to 3.5 micrometers.
20. A method for manufacturing a dry-powder medicament, comprising the steps of:
providing a cyclized peptide as an active agent, wherein the peptide consists of 7-17 amino acids and comprises the hexamer TPEGAE (SEP ID NO: 2\ wherein the peptide is cyclic, and wherein the peptide does not exhibit TNF-receptor-binding activity;
dissolving or diluting the active agent in a solvent, thereby yielding a solution with the total solids in solution consisting of the peptide; and
removing the solvent from said solution by spray drying, spray-freeze-drying, supercritical fluid precipitation, air-jet milling, lyophilisation or rotary evaporation to obtain the dry-powder medicament.