Stabilized liquid fosaprepitant formulations
The present invention relates to stable pharmaceutical compositions of fosaprepitant or a salt thereof in the form of ready-to-use or ready-to-dilute compositions suitable for parenteral administration.
1. A liquid composition comprising:
fosaprepitant or a salt thereof, an aqueous albumin vehicle, and at least one stabilizer selected from fatty acid metal salts, antioxidants, and chelating agents,
wherein after storage at 2-8° C. for at least 1 month, aprepitant is present in an amount concentration of no more than 10%.
2. The liquid composition according to claim 1 , comprising a chelating agent selected from the group consisting of ethylenediaminetetraacetic acid, hydroxyethylethylenediaminetriacetic acid, diethylenetriaminepentaacetic acid, nitrilotriacetic acid, ethanol diglycine, 1,3-propylenediaminetetraacetic acid, or a pharmaceutically acceptable salt thereof.
3. The liquid composition according to claim 2 , wherein the chelating agent comprises ethylenediaminetetraacetic acid or pharmaceutically acceptable salt thereof.
4. The liquid composition according to claim 1 , wherein the aqueous albumin vehicle comprises a 25% aqueous albumin vehicle.
5. The liquid composition according to claim 1 , wherein the fosaprepitant is fosaprepitant dimeglumine.
6. The liquid composition according to claim 1 , further comprising an additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).
7. The liquid composition according to claim 6 , wherein the additional agent comprises a corticosteroid, a 5HT 3 receptor antagonist, GABA B receptor agonist, or a combination thereof.
8. The liquid composition according to claim 7 , wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, or baclofen.
9. A method of treating chemotherapy-induced nausea and vomiting (CINV), wherein the method comprises administering a liquid pharmaceutical composition according to claim 1 .
10. The method according to claim 9 , comprising administering at least one additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).
11. The method according to claim 10 , wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, baclofen, or a combination thereof.
12. A liquid composition comprising fosaprepitant or a salt thereof, a solubilizer comprising at least one alcohol, at least one glycol, or a combination thereof, wherein after storage at 2-8° C. for at least 1 month, aprepitant is present in an amount concentration of no more than 10%, wherein the composition is ready-to-use or ready-to-dilute.
13. The liquid composition according to claim 12 , wherein the alcohol comprises ethanol, octanol, glycofurol or a mixture thereof.
14. The liquid composition according to claim 12 , comprising a glycol comprising propylene glycol, glycerol, polyethylene glycol, or a mixture thereof.
15. The liquid composition according to claim 12 , comprising ethanol and propylene glycol.
16. The liquid composition according to claim 12 , further comprising an additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).
17. The liquid composition according to claim 12 , wherein the additional agent comprises a corticosteroid, a 5HT 3 receptor antagonist, GABA B receptor agonist, or a combination thereof.
18. The liquid composition according to claim 12 , wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, or baclofen.
19. A method of treating chemotherapy-induced nausea and vomiting (CINV), wherein the method comprises administering a liquid pharmaceutical composition according to claim 12 .
20. The method according to claim 19 , comprising administering at least one additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).
21. The method according to claim 20 , wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, baclofen, or a combination thereof.