Liquid pharmaceutical formulations of palonosetron
The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.
1. A formulation comprising a pharmaceutical sterile aqueous intravenous solution, wherein said pharmaceutical sterile aqueous intravenous solution comprises:
palonosetron hydrochloride or another pharmaceutically acceptable salt of palonosetron at a concentration of 0.05 mg/mL based on the weight of the palonosetron free base; and
from 10 mg/mL to 80 mg/mL mannitol;
wherein the pharmaceutical sterile aqueous intravenous solution has a pH of 4.0 to 6.0.
2. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution comprises palonosetron hydrochloride or another pharmaceutically acceptable salt of palonosetron is in an amount of 0.25 mg.
3. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution comprises from 20 mg/mL to 60 mg/mL mannitol.
4. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution comprises from 40 mg/mL to 45 mg/mL mannitol.
5. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution comprises 41.5 mg/mL mannitol.
6. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution comprises a chelating agent.
7. The formulation of claim 6 , wherein said chelating agent is EDTA.
8. The formulation of claim 7 , wherein said pharmaceutical sterile aqueous intravenous solution comprises from 0.3 mg/mL to 0.7 mg/mL EDTA.
9. The formulation of claim 7 , wherein said pharmaceutical sterile aqueous intravenous solution comprises 0.5 mg/mL EDTA.
10. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution has a pH of 5.0±0.5.
11. The formulation of claim 1 , wherein said pharmaceutical sterile aqueous intravenous solution comprises a citrate buffer.
12. A formulation comprising a pharmaceutical sterile aqueous intravenous solution, wherein said pharmaceutical sterile aqueous intravenous solution comprises:
palonosetron hydrochloride or another pharmaceutically acceptable salt of palonosetron at a concentration of 0.05 mg/mL based on the weight of the palonosetron free base;
from 10 mg/mL to 80 mg/mL mannitol; and
from 0.3 mg/mL to 0.7 mg/mL EDTA.
13. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution comprises palonosetron hydrochloride or another pharmaceutically acceptable salt of palonosetron is in an amount of 0.25 mg.
14. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution has a pH of 4.0 to 6.0.
15. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution has a pH of 5.0±0.5.
16. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution comprises from 20 mg/mL to 60 mg/mL mannitol.
17. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution comprises from 40 mg/mL to 45 mg/mL mannitol.
18. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution comprises 41.5 mg/mL mannitol and 0.5 mg/mL EDTA.
19. The formulation of claim 12 , wherein said pharmaceutical sterile aqueous intravenous solution comprises a citrate buffer.