LIQUID PHARMACEUTICAL FORMULATIONS OF PALONOSETRON

• US 20150141454A1
• Filed: 01/15/2015
• Published: 05/21/2015
• Est. Priority Date: 01/30/2003
• Status: Active Grant

• Current Assignee: Helsinn Advanced Synthesis SA (Helsinn Healthcare SA), Helsinn Therapeutics (U.S.), Inc (Helsinn Healthcare SA), Helsinn Birex Pharmaceuticals Ltd. (Helsinn Holding SA)
• Original Assignee: Helsinn Healthcare SA, Roche Palo Alto LLC (Roche Holding AG)
• Inventors: Calderari, Giorgio, Bonadeo, Daniele, Cannella, Roberta, Macciocchi, Alberto, Miksztal, Andrew, Malefyt, Thomas, Lee, Kathleen M
• Granted Patent: US 9,125,905 B2
• Time in Patent Office: Days
• US Class Current: 514/296
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 47/00 Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/183 Amino acids, e.g. glycine, EDTA or aspartame
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: B65B 55/02 Sterilising, e.g. of complete packages
• CPC Class Codes: B65B 7/16 Closing semi-rigid or rigid containers or receptacles not deformed by, or not taking-up shape of, contents, e.g. boxes or cartons

Abstract

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.

Claims

1-9. -9. (canceled)

10. A formulation comprising a pharmaceutical sterile aqueous intravenous solution, wherein said pharmaceutical sterile aqueous intravenous solution comprises palonosetron or a pharmaceutically acceptable salt thereof in an amount of 0.25 mg and a concentration of from 0.03 mg/mL to 0.2 mg/mL based on the weight of the palonosetron free base.

11. The formulation of claim 10, wherein said pharmaceutical sterile aqueous intravenous solution has a pH of from 4 to 6.

12. The formulation of claim 10, wherein said pharmaceutical sterile aqueous intravenous solution has a pH of 5.0±

0.5.

13. A method of manufacturing a finished container of a pharmaceutical formulation comprising palonosetron or a pharmaceutically acceptable salt thereof, said method comprising:

a) providing an open container;

b) filling said container with an aqueous intravenous solution comprising said palonosetron or pharmaceutically acceptable salt thereof in an amount of 0.25 mg and a concentration of from 0.03 mg/mL to 0.2 mg/mL based on the weight of the palonosetron free base;

c) sealing said filled container; and

d) terminally sterilizing said sealed, filled container to obtain said finished container.

14. The method of claim 13, wherein said aqueous intravenous solution has a pH of from 4 to 6.

15. The method of claim 13, wherein said aqueous intravenous solution has a pH of 5.0±

0.5.

16. A finished container of palonosetron or a pharmaceutically acceptable salt thereof, manufactured and terminally sterilized by the process of claim 13.

17. The finished container of claim 16, wherein said aqueous intravenous solution has a pH of from 4 to 6.

18. The finished container of claim 16, wherein said aqueous intravenous solution has a pH of 5.0±

0.5.