Liquid pharmaceutical formulations of palonosetron

• US 9,439,854 B2
• Filed: 07/07/2015
• Issued: 09/13/2016
• 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
• Inventors: Calderari, Giorgio, Bonadeo, Daniele, Cannella, Roberta, Macciocchi, Alberto, Miksztal, Andrew, Malefyt, Thomas, Lee, Kathleen M
• Primary Examiner(s): Gembeh, Shirley V
• Application Number:
  US14/793,233
• Publication Number:
  US 20150306032A1
• Time in Patent Office: 434 Days
• Field of Search: 514/296, 514/397
• US Class Current: 1/1
• 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. A formulation for reducing emesis or reducing the likelihood of emesis in a human, the formulation comprising a pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution comprising palonosetron or a pharmaceutically acceptable salt thereof in a concentration of 0.05 mg/mL based on the weight of the palonosetron free base and in a volume of from 1 mL to 5 mL.

2. The formulation of claim 1, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution has a pH of from 4.0 to 6.0.

3. The formulation of claim 2, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution comprises a tonicifying agent.

4. The formulation of claim 3, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution comprises a chelating agent.

5. The formulation of claim 3, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution comprises from 40.0 mg/mL to 45.0 mg/mL mannitol.

6. The formulation of claim 4, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution comprises from 0.3 mg/mL to 0.7 mg/mL EDTA.

7. The formulation of claim 5, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution further comprises from 0.3 mg/mL to 0.7 mg/mL EDTA.

8. The formulation of claim 7, wherein said pharmaceutical single-use, unit-dose, sterile aqueous intravenous solution comprises 41.5 mg/mL mannitol and 0.5 mg/mL EDTA.