Liquid pharmaceutical formulations of palonosetron

• US 7,960,424 B2
• Filed: 03/24/2006
• Issued: 06/14/2011
• Est. Priority Date: 01/30/2003
• Status: Expired due to Term

• 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: Cannella, Roberta, Braglia, Enrico, Lee, Kathleen M., Malefyt, Thomas, Miksztal, Andrew, Bonadeo, Daniele, Calderari, Giorgio, Braglia, Riccardo
• Primary Examiner(s): Hartley; Michael G
• Assistant Examiner(s): Gembeh; Shirley V
• Application Number:
  US11/388,270
• Publication Number:
  US 20060167073A1
• Time in Patent Office: 1,908 Days
• Field of Search: 514/397
• US Class Current: 514/397
• CPC Class Codes: A61J 3/00 Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
• CPC Class Codes: A61K 31/4178 not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 31/4747 spiro-condensed
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/16 containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
• 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 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• 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: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: B65B 3/04 Methods of, or means for, filling the material into the containers or receptacles
• CPC Class Codes: B65B 55/02 Sterilising, e.g. of complete packages

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 pharmaceutically stable isotonic intravenous solution of palonosetron hydrochloride for reducing emesis or reducing the likelihood of emesis comprising

a) from about 0.03 mg/mL to about 0.2 mg/mL palonosetron as palonosetron hydrochloride,

b) a sterile pharmaceutically acceptable aqueous carrier comprising mannitol as a tonicity agent, at a pH of from 4.0 to 6.0, and

c) EDTA in an amount of from 0.005 to 1.0 mg/mL.

2. The solution of claim 1 wherein the palonosetron is in a concentration of about 0.05 mg/mL as palonosetron hydrochloride.

3. The solution of claim 1 wherein the pH is from 4.5 to 5.5.

4. The solution of claim 1 wherein the pharmaceutically acceptable carrier further comprises citric acid.

5. The solution of claim 1 wherein:

a) said palonosetron is present in a concentration of 0.05 mg/ml, as palonosetron hydrochloride; and

b) said EDTA is present in a concentration of from 0.005 to 1.0 mg/ml.

6. The solution of claim 5 wherein said pH is from 4.5 to 5.5.