Liquid pharmaceutical formulations of palonosetron

Patent metadata

Field	Value
Publication number	US-9439854-B2
Application number	US-201514793233-A
Country	US
Kind code	B2
Filing date	Jul 7, 2015
Priority date	Jan 30, 2003
Publication date	Sep 13, 2016
Grant date	Sep 13, 2016

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.

First claim

What is claimed is:

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.

Assignees

• Helsinn Healthcare Sa

Inventors

• Calderari Giorgio
• Bonadeo Daniele
• Cannella Roberta
• Macciocchi Alberto
• Miksztal Andrew
• Malefyt Thomas
• Lee Kathleen M

Classifications

• A61K9/0019

  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 title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• B65B7/16

  Closing semi-rigid or rigid containers or receptacles not deformed by, or not taking-up shape of, contents, e.g. boxes or cartons · CPC title

• A61K9/08 Primary

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61K47/183

  Amino acids, e.g. glycine, EDTA or aspartame · CPC title