Liquid pharmaceutical formulations of palonosetron

Patent metadata

Field	Value
Publication number	US-9457020-B2
Application number	US-201514855564-A
Country	US
Kind code	B2
Filing date	Sep 16, 2015
Priority date	Jan 30, 2003
Publication date	Oct 4, 2016
Grant date	Oct 4, 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 method of storing one or more containers in which are contained a solution of palonosetron or a pharmaceutically acceptable salt thereof comprising:
a) providing a room comprising said one or more containers;
b) adjusting or maintaining the temperature of the room at greater than ten degrees Celsius;
c) storing said containers in said room for one month or more, wherein (i) the palonosetron or pharmaceutical salt thereof is present in an intravenous formulation at a concentration of from 0.01 mg/mL to about 5.0 mg/mL, (ii) the pH of the solution is from about 4.0 to about 6.0, (iii) the solution comprises from 0.01 to about 5.0 mg/ml palonosetron or a pharmaceutically acceptable salt thereof, from about 10 to about 100 millimoles citrate buffer and from about 0.005 to about 1.0 mg/ml EDTA, (iv) the solution comprises mannitol, or (v) the solution comprises from about 10 to about 100 milliMoles of a citrate buffer.

2. A pharmaceutically stable solution for preventing or reducing emesis stored by the method of claim 1 , said solution comprising
a) from 0.01 to about 5.0 mg/ml palonosetron or a pharmaceutically acceptable salt thereof;
b) from 10 to about 100 millimoles citrate buffer;
c) from 0.005 to about 1.0 mg/ml EDTA;
d) mannitol,
and wherein the pH of said stable solution is from 4.0 to about 6.0.

3. A method of filling a container in which is contained a solution of palonosetron or a pharmaceutically acceptable salt thereof comprising:
a) providing one or more sterile open containers;
b) filling said containers with a solution of palonosetron in a non-aseptic environment
c) sealing said filled containers; and
d) sterilizing said sealed, filled containers, wherein (i) the palonosetron or pharmaceutical salt thereof is present in an intravenous formulation at a concentration of from 0.01 mg/mL to about 5.0 mg/mL, (ii) the pH of the solution is from 4.0 to about 6.0, (iii) the solution comprises from about 0.01 to about 5.0 mg/ml palonosetron or a pharmaceutically acceptable salt thereof, from 10 to about 100 millimoles citrate buffer and from 0.005 to about 1.0 mg/ml EDTA, (iv) the solution comprises mannitol, or (v) the solution comprises from 10 to about 100 milliMoles of a citrate buffer.

Assignees

• Helsinn Healthcare Sa
• Roche Palo Alto Llc

Inventors

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

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P1/08

  for nausea, cinetosis or vertigo; Antiemetics · CPC title

• A61K47/183

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

• A61J3/00

  Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms · CPC title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title