Liquid pharmaceutical formulations of palonosetron

Patent metadata

Field	Value
Publication number	US-2016000773-A1
Application number	US-201514855564-A
Country	US
Kind code	A1
Filing date	Sep 16, 2015
Priority date	Jan 30, 2003
Publication date	Jan 7, 2016
Grant date	—

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

1 - 55 . (canceled)

56 . A pharmaceutically stable solution for preventing or reducing emesis stored by the method of claim 57 , said solution comprising
a) from about 0.01 to about 5.0 mg/ml palonosetron or a pharmaceutically acceptable salt thereof; b) from about 10 to about 100 millimoles citrate buffer; and c) from about 0.005 to about 1.0 mg/ml EDTA; d) mannitol, and wherein the pH of said stable solution is from about 4.0 to about 6.0.

57 . 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 about ten degrees celcius; 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 about 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 about 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.

58 . 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 about 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 about 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.

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

• A61K9/08 Primary

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

• A61K31/473 Primary

  ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines · CPC title