IP Library Granted Patent US 8,518,981
Granted Patent B2
US 8,518,981 · App. 13/087,012 · Granted Aug 27, 2013

Liquid pharmaceutical formulations of palonosetron

Inventors: Giorgio Calderari (Rancate, CH); Daniele Bonadeo (Varese, IT); Roberta Cannella (Varese, IT); Andrew Miksztal (Palo Alto, CA); Thomas Malefyt (Carmel Valley, CA); Kathleen Lee (Palo Alto, CA)
Assignees: Helsinn Healthcare SA; Roche Palo Alto LLC
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Quick Facts
Patent No.
US 8,518,981
App. No.
13/087,012
Granted
Aug 27, 2013
Kind
B2
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 (12)

1. A method of manufacturing and terminally sterilizing a finished single unit dose vial of palonosetron or a pharmaceutically acceptable salt thereof comprising: a) providing one or more sterile open containers; b) filling said containers with a pharmaceutically stable solution of palonosetron or a pharmaceutically acceptable salt thereof; c) sealing said filled containers; d) terminally sterilizing said sealed, filled containers; and e) optionally adjusting the pH of said solution using HCl or NaOH prior to step (c), wherein the pharmaceutically stable solution has a pH of from about 4.0 to about 6.0 and comprises palonosetron hydrochloride in a concentration of from about 0.03 mg/mL to about 0.2 mg/mL based on the weight of the free base, an aqueous carrier, and a tonicity agent, and wherein the pharmaceutically stable solution optionally comprises one or a combination of mannitol, a chelating agent, and a citrate buffer.

2. The method of claim 1 , wherein said solution comprises 0.05 mg/ml of palonosetron hydrochloride based on the weight of the free base.

3. The method of claim 1 , wherein said solution comprises HCl or NaOH as a pH adjusting agent.

4. The method of claim 1 , wherein said solution has a pH of from 4.5 to 5.5, HCl or NaOH as a pH adjusting agent, and mannitol.

5. A single unit dose of palonosetron hydrochloride made by the method of claim 4 .

6. The method of claim 1 , wherein said solution has a pH of from 4.5 to 5.5, HCl or NaOH as a pH adjusting agent, a chelating agent and mannitol.

7. A single unit dose of palonosetron hydrochloric made by the method of claim 6 .

8. The method of claim 1 , wherein said solution comprises HCl or NaOH as a pH adjusting agent, a chelating agent and mannitol.

9. The method of claim 1 , wherein said solution comprises a chelating agent and mannitol.

10. The method of claim 1 , wherein said solution comprises a chelating agent.

11. The method of claim 1 , wherein said solution comprises mannitol.

12. A single unit dose of palonosetron hydrochloride made by the method of claim 1 .

Assignments (7)
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2023
From: HAMILTON SA LLC
To: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
Reel/Frame 064961/0567 →
SECURITY INTEREST Recorded Dec 30, 2022
From: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
To: HAMILTON SA LLC
Reel/Frame 062254/0888 →
CORRECTIVE ASSIGNMENT TO CORRECT THE 1. SPELLING OF ASSIGNEE NAME HELSINN BIREX PHARMACEUTICALS LTD.; 2. ADDRESSES OF ASSIGNEES PREVIOUSLY RECORDED ON REEL 047534 FRAME 0024. ASSIGNOR(S) HEREBY CONFIRMS THE PATENT CO-OWNERSHIP AGREEMENT. Recorded Nov 21, 2018
From: HELSINN HEALTHCARE SA
To: HELSINN ADVANCED SYNTHESIS SA; HELSINN BIREX PHARMACEUTICALS, LTD.; HELSINN THERAPEUTICS (U.S.), INC.
Reel/Frame 047617/0285 →
PATENT CO-OWNERSHIP AGREEMENT Recorded Nov 14, 2018
From: HELSINN HEALTHCARE SA
To: HELSINN ADVANCED SYNTHESIS SA; HELSINN BIREX PHARMACEUTIALS LTD.; HELSINN THERAPEUTICS (U.S.), INC.
Reel/Frame 047534/0024 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 11, 2016
From: ROCHE PALO ALTO LLC
To: HELSINN HEALTHCARE SA
Reel/Frame 038544/0269 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 15, 2012
From: MIKSZTAL, ANDREW; MALEFYT, THOMAS; LEE, KATHLEEN M.
To: ROCHE PALO ALTO LLC
Reel/Frame 029302/0296 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 5, 2012
From: CALDERARI, GIORGIO; BONADEO, DANIEL; CANNELLA, ROBERTA; BRAGLIA, ENRICO; BRAGLIA, RICCARDO
To: HELSINN HEALTHCARE SA
Reel/Frame 028899/0100 →
Continuity (4)
Continuation 11186311 · Jul 21, 2005
Continuation PCTEP2004000888 · Jan 30, 2004
Provisional Application 60444351 · Jan 30, 2003
Related Publication 20110192493A1 · Aug 11, 2011