Sublingual fentanyl spray

• US 8,486,972 B2
• Filed: 01/25/2007
• Issued: 07/16/2013
• Est. Priority Date: 01/25/2006
• Status: Active Grant

• Current Assignee: BTcP Pharma, LLC
• Original Assignee: INSYS Therapeutics, Inc.
• Inventors: Kottayil, S. George, Goskonda, Venkat R., Zhu, Zhongyuan, Parikh, Neha, Kattookaran, Linet
• Primary Examiner(s): LANDSMAN, ROBERT S
• Application Number:
  US11/698,739
• Publication Number:
  US 20070261695A1
• Time in Patent Office: 2,364 Days
• Field of Search: 514/329
• US Class Current: 514/329
• CPC Class Codes: A61K 31/435 having six-membered rings with one nitrogen as the only ring hetero atom
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61M 11/00 Sprayers or atomisers specially adapted for therapeutic purposes in general B05B; aerosol containers B65D83/14
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable salt thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations.

Claims

1. A unit dose of a non-propellant sublingual fentanyl formulation comprising discrete liquid droplets of an effective amount of fentanyl and a pharmaceutically acceptable liquid carrier, wherein the sublingual fentanyl formulation comprises:

from about 0.1% to about 0.8% by weight of fentanyl or a pharmaceutically acceptable salt thereof;

from about 20% to about 60% by weight of ethanol; and

from about 4% to about 6% by weight of propylene glycol;

wherein after sublingual administration to a human, said sublingual fentanyl formulation provides a mean time to maximum plasma concentration (T_max) of fentanyl of from about 5 to about 120 minutes.

2. The unit dose of claim 1, wherein said discrete liquid droplets have a size distribution of from about 10 μ

m to about 200 μ

m.

3. The unit dose of claim 1 wherein after sublingual administration to a human, the sublingual fentanyl formulation provides a mean time to maximum plasma concentration (T_max) of fentanyl of from about 10 to about 60 minutes.