Controlled Delivery System

Patent metadata

Field	Value
Publication number	US-2015111924-A1
Application number	US-201414464624-A
Country	US
Kind code	A1
Filing date	Aug 20, 2014
Priority date	Sep 17, 2004
Publication date	Apr 23, 2015
Grant date	—

Abstract

The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.

First claim

1 .- 181 . (canceled)

182 . A composition comprising:
about 5% to about 20% by weight bupivacaine free base relative to the total weight of the composition; about 25% to about 75% by weight sucrose acetate isobutyrate (SAIB) relative to the total weight of the composition; and about 10% to about 55% by weight of an organic solvent relative to the total weight of the composition.

183 . The composition of claim 182 , wherein the organic solvent is selected from ethanol, dimethyl sulfoxide, triethyl citrate, ethyl lactate, ethyl acetate, benzyl benzoate, benzyl alcohol, triacetin, N-methylpyrrolidone, propylene carbonate, polyethylene glycol, glycerol, glycofurol, 2-pyrrolidone, tetrafluoroethane, esters of caprylic and/or capric acids with glycerol or alkylene glycols, and combinations thereof.

184 . The composition of claim 182 , wherein the organic solvent comprises benzyl alcohol.

185 . The composition of claim 182 , wherein upon administration to a subject, the bupivacaine free base is released from the composition in an amount sufficient to provide a local anesthetic effect at a site of administration for at least 24 hours after administration.

186 . A method for providing sustained local anesthesia to a subject, said method comprising administering to the subject the composition of claim 182 .

187 . The method of claim 186 , wherein said administering is by topical application.

188 . The method of claim 186 , wherein said administering is by injection.

189 . The method of claim 186 , wherein said administering comprises administering as an implant.

190 . The method of claim 185 , wherein the composition is administered in or adjacent to a surgical wound.

191 . The composition of claim 182 , wherein said composition is suitable for topical, systemic, or parenteral administration.

192 . The composition of claim 182 , wherein said composition is suitable for administration via injection, pouring, spraying, dipping, aerosolizing, or via a coating applicator.

193 . The method of claim 186 , wherein said composition is administered by pouring.

194 . The method of claim 186 , wherein said subject is a human patient undergoing surgical inguinal hernia repair or an appendectomy.

195 . The method of claim 186 , wherein said composition is used to treat post-operative pain.

196 . The method of claim 186 , wherein less than about 50% of the bupivacaine free base present in the composition is released within 24 hours after administration.

197 . The composition of claim 182 , wherein the SAIB and the organic solvent form a low viscosity liquid carrier material having a viscosity ranging from 200 cP to 6000 cP.

198 . The composition of claim 182 , wherein the composition does not comprise a polymer.

199 . The method of claim 186 , wherein the administering does not comprise injection.

200 . The composition of claim 182 , wherein the organic solvent is present in an amount ranging from about 50% to about 15% by weight relative to the total weight of the composition.

201 . The composition of claim 185 , wherein the composition provides the local anesthetic effect up to 4 days after administration.

Assignees

• Durect Corp

Inventors

• Verity Adrian Neil

Classifications

• A61P41/00

  Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution · CPC title

• A61P25/02

  for peripheral neuropathies · CPC title

• A61P23/02

  Local anaesthetics · CPC title

• A61P17/02

  for treating wounds, ulcers, burns, scars, keloids, or the like · CPC title

• A61P23/00

  Anaesthetics · CPC title