Controlled Delivery System

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.

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.