US2019231762A1PendingUtilityA1

Controlled delivery system

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Assignee: DURECT CORPPriority: Sep 17, 2004Filed: Feb 20, 2019Published: Aug 1, 2019
Est. expirySep 17, 2024(expired)· nominal 20-yr term from priority
Inventors:Adrian Neil Verity
A61P 41/00A61P 25/02A61P 23/02A61P 23/00A61P 17/02A61K 47/26A61K 9/08A61K 9/7015A61K 31/445A61K 9/107A61K 45/06A61K 9/0024A61K 9/0014A61K 9/0019A61K 47/22
50
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Claims

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.

Claims

exact text as granted — not AI-modified
1 .- 181 . (canceled) 
     
     
         182 . A method for providing an anesthetic effect at a wound in a subject, comprising administering a controlled delivery composition into the wound, wherein the controlled delivery composition comprises bupivacaine, and further wherein the administering provides a sustained local anesthetic effect at the wound having a duration of at least 48 hours after the administration. 
     
     
         183 . The method of  claim 182 , wherein the sustained local anesthetic effect is for at least 72 hours after the administration. 
     
     
         184 . The method of  claim 182 , wherein the sustained local anesthetic effect is for up to 4 days after the administration. 
     
     
         185 . The method of  claim 182 , wherein the bupivacaine is present in the controlled delivery composition in an amount ranging from 1 wt % to 10 wt %, based on weight of the controlled delivery composition. 
     
     
         186 . The method of  claim 182 , wherein the bupivacaine is present in the controlled delivery composition in an amount ranging from 1 wt % to 5 wt %, based on weight of the controlled delivery composition. 
     
     
         187 . The method of  claim 182 , wherein the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition. 
     
     
         188 . The method of  claim 182 , wherein the bupivacaine is present in free base form. 
     
     
         189 . The method of  claim 182 , wherein the controlled delivery composition comprises a polymer. 
     
     
         190 . The method of  claim 189 , wherein the polymer comprises a polyorthoester. 
     
     
         191 . The method of  claim 182 , wherein the controlled delivery composition comprises an organic solvent. 
     
     
         192 . The method of  claim 191 , wherein the organic solvent comprises dimethyl sulfoxide and glyceryl triacetate. 
     
     
         193 . The method of  claim 191 , wherein the organic solvent is present in the controlled delivery composition in an amount ranging from 10 wt % to 55 wt %, based on weight of the controlled delivery composition. 
     
     
         194 . The method of  claim 191 , wherein the organic solvent is present in the controlled delivery composition in an amount ranging from 15 wt % to 50 wt %, based on weight of the controlled delivery composition. 
     
     
         195 . The method of  claim 191 , wherein the organic solvent is present in the controlled delivery composition in an amount ranging from 25 wt % to 55 wt %, based on weight of the controlled delivery composition. 
     
     
         196 . The method of  claim 191 , wherein the organic solvent is present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition. 
     
     
         197 . The method of  claim 182 , wherein the wound is a surgical wound. 
     
     
         198 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition; and   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition.   
     
     
         199 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition; and   the controlled delivery composition comprises a polymer comprising a polyorthoester.   
     
     
         200 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the controlled delivery composition comprises a polymer comprising a polyorthoester; and   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition.   
     
     
         201 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the controlled delivery composition comprises a polymer comprising a polyorthoester;   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition; and   the wound is a surgical wound.   
     
     
         202 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the bupivacaine is present in free base form;   the controlled delivery composition comprises a polymer comprising a polyorthoester;   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition; and   the wound is a surgical wound.   
     
     
         203 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition; and   the organic solvent comprises dimethyl sulfoxide and glyceryl triacetate.   
     
     
         204 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the controlled delivery composition comprises a polymer comprising a polyorthoester;   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition; and   the organic solvent comprises dimethyl sulfoxide and glyceryl triacetate.   
     
     
         205 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the controlled delivery composition comprises a polymer comprising a polyorthoester;   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition;   the organic solvent comprises dimethyl sulfoxide and glyceryl triacetate; and   the wound is a surgical wound.   
     
     
         206 . The method of  claim 182 , wherein
 the bupivacaine is present in the controlled delivery composition in an amount ranging from 2 wt % to 5 wt %, based on weight of the controlled delivery composition;   the bupivacaine is present in free base form;   the controlled delivery composition comprises a polymer comprising a polyorthoester;   the controlled delivery composition comprises an organic solvent present in the controlled delivery composition in an amount ranging from 25 wt % to 50 wt %, based on weight of the controlled delivery composition;   the organic solvent comprises dimethyl sulfoxide and glyceryl triacetate; and   the wound is a surgical wound.

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