US2016000758A1PendingUtilityA1

Chemical Compositions And Methods For Enhancing Transdermal Delivery Of Therapeutic Agents

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Assignee: INTEGURX THERAPEUTICS LLCPriority: Aug 24, 2012Filed: Sep 18, 2015Published: Jan 7, 2016
Est. expiryAug 24, 2032(~6.1 yrs left)· nominal 20-yr term from priority
Inventors:Kirti H. ValiaAgis Kydonieus
A61P 43/00A61P 25/28A61P 25/06A61P 25/04A61P 25/24A61P 25/16A61P 1/08A61P 17/00A61K 9/7023A61K 9/0014A61K 31/4178A61K 31/4709A61K 31/46A61K 31/439A61K 9/08A61K 47/12
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Claims

Abstract

The present application discloses chemical compositions and methods for enhancing the transdermal permeation of therapeutic agents through skin. The chemical compositions and methods of the invention can include combinations of a first fatty acid having about 14 or more carbon atoms and a second fatty acid having about 10 or less carbon atoms. These compositions are useful for the delivery of therapeutic agents, in particular hard to deliver drugs such as those that have fused rings, including ondansetron, and large drugs such as peptides. The compositions of the invention can be formulated as transdermal gels, lotions, creams, transdermal patches, sprays or mists.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
         1 . A composition for use on human skin comprising:
 a mixture comprising
 ondansetron, an ondansetron salt, or a mixture thereof; 
 a fatty acid or fatty acid derivative that is oleic acid, methyl oleate, ethyl oleate, oleyl alcohol, glycerol monooleate, linoleic acid, linolenic acid, or a combination thereof; and 
 levulinic acid. 
   
     
     
         2 . The composition of  claim 1 , comprising ondansetron. 
     
     
         3 . The composition of  claim 1 , comprising an ondansetron salt. 
     
     
         4 . The composition of  claim 3 , wherein the ondansetron salt is ondansetron hydrochloride. 
     
     
         5 . The compositions of  claim 1 , comprising a mixture of ondansetron and an ondansetron salt 
     
     
         6 . The composition of  claim 5 , wherein the ondansetron salt is ondansetron hydrochloride. 
     
     
         7 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is present in an amount of from about 0.1% to about 30%, by weight of the composition. 
     
     
         8 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is present in an amount of from about 2.5% to about 7.5%, by weight of the composition. 
     
     
         9 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is present in an amount of from about 1% to about 5%, by weight of the composition. 
     
     
         10 . The composition of  claim 1 , wherein the levulinic acid is present in an amount of from about 0.1% to about 30%, by weight of the composition. 
     
     
         11 . The composition of  claim 1 , wherein the levulinic acid is present in an amount of from about 1% to about 5%, by weight of the composition. 
     
     
         12 . The composition of  claim 1 , wherein the levulinic acid is present in an amount of from about 0.5% to about 2.5%, by weight of the composition. 
     
     
         13 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is methyl oleate, ethyl oleate, oleyl alcohol, glycerol monooleate, linoleic acid, or linolenic acid. 
     
     
         14 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is methyl oleate or ethyl oleate. 
     
     
         15 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is oleyl alcohol. 
     
     
         16 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is glycerol monooleate. 
     
     
         17 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is linoleic acid. 
     
     
         18 . The composition of  claim 1 , wherein the fatty acid or fatty acid derivative is linolenic acid. 
     
     
         19 . A transdermal patch comprising
 a mixture comprising
 ondansetron, an ondansetron salt, or a mixture thereof; 
 a fatty acid or fatty acid derivative that is oleic acid, methyl oleate, ethyl oleate, oleyl alcohol, glycerol monooleate, linoleic acid, linolenic acid, or a combination thereof; and 
 levulinic acid. 
   
     
     
         20 . The transdermal patch of  claim 19 , comprising ondansetron. 
     
     
         21 . The transdermal patch of  claim 19 , comprising an ondansetron salt. 
     
     
         22 . The transdermal patch of  claim 21 , wherein the ondansetron salt is ondansetron hydrochloride. 
     
     
         23 . The transdermal patch of  claim 19 , comprising a mixture of ondansetron and an ondansetron salt 
     
     
         24 . The transdermal patch of  claim 23 , wherein the ondansetron salt is ondansetron hydrochloride. 
     
     
         25 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is present in an amount of from about 0.1% to about 30%, by weight of the composition. 
     
     
         26 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is present in an amount of from about 2.5% to about 7.5%, by weight of the composition. 
     
     
         27 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is present in an amount of from about 1% to about 5%, by weight of the composition. 
     
     
         28 . The transdermal patch of  claim 19 , wherein the levulinic acid is present in an amount of from about 0.1% to about 30%, by weight of the composition. 
     
     
         29 . The transdermal patch of  claim 19 , wherein the levulinic acid is present in an amount of from about 1% to about 5%, by weight of the composition. 
     
     
         30 . The transdermal patch of  claim 19 , wherein the levulinic acid is present in an amount of from about 0.5% to about 2.5%, by weight of the composition. 
     
     
         31 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is methyl oleate, ethyl oleate, oleyl alcohol, glycerol monooleate, linoleic acid, or linolenic acid. 
     
     
         32 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is methyl oleate or ethyl oleate. 
     
     
         33 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is oleyl alcohol. 
     
     
         34 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is glycerol monooleate. 
     
     
         35 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is linoleic acid. 
     
     
         36 . The transdermal patch of  claim 19 , wherein the fatty acid or fatty acid derivative is linolenic acid.

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