Vehicle for topical delivery of anti-inflammatory compounds

Abstract

A vehicle for topical application which contains a liquid eutectic mixture of hydrophobic compounds to improve solubility of pharmaceutically active component and enhance topical and transdermal delivery.

1 . A vehicle for topical delivery of a pharmaceutically active component, comprising a liquid eutectic mixture containing a hydrophobic component.  
     
     
         2 . The vehicle as set forth in  claim 1 , wherein said hydrophobic component is selected from the group consisting of pharmaceutically acceptable glycerin esters, aliphatic esters, aromatic esters, waxes, lipids, fats, lipid soluble vitamins, hydrocarbons, silicone polymers, tocopherols, tocotrienols and related compounds, or mixture thereof.  
     
     
         3 . The vehicle as set forth in  claim 1 , wherein the ratio of said hydrophobic component and liquid eutectic mixture are in a ratio of between 1:10 to 10:1.  
     
     
         4 . The vehicle as set forth in  claim 1 , wherein the ratio of said hydrophobic component and liquid eutectic mixture are in a ratio of between 1:3 to 3:1.  
     
     
         5 . The vehicle as set forth  claim 1 , wherein said eutectic mixture comprises at least two compounds selected from the group consisting of camphor, menthol, thymol, resorcinol, phenol or substituted phenol derivativesThe vehicle as set forth  claim 5 , wherein said eutectic mixture is liquid at ambient temperature.  
     
     
         6 . A composition for topical delivery comprising an oil-in-water or water-in-oil emulsion or microemulsion, wherein the oil phase of said emulsion comprises a vehicle as set forth in  claim 3 .  
     
     
         7 . The composition as set forth in  claim 6 , wherein said pharmaceutically active component is dissolved in said oil phase of said emulsion or microemulsion.  
     
     
         8 . The composition as set forth in  claim 7 , wherein said oil phase comprises between 5% and 80% of said composition.  
     
     
         9 . The composition as set forth in  claim 7 , further including a surfactant.  
     
     
         10 . The composition as set forth in  claim 9 , wherein said pharmaceutically active component is selected from anti-inflammatory drugs.  
     
     
         11 . The composition as set forth in  claim 10 , wherein said anti-inflammatory drugs are selected from group of non-steroidal anti-inflammatory drugs (NSAIDs).  
     
     
         12 . The composition as set forth in  claim 11 , wherein said anti-inflammatory drugs are selected from the group consisting of indomethacin, diclofenac, ketorolac, piroxicam, meloxicam, tenoxicam, ketoprofen, flurbiprofen, ibuprofen, nimesulide, naproxen, rofecoxib, celecoxib and salicylic acid.  
     
     
         13 . The composition as set forth in  claim 10 , further including additional pharmaceutically active components, pharmaceutically acceptable surfactants, viscosity regulating agents, antibacterial preservatives, skin penetration enhancers, fragrances and colorants.  
     
     
         14 . The composition as set forth in  claim 9 , wherein said surfactant is non-ionic surfactant, phospholipid or mixture thereof.  
     
     
         15 . A method for increasing the solubility of a pharmaceutically active component in a vehicle for topical delivery of said pharmaceutically active component, comprising: 
 providing a pharmaceutically active component;    providing at least two compounds selected from the group consisting of camphor, menthol, thymol, resorcinol, phenol or substituted phenol derivatives; and    forming a eutectic mixture containing said pharmaceutically active component and said at least two members whereby said mixture contains a greater amount of solubilzed active component relative to a non eutectic mixture.    
     
     
         16 . The method as set forth in  claim 15 , wherein said two selected compounds are camphor and menthol.  
     
     
         17 . The method as set forth in  claim 15 , wherein said pharmaceutically active component comprises a non steroidal anti-inflammatory drug (NSAID).  
     
     
         18 . A composition for topical delivery having an increased amount of a solubilized pharmaceutically active component comprising an emulsion selected from the group consisting of an oil-in-water, water-in-oil and microemulsion, wherein said oil phase of said emulsion comprises a vehicle as set forth in  claim 3 , wherein said hydrophobic component is selected from the group consisting of pharmaceutically acceptable glycerin esters, aliphatic esters, aromatic esters, waxes, lipids, fats, lipid soluble vitamins, hydrocarbons, silicone polymers, tocopherols, tocotrienols and related compounds, or mixture thereof, said eutectic; mixture comprising at, least two members selected from the group consisting of camphor, menthol, thymol, resorcinol, phenol or substituted phenol derivatives; and a pharmaceutically active component, said composition having an increased solubilized amount of said pharmaceutically active component relative to a non eutectic composition.