Immunstimulating lipid formulation

Abstract

A pharmaceutical formulation for parenteral or mucosal administration of antigens and/or vaccines to humans and animals, comprising monglyceride preparations having at least 80% monoglyceride content and where the acyl group contains from 6 to 24 carbon atoms, together with fatty acids where the number of carbon atoms may be varied between 4 and 22.

1 . A pharmaceutical formulation for parenteral or mucosal administration of antigens and/or vaccines to an animal, characterized by comprising one or more substances selected from
 a) monoglyceride preparations having at least 80% monoglyceride content and having the general formula   
       
         
           
           
               
               
           
         
       
       wherein R 1  and R 2  is H and R 3  is one acyl group containing from 6 to 24 carbon atoms, and where the acyl chains may contain one or more unsaturated bonds 
       and
 b) fatty acids of the general formula
   CH 3 —(CH 2 ) n —COOH 
 
 where “n” may be varied between 4 and 22, and where the acyl chain may contain one or more unsaturated bonds. 
 
     
     
         2 . A pharmaceutical formulation according to  claim 1 , characterized by having a monoglyceride preparation content of at least 90%, preferably at least 95%. 
     
     
         3 . A pharmaceutical formulation according to  claim 1 , wherein the acyl chains of the monoglyceride preparations contains 8 to 20 carbon atom, preferably 14 to 20 carbon atoms and where the acyl chains may contain one or more unsaturated bonds. 
     
     
         4 . A pharmaceutical formulation according to  claim 1 , wherein the acyl chains of the fatty acid contains 8 to 20 carbon atom, preferably 14 to 20 carbon atoms and where the acyl chains may contain one or more unsaturated bonds. 
     
     
         5 . A pharmaceutical formulation according to  claim 1 , wherein the antigen comprises an antigen and/or vaccine that is selected among the antigen and/or vaccines relevant to humans or animals, including marine animals. 
     
     
         6 . A pharmaceutical formulation according to  claim 1 , wherein the formulation comprises additional pharmaceutical excipients selected from the one or several of the following groups; preservatives and osmotic pressure controlling agents, pH-controlling agents, organic solvents, hydrophobic agents, enzyme inhibitors, water absorbing polymers, surfactants and absorption promoters, anti-oxidative agents, and the like. 
     
     
         7 . A pharmaceutical formulation according to  claim 1 , wherein the formulation comprises additional adjuvants. 
     
     
         8 . A pharmaceutical formulation according to  claim 1 , wherein the formulation is in a form suitable for parenteral or mucosal administration. 
     
     
         9 . A pharmaceutical formulation according to  claim 8 , wherein the formulation is in a form suitable for administration to the mucosa of the nose, mouth, vagina, rectum or the intestine. 
     
     
         10 . A pharmaceutical formulation according to  claim 8 , wherein the formulation is in a form suitable for administration to the mucosa of the nose. 
     
     
         11 . A vaccine or antigen formulation, characterized by that 100 g of the final formulation contains:
 from 0.01 to 90 g of the antigen/vaccine component   from 0.1 to 90 g of the monoglyceride   from 0.1 to 90 g of the fatty acid   from 0.01 to 99 g of the water   from 0.01 to 99 g of PBS/saline   
       and optionally one or more adjuvant and/or excipient. 
     
     
         12 . The use of compounds selected from
 a) monoglyceride preparations having at least 80% monoglyceride content and having the general formula   
       
         
           
           
               
               
           
         
         wherein R 1  and R 2  is H and R 3  is one acyl group containing from 6 to 24 carbon atoms, and where the acyl chains may contain one or more unsaturated bonds 
       
       and
 b) fatty acids of the general formula
   CH 3 —(CH 2 ) n —COOH 
 
 where “n” may be varied between 4 and 22, and where the acyl chain may contain one or more unsaturated bonds in an amount of 0.01 to 15 g/100 ml of total volume of the formulation as adjuvants/vehicles in pharmaceutical formulations for parenteral or mucosal administration of antigens and/or vaccines to humans or animals, including marine animals. 
 
     
     
         13 . The use of compounds according to  claim 12 , characterized by having a monoglyceride preparation content of at least 90%, preferably at least 95%. 
     
     
         14 . The use of compounds according to  claim 12 , wherein the acyl chains of the monoglyceride preparations contains 8 to 20 carbon atom, preferably 14 to 20 carbon atoms and where the acyl chains may contain one or more unsaturated bonds. 
     
     
         15 . The use of compounds according to  claim 12 , wherein the acyl chains of the fatty acid contains 8 to 20 carbon atom, preferably 14 to 20 carbon atoms and where the acyl chains may contain one or more unsaturated bonds.