Controlled release delivery system for nasal applications

Abstract

This invention relates to a pernasally administrable preparation for the controlled release of sexual hormones to the systemic circulation, in particular to a formulation which enables its active ingredient to be absorbed in a sustained manner providing a better bioavailability at very low doses and longer duration of action.

1 . A formulation for nasal application comprising 
 a) at least one sexual hormone drug;    b) at least one lipophilic or partly lipophilic carrier; and    c) a compound or a mixture of compounds having surface tension decreasing activity, an amount effective for in situ generation of an emulsion upon contact of the formulation with water.    
     
     
         2 . The formulation according to  claim 1 , wherein the lipophilic carrier comprises an oil.  
     
     
         3 . The formulation according to  claim 2 , wherein said oil is a vegetable oil.  
     
     
         4 . The formulation according to  claim 3 , wherein said oil is castor oil.  
     
     
         5 . The formulation according to  claim 2 , wherein the amount of oil comprises between 30% and 98% by weight, preferably between 60 and 98% by weight, more preferably between 75% and 95% by weight, even more preferably between 85% and 95% by weight and most preferably around 90% by weight of the formulation.  
     
     
         6 . The formulation according to  claim 1 , wherein component (c) comprises at least one surfactant selected from the group consisting of lecithin, fatty acid ester of polyvalent alcohols, of sorbitanes, of polyoxyethylensorbitans, of polyoxyethylene, of sucrose, of polyglycerol and/or at least one humectant selected from the group consisting of sorbitol, glycerine, polyethylene glycol, and macrogol glycerol fatty acid ester, or a mixture thereof.  
     
     
         7 . The formulation according to  claim 6 , wherein component (c) comprises an oleoyl macrogolglyceride or a mixture of oleoyl macrogolglycerides.  
     
     
         8 . The formulation according to  claim 6 , wherein component (c) is comprised within the formulation in an amount of from 1 to 20% by weight, preferably 1 to 10% by weight, more preferably 1 to 5% by weight, and most preferably at around 4% by weight.  
     
     
         9 . The formulation according to  claim 1 , further comprising a viscosity regulating agent.  
     
     
         10 . The formulation according to  claim 9 , wherein said viscosity regulating agent comprises a thickener or gelling agent selected from the group consisting of cellulose and cellulose derivatives, polysaccharides, carbomers, polyvinyl alcohol, povidone, colloidal silicon dioxide, cetyl alcohols, stearic acid, beeswax, petrolatum, triglycerides and lanolin, or a mixture thereof.  
     
     
         11 . The formulation according to  claim 10 , wherein said viscosity increasing agent is colloidal silicon dioxide.  
     
     
         12 . The formulation according to  claim 9 , wherein the viscosity regulating agent is comprised within the formulation in an amount of from 0.5 to 10% by weight, preferably 0.5 to 5% by weight, more preferably 1 to 3% by weight, and most preferably at around 3% by weight.  
     
     
         13 . The formulation according to  claim 1 , wherein the sexual hormone drug is testosterone.  
     
     
         14 . The formulation according to  claim 1 , wherein the sexual hormone drug is comprised within the formulation in an amount of from 0.5 to 6% by weight, preferably 2 to 4% by weight, more preferably 0.5 to 2% by weight, and most preferably at around 2% by weight.