Pharmaceutical composition for transdermal or transmucous administration

Abstract

The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition.

1 . Pharmaceutical composition for transdermal or transmucous administration of at least one active substance, comprising at least one fatty acid as percutaneous absorption promoter, at least one alcoholic vehicle, and also at least one stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition. 
     
     
         2 . Pharmaceutical composition according to  claim 1 , wherein the fatty acid(s) is (are) selected from the group consisting of capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, palmitoleic acid, linoleic acid and linolenic acid. 
     
     
         3 . Pharmaceutical composition according to  claim 1 , having a fatty acid content of between 0.1% and 20%, preferably between 0.2% and 10% and even more preferably between 0.5% and 5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. 
     
     
         4 . Pharmaceutical composition according to  claim 1 , wherein the stabilizer(s) is (are) selected from the group consisting of buffers and/or esters of the said fatty acids. 
     
     
         5 . Pharmaceutical composition according to  claim 1 , having a pH of between 4 and 10, preferably between 5 and 9 and even more preferably between 6 and 8. 
     
     
         6 . Pharmaceutical composition according to  claim 4 , wherein the buffer(s) is (are) selected from the group consisting of :
 basifying or basic buffers such as a phosphate buffer (for example dibasic or monobasic sodium phosphate), a citrate buffer (for example sodium citrate or potassium citrate), sodium carbonate, sodium bicarbonate, preferably a mixture of sodium carbonate and sodium bicarbonate, or   neutral buffers such as a Tris buffer, preferably a phosphate buffer.   
     
     
         7 . Pharmaceutical composition according to  claim 6 , having a buffer content of between 1% and 80%, preferably between 5% and 70% and even more preferably between 10% and 50%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. 
     
     
         8 . Pharmaceutical composition according to  claim 2 , wherein the fatty acid esters are selected from the group consisting of ethyl oleate, isopropyl oleate, isopropyl myristate, isopropyl palmitate, ethyl octanoate, ethyl dodecanoate, ethyl linoleate and ethyl linolenate. 
     
     
         9 . Pharmaceutical composition according to  claim 8 , having a fatty acid ester content of between 0.1% and 10%, preferably between 0.2% and 5% and even more preferably between 0.5% and 2.5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. 
     
     
         10 . Pharmaceutical composition according to  claim 1 , wherein the alcoholic vehicle(s) is (are) selected from the group consisting of ethanol and/or isopropanol, preferably ethanol. 
     
     
         11 . Pharmaceutical composition according to  claim 10 , having an alcoholic vehicle content of between 10% and 90%, preferably between 20% and 80% and even more preferably between 40% and 70%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. 
     
     
         12 . Pharmaceutical composition according to  claim 1 , further comprising a co-solvent preferably selected from the group consisting of glycerol, propylene glycol and polyethylene glycol, and mixtures thereof. 
     
     
         13 . Pharmaceutical composition according to  claim 12 , having a co-solvent content of between 0.5 and 20% and preferably between 1% and 10%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. 
     
     
         14 . Pharmaceutical composition according to  claim 1 , being in the form of a gel, a solution, a cream, a lotion, a milk, an ointment, an aerosol or a patch, preferably a gel or a solution. 
     
     
         15 . Pharmaceutical composition according to  claim 1 , being in the form of a gel, and having a content of between 0.2% and 30% of a gelling agent, preferably between 0.5% and 10% and even more preferably between 0.3% and 5%, these percentages being expressed on a weight basis relative to 100 g of formulation. 
     
     
         16 . Pharmaceutical composition according to  claim 15 , wherein the gelling agent is selected from the group consisting of carbomers, non-preneutralized acrylic polymers, cellulose derivatives, poloxamers, poloxamines, chitosan, dextran, pectins, natural gums, and mixtures thereof, preferably carbomers and/or cellulose derivatives, and even more preferably Carbopol® 980 and/or hydroxypropylcellulose. 
     
     
         17 . Pharmaceutical composition according to  claim 15 , further comprising a neutralizer. 
     
     
         18 . Pharmaceutical composition according to  claim 17 , wherein the neutralizer is selected from the group consisting of triethanolamine, sodium hydroxide, ammonium hydroxide, potassium hydroxide, arginine, aminomethylpropanol and tromethamine, and mixtures thereof, preferably triethanolamine and/or tromethamine. 
     
     
         19 . Pharmaceutical composition according to  claim 17 , wherein the neutralizer/gelling agent ratio is between 10/1 and 0.1/1, preferably between 7/1 and 0.5/1 and even more preferably between 4/1 and 1/1. 
     
     
         20 . Pharmaceutical composition according to  claim 1 , wherein the active substance(s) is (are) selected from the group consisting of oestrogens, progestins, androgens, anti-oestrogens and anti-androgens, or mixtures thereof. 
     
     
         21 . Pharmaceutical composition according to  claim 20 , having an active substance content of between 0.01% and 5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition.