Cosmetic antimycotic composition for skin applications and pharmaceutical composition for the treatment of tumorous cells, bladder or nerve disorders

Abstract

A method for destructive treatment of tumorous cells including the use of glycopropylene of retinoic acid in a pharmaceutical composition, a method for bladder irrigation having antitumoral properties including the use of a glycopropylene ester of retinoic acid together with a pharmaceutically compatible liquid vector, a method for treatment of nerve disorders including the use of a glycopropylene ester of retinoic acid for preparation of a pharmaceutical composition and a pharmaceutical composition for the same.

1 . A cosmetic, antimycotic composition for skin application, in particular for treating unsightly skin disorders such as acne, stretch marks, scars and dark spots; 
 characterized by comprising at least a glycol or glyceric ester of retinoic acid dissolved in a glyco-alcohol, hydro-alcohol or glyco-hydro-alcohol solution.    
     
     
         2 . A composition as claimed in  claim 1 , characterized by comprising the glycopropylene ester of retinoic acid.  
     
     
         3 . A composition as claimed in  claim 1  or  2 , characterized by also comprising, in association with said glycol or glyceric ester, the ethyl ester of retinoic acid, also dissolved in said glyco-alcohol, hydro-alcohol or glyco-hydro-alcohol solution.  
     
     
         4 . A composition as claimed in one of the foregoing claims, characterized by also comprising hydroquinone, which is dissolved in said glyco-alcohol, hydro-alcohol or glyco-hydro-alcohol solution together with said esters of retinoic acid.  
     
     
         5 . A composition as claimed in one of the foregoing claims, characterized in that said glyco-alcohol solution comprises propylene glycol and, in lesser proportions, ethyl alcohol.  
     
     
         6 . A composition as claimed in one of the foregoing claims, characterized in that said glyco-alcohol solution also contains propylene glycol ether.  
     
     
         7 . A composition as claimed in any one of the foregoing claims, characterized by comprising a glyco-alcohol solution of 0.10 to 0.25 N of ethyl ester of retinoic acid and 0.15 to 0.30 N of glycopropylene ester of retinoic acid.  
     
     
         8 . A composition as claimed in  claim 7 , characterized in that said glyco-alcohol solution presents a propylene glycol base, and also contains 0.001 to 0.002 N of ethyl-glycopropylene ether.  
     
     
         9 . A composition as claimed in any one of the foregoing claims, characterized by comprising solid or semisolid excipients in which 2 to 10% by weight of said glyco-alcohol, hydro-alcohol or glyco-hydro-alcohol solution of said esters of retinoic acid is dispersed, so that said composition is in the form of a cream.  
     
     
         10 . A composition as claimed in any one of the foregoing claims, characterized by also comprising a substance selected from the group comprising: a cortisone, an anti-inflammatory substance, one or more liposoluble vitamins, salicylic acid, the glycopropylene ester of salicylic acid, and mixtures thereof.  
     
     
         11 . A composition as claimed in  claim 10 , characterized in that said anti-inflammatory substance is selected from the group comprising: niflumic acid, indomethacin, and naproxene.  
     
     
         12 . A composition as claimed in any one of the foregoing claims, characterized by also comprising sodium heparin in gel form.  
     
     
         13 . A method of preparing a cosmetic, antimycotic composition as claimed in one of the foregoing claims, characterized by comprising the steps of: 
 producing an esterification reaction between retinoic acid and propylene glycol in a glyco-alcohol solution with a large excess of propylene glycol, so that substantially all the retinoic acid in the solution is esterified; and    using said solution as such, at the end of the esterification reaction, without removing the surplus reactants or the reaction products.    
     
     
         14 . A method as claimed in  claim 13 , characterized in that said esterification reaction is conducted in the presence of 1.35 to 23.9% by weight of hydroquinone dissolved in said glyco-alcohol solution.  
     
     
         15 . A method as claimed in  claim 13  or  14 , characterized in that said esterification reaction is accelerated in the presence of an acid catalyst and/or by heating the reaction mixture.  
     
     
         16 . A method as claimed in  claim 15 , characterized in that said acid catalyst is salicylic acid.  
     
     
         17 . A method as claimed in  claim 15 , characterized in that said acid catalyst is thionyl chloride.  
     
     
         18 . A cosmetic method of treating unsightly skin disorders such as acne, scars, stretch marks and dark spots, characterized in that: 
 a glycol or glyceric ester of retinoic acid is prepared in a glyco-alcohol solution by esterifying the acid with the corresponding polyalcohol and operating with a large excess of polyalcohol in the presence of hydroquinone; and    the resulting solution, containing the ester produced by the reaction, and possibly aged in atmospheric air at ambient temperature, is applied to the skin region for treatment to produce surface peeling of the region.    
     
     
         19 . A cosmetic method of treating unsightly skin disorders such as acne, scars, stretch marks and dark spots, characterized in that: 
 the glycopropylene ester of retinoic acid is prepared in a solution comprising propylene glycol as the only solvent and containing 0 to 8.5% by weight, of the total weight of the solution, of hydroquinone, by dissolving, in said solution, 0.01 to 4% by weight, of the total weight of the solution, of retinoic acid; and    said solution containing the prepared ester is applied to the skin region for treatment.    
     
     
         20 . A cosmetic method of treating unsightly skin disorders such as acne, scars, stretch marks and dark spots, characterized in that: 
 a mixture of glycopropylene and ethyl esters of retinoic acid is prepared in a solution comprising equal proportions by volume of ethyl alcohol and propylene glycol as solvents and containing 1 to 13% by weight, of the total weight of the solution, of hydroquinone, by dissolving, in said solution, 0.01 to 0.13% by weight, of the total weight of the solution, of retinoic acid; and    said solution containing the prepared mixture of esters is applied to the skin region for treatment.    
     
     
         21 . A cosmetic method of treating unsightly skin disorders such as acne, scars, stretch marks and dark spots, characterized in that said solutions containing the reaction products and formed according to the methods claimed in claims  19  and  20  are mixed together to a predetermined ratio; the resulting solution being stored stably in a refrigerator, and being applied in a predetermined quantity to the skin region for treatment by means of a sponge, cotton cloth, cotton-wool or any other appropriate means soaked in the solution.  
     
     
         22 . A cosmetic method as claimed in  claim 21 , characterized in that the two solutions are mixed to a ratio of 1:1 to 1:1.5 by volume.  
     
     
         23 . A cosmetic method as claimed in  claim 21  or  22 , characterized in that the solution is applied: 
 once a day for 6-10 days; said application cycle being repeatable after a suspension of 4-6 months; or: 
 twice a week for 6-7 weeks.  
 
 
     
     
         24 . A cosmetic method as claimed in  claim 21  or  22 , characterized in that said resulting solution is converted, by the addition of appropriate excipients, into a cream containing 2 to 10% by weight of said solution, and is applied as such, with no appreciable peeling effect, once a day for 3-6 months.  
     
     
         25 . A cosmetic method of treating unsightly skin disorders such as acne, scars, stretch marks and dark spots, characterized in that the methods claimed in claims  23  and  24  are applied jointly.  
     
     
         26 . A cosmetic method as claimed in  claim 20  or  21 , characterized in that said esterification reaction is conducted in the absence of hydroquinone in said glyco-alcohol solution, or by subsequently eliminating the hydroquinone from said reaction solution; the resulting solution then being up to diluted 30 times in propylene glycol, and used for treating particularly delicate skin regions such as lips and genital regions.  
     
     
         27 . Use of the glycopropylene ester of retinoic acid for the preparation of a pharmaceutical composition for local destructive treatment of tumorous cells.  
     
     
         28 . Use of the glycopropylene ester of retinoic acid, together with a liquid vector pharmaceutically compatible with said ester, for the preparation of a therapeutic solution for bladder irrigation and presenting antitumoral properties.  
     
     
         29 . Use of the glycopropylene ester of retinoic acid for the preparation of a pharmaceutical composition administered orally for the treatment of nerve disorders.  
     
     
         30 . Use as claimed in  claim 29 , characterized in that said pharmaceutical composition contains a concentration of 0.0015 to 0.20 N of said ester.  
     
     
         31 . A pharmaceutical composition, characterized by comprising as an active principle the glycopropylene ester of retinoic acid in association with excipients pharmaceutically compatible with said ester.