Cationic pharmaceutically active ingredient containing composition, and methods for manufacturing and using

Abstract

A cationic pharmaceutically active ingredient containing composition is provided. The composition includes a cationic pharmaceutically active ingredient, a hydrophobic polymer/hydrophilic polymer adduct comprising a poly(vinylpyrrolidone/alkylene) polymer and a polymer comprising carboxylic acid groups, hydroxyl groups, or a mixture of carboxylic acid groups and hydroxyl groups, a compatibilizing amount of a long chain organic acid having a carbon chain of at least 8 carbon atoms, and at least about 50 wt. % water.

We claim: 
     
         1 . A cationic pharmaceutically active ingredient containing composition comprising:
 (a) about 0.0001 wt. % to about 5 wt. % cationic pharmaceutically active ingredient;   (b) at least about 3 wt. % of a hydrophobic polymer/hydrophilic polymer adduct comprising a poly(vinylpyrrolidone-alkylene) polymer and a polymer comprising carboxylic acid groups, hydroxyl groups, or mixture of carboxylic acid groups and hydroxyl groups;   (c) a compatibilizing amount of a long chain organic acid having a carbon chain of at least about 8 carbon atoms; and   (d) at least about 50 wt. % water.   
     
     
         2 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the poly(vinlypyrrolidone-alkylene) polymer comprises a polymer having an alkylene group containing about 10 carbon atoms to about 30 carbon atoms. 
     
     
         3 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the hydrophobic polymer/hydrophilic polymer adduct has a ratio of pyrrolidone groups to a combination of carboxylic acid groups and hydroxyl groups of about 1:1 to about 5:1. 
     
     
         4 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the long chain organic acid has a carbon chain of about 10 carbon atoms to about 20 carbon atoms. 
     
     
         5 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the long chain organic acid has a carbon chain of about 12 carbon atoms to about 16 carbon atoms. 
     
     
         6 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the long chain organic acid comprises at least one of lauric acid, stearic acid, palmitic acid, myristic acid, or a mixture thereof. 
     
     
         7 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the composition comprises at least about 0.05 wt. % of the long chain organic acid. 
     
     
         8 . A cationic pharmaceutically active ingredient containing composition according to  claim 1 , wherein the two hour release from a nylon membrane property of the cationic pharmaceutically active ingredient is less than 80%. 
     
     
         9 . A method of using a cationic pharmaceutically active ingredient containing composition, the method comprises:
 (a) applying a cationic pharmaceutically active ingredient containing composition to skin tissue, the cationic pharmaceutically active ingredient containing composition comprising:   (i) about 0.0001 wt. % to about 5 wt. % cationic pharmaceutically active ingredient;   (ii) at least about 3 wt. % of a hydrophobic polymer/hydrophilic polymer adduct comprising a poly(vinylpyrrolidone-alkylene) polymer and a polymer comprising carboxylic acid groups, hydroxyl groups, or mixture of carboxylic acid groups and hydroxyl groups;   (iii) a compatibilizing amount of a long chain organic acid having a carbon chain of at least about 8 carbon atoms; and   (iv) at least about 50 wt. % water.   
     
     
         10 . A method according to  claim 9 , wherein the poly(vinlypyrrolidone-alkylene) polymer comprises a polymer having an alkylene group containing about 10 carbon atoms to about 30 carbon atoms. 
     
     
         11 . A method according to  claim 9 , wherein the hydrophobic polymer/hydrophilic polymer adduct has a ratio of pyrrolidone groups to a combination of carboxylic acid groups and hydroxyl groups of about 1:1 to about 5:1. 
     
     
         12 . A method according to  claim 9 , wherein the composition comprises about 0.5 wt. % to about 6 wt. % of a surfactant. 
     
     
         13 . A method according to  claim 9 , wherein the composition comprises about 0.1 wt. % to about 2 wt. % of a thickener. 
     
     
         14 . A method according to  claim 9 , wherein the composition comprises about 0.5 wt. % to about 5 wt. % of a moisturizer. 
     
     
         15 . A method according to  claim 9 , wherein the long chain organic acid has a carbon chain of about 10 carbon atoms to about 20 carbon atoms. 
     
     
         16 . A method according to  claim 9 , wherein the long chain organic acid has a carbon chain of about 12 carbon atoms to about 16 carbon atoms. 
     
     
         17 . A method according to  claim 9 , wherein the long chain organic acid comprises at least one of lauric acid, stearic acid, palmitic acid, myristic acid, or a mixture thereof. 
     
     
         18 . A method according to  claim 9 , wherein the composition comprises at least about 0.05 wt. % of the long chain organic acid. 
     
     
         19 . A method according to  claim 9 , wherein the two hour release from a nylon membrane property for the cationic pharmaceutically active ingredient is less than 80%. 
     
     
         20 . A method for manufacturing a cationic pharmaceutically active ingredient containing composition, the method comprising:
 (a) forming a polymer adduct comprising a poly (vinylpyrrolidone-alkylyne) polymer and a polymer comprising carboxylic acid groups, hydroxyl groups, or a mixture of carboxylic acid groups and hydroxyl groups. In the presence of less than one wt. percent water, if water is present at all;   (b) forming an emulsion containing the polymer adduct and water, wherein the water is present in an amount of at least about 50 wt. %; and   (c) adding a long chain organic acid having a carbon chain of at least about 8 carbon atoms and a cationic pharmaceutically active ingredient.