Aliphatic anionic compounds and oxidative compounds with improved stability and efficacy for use in pharmaceutical compositions

Abstract

Various embodiments described herein provide for a multi-component compositions and methods for its pharmaceutical and cosmetic use, comprising a combination of an aliphatic anionic compound, an oxidative compound, and a buffering system. Source of fluoride ion and other carriers are optional ingredients. The aliphatic anionic compound and the oxidative compound function together, in presence or absence of fluoride ion source, to protect the oxidative compounds from degradation prior to use and upon use, and to enhance the efficacy of the composition. In addition to achieving greater stability, combined effects of the aliphatic anionic compound, oxidative compound and source of fluoride ion achieve enhanced fluoride uptake, higher enamel protection by enhanced remineralization and reduced demineralization, increased plaque removal, reduced re-growth of plaque polymicrobial biofilm, greater amount of chlorite ion availability and effective oxidation of salivary biomolecules.

1 . A method for effecting enhanced fluoride uptake into the tooth enamel, comprising:
 preparing an oral care single phase composition comprising from about 0.01% to about 5.0% of an aliphatic anionic compound, based on a total weight of the composition, from about 0.001 to about 8.0% of an oxidative compound, based on a total weight of the composition, from about 0.01% to 0.8% of fluoride ion source, based on a total weight of the composition, a buffering system, wherein pH of the oral care single phase composition is between 6.0 and 8.0, water, wherein the aliphatic anionic compound provides enhanced stability for the oxidative compound, wherein the oxidative compound is sodium chlorite, wherein the buffering system comprises disodium hydrogen phosphate and sodium dihydrogen phosphate, wherein the aliphatic anionic compound is an N-acyl sarcosinate, wherein the N-acyl sarcosinate is at least one of sodium lauroyl sarcosinate, sodium cocoyl sarcosinate, sodium myristoyl sarcosinate, sodium oleoyl sarcosinate, or sodium stearoyl sarcosinate, wherein the composition exhibits less than 35% loss of the oxidative compound for a period of 24 months at about 25° C.; and   applying the oral care single phase composition to the oral cavity.   
     
     
         2 . The method of  claim 1 , wherein the enhanced fluoride uptake into the tooth enamel is increased by up to 4-fold. 
     
     
         3 . The method of  claim 1 , further comprising adding, to the oral care single phase composition, an orally acceptable aqueous vehicle comprising at least one of a humectant, an abrasive, a pharmaceutically acceptable carrier, a fluoride ion source, and a thickening agent. 
     
     
         4 . The method of  claim 1 , further comprising formulating the oral care single phase composition into a form of, at least one of, a mouth rinse, a gum, a gel, a paste, a cream, spray, and a lozenge. 
     
     
         5 . A method for effecting enhanced remineralization of the tooth enamel, comprising:
 preparing an oral care single phase composition comprising from about 0.01% to about 5.0% of an aliphatic anionic compound, based on a total weight of the composition, from about 0.001 to about 8.0% of an oxidative compound, based on a total weight of the composition, from about 0.01% to 0.8% of fluoride ion source, based on a total weight of the composition, a buffering system, wherein pH of the oral care single phase composition is between 6.0 and 8.0, water, wherein the aliphatic anionic compound provides enhanced stability for the oxidative compound, wherein the oxidative compound is sodium chlorite, wherein the buffering system comprises disodium hydrogen phosphate and sodium dihydrogen phosphate, wherein the aliphatic anionic compound is an N-acyl sarcosinate, wherein the N-acyl sarcosinate is at least one of sodium lauroyl sarcosinate, sodium cocoyl sarcosinate, sodium myristoyl sarcosinate, sodium oleoyl sarcosinate, or sodium stearoyl sarcosinate, wherein the composition exhibits less than 35% loss of the oxidative compound for a period of 24 months at about 25° C.; and   applying the oral care single phase composition to the oral cavity.   
     
     
         6 . The method of  claim 5 , wherein the enhanced remineralization of the tooth enamel is increased by up to 2-fold. 
     
     
         7 . The method of  claim 5 , further comprising adding, to the oral care single phase composition, an orally acceptable aqueous vehicle comprising at least one of: a humectant, an abrasive, a pharmaceutically acceptable carrier, a fluoride ion source, and a thickening agent. 
     
     
         8 . The method of  claim 5 , further comprising formulating the oral care single phase composition into a form of, at least one of, a mouth rinse, a gum, a gel, a paste, a cream, spray, and a lozenge. 
     
     
         9 . A method for decreasing and delaying the regrowth of oral polymicrobial biofilm, comprising:
 applying, to an oral cavity, an oral care single phase composition comprising from about 0.01% to about 5.0% of an aliphatic anionic compound, based on a total weight of the composition, from about 0.001 to about 8.0% of an oxidative compound, based on a total weight of the composition, from about 0.01% to 0.8% of fluoride ion source, based on a total weight of the composition, a buffering system, wherein pH of the composition is between 6.0 and 8.0, water, wherein the aliphatic anionic compound provides enhanced stability for the oxidative compound, wherein the oxidative compound is sodium chlorite, wherein the buffering system comprises disodium hydrogen phosphate and sodium dihydrogen phosphate, wherein the aliphatic anionic compound is an N-acyl sarcosinate, wherein the N-acyl sarcosinate is at least one of sodium lauroyl sarcosinate, sodium cocoyl sarcosinate, sodium myristoyl sarcosinate, sodium oleoyl sarcosinate, or sodium stearoyl sarcosinate, wherein the composition exhibits less than 35% loss of the oxidative compound for a period of 24 months at about 25° C.   
     
     
         10 . The method of  claim 9 , wherein the oral care single phase composition decreases oral polymicrobial biofilm and delays its regrowth for up to 24 hours. 
     
     
         11 . The method of  claim 9 , wherein the oral care single phase composition further comprises an orally acceptable aqueous vehicle comprising at least one of a humectant, an abrasive, a pharmaceutically acceptable carrier, a fluoride ion source, and a thickening agent. 
     
     
         12 . The method of  claim 9 , wherein the oral care single phase composition is formulated into a form of, at least one of, a mouth rinse, a gum, a gel, a paste, a cream, spray, and a lozenge. 
     
     
         13 . A method for oxidizing salivary biomolecules, comprising:
 preparing an oral care single phase composition comprising from about 0.01% to about 5.0% of an aliphatic anionic compound, based on a total weight of the composition, from about 0.001 to about 8.0% of an oxidative compound, based on a total weight of the composition, from about 0.01% to 0.8% of fluoride ion source, based on a total weight of the composition, a buffering system, wherein pH of the composition is between 6.0 and 8.0, water, wherein the aliphatic anionic compound provides enhanced stability for the oxidative compound, wherein the oxidative compound is sodium chlorite, wherein the buffering system comprises disodium hydrogen phosphate and sodium dihydrogen phosphate, wherein the aliphatic anionic compound is an N-acyl sarcosinate, wherein the N-acyl sarcosinate is at least one of sodium lauroyl sarcosinate, sodium cocoyl sarcosinate, sodium myristoyl sarcosinate, sodium oleoyl sarcosinate, or sodium stearoyl sarcosinate, wherein the composition exhibits less than 35% loss of the oxidative compound for a period of 24 months at about 25° C.   
     
     
         14 . The method of  claim 13 , wherein the salivary biomolecules are comprised of at least one of pyruvate and L-methionine.  21 . The method of  claim 18 , further comprising oxidizing a salivary biomolecule comprising at least one of pyruvate and L-methionine within 30 to 60 seconds of contact time. 
     
     
         15 . The method of  claim 13 , further comprising adding, to the oral care single phase composition, an orally acceptable aqueous vehicle comprising at least one of the following: a humectant, an abrasive, a pharmaceutically acceptable carrier, a fluoride ion source, and a thickening agent. 
     
     
         16 . The method of  claim 14 , further comprising formulating the oral care single phase composition into a form of, at least one of the following: a mouth rinse, a gum, a gel, a paste, a cream, spray, and a lozenge. 
     
     
         17 . A method for preparation of oral care single phase toothpaste composition comprising:
 dissolving a gelling agent in water in a tank equipped with a stirring system to form an aqueous solution;   adding a buffering compound until a pH range of between 6.0 to 8.5 is achieved;   adding the chlorite ion source to the aqueous solution;   adding at least one additional ingredient comprising at least of a humectant, a sweetening agent, a coloring agent, an abrasive agent, a fluoride ion source, a flavoring agent, an emollient agent, a suspending agent, an emulsifying agent, an N-acyl sarcosinate, or water;   stirring the composition for about 40- to 60-minutes under vacuum;   releasing the vacuum; and   filling the composition in a container for use, wherein all compounding operations occur at ambient temperature.   
     
     
         18 . A method of  claim 17 , wherein the composition is a gel or cream. 
     
     
         19 . A method for preparation of oral care single phase rinse composition comprising:
 dissolving a base compound in water in a tank equipped with a stirring system to form an aqueous solution;   adding the chlorite ion source to the aqueous solution;   adding at least one additional ingredient comprising at least one of a sweetening agent, a fluoride ion source, a flavoring agent, an N-acyl sarcosinate, and water′   adding a weak acid compound until a final pH range of 6.0 to 8.5 is achieved;   stirring the composition for about 40- to 60-minutes; and   filling the composition in a container for use, wherein all compounding operations occur at ambient temperature.   
     
     
         20 . A method for preparation of oral care single phase spray composition comprising;
 dissolving a base compound in water in a tank equipped with a stirring system to form an aqueous solution;   adding a chlorite ion source to the aqueous solution;   adding at least one additional ingredient comprising at least one of a sweetening agent, a fluoride ion source, a flavoring agent, an N-acyl sarcosinate, a dispersing agent, a humectant, and water;   adding a weak acid compound until a final pH range of 6.0 to 8.5 is achieved;   stirring the composition for about 40- to 60-minutes; and   filling the composition in container for use, wherein all compounding operations occur at ambient temperature.