Oral care compositions comprising benzocaine and mucoadhesive thin films formed therefrom

Abstract

The present invention provides oral care compositions. The compositions may be provided in a solid form, such as a film. The compositions can comprise one or more film forming polymers, one or more bioadhesive agents, one or more plasticizers, benzocaine (and optionally one or more further active ingredients), one or more polymeric solvents, and an aqueous solvent. The oral care composition can be a solid or semi-solid composition up to a temperature of at least 40° C. Methods of providing such an oral care compositions are also provided herein.

1 . An oral care composition comprising:
 one or more film forming polymers in a total amount of about 40% to about 80% by weight;   one or more bioadhesive agents in a total amount of about 0.5% to about 10% by weight;   one or more plasticizers in a total amount of about 0.5% to about 8% by weight;   one or more active agents in a total amount of about 2% to about 35% by weight, said one or more active agents including benzocaine;   one or more polymeric solvents in which the one or more active agents is solubilized, the one or more polymeric solvents being in a total amount of about 5% to about 20% by weight; and   an aqueous medium in an amount of about 0.5% to about 15% by weight;   each of the foregoing amounts being based on the total weight of the oral care composition;   wherein the oral care composition is in the form of a film having a thickness of about 50 μm to about 500 μm.   
     
     
         2 . The oral care composition of  claim 1 , wherein the one or more film forming polymers comprises one or more of a polyvinylpyrrolidone, a polysaccharide, and a cellulose derivative. 
     
     
         3 . The oral care composition of  claim 1 , wherein the one or more film forming polymers is selected from the group consisting of a polyvinylpyrrolidone, pullulan, hydroxypropyl cellulose, pectin, and combinations thereof. 
     
     
         4 . The oral care composition of  claim 1 , wherein the one or more film forming polymers includes a polyvinylpyrrolidone in an amount of about 20% to about 40% by weight and pullulan in an amount of about 20% to about 40% by weight, based on the total weight of the oral care composition. 
     
     
         5 . The oral care composition of  claim 1 , wherein the one or more bioadhesive agents comprises a polycarbophil. 
     
     
         6 . The oral care composition of  claim 1 , wherein the one or more plasticizers includes glycerol in an amount of about 0.25% to about 5% by weight, based on the total weight of the oral care composition. 
     
     
         7 . The oral care composition of  claim 1 , wherein the one or more active ingredients further includes menthol. 
     
     
         8 . The oral care composition of  claim 1 , wherein the one or more active ingredients includes benzocaine in an amount of about 2% to about 15% by weight and menthol in an amount of about 2% to about 20% by weight based on the total weight of the oral care composition. 
     
     
         9 . The oral care composition of  claim 1 , wherein the one or more polymeric solvents comprises one or more different polyalkylene glycols. 
     
     
         10 . The oral care composition of  claim 1 , wherein the one or more polymeric solvents includes a first polyethylene glycol (PEG) having a molecular weight of 1,500 grams per mole or less and a second polyethylene glycol (PEG) having a molecular weight of 2,000 grams per mole or greater. 
     
     
         11 . The oral care composition of  claim 10 , wherein the first PEG is present in an amount of about 2% to about 15% by weight, and the second PEG is present in an amount of about 2% to about 10% by weight, based on the total weight of the oral care composition. 
     
     
         12 . The oral care composition of  claim 1 , wherein the aqueous medium is present in an amount of about 3% to about 12% by weight, based on the total weight of the oral care composition. 
     
     
         13 . The oral care composition of  claim 1 , wherein the composition further comprises one or more opacifiers in a total amount of about 0.02% to about 2% by weight based on the total weight of the composition. 
     
     
         14 . The oral care composition of  claim 13 , wherein the opacifier includes titanium dioxide. 
     
     
         15 . The oral care composition of  claim 1 , wherein the film is configured to dissolve substantially completely in contact with oral mucosa in a time of about 15 minutes to about 120 minutes. 
     
     
         16 . A method of making an oral care composition comprising:
 solubilizing one or more active agents in one or more polymeric solvents while heating to a temperature of about 50° C. to about 120° C. to form a premix, wherein the one or more active agents includes benzocaine;   mixing into the premix each of the following components to form a liquid composition:
 one or more film forming polymers; 
 one or more bioadhesive agents; 
 one or more plasticizers; and 
 water; 
   coating the liquid composition onto a backing sheet to form a layer of the composition having a thickness of about 100 μm to about 500 μm;   drying the layer to form a film of the oral care composition having a total water content of about 3% to about 15% by weight based on the total weight of the film.   
     
     
         17 . The method of  claim 16 , wherein the film of the oral care composition comprises:
 a total of about 2% to about 35% by weight of the one or more active agents;   a total of about 5% to about 20% by weight of the one or more polymeric solvents:   a total of about 40% to about 80% by weight of the one or more film forming polymers;   a total of about 0.5% to about 10% by weight of the one or more bioadhesive agents; and   a total of about 0.5% to about 8% by weight of the one or more plasticizers;   each of the foregoing amounts being based on the total weight of the film of the oral care composition.   
     
     
         18 . The method of  claim 16 , wherein the drying comprises applying heated air to the layer of the composition on the backing sheet for a time of about 20 minutes to about 150 minutes. 
     
     
         19 . The method of  claim 18 , wherein the heated air is applied only from above the layer of the composition. 
     
     
         20 . The method of  claim 18 , wherein the drying is carried out by passing the layer of the composition on the backing sheet through a drying tunnel. 
     
     
         21 . The method of  claim 16 , further comprising cutting the film of the oral care composition into individual strips having a width of about 10 mm to about 20 mm and having a length of about 20 mm to about 30 mm.