Limited release lingual thioctic acid delivery systems

Abstract

A diffusion rate limiting matrix is utilized to buccally, lingually and/or sublingually deliver thioctic acid. This limited release matrix is intended for general nutritional supplementation and/or the treatment of various physiological disorders. Due to its lingual nature, this rate limiting matrix can deliver approximately IV-equivalent plasma levels of thioctic acid and is not meant to be swallowed.

We claim: 
     
         1 - 33 . (canceled) 
     
     
         34 ) A method of minimizing a thioctic acid burn effect by preventing high concentrations of thioctic acid in a mouth when administering thioctic acid to the mouth, including lingual and sublingual administration, comprising:
 (A) a thioctic acid burn effect;   (B) providing a formulation comprising:
 (i) a slow release matrix; 
 (ii) a composition and method of manufacture of said matrix; 
 (iii) wherein a dissolution rate of said matrix being dependent on said matrix composition and method of manufacture; 
 (iv) a concentration of thioctic acid ranging from 1% to 25% by mass; 
 (v) a first particular 36 gram lozenge having a first density equal to typical sucrose-based hard candies; 
 (vi) a formulation surface area; 
 (vii) wherein a size of said formulation surface area being less than a minimum surface area of said first lozenge; 
 (viii) a thioctic acid release rate; 
 (ix) wherein said thioctic acid release rate determining the degree of said thioctic acid burn effect, 
 (x) wherein determining said thioctic acid release rate as being acceptably slow, when said thioctic acid burn effect being minimized to acceptable levels, while said formulation dissolving in a user's mouth and said formulation remaining intact, to the degree that said formulation surface area not exceeding said formulation's original surface area; 
 (xi) wherein selecting said matrix method of manufacture and matrix composition, selecting said thioctic acid concentration, and selecting said formulation surface area, for providing said acceptably slow thioctic acid release rate; 
   (C) administering said formulation to said user's mouth;   (D) wherein said formulation remaining in said user's mouth while dissolving; and   (E) said formulation remaining intact while dissolving, to a degree that said formulation surface area remaining less than said formulation's original surface area.   
     
     
         35 ) The method of  claim 34 , comprising:
 (i) a second particular hard candy lozenge having a second matrix composition consisting of 185 grams of sugar, 148 grams of light corn syrup, 64 grams of water, 1.3 grams of red food coloring, and 2.7 grams of cinnamon oil;   (ii) wherein a method of manufacturing said second lozenge comprising heating said second matrix to 300 degrees Fahrenheit;   (iii) wherein a second lozenge formulation having a second thioctic acid concentration of 9% by mass;   (iv) wherein said second lozenge being a 6 gram spherical hard candy lozenge defining a size of a second surface area, or other second lozenge masses and shapes providing equivalent size surface areas;   (v) wherein said formulation's acceptably slow thioctic acid release rate being slower than a most rapid thioctic acid release rate of said second lozenge when said second lozenge dissolving in said user's mouth; and   (vi) wherein said second lozenge remaining intact to the degree that said second surface area size remaining smaller than the original size of said second surface area.   
     
     
         36 ) The method of  claim 35 , comprising:
 (i) a thioctic acid dose;   (ii) an administration of thioctic acid to a user providing plasma levels of thioctic acid to said user's systemic bloodstream;   (iii) an administration of thioctic acid, using currently available means, to a GI tract providing a GI peak plasma level of thioctic acid;   (iv) an administration of thioctic acid directly to said bloodstream, by an IV, providing an IV peak plasma level of thioctic acid;   (v) an administration of thioctic acid to a mouth providing a mouth peak plasma level of thioctic acid; and   (vi) wherein, when administering a comparable thioctic acid dose, said mouth peak plasma level being a quantity more closely approximating said IV peak plasma level than said GI peak plasma level;   (vii) wherein said formulation ranging from 1.0 gram to 30.0 grams; and   (viii) wherein said first matrix composition and method of manufacturing being the same as said second matrix composition and manufacturing method.   
     
     
         37 ) The method of  claim 36 , wherein said formulation comprising at least one of sucrose, glucose and fructose. 
     
     
         38 ) The method of  claim 36 , wherein:
 (i) said second concentration of thioctic acid being 7.5%,   (ii) said formulation concentration of thioctic acid being less than 12%; and   (iii) said first lozenge being less than 18 grams.   
     
     
         39 ) The method of  claim 38 , wherein said formulation comprising at least one of sucrose, glucose and fructose. 
     
     
         40 ) The method of  claim 36 , wherein:
 (i) said second concentration of thioctic acid being 6%,   (ii) said formulation concentration of thioctic acid being less than 9%; and   (iii) said first lozenge being less than 12 grams.   
     
     
         41 ) The method of  claim 40 , wherein:
 (i) said formulation concentration of thioctic acid being less than 6%;   (ii) said slow release matrix being a sustained release matrix; and   (iii) said formulation being a compression tablet.   
     
     
         42 ) A method of minimizing a thioctic acid burn effect by preventing high concentrations of thioctic acid in a mouth when administering thioctic acid to the mouth, including lingual and sublingual administration, comprising:
 (A) a thioctic acid burn effect;   (B) providing a formulation comprising:
 (i) a limited release matrix; 
 (ii) a composition and method of manufacture of said matrix; 
 (iii) wherein a dissolution rate of said matrix being dependent on said matrix composition and method of manufacture; 
 (iv) a concentration of thioctic acid ranging from 1% to 25% by mass; 
 (v) a first particular 36 gram lozenge having a first density equal to typical sucrose-based hard candies; 
 (vi) a formulation surface area; 
 (vii) wherein a size of said formulation surface area being less than a minimum surface area of said first lozenge; 
 (viii) a thioctic acid release rate; 
 (ix) wherein said thioctic acid release rate determining the degree of said thioctic acid burn effect, 
 (x) wherein determining said thioctic acid release rate as being acceptably slow, when said thioctic acid burn effect being minimized to acceptable levels, while said formulation dissolving in a user's mouth and said formulation remaining intact, to the degree that said formulation surface area not exceeding said formulation's original surface area; 
 (xi) wherein selecting said matrix method of manufacture and matrix composition, selecting said thioctic acid concentration, and selecting said formulation surface area, for providing said acceptably slow thioctic acid release rate; 
   (C) administering said formulation to said user's mouth;   (D) wherein said formulation remaining in said user's mouth while dissolving; and   (E) said formulation remaining intact while dissolving, to a degree that said formulation surface area remaining less than said formulation's original surface area.   
     
     
         43 ) The method of  claim 42 , comprising:
 (i) a second particular hard candy lozenge having a second matrix composition consisting of 185 grams of sugar, 148 grams of light corn syrup, 64 grams of water, 1.3 grams of red food coloring, and 2.7 grams of cinnamon oil;   (ii) wherein a method of manufacturing said second lozenge comprising heating said second matrix to 300 degrees Fahrenheit;   (iii) wherein a second lozenge formulation having a second thioctic acid concentration of 9% by mass;   (iv) wherein said second lozenge being a 6 gram spherical hard candy lozenge defining a size of a second surface area, or other second lozenge masses and shapes providing equivalent size surface areas;   (v) wherein said formulation's acceptably slow thioctic acid release rate being slower than a most rapid thioctic acid release rate of said second lozenge when said second lozenge dissolving in said user's mouth; and   (vi) wherein said second lozenge remaining intact to the degree that said second surface area size remaining smaller than the original size of said second surface area.   
     
     
         44 ) The method of  claim 43 , comprising:
 (i) a thioctic acid dose;   (ii) an administration of thioctic acid to a user providing plasma levels of thioctic acid to said user's systemic bloodstream;   (iii) an administration of thioctic acid, using currently available means, to a GI tract providing a GI peak plasma level of thioctic acid;   (iv) an administration of thioctic acid directly to said bloodstream, by an IV, providing an IV peak plasma level of thioctic acid;   (v) an administration of thioctic acid to a mouth providing a mouth peak plasma level of thioctic acid; and   (vi) wherein, when administering a comparable thioctic acid dose, said mouth peak plasma level being a quantity more closely approximating said IV peak plasma level than said GI peak plasma level;   (vii) wherein said formulation ranging from 1.0 gram to 30.0 grams; and   (viii) wherein said first matrix composition and method of manufacturing being the same as said second matrix composition and manufacturing method.   
     
     
         45 ) The method of  claim 44 , wherein said formulation comprising at least one of sucrose, glucose and fructose. 
     
     
         46 ) The method of  claim 44 , wherein:
 (i) said second concentration of thioctic acid being 6%,   (ii) said formulation concentration of thioctic acid being less than 9%; and   (iii) said first lozenge being less than 12 grams.   
     
     
         47 ) The method of  claim 46 , wherein said formulation concentration of thioctic acid being less than 6%. 
     
     
         48 ) The method of  claim 44 , wherein:
 (i) said second concentration of thioctic acid being 7.5%,   (ii) said formulation concentration of thioctic acid being less than 12%; and   (iii) said first lozenge being less than 18 grams.   
     
     
         49 ) The method of  claim 48 , wherein said formulation comprising at least one of sucrose, glucose and fructose. 
     
     
         50 ) The method of  claim 48 , wherein said formulation comprising at least one of sucrose and glucose. 
     
     
         51 ) The method of  claim 48 , wherein said formulation being a hard candy lozenge comprising a molten matrix phase during said manufacturing. 
     
     
         52 ) The method of  claim 51 , wherein said formulation comprising at least one of sucrose, glucose and fructose. 
     
     
         53 ) The method of  claim 51 , wherein:
 (i) said second concentration of thioctic acid being 6%,   (ii) said formulation concentration of thioctic acid being less than 9%; and   (iii) said first lozenge being less than 12 grams.