Limited release lingual thioctic acid delivery systems

Abstract

The invention provides new methods of administering alpha-lipoic acid to patients. A diffusion rate limiting matrix is utilized to buccally, lingually and/or sublingually deliver the alpha-lipoic acid acid. This limited release matrix is intended for general nutritional supplementation and/or the treatment of various physiological disorders, such as diabetic neuropathy. 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.

1 . A method of increasing the concentration of alpha-lipoic acid in the blood of a patient diagnosed as suffering from a disease or condition treatable by an increased bloodstream concentration of alpha-lipoic acid comprising lingually administering a dissolvable tablet comprising alpha-lipoic acid in a concentration of at least 12% to the patient and instructing the patient to maintain the tablet in the patient's mouth until the tablet is fully dissolved, thereby causing the alpha-lipoic acid to be lingually absorbed and the concentration of alpha-lipoic acid in the patient's bloodstream to be increased to a level associated with the treatment of the disease or condition. 
     
     
         2 . The method of  claim 1 , wherein the alpha-lipoic acid is the primary or only pharmaceutically active ingredient in the tablet. 
     
     
         3 . The method of  claim 2 , wherein the concentration of alpha-lipoic acid in the tablet is at least 13.5%. 
     
     
         4 . The method of  claim 3 , wherein the tablet comprises an amount of a sugar in an amount that detectably enhances lingual absorption of the alpha-lipoic acid, detectably enhances uptake of the alpha-lipoic acid in the bloodstream, increases the number of patients that can tolerate dissolving the entire tablet in the mouth, or a combination of any or all thereof. 
     
     
         5 . The method of  claim 4 , wherein the sugar is monosaccharide or a disaccharide. 
     
     
         6 . The method of  claim 5 , wherein the sugar comprises glucose. 
     
     
         7 . The method of  claim 3 , wherein the alpha-lipoic acid is racemic ALA. 
     
     
         8 . The method of  claim 4 , wherein the alpha-lipoic acid is racemic ALA. 
     
     
         9 . The method of  claim 5 , wherein the tablet is formed by a method comprising compressing the alpha-lipoic acid and other tablet ingredients without heating the alpha-lipoic acid and the other ingredients of the tablet to a temperature at which any of the other ingredients of the tablet melt. 
     
     
         10 . The method of  claim 1 , wherein a majority of patients treated with the tablet find completely dissolving the tablet in the mouth to be tolerable. 
     
     
         11 . The method of  claim 3 , wherein a majority of patients treated with the tablet find completely dissolving the tablet in the mouth to be tolerable. 
     
     
         12 . The method of  claim 8 , wherein a majority of patients treated with the tablet find completely dissolving the tablet in the mouth to be tolerable. 
     
     
         13 . The method of  claim 1 , wherein the blood concentration of alpha-lipoic acid in the patient is about 85% of the concentration achieved by intravenous administration of the same amount of alpha-lipoic acid. 
     
     
         14 . The method of  claim 3 , wherein the blood concentration of alpha-lipoic acid in the patient is about 85% of the concentration achieved by intravenous administration of the same amount of alpha-lipoic acid. 
     
     
         15 . The method of  claim 1 , wherein the disease or condition comprises diabetic neuropathy. 
     
     
         16 . The method of  claim 3 , wherein the disease or condition comprises diabetic neuropathy. 
     
     
         17 . The method of  claim 7 , wherein the disease or condition comprises diabetic neuropathy. 
     
     
         18 . The method of  claim 10 , wherein the disease or condition comprises diabetic neuropathy. 
     
     
         19 . The method of  claim 16 , wherein alpha-lipoic acid is the only active pharmaceutical ingredient in the tablet. 
     
     
         20 . The method of  claim 17 , wherein alpha-lipoic acid is the only active pharmaceutical ingredient in the tablet. 
     
     
         21 . The method of  claim 18 , wherein alpha-lipoic acid is the only active pharmaceutical ingredient in the tablet. 
     
     
         22 . The method of  claim 1 , wherein the method comprises testing the patient's reaction to one or more tablets and determining an administration regimen for the patient comprising the concentration of one or more tablets to be taken by the patient and the frequency of administration of the tablets.