Solid composition for the oral administration of dyes and diagnostic use thereof

Abstract

The present application discloses solid compositions for the oral administration of dyes, and diagnostic use thereof. Preferably, such diagnostic use is aimed at the diagnostic evaluation of the gastrointestinal tract.

1 . A method of detecting a pathology in a subject undergoing colonoscopy, comprising the subject swallowing one or more doses of an extended release tablet prior to the colonoscopy, the tablets comprising:
 (a) methylene blue;   (b) at least one lipophilic compound; and   (c) at least one hydrophilic compound;   and wherein the tablet is coated with a composition comprising at least one gastro-resistant substance.   
     
     
         2 . The method according to  claim 1 , wherein the pathology is selected from inflammatory, ulcerative, dysplastic, pre-neoplastic and neoplastic pathologies. 
     
     
         3 . The method according to  claim 2 , wherein the pathology is a pre-neoplastic pathology or a neoplastic pathology. 
     
     
         4 . The method according to  claim 3 , wherein the pathology is selected from cancerous forms, pre-cancerous forms, polyps and pseudopolyps 
     
     
         5 . The method according to  claim 1 , wherein the extended release tablet comprises 25 mg of methylene blue. 
     
     
         6 . The method according to  claim 1 , wherein the at least one lipophilic compound is selected from saturated, unsaturated or hydrogenated long chain alcohols, saturated, unsaturated or hydrogenated fatty acids, salts thereof, esters or amides, mono-, di- or triglycerides of fatty acids, polyethoxylated derivatives thereof, waxes, ceramides, cholesterol, and cholesterol derivatives. 
     
     
         7 . The method according to  claim 6 , wherein the at least one lipophilic compound is stearic acid or a salt thereof. 
     
     
         8 . The method according to  claim 7 , wherein the at least one lipophilic compound is stearic acid. 
     
     
         9 . The method according to  claim 7 , wherein the at least one lipophilic compound is magnesium stearate. 
     
     
         10 . The method according to  claim 1 , wherein the at least one hydrophilic compound is selected from polymers or copolymers of the acrylic or methacrylic acid, alkyl vinyl polymers, alkyl celluloses, hydroxyalkyl celluloses, carboxyalkyl celluloses, modified celluloses, plurisubstituted celluloses, polysaccharides, dextrins, pectins, starches, complex starches, starch derivatives, alginic acid, synthetic rubber, natural rubber, and polyalcohol. 
     
     
         11 . The method according to  claim 10 , wherein the at least one hydrophilic compound is selected from alkyl celluloses, hydroxyalkyl celluloses, carboxyalkyl celluloses, modified celluloses, plurisubstituted celluloses, polysaccharides, dextrins, pectins, and starches. 
     
     
         12 . The method according to  claim 11 , wherein the at least one hydrophilic compound is selected from alkyl celluloses, hydroxyalkyl celluloses, carboxyalkyl celluloses, and starches. 
     
     
         13 . The method according to  claim 12 , wherein the at least one hydrophilic compound is selected from hydroxyalkyl celluloses. 
     
     
         14 . The method according to  claim 13 , wherein the at least one hydrophilic compound is selected from hydroxypropyl cellulose, methyl hydroxypropyl cellulose, and hydroxyethyl cellulose. 
     
     
         15 . A method for delivering methylene blue to the colon of a subject, comprising administering to the subject an extended release tablet comprising:
 (a) methylene blue;   (b) at least one lipophilic compound; and   (c) at least one hydrophilic compound;   and wherein the tablet is coated with a composition comprising at least one gastro-resistant substance.   
     
     
         16 . The method according to  claim 15 , wherein the extended release tablet comprises 25 mg of methylene blue. 
     
     
         17 . The method according to  claim 15 , wherein the at least one lipophilic compound is selected from saturated, unsaturated or hydrogenated long chain alcohols, saturated, unsaturated or hydrogenated fatty acids, salts thereof, esters or amides, mono-, di- or triglycerides of fatty acids, polyethoxylated derivatives thereof, waxes, ceramides, cholesterol, and cholesterol derivatives. 
     
     
         18 . The method according to  claim 17 , wherein the at least one lipophilic compound is stearic acid or a salt thereof. 
     
     
         19 . The method according to  claim 18 , wherein the at least one lipophilic compound is stearic acid. 
     
     
         20 . The method according to  claim 18 , wherein the at least one lipophilic compound is magnesium stearate. 
     
     
         21 . The method according to  claim 15 , wherein the at least one hydrophilic compound is selected from polymers or copolymers of the acrylic or methacrylic acid, alkyl vinyl polymers, alkyl celluloses, hydroxyalkyl celluloses, carboxyalkyl celluloses, modified celluloses, plurisubstituted celluloses, polysaccharides, dextrins, pectins, starches, complex starches, starch derivatives, alginic acid, synthetic rubber, natural rubber, and polyalcohol. 
     
     
         22 . The method according to  claim 21 , wherein the at least one hydrophilic compound is selected from alkyl celluloses, hydroxyalkyl celluloses, carboxyalkyl celluloses, modified celluloses, plurisubstituted celluloses, polysaccharides, dextrins, pectins, and starches. 
     
     
         23 . The method according to  claim 22 , wherein the at least one hydrophilic compound is selected from alkyl celluloses, hydroxyalkyl celluloses, carboxyalkyl celluloses, and starches. 
     
     
         24 . The method according to  claim 23 , wherein the at least one hydrophilic compound is selected from hydroxyalkyl celluloses. 
     
     
         25 . The method according to  claim 24 , wherein the at least one hydrophilic compound is selected from hydroxypropyl cellulose, methyl hydroxypropyl cellulose, and hydroxyethyl cellulose. 
     
     
         26 . The method according to  claim 23 , wherein the at least one hydrophilic compound is sodium starch glycolate. 
     
     
         27 . The method according to  claim 15 , wherein the at least one gastro-resistant substance is soluble at a pH of between about 5 and about 7. 
     
     
         28 . The method according to  claim 27 , wherein the at least one gastro-resistant substance is selected from of polymers of acrylic acid, polymers of methacrylic acid, copolymers of acrylic acid, copolymers of methacrylic acid, cellulose derivatives, hydroxybutyrate-based polymers, and shellac. 
     
     
         29 . The method according to  claim 28 , wherein the at least one gastro-resistant substance is selected from polymers of acrylic acid, polymers of methacrylic acid, copolymers of acrylic acid, and copolymers of methacrylic acid. 
     
     
         30 . The method according to  claim 15 , wherein the at least one gastro-resistant substance is selected from methacrylic acid copolymer type A and methacrylic acid copolymer type B.