Suckable and/or melt-in-mouth tablet based on hyaluronic acid and chondroitin sulphate and salts thereof

Abstract

The present invention relates to a suckable and/or melt-in-mouth tablet based on hyaluronic chondroitin sulphate and/or salts thereof.

1 . A composition for oral use in the solid form of a suckable and/or melt-in-mouth and/or mouth dissolving tablet or the like, comprising:
 I) a mixture which comprises or, alternatively, consists of:
 a hyaluronic acid, or a salt thereof, and 
 a chondroitin, or a salt thereof 
   and, optionally,   II) at least one food or pharmaceutical grade excipient or additive;   said composition being for use:
 i) in a method for the treatment of disorders or symptoms caused or provoked by gastroesophageal reflux (GERD), or 
 ii) in a method for the treatment of extraesophageal disorders or symptoms caused by the upflow of gastric contents and/or gastric vapours from the stomach to the oral cavity (also known as refluxate, which comprises pepsin, acid and/or mildly acidic or non-acidic but irritating contents), or 
 iii) in a method for the treatment of ulcers or lacerations provoked in the gastric mucosa (stomach lining), in the esophageal mucosa, in the laryngopharyngeal mucosa or in the tissues lining the oral cavity, so as to protect the mucosa and the tissues from the damage provoked thereto 
 in subjects in a state of need for said treatments. 
   
     
     
         2 . A composition for use according to  claim 1 , wherein said solid form of a chewable and/or suckable and/or melt-in-mouth and/or orally dissolving tablet, or the like, has the function of causing the dissolution of at least said hyaluronic acid, or a salt thereof, and said chondroitin, or a salt thereof and in the saliva of the subjects to whom said composition is administered so as to form a viscous gel that adheres to the mucosa of the various anatomical parts from the oral cavity to the stomach by swallowing of said gel. 
     
     
         3 . A composition for use according to  claim 1 , wherein said hyaluronic acid, or a salt thereof, and said chondroitin, or a salt thereof, both have an average molecular weight comprised from greater than 1 KDa to less than 1,000 KDa. 
     
     
         4 . The composition for use according to  claim 1 , wherein said hyaluronic acid is a linear, branched, cross-linked or substituted hyaluronic acid having an average molecular weight comprised from 200 KDa to 800 KDa; more preferably said linear, branched, cross-linked or substituted hyaluronic acid has an average molecular weight comprised from 400 KDa to about 600 KDa. 
     
     
         5 . The composition for use according to  claim 1 , wherein said hyaluronic acid is the hyaluronic acid having the CAS no. 9004-61-9. 
     
     
         6 . The composition for use according to  claim 1 , wherein said hyaluronic acid is in the form of a salt, wherein said salt is a hyaluronate of an alkali metal or a hyaluronate of an alkaline earth metal; said salt is preferably selected from the group comprising or, alternatively, consisting of sodium hyaluronate, potassium hyaluronate, calcium hyaluronate and magnesium hyaluronate. 
     
     
         7 . The composition for use according to  claim 1 , wherein said salt is sodium hyaluronate; it is preferably sodium hyaluronate having CAS no. 9067-32-7. 
     
     
         8 . The composition for use according to  claim 1 , wherein said chondroitin, or a salt thereof, is a chondroitin or a chondroitin sulphate or a chondroitin sulphate sodium, wherein said chondroitin is of animal origin or of another origin, wherein said chondroitin of animal origin is extracted from an animal selected from the group comprising or, alternatively, consisting of: chickens, bovines, swine, fish and crustaceans, preferably crabs, lobsters or prawn shells. 
     
     
         9 . The composition for use according to  claim 1 , wherein said chondroitin, or a salt thereof, has an average molecular weight comprised from 200 KDa to 800 KDa; said chondroitin, or a salt thereof, preferably has an average molecular weight comprised from 400 KDa to 600 KDa. 
     
     
         10 . The composition for use according to  claim 1 , wherein said chondroitin is a chondroitin sulphate; preferably, said chondroitin sulphate is at least 90% chicken chondroitin sulphate sodium. 
     
     
         11 . The composition for use according to  claim 1 , wherein said mixture can also comprise a basic substance with antacid properties; preferably, said substance with antacid properties is a substance selected from the group comprising or, alternatively, consisting of a salt of a cation of an alkali metal, or a cation of an alkaline earth metal, or a cation of a metal (III) wherein said salt is in the form of an oxide, a hydroxide, a carbonate, a bicarbonate, a silicate, a trisilicate, a sulphate or a citrate. 
     
     
         12 . The composition for use according to  claim 11 , wherein said cation of an alkali metal, or a cation of an alkaline earth metal, or a cation of a metal (III) present in said salt as a basic substance with antacid properties is selected from the group comprising or, alternatively, consisting of: sodium cation, potassium cation, calcium cation, magnesium cation or aluminium cation; said cation of an alkaline earth metal is preferably the magnesium cation. 
     
     
         13 . The composition for use according to  claim 11 , wherein said salt, as a basic substance with antacid properties, is selected from the group comprising or, alternatively, consisting of aluminium hydroxide, magnesium hydroxide or, magnesium trisilicate or mixtures thereof; said salt is preferably magnesium trisilicate in a hydrate form, such as CAS no. 14987-04-3 (EINECS no. 239-076-7); said salt is preferably aluminium hydroxide on its own or aluminium hydroxide and sodium bicarbonate in a 2:1 ratio by weight; or magnesium hydroxide on its own or magnesium hydroxide and sodium bicarbonate in a 2:1 ratio by weight; or magnesium trisilicate on its own or magnesium trisilicate and sodium bicarbonate in a 2:1 ratio by weight. 
     
     
         14 . The composition for use according to  claim 1 , wherein said mixture can further comprise also a proton pump inhibitor compound PPI; said proton pump inhibitor compound is selected from the group comprising, or alternatively, consisting of: omeprazole, lansoprazole, esomeprazole, pantoprazole, rabeprazole sodium, ilaprazole and tenatoprazole, more preferably omeprazole. 
     
     
         15 . The composition for use according to  claim 1 , wherein said composition is administered to subjects who also undergo a concomitant treatment with PPIs; the PPIs are preferably selected from the group comprising or, alternatively, consisting of: omeprazole, lansoprazole, esomeprazole, pantoprazole, rabeprazole sodium, ilaprazole and tenatoprazole. 
     
     
         16 . A method of treatment, comprising:
 orally administering a composition of  claim 1  to a subject, wherein the subject has:   i) a disorder or symptom caused or provoked by gastroesophageal reflux (GERD);   ii) an extraesophageal disorders or symptom caused by the upflow of gastric contents and/or gastric vapours from the stomach to the oral cavity (also known as refluxate, which comprises pepsin, acid and/or mildly acidic or non-acidic but irritating contents); or   iii) an ulcer or laceration provoked in the gastric mucosa (stomach lining), in the esophageal mucosa, in the laryngopharyngeal mucosa or in the tissues lining the oral cavity, so as to protect the mucosa and the tissues from the damage provoked thereto.   
     
     
         17 . The method of  claim 16 , wherein said hyaluronic acid, or a salt thereof, and said chondroitin, or a salt thereof, both have an average molecular weight comprised from greater than 1 KDa to less than 1,000 KDa. 
     
     
         18 . The method of  claim 16 , wherein said hyaluronic acid is a linear, branched, cross-linked or substituted hyaluronic acid having an average molecular weight comprised from 200 KDa to 800 KDa; more preferably said linear, branched, cross-linked or substituted hyaluronic acid has an average molecular weight comprised from 400 KDa to about 600 KDa. 
     
     
         19 . The method of  claim 16 , wherein said hyaluronic acid is the hyaluronic acid having the CAS no. 9004-61-9. 
     
     
         20 . The method of  claim 16 , wherein said hyaluronic acid is in the form of a salt, wherein said salt is a hyaluronate of an alkali metal or a hyaluronate of an alkaline earth metal; said salt is preferably selected from the group comprising or, alternatively, consisting of sodium hyaluronate, potassium hyaluronate, calcium hyaluronate and magnesium hyaluronate.