Agent for applying to mucosa and method for the production thereof

Abstract

An agent for applying to mucosa capable of persistently exerting a therapeutic effect on disorders such as inflammation and lesions in the mucosa even by a lower frequency of administration because the agent can stay at a diseased site for a long period of time by exhibiting a high staying properly in a mucosal epithelial layer is provided, said agent for application to mucosa containing glycosaminoglycan (GAG) into which a hydrophobic group is introduced via a binding chain, as an active ingredient.

1 - 18 . (canceled) 
     
     
         19 . A method of producing a glycosaminoglycan into which a hydrophobic group is introduced via a binding chain, comprising:
 reacting a glycosaminoglycan with a hydrophobic compound in which said hydrophobic group is bound to a functional group selected from the group consisting of hydroxyl, carboxyl, amino, and sulfonate group to form a bond selected from the group consisting of an ether bond, a carboxylate ester bond, a sulfate ester bond, carboxylic acid amide bond, or a sulfonate amide bond together with a carboxyl, hydroxyl or sulfonate group in said glycosaminoglycan.   
     
     
         20 . A method according to  claim 19 , wherein a hydrophobic compound, in which said functional group is an amino group, is reacted with a glycosaminoglycan, which contains a carboxyl group, to obtain a carboxylic acid amide bond. 
     
     
         21 . A method according to  claim 19 , wherein a hydrophobic compound, in which said functional group is a hydroxyl group, is reacted with a glycosaminoglycan, which contains a carboxyl group, to obtain a carboxylate ester bond. 
     
     
         22 . A method according to  claim 19 , wherein a hydrophobic compound, in which said functional group is a carboxyl group, is reacted with a glycosaminoglycan, which contains a hydroxyl group, to obtain a carboxylate ester bond. 
     
     
         23 . A method according to  claim 19 , wherein a hydrophobic compound, in which said functional group is a hydroxyl group, is reacted with a glycosaminoglycan, which contains a hydroxyl group, to obtain an ether bond. 
     
     
         24 . A method according to  claim 19 , wherein a hydrophobic compound, in which said functional group is a hydroxyl group, is reacted with a glycosaminoglycan, which contains a sulfonate group, to obtain a sulfonate ester bond. 
     
     
         25 . A method according to  claim 19 , wherein a hydrophobic compound, in which said functional group is a sulfonate group, is reacted with a glycosaminoglycan, which contains a hydroxyl group, to obtain a sulfonate ester bond. 
     
     
         26 . A method according to  claim 19 , wherein said glycosaminoglycan is selected from the group consisting of hyaluronic acid, chondroitin, chondroitin sulfate, heparin, heparan sulfate, dermatan sulfate and keratan sulfate, and a salt thereof. 
     
     
         27 . A method according to  claim 19 , wherein said glycosaminoglycan is sodium hyaluronate. 
     
     
         28 . A method according to  claim 19 , wherein said hydrophobic group is selected from the group consisting of an alkyl group having 2 to 18 carbon atoms, an alkenyl group having 2 to 18 carbon atoms, an alkynyl group having 2 to 18 carbon atoms, an aryl group, a heteroaryl group, an arylalkyl group, an arylalkenyl group, an arylalkynyl group, and an amino acid group. 
     
     
         29 . A method according to  claim 19 , wherein said hydrophobic group is an arylalkenyl group. 
     
     
         30 . A method according to  claim 19 , wherein said hydrophobic group is a phenylethenyl group.