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 property 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 for producing an eye drop containing a glycosaminoglycan into which a hydrophobic group is introduced via the spacer chain as an active ingredient, the method comprising:
 introducing the spacer chain and the hydrophobic group to a hyaluronic acid or pharmaceutically acceptable salt thereof,   with the proviso that the method not comprising a photodimerization reaction or a photopolymerization reaction to cross link the glycosaminoglycan with one another,   wherein the eye drop is liquid preparation in which concentration of the glycosaminoglycan is 0.1 to 0.3% by weight,   wherein the glycosaminoglycan having a repeat unit of a structural unit represented by chemical formula (I):   
       
         
           
           
               
               
           
         
         wherein, R represents R 1  or R 2 ; 
         Ac represents an acetyl group; 
         R 1  represents ONa or OH; 
         R 2  represents (1) Ph-CH═CH—COO—(CH 2 ) m —NH—; 
         (2) Ph-CH═CH—COO—CH 2 —(OCH 2 ) n —NH—; 
         (3) Ph-CH═CH—CONH—(CH 2 ) m —NH—; 
         (4) Ph-CH═CH—CONH—CH 2 —(OCH 2 )n-NH—; 
         (5) Ph-CH═CH—COO—(CH 2 ) m —O—; 
         (6) Ph-CH═CH—COO—CH 2 —(OCH 2 ) n —O—; 
         (7) Ph-CH═CH—CONH—(CH 2 ) m —O—; or 
         (8) Ph-CH═CH—CONH—CH 2 —(OCH 2 ) n —O—; 
         wherein, Ph represents phenyl group, m and n represent integers of 1 to 18, respectively, and 1 represents 0 or an integer of 1 to 18, as a basic skeleton, wherein the ratio of the above structural unit wherein R represents R 2  is 5 to 30% in molar equivalent relative to the disaccharide repeat unit in molar equivalent of the glycosaminoglycan. 
       
     
     
         20 . The method according to claim  1 , wherein the glycosaminoglycan into which the hydrophobic group is introduced via the spacer chain blocks transmission of the ultraviolet ray at a wavelength of 200 to 300 nm by 70 to 100%, when the glycosaminoglycan into which the hydrophobic group is introduced via the spacer chain is made into an aqueous solution of 0.1% by weight.