Composition for topical administration

Abstract

The present invention provides a composition for topical administration comprising an interleukin 2 inhibitor and an antimicrobial agent as active ingredients thereof, wherein said interleukin 2 inhibitor contains a tricyclo compound as shown by the general formula (I) or pharmaceutically acceptable salt thereof. The present invention further provides a method for treating inflammations and/or infections comprising topical administration of an effective amount of an interleukin 2 inhibitor and an antimicrobial agent to a subject in need of the treatment of inflammations and/or infections.

1 - 7 . (canceled)  
   
   
       8 . A method for treating inflammations and/or infections comprising topical administration of an effective amount of an interleukin 2 inhibitor and an effective amount of an antimicrobial agent to a subject in need of the treatment of inflammations and/or infections.  
   
   
       9 . (canceled)  
   
   
       10 . The method of  claim 8 , wherein said interleukin 2 inhibitor is a macrolide compound or cyclosporins.  
   
   
       11 . The method of  claim 10 , wherein said macrolide compound is a tricycle compound as shown by the following general formul;a (I) or pharmaceutically acceptable salt thereof:  
     
       
         
         
             
             
         
       
     
     wherein adjacent pairs of R 1  and R 3 , and R 4 , and R 5  and R 6  each independently 
 a) are two adjacent hydrogen atoms, wherein R 2 is optionally alkyl, or  
 b) form another bond optionally between carbon atoms binding with the members of said pairs;  
 R 7  is hydrogen atom, hydroxy, alkyloxy or protected hydroxyl, or may form oxo with R 1 ;  
 R 8  and R 9  each independently are hydrogen atom or hydroxy;  
 R 10  is hydrogen atom, alkyl, alkenyl, alkyl substituted by one or more hydroxy, alkenyl substituted by one or more hydroxy or alkyl substituted by oxo;  
 X is oxo, (hydrogen atom, hydroxy), (Hydrogen atom, Hydrogen atom), or a group of the formula —CH 2 O—;  
 Y is oxo, (hydrogen atom, hydroxy), (hydrogen atom, hydrogen atom), or a group of the formula N—NR 11 R 12  or N—OR 13 ;  
 R 11  and R 12  each independently are hydrogen atom, alkyl, aryl or tosyl;  
 R 13  R 14 , R 15 , R 16 , R 17 , R 18 , R 19 , R 22  and R 23  each independently are hydrogen atom or alkyl;  
 R 24  is an optionally substituted ring that may contain one or more heteroatom(s); and  
 n is 1 or 2;  
 wherein  
 Y, R 10  and R 23  may be, together with the carbon atom they bind with, a saturated or unsaturated 5 or 6-membered heterocyclic group containing nitrogen atom, sulfur atom and/or oxygen atom, wherein the heterocyclic group may be optionally substituted by one or more group(s) selected from the group consisting of alkyl, hydroxy, alkyloxy, benzyl, a group of the formula —CH 2 Se (C 6 H 5 ), and alkyl substituted by one or more hydroxy.  
 
   
   
       12 . The method of  claim 11 , wherein said tricycle compound is FK506.  
   
   
       13 . The method of any of claims  8  and  10  to  12 , wherein said antimicrobial agent is quinolone antimicrobial agent.  
   
   
       14 . The method of  claim 13 , wherein said quinolone antimicrobial agent is nalidixic acid, pipemidic acid, piromidic acid, norfloxacin, ofloxacin, levofloxacin, ciprofloxacin, lomefloxacin, tosufloxacin, fleroxacin, sparfloxacin, enrofloxacin and enoxacin or a mixture thereof.  
   
   
       15 . The method of  claim 14 , wherein said quinolone antimicrobial agent is ofloxacin.  
   
   
       16 . The method of  claim 8 , wherein said topical administration is skin administration.