Glutathione derivatives and their dosage forms

Abstract

A glutathione derivative having a dramatically enhanced hematopoiesis promoting effect in the living body, said derivative being represented by the formula (I): wherein, A represents H or a C1-C20 acyl group, R 1 represents a C1-C26 alkyl group or a C3-C26 alkenyl group, and R 2 represents H, a C1-C26 alkyl group, or a C3-C26 alkenyl group, provided that cases in which R 1 represents a C1-C10 alkyl group or a C3-C10 alkenyl group and R 2 represents H, a C1-C10 alkyl group, or a C3-C10 alkenyl group are excluded, a salt of said glutathione derivative, or a colloidal composition that enables the safe and effective development of the effects of said glutathione derivative in the living body.

1 . A glutathione derivative represented by the formula (I):  
       
         
           
           
               
               
           
         
       
       wherein, A represents H or a C1-C20 acyl group; R 1  represents a C1-C26 alkyl group or a C3-C26 alkenyl group, and R 2  represents H, a C1-C26 alkyl group or a C3-C26 alkenyl group, provided that the case in which R 1  represents a C1-C10 alkyl group or a C3-C10 alkenyl group and R 2  represents H, a C1-C10 alkyl group or a C3-C10 alkenyl group are excluded, or a salt thereof.  
     
     
         2 . The glutathione derivative according to  claim 1  wherein R 1  represents a C1-C22 alkyl group or a C10-C22 alkenyl group, or a salt thereof.  
     
     
         3 . The glutathione derivative according to  claim 1  wherein R 1  represents an ethyl group, a C10-C22 alkyl group or a C16-C20 alkenyl group, or a salt thereof.  
     
     
         4 . The glutathione derivative according to any of claims  1 - 3  wherein R 2  represents H, a C1-C22 alkyl group or a C3-C22 alkenyl group, or a salt thereof.  
     
     
         5 . The glutathione derivative according to any of claims  1 - 3  wherein R 2  represents H, an ethyl group or a C10-C18 alkyl group, or a salt thereof.  
     
     
         6 . The glutathione derivative according to any of claims  1 - 5  wherein A represents H or an acetyl group, or a salt thereof.  
     
     
         7 . The glutathione derivative according to  claim 1  or  6  wherein R 1  represents a C12-C22 alkyl group or a C18-C22 alkenyl group, and R 2  represents an ethyl group; or R 1  is an ethyl group, and R 2  is a C12-C18 alkyl group, or a salt thereof.  
     
     
         8 . A pharmaceutical composition comprising a glutathione derivative according to any of  claims 1  to  7  or a salt thereof.  
     
     
         9 . The pharmaceutical composition according to  claim 8  wherein said pharmaceutical composition is colloidal.  
     
     
         10 . The pharmaceutical composition according to  claim 8  wherein said pharmaceutical composition is at least a form selected from the group consisting of a fat emulsion, a liposome and a solid suspension.  
     
     
         11 . The pharmaceutical composition according to  claim 8  wherein said pharmaceutical composition is a fat emulsion.  
     
     
         12 . A hematopoiesis promoting agent comprising a glutathione derivative according to any of  claims 1  to  7  or a salt thereof.  
     
     
         13 . The hematopoiesis promoting agent according to  claim 12  wherein said hematopoiesis promoting agent is colloidal.  
     
     
         14 . The hematopoiesis promoting agent according to  claim 12  wherein said hematopoiesis promoting agent is at least a form selected from the group consisting of a fat emulsion, a liposome and a solid suspension.  
     
     
         15 . The pharmaceutical composition according to  claim 12  wherein said hematopoiesis promoting agent is a fat emulsion.  
     
     
         16 . A pharmaceutical composition having an enhanced retention in the blood comprising a substance that has a carboxyl group and an ability of inhibiting or binding glutathione S-transferase wherein the carboxyl group has been changed to a C12-C26 alkyl or alkenyl ester.  
     
     
         17 . The pharmaceutical composition according to  claim 16  wherein said pharmaceutical composition is colloidal.  
     
     
         18 . The pharmaceutical composition according to  claim 16  wherein said pharmaceutical composition is a fat emulsion.  
     
     
         19 . A hematopoiesis promoting agent comprising the pharmaceutical composition according to any of  claims 16  to  18 .