Sulfonamide pharmaceutical composition

Abstract

A sulfonamide pharmaceutical composition. The present invention relates to a sulfonamide compound injectable preparation comprising a sulfonamide compound or a derivative thereof. The injectable preparation is prepared from the sulfonamide compound and a pharmaceutically acceptable carrier through certain preparation technologies. The sulfonamide compound injectable preparation involved in the present invention is stable and controllable in quality and effective.

1 . A sulfonamide pharmaceutical composition, prepared from the following raw materials: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Raw materials 
                   Percentage by weight 
                 
                     
                     
                 
                     
                   sulfonamide compound 
                   20%-40% 
                 
                     
                   PEG-400 
                   20%-40% 
                 
                     
                   1,2-propanediol 
                    5%-10% 
                 
                     
                   Sebacic acid 
                   2%-5% 
                 
                     
                   2-ethyl-1,3-hexanediol 
                   10%-20% 
                 
                     
                   Dimethyl sulfoxide 
                        0-10% 
                 
                     
                   Anhydrous ethanol 
                         0-10%. 
                 
                     
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         2 . The sulfonamide pharmaceutical composition of  claim 1 , wherein the sulfonamide compound is one, or a mixture of two or more, at any ratio, of the following: 
       
         
           
           
               
               
           
         
         wherein R═H, C 2 H 5 , or 
       
       
         
           
           
               
               
           
         
       
     
     
         3 . The sulfonamide pharmaceutical composition of  claim 1 , wherein the sulfonamide compound is: 
       
         
           
           
               
               
           
         
       
     
     
         4 . The sulfonamide pharmaceutical composition of  claim 1 , prepared from the following raw materials: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Raw materials 
                   Percentage by weight 
                 
                     
                     
                 
                     
                   p-Toluenesulfonamide 
                   20%-40% 
                 
                     
                   PEG-400 
                   20%-40% 
                 
                     
                   1,2-propanediol 
                    5%-10% 
                 
                     
                   Sebacic acid 
                   2%-5% 
                 
                     
                   2-ethyl-1,3-hexanediol 
                   10%-20% 
                 
                     
                   Dimethyl sulfoxide 
                        0-10% 
                 
                     
                   Anhydrous ethanol 
                         0-10%. 
                 
                     
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         5 . The sulfonamide pharmaceutical composition of  claim 1 , prepared from the following raw materials: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Raw materials 
                   Percentage by weight 
                 
                     
                     
                 
                     
                   p-Toluenesulfonamide 
                   30%  
                 
                     
                   PEG-400 
                   30%  
                 
                     
                   1,2-propanediol 
                   8% 
                 
                     
                   Sabacic acid 
                   4% 
                 
                     
                   2-ethyl-1,3-hexanediol 
                   15%  
                 
                     
                   Dimethyl sulfoxide 
                   5% 
                 
                     
                   Anhydrous ethanol 
                    8%. 
                 
                     
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         6 . The sulfonamide pharmaceutical composition of  claim 1 , wherein said pharmaceutical composition is injectable. 
     
     
         7 . A method to prepare the sulfonamide pharmaceutical composition of  claim 1 , comprising the steps of:
 1) Putting a prescription amount of sulfonamide compound, PEG-400, and 2-ethyl-1,3-hexanediol into a container, stirring slowly at 85° C.-95° C. to form a miscible solution, Solution A, for later use;   2) Putting a prescription amount of sebacic acid and 1,2-propanediol, into a separate container, stirring slowly at 85° C.-95° C. to form a miscible solution, Solution B, for later use;   3) Mixing Solution A and Solution B while maintaining the temperature at 85° C.-95° C., and stirring to obtain a homogenous solution for later use;   4) Putting a prescription amount of dimethyl sulfoxide and a small amount of anhydrous ethanol into a container, stirring and mixing well to obtain a homogenous solution, Solution C, for later use;   5) Cooling the mixture of Solution A and Solution B to 60° C., adding Solution C to the mixture, stirring and mixing well before cooling down to room temperature, adding the remaining amount of anhydrous ethanol and mixing well;   6) Filtering with 0.45 um microporous membrane, aliquoting into 5 ml ampoules and sealing the ampoules; and   7) Sterilizing at 121° C. for 30 minutes.   
     
     
         8 . A method to prepare the sulfonamide pharmaceutical composition of  claim 1  from the following raw materials, comprising the steps of: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Raw materials 
                   Percentage by weight 
                 
                     
                     
                 
                     
                   p-Toluenesulfonamide 
                   30%  
                 
                     
                   PEG-400 
                   30%  
                 
                     
                   1,2-propanediol 
                   8% 
                 
                     
                   Sebacic acid 
                   4% 
                 
                     
                   2-ethyl-1,3-hexanediol 
                   15%  
                 
                     
                   Dimethyl sulfoxide 
                   5% 
                 
                     
                   Anhydrous ethanol 
                   8% 
                 
                     
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
               
            
           
         
         1) Putting a prescription amount of sulfonamide compound, PEG-400, and 2-ethyl-1,3-hexanediol into a container, stirring slowly at 85° C.-95° C. to form a miscible solution, Solution A, for later use; 
         2) Putting a prescription amount of sebacic acid and 1,2-propanediol, into a separate container, stirring slowly at 85° C.-95° C. to form a miscible solution, Solution B, for later use; 
         3) Mixing Solution A and Solution B while maintaining the temperature at 85° C.-95° C., and stirring well to obtain a homogenous solution for later use; 
         4) Putting a prescription amount of dimethyl sulfoxide and a small amount of anhydrous ethanol into a container, stirring and mixing well to obtain a homogenous solution, Solution C, for later use; 
         5) Cooling the mixture of Solution A and Solution B to 60° C., adding Solution C to the mixture, stirring and mixing well before cooling down to room temperature, adding the remaining amount of anhydrous ethanol and mixing well; 
         6) Filtering with 0.45 um microporous membrane, aliquoting into 5 ml ampoules and sealing the ampoules; and 
         7) Sterilizing at 121° C. for 30 minutes. 
       
     
     
         9 - 10 . (canceled) 
     
     
         11 . A method to treat cancer in a subject, comprising administering the sulfonamide pharmaceutical composition of  claim 1  to said subject. 
     
     
         12 . The method of  claim 11 , wherein the cancer is central type lung cancer.