Lyophilized mesna compositions

Abstract

The invention provides a sterile lyophilizate composition having improved stability and shelf-life, the lyophilizate comprising from 30 to 100% of Mesna and 0 to 70% of an excipient. The invention further provides a process for the preparation of said sterile lyophilizate composition and a dosage unit formulation comprising said lyophilizate composition.

What is claimed is: 
     
         1 . A lyophilizate composition having improved stability and shelf-life, the lyophilizate comprising at least from 30 to 100% of Mesna and optionally an excipient. 
     
     
         2 . The lyophilizate composition according to  claim 1 , wherein the composition comprises an excipient and wherein the concentration of the excipient in the composition is 0 to 70%. 
     
     
         3 . The lyophilizate composition according to  claim 2 , wherein the excipient is selected from the group consisting of mannitol, trehalose, sucrose and any combination thereof. 
     
     
         4 . The lyophilizate composition according to  claim 1 , wherein said lyophilizate is sterile. 
     
     
         5 . A method for the preparation of a lyophilizate composition having improved stability and shelf-life, which comprises
 freezing an aqueous solution comprising from 30 to 100% of Mesna and 0 to 70% of an excipient, to a temperature of about −40° C. and   removing both nonadsorptively bound and adsorptively bound water by sublimation at a temperature between about −40° C. and about +28° C. and at a pressure between 200 and 10 Pa.   
     
     
         6 . The method according to  claim 5  further comprising the step of sterilizing said aqueous solution prior to freezing. 
     
     
         7 . The method according to  claim 6  wherein said sterilization is performed by ultrafiltration. 
     
     
         8 . The method according to  claim 5 , wherein the excipient is selected from the group consisting of mannitol, trehalose, sucrose and any combination thereof. 
     
     
         9 . A dosage unit formulation comprising the lyophilizate composition of  claim 1  in a container for reconstitution with a solvent thereby giving a solution of desired Mesna concentration. 
     
     
         10 . The dosage unit formulation according to  claim 9 , wherein the lyophilizate composition comprises from 300 mg to 100 g of Mesna. 
     
     
         11 . The dosage unit formulation according to  claim 9 , wherein the lyophilizate composition comprises from 3 g to 50 g of Mesna. 
     
     
         12 . The dosage unit formulation according to  claim 9 , wherein said container is made of plastic or glass. 
     
     
         13 . A method of performing surgery comprising administering the lyophilizate composition according to  claim 1  at a cleavage plane. 
     
     
         14 . A method of performing surgery comprising administering the dosage unit formulation according to  claim 9  at a cleavage plane. 
     
     
         15 . The method according to  claim 5 , wherein the pressure is between about 100 and 10 Pa. 
     
     
         16 . The method according to  claim 5 , wherein the pressure is between about 93 and 13 Pa. 
     
     
         17 . A method of treating a patient comprising administering the lyophilizate composition according to  claim 1  to the patient in need thereof. 
     
     
         18 . A method of treating a patient comprising administering the dosage unit formulation according to  claim 9  to the patient in need thereof.