Method for the production of a medicament containing tadalafil

Abstract

The invention relates to a method for producing a medicament containing tadalafil. In said method, tadalafil is mixed with suitable adjuvants and is heated to a temperature of about 100° C. to about 200° C., preferably about 150° C. to about 200° C., especially about 200° C.

1 - 11 . (canceled) 
     
     
         12 . A pharmaceutical containing a solid or semi-solid solution of tadalafil, characterized in that it can be produced by a method for the production of a pharmaceutical containing tadalafil, characterized in that tadalafil is mixed with one or more suitable excipients and is heated to a temperature from approx. 100° C. to approx. 200° C., preferably from approx. 150° C. to approx. 200° C., and in particular approx. 200° C. 
     
     
         13 . The pharmaceutical as claimed in  claim 12 , characterized in that the excipient or excipients are selected from polyethylene glycol (PEG), copovidone, a polyoxyethylene glycol monostearate, glycerol-polyethylene glycol-ricinoleate, polyvinyl-pyrrolidone and/or vinylpyrrolidone-vinyl acetate copolymer. 
     
     
         14 . The pharmaceutical as claimed in  claim 13 , characterized in that the PEG is selected from PEG 200, PEG 400, PEG 600, PEG 800, PEG 1500, PEG 4000, PEG 6000, PEG 8000, PEG 10000 and/or PEG 20000, in particular from PEG 400, PEG 4000, PEG 6000 and/or PEG 20000 and quite especially from PEG 400 and/or PEG 4000. 
     
     
         15 . The pharmaceutical as claimed in  claim 13 , characterized in that the polyvinylpyrrolidone has a molecular weight of approx. 40000 and the vinylpyrrolidone-vinyl acetate copolymer has a molecular weight of approx. 60000. 
     
     
         16 . The pharmaceutical as claimed in  claim 12 , characterized in that the heating takes place in an extruder or homogenizer. 
     
     
         17 . The pharmaceutical as claimed in  claim 16 , characterized in that polyvinylpyrrolidone and/or vinylpyrrolidone-vinyl acetate copolymer, in particular polyvinylpyrrolidone with a molecular weight of approx. 40000 and/or vinylpyrrolidone-vinyl acetate copolymer with a molecular weight of approx. 60000 is used as excipient during extrusion. 
     
     
         18 . The pharmaceutical as claimed in  claim 12 , characterized in that the proportion of tadalafil is approx. 2 wt. % to approx. 15 wt. %, preferably approx. 3 wt. % to approx. 10 wt. %, in particular approx. 5 wt. % to approx. 10 wt. %, and quite especially approx. 7.5 wt. % to approx. 10 wt. % in the pharmaceutical. 
     
     
         19 . The pharmaceutical as claimed in  claim 12 , characterized in that the pharmaceutical is in the form of a tablet or a capsule, preferably a hard capsule. 
     
     
         20 . A pharmaceutical containing a solid or semi-solid solution of tadalafil, characterized in that 80% of the tadalafil is released in vitro after 8-120 minutes, preferably after 20 minutes. 
     
     
         21 . The pharmaceutical as claimed in  claim 21 , characterized in that it can be produced by a method for the production of a pharmaceutical containing tadalafil, characterized in that tadalafil is mixed with one or more suitable excipients and is heated to a temperature from approx. 100° C. to approx. 200° C., preferably from approx. 150° C. to approx. 200° C., and in particular approx. 200° C. 
     
     
         22 . The pharmaceutical as claimed in  claim 21 , characterized in that the excipient or excipients are selected from polyethylene glycol (PEG), copovidone, a polyoxyethylene glycol monostearate, glycerol-polyethylene glycol-ricinoleate, polyvinyl-pyrrolidone and/or vinylpyrrolidone-vinyl acetate copolymer. 
     
     
         23 . The pharmaceutical as claimed in  claim 22 , characterized in that the PEG is selected from PEG 200, PEG 400, PEG 600, PEG 800, PEG 1500, PEG 4000, PEG 6000, PEG 8000, PEG 10000 and/or PEG 20000, in particular from PEG 400, PEG 4000, PEG 6000 and/or PEG 20000 and quite especially from PEG 400 and/or PEG 4000. 
     
     
         24 . The pharmaceutical as claimed in  claim 22 , characterized in that the polyvinylpyrrolidone has a molecular weight of approx. 40000 and the vinylpyrrolidone-vinyl acetate copolymer has a molecular weight of approx. 60000. 
     
     
         25 . The pharmaceutical as claimed in  claim 21 , characterized in that the heating takes place in an extruder or homogenizer. 
     
     
         26 . The pharmaceutical as claimed in  claim 25 , characterized in that polyvinylpyrrolidone and/or vinylpyrrolidone-vinyl acetate copolymer, in particular polyvinylpyrrolidone with a molecular weight of approx. 40000 and/or vinylpyrrolidone-vinyl acetate copolymer with a molecular weight of approx. 60000 is used as excipient during extrusion. 
     
     
         27 . The pharmaceutical as claimed in  claim 21 , characterized in that the proportion of tadalafil is approx. 2 wt. % to approx. 15 wt. %, preferably approx. 3 wt. % to approx. 10 wt. %, in particular approx. 5 wt. % to approx. 10 wt. %, and quite especially approx. 7.5 wt. % to approx. 10 wt. % in the pharmaceutical.