Method for the production of a medicament containing tadalafil
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. A method for production of a pharmaceutical containing tadalafil, wherein tadalafil is mixed with a copolymer excipient comprising vinylpyrrolidone-vinyl acetate copolymer and is heated by melt extrusion in an extruder to a temperature from approximately 100° C. to approximately 200° C., wherein tadalafil is distributed, without agglomerates, in the copolymer excipient as a molecular dispersion, wherein the pharmaceutical containing tadalafil is a solid or semi-solid solution, wherein 80% of the tadalafil is released in vitro within 8-10 minutes.
2. The method as claimed in claim 1 , wherein the vinylpyrrolidone-vinyl acetate copolymer has a molecular weight of approximately 60000.
3. The method as claimed in claim 1 , wherein the proportion of tadalafil is approximately 2 wt. % to approximately 15 wt. % in the pharmaceutical.
4. The method as claimed in claim 2 , wherein the temperature is from approximately 150° C. to approximately 200° C.
5. The method as claimed in claim 4 , wherein the temperature is approximately 200° C.
6. A method for production of a pharmaceutical containing tadalafil, wherein tadalafil is mixed with a copolymer excipient comprising vinylpyrrolidone-vinyl acetate copolymer and is heated by melt extrusion in an extruder to a temperature from approximately 100° C. to approximately 200° C., wherein tadalafil is distributed, without agglomerates, in the copolymer excipient as a molecular dispersion, wherein the pharmaceutical containing tadalafil is a solid or semi-solid solution, wherein 80% of the tadalafil is released in vitro within 8-10 minutes, wherein the proportion of the molecularly dispersed tadalafil which is present in soluble form is approximately 2 wt. % to approximately 15 wt. %.
7. The method as claimed in claim 6 , wherein the proportion of the molecularly dispersed tadalafil which is present in soluble form is approximately 7.5 wt % to approximately 10 wt. %.
8. The method as claimed in claim 6 , wherein the proportion of the molecularly dispersed tadalafil which is present in soluble form is approximately 5 wt % to 10 wt. %.