Process for the production of an abuse-proofed solid dosage form
View Patent ↗The present invention relates to a process for the production of an abuse-proofed solid dosage form containing at least one active ingredient with potential for abuse and a synthetic or natural polymer with a breaking strength of =500 N, characterized in that a corresponding mixture is processed by melt extrusion with the assistance of a planetary-gear extruder.
1. A process for the production of an abuse-proofed solid dosage form comprising (i) at least one active ingredient with potential for abuse and (ii) polyalkylene oxide (C), said at least one active ingredient with potential for abuse being selected from the group consisting of oxymorphone and the esters, ethers, amides, salts and solvates thereof, said polyalkylene oxide (C) being present at a molecular weight of from 1 million to 15 million and in an amount of at least 35% by weight, based on the weight of the dosage form, wherein said dosage form has a breaking strength of at least 500 N, and said process comprises processing a mixture comprising the at least one active ingredient with potential for abuse and the polyalkylene oxide (C) by melt extrusion with the assistance of a planetary-gear extruder into formed articles, which formed articles are optionally subjected to singulation and shaping to yield the dosage form.
2. A process according to claim 1 , wherein the polyalkylene oxide (C) is at least one polymer selected from among the group consisting of polyethylene oxides and copolymers thereof with at least one polymer selected from the group consisting of polyethylenes, polypropylenes, polyvinyl chlorides, polycarbonates, polystyrenes, and polyacrylates.
3. A process according to claim 1 , wherein the mixture additionally comprises further auxiliary substances.
4. A process according to claim 1 , wherein the planetary-gear extruder has at least three planetary spindles.
5. A process according to claim 1 , wherein the planetary-gear extruder has a feed screw and a central spindle with planetary spindles.
6. A process according to claim 1 , which further comprises heating the mixture in the planetary-gear extruder at least until the polyalkylene oxide (C) has softened, and thereafter compacting and extruding the mixture.
7. A process according to claim 1 , wherein a plastic extrudate is finally formed as a result of said melt extrusion and optionally singulated.
8. A process according to claim 1 , wherein an extrudate is formed as a result of said melt extrusion and formed into tablets.
9. A process according to claim 8 , wherein the tablets are formed with press molding with the assistance of two counter-rotating rolls with mutually opposing recesses, the construction of which recesses determines the tablet shape.
10. A process according to claim 8 , wherein the tablets are in each case formed with the assistance of a die and at least one shaping punch.
11. A process according to claim 1 , wherein the extrudate is singulated into a multiparticulate form, and optionally formed and optionally press-molded into tablets or packaged in capsules.
12. An abuse-proofed dosage form obtainable by a process according to claim 1 .
13. A method of treating pain comprising administering to a patient in need thereof an effective amount to treat pain of at least one active ingredient with potential for abuse selected from the group consisting of oxymorphone and physiologically acceptable compounds and derivatives thereof, wherein said at least one active ingredient with potential for abuse is administered to said patient in the form of a dosage form according to claim 12 .