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Claims for Patent: 8,192,722

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Claims for Patent: 8,192,722

Title:Abuse-proof dosage form
Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.
Inventor(s): Arkenau-Maric; Elisabeth (Koln, DE), Bartholomaus; Johannes (Aachen, DE), Kugelmann; Heinrich (Aachen, DE)
Assignee: Grunenthal GmbH (Aachen, DE)
Application Number:12/140,665
Patent Claims: 1. An abuse-proofed dosage form thermoformed by extrusion without discoloration comprising one or more active ingredients with abuse potential (A), optionally physiologically acceptable auxiliary substances (B), at least one synthetic or natural polymer (C) and optionally at least one wax (D), wherein the dosage form exhibits a breaking strength of at least 500 N, the one or more active ingredients with abuse potential (A) are selected from the group consisting of oxymorphone and physiologically acceptable compounds and derivatives thereof, and the polymer (C) comprises polyethylene oxide having a molecular weight of at least 0.5 million g/mol.

2. The dosage form according to claim 1, which is in the form of a tablet.

3. The dosage form according to claim 1, wherein the molecular weight of the polyethylene oxide (C) is at least 1 million g/mol.

4. The dosage form according to claim 3, wherein the molecular weight of the polyethylene oxide is in the range of from about 1 to about 15 million g/mol.

5. The dosage form according to claim 1, which comprises the wax (D), and the wax (D) is at least one natural, semi-synthetic or synthetic wax with a softening point of at least 60.degree. C.

6. The dosage form according to claim 5, wherein the wax (D) is carnauba wax or beeswax.

7. The dosage form according to claim 1, which additionally comprises: (a) at least one substance which irritates the nasal passages and/or pharynx; and/or (b) at least one viscosity-increasing agent, which in the presence of an active ingredient extracted from the dosage form using a liquid medium, forms a gel with the extract obtained from the dosage form, which gel optionally remains visually distinguishable when introduced into a further quantity of an aqueous liquid; and/or (c) at least one antagonist for the active ingredient or active ingredients with abuse potential; and/or (d) at least one emetic; and/or (e) at least one dye; and/or (f) at least one bitter substance.

8. The dosage form according to claim 7, wherein component (b) is at least one viscosity-increasing agent selected from the group consisting of microcrystalline cellulose combined with carboxymethylcellulose sodium, polyacrylic acid, locust bean flour, pectins, waxy maize starch, sodium alginate, guar flour, iota carrageenan, karaya gum, gellan gum, galactomannan, tara bean flour, propylene glycol alginate, apple pectin, sodium hyaluronate, tragacanth, tara gum, fermented polysaccharide welan gum, and xanthan gum.

9. The dosage form according to claim 1, which comprises at least one active ingredient with abuse potential (A) at least partially in controlled release form.

10. The dosage form according to claim 9, wherein each of the active ingredients with abuse potential (A) is present in a controlled release matrix.

11. The dosage form according to claim 10, wherein the controlled release matrix material comprises component (C) and/or the optionally present component (D).

12. The dosage form according to claim 1, which comprises a core and a tubular domain surrounding the core, wherein said tubular domain has a morphology different from that of the core.

13. The dosage form according to claim 12, wherein the core and the tubular domain have substantially the same chemical composition.

14. The dosage form according to claim 12, wherein the tubular domain does not completely cover the core.

15. The dosage form according to claim 1, which comprises a physiologically acceptable auxiliary substance (B), and the physiologically acceptable auxiliary substance (B) is an antioxidant.

16. The dosage form according to claim 15, wherein the antioxidant is selected from the group consisting of ascorbic acid, salts of ascorbic acid, butylhydroxyanisole, butylhydroxytoluene, monothioglycerol, phosphorous acid, vitamin C, vitamin E and the derivatives thereof, sodium bisulfite and .alpha.-tocopherol.

17. A process for the production of a dosage form according to claim 1, comprising: I) mixing components (A), the optionally present component (B), (C) and the optionally present component (D); II) heating the resultant mixture in the extruder at least up to the softening point of component (C) and extruding the mixture as extrudate through the outlet orifice of the extruder by application of force; and III) singulating and forming the still plastic extrudate into the dosage form; or IV) cooling and forming the optionally reheated singulated extrudate into the dosage form.

18. The process according to claim 17, wherein process step II) is performed by means of a twin-screw-extruder.

19. The process according to claim 17, wherein process steps II) and III) and optionally process steps I) and IV) are performed under an inert gas atmosphere.

20. The process according to claim 19, wherein nitrogen is used as the inert gas atmosphere.

21. The process according to claim 17, wherein mixing of the components according to process step I) proceeds in the extruder under an inert gas atmosphere.

22. The process according to claim 17, wherein the mixture according to process step I) is extruded through a die with at least one bore.

23. The process according to claim 17, wherein the extrudate is singulated by cutting.

24. The process according to claim 17, wherein the extrudate is in the form of a strand and is shaped and singulated with the assistance of counter rotating calender rolls comprising opposing recesses in their outer sleeve.

25. The process according to claim 17, wherein the singulated extrudate is pelletized or pressed into tablets.

26. The process according to claim 17, wherein swelling and expansion of the dosage form upon storage is suppressed by press forming the singulated extrudate at a pressure of at least 1 kN and a temperature of between 25.degree. C. and 40.degree. C. below the melting range of the mixture of the components.

27. A dosage form according to claim 1, wherein the physiologically acceptable compounds and derivatives are salts, solvates, esters, ethers and amides.
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