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Claims for Patent: 8,309,060

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Claims for Patent: 8,309,060

Title:Abuse-proofed dosage form
Abstract: An abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.
Inventor(s): Bartholomaus; Johannes (Aachen, DE), Kugelmann; Heinrich (Aachen, DE), Arkenau-Mari ; Elisabeth (Koln, DE)
Assignee: Grunenthal GmbH (Aachen, DE)
Application Number:13/346,257
Patent Claims: 1. An abuse-proofed, thermoformed dosage form comprising one or more active ingredients with abuse potential (A) optionally together with physiologically acceptable auxiliary substances (B), at least one synthetic or natural polymer (C), wherein the polymer (C) has a molecular weight of at least 0.5 million according to rheological measurements, and optionally at least one wax (D), wherein the dosage form exhibits a breaking strength of at least 500 N.

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

3. A dosage form according to claim 1, which is in multiparticulate form.

4. A dosage form according to claim 1, wherein the polymer (C) is at least one polymer selected from the group consisting of polyethylene oxide, polymethylene oxide, polypropylene oxide, polyethylene, polypropylene, polyvinyl chloride, polycarbonate, polystyrene, polyacrylate, copolymers and the mixtures thereof.

5. A dosage form according to claim 1, wherein the molecular weight is 1-15 million.

6. A 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.

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

8. A dosage form according to claim 1, wherein the active ingredient (A) is at least one active ingredient selected from the group consisting of opiates, opioids, tranquillisers, stimulants, barbiturates and further narcotics.

9. A dosage form according to claim 1, which additionally comprises at least one of the following components a)-f): (a) at least one substance which irritates the nasal passages and/or pharynx, (b) at least one viscosity-increasing agent, which, with the assistance of a necessary minimum quantity of an aqueous liquid, 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, c) at least one antagonist for the active ingredient or active ingredients with abuse potential, (d) at least one emetic, (e) at least one dye as an aversive agent, (f) at least one bitter substance.

10. A dosage form according to claim 9, wherein the component (a) irritant substance causes burning, itching, an urge to sneeze, increased formation of secretions or a combination of at least two of these stimuli.

11. A dosage form according to claim 10, wherein the component (a) irritant substance is based on one or more constituents of at least one hot substance drug.

12. A dosage form according to claim 11, wherein the hot substance drug is at least one drug selected from the group consisting of Allii sativi bulbus (garlic), Asari rhizoma cum herba (Asarum root and leaves), Calami rhizoma (calamus root), Capsici fructus (capsicum), Capsici fructus acer (cayenne pepper), Curcumae longae rhizoma (turmeric root), Curcumae xanthorrhizae rhizoma (Javanese turmeric root), Galangae rhizoma (galangal root), Myristicae semen (nutmeg), Piperis nigri fructus (pepper), Sinapis albae semen (erucae/white mustard seed), Sinapis nigri semen (black mustard seed), Zedoariae rhizoma (zedoary root) and Zingiberis rhizoma (ginger root).

13. A dosage form according to claim 11, wherein the constituent of the hot substance drug is an o-methoxy(methyl)phenol compound, an acid amide compound, a mustard oil or a sulfide compound or is derived from such a compound.

14. A dosage form according to claim 11, wherein the constituent of the hot substance drug is at least one constituent selected from the group consisting of myristicin, elemicin, isoeugenol, .beta.-asarone, safrole, gingerols, xanthorrhizol, capsaicinoids, piperine, glucosinolates, and a compound derived from these constituents.

15. A dosage form according to claim 9, wherein component (b) is at least one viscosity-increasing agent selected from the group consisting of microcrystalline cellulose with 11 wt. % carboxymethylcellulose sodium (Avicel.RTM. RC 591), carboxymethylcellulose sodium (Blanose.RTM., CMC-Na C300P.RTM., Frimulsion BLC-5.RTM., Tylose C300 P.RTM.), polyacrylic acid (Carbopol.RTM. 980 NF, Carbopol.RTM. 981), locust bean flour (Cesagum.RTM. LA-200, Cesagum.RTM. LID/150, Cesagum.RTM. LN-1), citrus pectin (Cesapectin.RTM. HM Medium Rapid Set), waxy maize starch (C*Gel 042010.RTM.), sodium alginate (Frimulsion ALG (E401).RTM.), guar flour (Frimulsion BM.RTM., Polygum 26/1-75.RTM.), iota carrageen (Frimulsion D021.RTM.), karaya gum, gellan gum (Kelcogel F.RTM., Kelcogel LT100.RTM.), galactomannan (Meyprogat 150 .RTM.), tara bean flour (Polygum 43/1.RTM.), propylene glycol alginate (Protanal-Ester SD-LB.RTM.), sodium hyaluronate, apple pectin, pectin from lemon peel, sodium hyaluronate, tragacanth, tara gum (Vidogum SP 200.RTM.), fermented polysaccharide welan gum (K1A96) and xanthan gum (Xantural 180.RTM.).

16. A dosage form according to claim 9, wherein component (c) is at least one opiate or opioid antagonist selected from the group consisting of naloxone, naltrexone, nalmefene, nalid, nalmexone, nalorphine, naluphine and a corresponding physiologically acceptable compound.

17. A dosage form according to claim 9, wherein component (c) is at least one neuroleptic stimulant antagonist.

18. A dosage form according to claim 9, wherein component (d) emetic is based on one or more constituents of radix ipecacuanha (ipecac root) and/or is apomorphine.

19. A dosage form according to claim 9, wherein component (e) is at least one physiologically acceptable dye.

20. A dosage form according to claim 9, wherein component (f) is at least one bitter substance selected from the group consisting of aromatic oils, fruit aroma substances, denatonium benzoate and mixtures thereof.

21. A dosage form according to claim 9, wherein the active ingredient or active ingredients (A) is/are spatially separated from component (c) and/or (d) and/or (f), wherein the active ingredient or active ingredients (A) is/are optionally present in at least one subunit (X) and components (c) and/or (d) and/or (f) is/are present in at least one subunit (Y), and, when the dosage form is correctly administered, components (c) and/or (d) and/or (f) from subunit (Y) do not exert their effect in the body and/or on taking.

22. A dosage form according to claim 1, which comprises at least one active ingredient at least partially in controlled release form.

23. A dosage form according to claim 22, wherein each of the active ingredients with abuse potential (A) is present in a controlled release matrix.

24. A dosage form according to claim 23, wherein component (C) and/or component (D) also serve as a controlled release matrix material.

25. A process for the production of a dosage form according to claim 1, comprising: mixing components (A), (B), (C) and the optionally present component (D) and the optionally present components (a) to (f) to form a resultant mixture, and press-forming the resultant mixture, optionally after granulation, to yield the dosage form with preceding, simultaneous, or subsequent exposure to heat.

26. A process according to claim 25, wherein granulation is performed by means of a melt process.

27. A dosage form obtainable by a process according to claim 25.

28. A method of treating a therapeutic condition in a patient suffering therefrom, said method comprising administering to said patient a dosage form according to claim 1.

29. The method according to claim 28, wherein the therapeutic condition is pain.

30. A dosage form according to claim 1, wherein the polymer (C) is polyethylene oxide having a molecular weight of from 1-15 million g/mol.

31. A dosage form according to claim 1, wherein the one or more active ingredients with abuse potential (A) is/are selected from the group consisting of oxymorphone, oxycodone, tapentadol and the physiologically acceptable salts thereof.

32. A dosage form according to claim 31, which is in the form of a tablet.

33. A dosage form according to claim 1, wherein the content of polymer (C) is at least 30% by weight relative to the total weight of the dosage form.

34. A dosage form according to claim 1, which is in the form of a tablet, wherein the one or more active ingredients with abuse potential (A) is/are selected from the group consisting of oxymorphone, oxycodone, tapentadol and the physiologically acceptable salts thereof; wherein the polymer (C) is polyethylene oxide having a molecular weight of from 1-15 million g/mol; and wherein the content of polymer (C) is at least 30% by weight relative to the total weight of the dosage form.
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