Details for Patent: 8,114,384
✉ Email this page to a colleague
| Title: | Process for the production of an abuse-proofed solid dosage form |
| Abstract: | 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. |
| Inventor(s): | Arkenau; Elisabeth (Aachen, DE), Bartholom us; Johannes (Aachen, DE) |
| Assignee: | Gruenenthal GmbH (Aachen, DE) |
| Filing Date: | Jul 14, 2004 |
| Application Number: | 10/890,704 |
| Claims: | 1. A process for the production of an abuse-proofed solid dosage form with a breaking strength of at least 500N, said dosage form comprising at least one opioid active ingredient with potential for abuse and 50-99.9 wt%, relative to the total weight of the dosage form, of polyethylene oxide having a molecular weight of at least one million Daltons, said process comprising heating a mixture comprising the at least one opioid active ingredient with potential for abuse and the polyethylene oxide in a planetary-gear extruder at least until the polyethylene oxide has softened, and thereafter compacting and extruding the mixture with the planetary-gear extruder into formed articles, which are optionally subjected to singulation and shaping to yield a nonmultiparticulate dosage form with a breaking strength of at least 500 N. 2. A process according to claim 1, wherein the active ingredient is selected from the group consisting of oxycodone, morphine, hydromorphone, tramadol and the physiologically acceptable salts thereof. 3. A process according to claim 1, wherein the mixture additionally comprises further auxiliary substances. 4. A process according to claim 1, wherein the planerary-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, wherein the formed articles are finally formed and optionally singulated. 7. A process according to claim 1, wherein the formed articles are formed into tablets. 8. A process according to claim 7, 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. 9. A process according to claim 7, wherein the tablets are in each case formed with the assistance of a die and at least one shaping punch. 10. An abuse-proofed dosage form with a breaking strength of at least 500N obtainable by a process according to claim 1. 11. A process according to claim 2, where the active ingredient is the hydrochloride of oxycodone, morphine, hydromorphine, or tramadol. 12. A process according to claim 3, where the further auxiliary substances are one or more substances selected from the group consisting of waxes (D), antioxidants and plasticizers. 13. A process according to claim 1, where the opioid is in a form selected from the group consisting of physiologically acceptable enantiomers, stereoisomers, diastereomers, racemates and derivatives thereof. 14. A process of claim 13, where the physiologically acceptable derivatives thereof are selected from the group consisting of ethers, esters and amides. |
