# US 10,369,109 B2 · Abuse-proofed dosage form > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,369,109 B2 - Document ID: US10369109B2 - Status: Granted - Kind: B2 - Application number: 16/032,533 - Filed: 2018-07-11 - Published: 2018-11-08 - Granted: 2019-08-06 - Earliest claimed: 2002-06-17 - Assignees: GrüNenthal GmbH - Applicants: GrüNenthal GmbH - Inventors: Johannes Bartholomaeus; Heinrich Kugelmann - Web page: https://patentgrep.com/patent/US10369109B2 ## CPC - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/2009: {Inorganic compounds} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin} - A61K 9/4866: {Organic macromolecular compounds} - A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} - A61K 31/485: Morphinan derivatives, e.g. morphine, codeine - A61K 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine} - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/38: Cellulose; Derivatives thereof - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/26: Psychostimulants, e.g. nicotine, cocaine - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid. ## Claims ### Claim 1 A tablet for oral administration with reduced potential for parenteral abuse, said tablet comprising: (a) one or more active ingredients having potential for abuse selected from the group consisting of hydrocodone, morphine, oxycodone, tramadol, and pharmaceutically acceptable salts and solvates thereof; and (b) at least one viscosity-increasing agent in a quantity such that an aqueous extract of a total content of the tablet when comminuted and combined with 10 ml of water at 25° C. forms a gel that can be drawn up into and injected back out of a hypodermic needle having a diameter of 0.9 mm, into a further quantity of water, wherein threads of the gel injected from said needle remain visible to the naked eye in said further quantity of water at 37° C. ### Claim 2 (depends on 1) The tablet according to claim 1, wherein the active ingredient is oxycodone or a salt or solvate thereof. ### Claim 3 (depends on 1) The tablet according to claim 1, wherein the active ingredient is hydrocodone or a salt or solvate thereof. ### Claim 4 (depends on 1) The tablet according to claim 1, wherein the active ingredient is morphine or a salt or solvate thereof. ### Claim 5 (depends on 1) The tablet according to claim 1, wherein the one or more viscosity-increasing agents are selected from the group consisting of microcrystalline cellulose with 11 wt. % carboxymethylcellulose sodium, carboxymethylcellulose sodium, polyacrylic acid, locust bean flour, citrus pectin, waxy maize starch, sodium alginate, guar flour, iota-carrageenan, karaya gum, gellan gum, galactomannan, tara stone flour, propylene glycol alginate, apple pectin, lemon peel pectin, sodium hyaluronate, tragacanth, tara gum, fermented polysaccharide welan gum and xanthan gum. ### Claim 6 (depends on 1) The tablet according to claim 1, comprising at least one active ingredient in controlled release form. ### Claim 7 (depends on 1) The tablet according to claim 1, comprising a coating resistant to gastric juices. ### Claim 8 (depends on 1) The tablet according to claim 1, in multiparticulate form, wherein said multiparticulate form is in the form of microtablets, microcapsules, micropellets, granules, spheroids, beads or pellets, packaged in capsules or press-molded into tablets. ### Claim 9 (depends on 1) The tablet according to claim 1, wherein said threads remain visible to the naked eye in said further quantity of water for at least one minute. ### Claim 10 (depends on 1) The tablet according to claim 1, wherein said threads remain visible to the naked eye in said further quantity of water for at least ten minutes. ### Claim 11 (depends on 1) The tablet according to claim 1, which further comprises microcrystalline cellulose. ### Claim 12 (depends on 1) The tablet according to claim 1, which further comprises hydroxypropylmethylcellulose. ### Claim 13 A solid dosage form for oral administration with reduced potential for parenteral abuse, said dosage form comprising: (a) one or more active ingredients having potential for abuse selected from the group consisting of hydrocodone, morphine, oxycodone, tramadol, and pharmaceutically acceptable salts and solvates thereof; and (b) one or more viscosity-increasing components, in a total quantity, for all said components combined, that is equal to or greater than 5 mg per dosage form, that quantity being selected such that an aqueous extract of a total content of the dosage form, when comminuted and combined with 10 ml of water at 25° C., forms a gel that is capable of being drawn into and then expelled from a hypodermic needle having a diameter of 0.9 mm, wherein threads of said gel, formed upon exit from said needle into a further quantity of water at 37° C., remain visible to the naked eye. ### Claim 14 (depends on 13) The dosage form according to claim 13, wherein the active ingredient is oxycodone or a salt or solvate thereof. ### Claim 15 (depends on 13) The dosage form according to claim 13, wherein the active ingredient is hydrocodone or a salt or solvate thereof. ### Claim 16 (depends on 13) The dosage form according to claim 13, wherein the active ingredient is morphine or a salt or solvate thereof. ### Claim 17 (depends on 13) The dosage form according to claim 13, wherein said threads remain visible to the naked eye in said further quantity of water for at least one minute. ### Claim 18 (depends on 13) The dosage form according to claim 13, wherein said threads remain visible to the naked eye in said further quantity of water for at least ten minutes. ### Claim 19 (depends on 13) The dosage form according to claim 13, comprising at least one active ingredient in controlled release form. ### Claim 20 (depends on 13) The dosage form according to claim 13, which further comprises microcrystalline cellulose. ### Claim 21 (depends on 13) The dosage form according to claim 13, which further comprises hydroxypropylmethylcellulose. ### Claim 22 A tablet for oral administration with reduced potential for parenteral abuse, said tablet comprising: (a) one or more active ingredients with potential for abuse selected from the group consisting of hydrocodone, morphine, oxycodone, tramadol and pharmaceutically acceptable salts and/or solvates thereof; and (b) one or more viscosity-increasing agents; wherein the tablet when its total content is comminuted and combined with 10 ml of water at 25° C. forms an injectable gel that can be drawn up into and injected back out of a syringe having a diameter of 0.9 mm, but wherein the injectable gel cannot be safely injected from said syringe into a blood vessel of an abuser because the presence of the injectable gel in the abuser's blood vessels would obstruct one or more of said abuser's blood vessels. ### Claim 23 (depends on 22) The tablet according to claim 22, wherein the active ingredient is oxycodone or a salt or solvate thereof. ### Claim 24 (depends on 22) The tablet according to claim 22, wherein the active ingredient is hydrocodone or a salt or solvate thereof. ### Claim 25 (depends on 22) The tablet according to claim 22, wherein the active ingredient is morphine or a salt or solvate thereof. ### Claim 26 (depends on 22) The tablet according to claim 22, which further comprises microcrystalline cellulose. ### Claim 27 (depends on 22) The tablet according to claim 22, which further comprises hydroxypropylmethylcellulose. ### Claim 28 (depends on 22) The tablet according to claim 22, comprising at least one active ingredient in controlled release form.