# US 9,040,085 B2 · Delayed release tablet with defined core geometry > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,040,085 B2 - Document ID: US9040085B2 - Status: Granted - Kind: B2 - Application number: 14/329,631 - Filed: 2014-07-11 - Published: 2014-11-06 - Granted: 2015-05-26 - Earliest claimed: 2003-04-24 - Assignees: Jagotec AG - Applicants: Jagotec AG - Inventors: Guy Vergnault; Pascal Grenier; Christophe Dragan - Web page: https://patentgrep.com/patent/US9040085B2 ## CPC - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61J 1/03: for pills or tablets (containers for pills or tablets with special dispensing means therefor B65D83/04) - A61K 9/0002: {Galenical forms characterised by the drug release technique; Application systems commanded by energy} - A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} - A61K 9/2009: {Inorganic compounds} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2813: {Inorganic compounds} - A61K 9/282: {Organic compounds, e.g. fats} - A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone} - A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377) - A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 11/06: Antiasthmatics - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) - 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) - A61J: CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract A tablet comprising a core containing an active agent, and a coating, the core being disposed within the coating such that the coating has a thickness about a longitudinal axis (X-Y) of about 4.85 to 4.95 mm. The position of the core within the coating dictating that the active agent is released rapidly after a lag time during which time no active agent is released. ## Claims ### Claim 1 A method of administering a glucocorticosteroid active substance selected from prednisone, prednisolone, and methylprednisolone to a patient in need thereof comprising administering to the patient an oral dosage form comprising a defined core and a compression coating completely covering the core, wherein the core comprises the glucocorticosteroid active substance and further comprises at least one disintegrating agent that, upon exposure to aqueous media, provides a force to rupture the coating, wherein the compression coating comprises at least one excipient selected from fatty acids or their esters or salts; long chain fatty alcohols; polyoxyethylene alkyl ethers; polyoxyethylene stearates; sugar esters; lauroyl macrogol-32 glyceryl; and stearoyl macrogol-32 glyceryl, wherein the compression coating lacks ingredients that swell and gel to such an extent that the compression coating acts as a diffusion barrier to the release of the active substance, and further provided that the compression coating contains substantially no natural synthetic gum, and wherein the oral dosage form has an in vitro dissolution profile, as determined using purified water, with a volume of 500 mL in a USP dissolution apparatus No. 2 (paddles) with stationary baskets and a stirring rate of 100 rpm, such that after 4 hours, no active substance is released from the oral dosage form; and by 5 hours, 100% of the active substance is released from the oral dosage form. ### Claim 2 (depends on 1) The method according to claim 1, wherein the compression coating further comprises at least one excipient selected from cellulosic derivatives and polymers and polymethacrylic polymers. ### Claim 3 (depends on 1) The method according to claim 1, wherein the compression coating further comprises alkylcellulose. ### Claim 4 (depends on 1) The method according to claim 1, wherein the dosage form comprises 1 mg prednisone. ### Claim 5 (depends on 1) The method according to claim 1, wherein the dosage form comprises 5 mg prednisone. ### Claim 6 A method of administering a glucocorticosteroid active substance selected from prednisone, prednisolone, and methylprednisolone to a patient in need thereof comprising administering to the patient an oral dosage form comprising a defined core and a compression coating completely covering the core, wherein the core comprises the glucocorticosteroid active substance substance and further comprises at least one disintegrating agent that, upon exposure to aqueous media, provides a force to rupture the coating, wherein the compression coating comprises at least one excipient selected from fatty acids or their esters or salts; long chain fatty alcohols; polyoxyethylene alkyl ethers; polyoxyethylene stearates; sugar esters; lauroyl macrogol-32 glyceryl; and stearoyl macrogol-32 glyceryl, wherein the compression coating lacks ingredients that swell and gel to such an extent that the compression coating acts as a diffusion barrier to the release of the active substance, and further provided that the compression coating contains substantially no natural or synthetic gum, and wherein the compression coating ruptures upon immersion in an aqueous medium after a period of time between about 2 to about 6 hours to release the glucocorticosteroid active substance. ### Claim 7 (depends on 6) The method according to claim 6, wherein the dosage form comprises 1 mg prednisone. ### Claim 8 (depends on 6) The method according to claim 6, wherein the dosage form comprises 5 mg prednisone. ### Claim 9 A method of administering a glucocorticosteroid active substance selected from prednisone, prednisolone, and methylprednisolone to a patient in need thereof comprising administering to the patient an oral dosage form comprising a defined core and a compression coating completely covering the core, wherein the core comprises the glucocorticosteroid active substance substance and further comprises at least one disintegrating agent that, upon exposure to aqueous media, provides a force to rupture the coating, wherein the compression coating comprises at least one excipient selected from fatty acids or their esters or salts; long chain fatty alcohols; polyoxyethylene alkyl ethers; polyoxyethylene stearates; sugar esters; lauroyl macrogol-32 glyceryl; and stearoyl macrogol-32 glyceryl, wherein the compression coating lacks ingredients that swell and gel to such an extent that the compression coating acts as a diffusion barrier to the release of the active substance, and further provided that the compression coating contains substantially no natural or synthetic gum, and wherein the oral dosage form releases not more than 10% of the active substance prior to expiry of a lag time; the oral dosage form releases substantially all of the active substance within about 1 hour after the expiry of the lag time; and the lag time is a time between 2 to 6 hours after administration of the oral dosage form to the patient. ### Claim 10 (depends on 9) The method according to claim 9, wherein the dosage form comprises 1 mg prednisone. ### Claim 11 (depends on 9) The method according to claim 9, wherein the dosage form comprises 5 mg prednisone.