# US 11,896,599 B2 · Modified release preparations containing oxcarbazepine and derivatives thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,896,599 B2 - Document ID: US11896599B2 - Status: Granted - Kind: B2 - Application number: 16/252,106 - Filed: 2019-01-18 - Published: 2019-12-19 - Granted: 2024-02-13 - Earliest claimed: 2006-04-26 - Assignees: Supernus Pharmaceuticals, Inc. - Applicants: Supernus Pharmaceuticals, Inc. - Inventors: Padmanabh P. Bhatt; Argaw Kidane; Kevin Edwards - Web page: https://patentgrep.com/patent/US11896599B2 ## CPC - A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole - A61K 9/0073: {Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M)} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers} - A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61P 25/08: Antiepileptics; Anticonvulsants - A61K 2800/56: Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms - 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 Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed. ## Claims ### Claim 1 A pharmaceutical controlled release formulation comprising a homogeneous matrix, which comprises (a) oxcarbazepine, (b) a matrix-forming polymer selected from the group consisting of cellulosic polymers, alginates, gums, cross-linked polyacrylic acid, carageenan, polyvinyl pyrrolidone, polyethylene oxides, and polyvinyl alcohol, and (c) at least one agent that enhances the solubility of oxcarbazepine. ### Claim 2 (depends on 1) The formulation of claim 1, wherein the at least one agent that enhances the solubility of oxcarbazepine is selected from the group consisting of surface active agents, complexing agents, cyclodextrins, and pH modifying agents. ### Claim 3 (depends on 2) The formulation of claim 2, wherein the surface active agent is selected from the group consisting of sodium docusate, sodium lauryl sulfate, sodium stearyl fumarate, polyethylene oxide (PEO) modified sorbitan monoesters, fatty acid sorbitan esters, polyethylene oxide-polypropylene oxide-(poly(ethylene oxide)) block copolymers, or combinations thereof. ### Claim 4 (depends on 1) The formulation of claim 1, wherein in vitro: (i) between 20 and 74% of the total oxcarbazepine is released by 2 hours; and (ii) between 44 and 96% of the total oxcarbazepine is released by 4 hours. ### Claim 5 (depends on 1) The formulation of claim 1, wherein the cellulosic polymers are selected from the group consisting of hydroxypropylmethylcellulose (HPMC), hydroxypropylcellulose (HPC), hydroxyethylcellulose (HEC), methylcellulose (MC), powdered cellulose, cellulose acetate, sodium carboxymethylcellulose, calcium salt of carboxymethylcellulose, and ethylcellulose. ### Claim 6 (depends on 1) The formulation of claim 1, wherein the matrix-forming polymer is present in the amount of from 1% to 50% by weight of the formulation. ### Claim 7 (depends on 1) The formulation of claim 1, further comprising at least one release promoting agent. ### Claim 8 (depends on 7) The formulation of claim 7, wherein the at least one release promoting agent comprises a polymer having pH dependent solubility that dissolves at pH values of more than 5. ### Claim 9 (depends on 8) The formulation of claim 8, wherein the polymer having pH dependent solubility dissolves at pH values of more than 6. ### Claim 10 (depends on 7) The formulation of claim 7, wherein the release promoting agent is incorporated in an amount from 10% to 90% by weight of the formulation, and the agent that enhances the solubility of oxcarbazepine is incorporated in an amount from 1% to 80% by weight of the formulation. ### Claim 11 (depends on 10) The formulation of claim 10, wherein the release promoting agent is incorporated in an amount from 30% to 70% by weight of the formulation, and the agent that enhances the solubility of oxcarbazepine is incorporated in an amount from 1% to 80% by weight of the formulation. ### Claim 12 (depends on 1) The formulation of claim 1, further comprising a lubricant selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, stearic acid, polyethylene glycol, leucine, glyceryl behenate, sodium stearyl fumarate, hydrogenated vegetable oil, and wax. ### Claim 13 (depends on 12) The formulation of claim 12, wherein the wax is selected from the group consisting of beeswax, carnauba wax, cetyl alcohol, glyceryl stearate, glyceryl palmitate, and stearyl alcohol. ### Claim 14 (depends on 12) The formulation of claim 12, wherein the lubricant is incorporated in an amount of from 0.1% to 20% by weight of the formulation. ### Claim 15 (depends on 1) The formulation of claim 1, wherein the amount of oxcarbazepine is effective to produce a steady state blood level of monohydroxy derivative of oxcarbazepine in the range of about 2 μg/ml to about 10 μg/ml. ### Claim 16 (depends on 1) The formulation of claim 1, wherein the amount of oxcarbazepine is 600 mg. ### Claim 17 (depends on 1) The formulation of claim 1, in the form of pellets, tablets, granules or capsules. ### Claim 18 (depends on 17) The formulation of claim 17, in the form of tablets. ### Claim 19 (depends on 18) The formulation of claim 18, wherein the tablets comprise 600 mg of oxcarbazepine. ### Claim 20 (depends on 7) The formulation of claim 7, wherein the at least one release promoting agent comprises a polymer having pH dependent solubility that dissolves at pH values of more than 4.