# US 2016/0354348 A1 · Methods for prophylatic appetite suppression > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2016/0354348 A1 - Document ID: US20160354348A1 - Status: Published application - Kind: A1 - Application number: 15/004,269 - Filed: 2016-01-22 - Published: 2016-12-08 - Earliest claimed: 2005-11-28 - Assignees: Orexigen Therapeutics, Inc. - Applicants: Orexigen Therapeutics, Inc. - Inventors: Anthony A. McKinney; Gary Tollefson; Simon Kwok-Pan Yau; Ronald S. Vladyka; Rick Soltero - Web page: https://patentgrep.com/patent/US20160354348A1 ## CPC - A61K 31/423: condensed with carbocyclic rings - A61K 9/0002: {Galenical forms characterised by the drug release technique; Application systems commanded by energy} - A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)} - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 9/5084: {Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs (tablets containing such a mixture A61K9/2077)} - A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} - A61K 31/42: Oxazoles - A61K 31/485: Morphinan derivatives, e.g. morphine, codeine - A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) - A61P 3/04: Anorexiants; Antiobesity agents - A61P 25/08: Antiepileptics; Anticonvulsants - 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 Pharmaceutical formulations comprise sustained-release zonisamide. Methods of preparing such pharmaceutical formulations involve intermixing zonisamide with a suitable excipient configured to control the dissolution profile of the zonisamide. Methods of treatment involve administering the pharmaceutical formulations to patients in need of such treatment. ## Claims ### Claim 1 A pharmaceutical formulation comprising a controlled-release zonisamide. ### Claim 2 (depends on 1) The pharmaceutical formulation of claim 1 wherein said controlled-release zonisamide comprises a sustained-release zonsisamide. ### Claim 3 (depends on 2) The pharmaceutical formulation of claim 2 further comprising a retardant excipient configured to modify a dissolution profile of said sustained-release zonisamide. ### Claim 4 (depends on 3) The pharmaceutical formulation of claim 3, wherein said retardant excipient comprises at least one selected from hydroxypropyl methylcellulose (HPMC), hydroxyethylcellulose, hydroxypropylcellulose (HPC), methylcellulose, ethylcellulose, cellulose acetate butyrate, cellulose acetate phthalate, hydroxypropylmethyl cellulose phthalate, microcrystalline cellulose, corn starch, polyethylene oxide, polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), cross-linked PVP, polyvinyl acetate phthalate, polyethylene glycol, zein, poly-DL-lactide-co-glycolide, dicalcium phosphate, calcium sulfate, and mixtures thereof. ### Claim 5 (depends on 3) The pharmaceutical formulation of claim 3, wherein the dissolution profile comprises a dissolution rate that is slower than a dissolution rate of a comparable immediate-release zonisamide formulation under comparable conditions. ### Claim 6 (depends on 3) The pharmaceutical formulation of claim 3, wherein said dissolution profile comprises at least one dissolution characteristic selected from: (a) less than about 70% of zonisamide in the sustained-release zonisamide is dissolved within a first hour in a standard dissolution test, (b) less than about 40% of the zonisamide in the sustained-release zonisamide is dissolved within a first hour in a standard dissolution test, (c) less than about 30% of the zonisamide in the sustained-release zonisamide is dissolved within a first hour in a standard dissolution test, (d) less than about 75% of the zonisamide in the sustained-release zonisamide is dissolved within a second hour in a standard dissolution test, (e) less than about 55% of the zonisamide in the sustained-release zonisamide is dissolved within a second hour in a standard dissolution test, and (f) less than about 35% of the zonisamide in the sustained-release zonisamide is dissolved within a second hour in a standard dissolution test. ### Claim 7 (depends on 3) The pharmaceutical formulation of claim 3, wherein said pharmaceutical formulation comprises at least about 5% by weight of said retardant excipient. ### Claim 8 (depends on 3) The pharmaceutical formulation of claim 3, wherein said pharmaceutical formulation comprises at least about 10% by weight of said retardant excipient. ### Claim 9 (depends on 3) The pharmaceutical formulation of claim 3, wherein said retardant excipient is configured to provide, upon administration to a patient, an average free serum zonisamide Cmax value that is less than an average free serum zonisamide Cmax value of a comparable immediate-release zonisamide under comparable conditions. ### Claim 10 (depends on 3) The pharmaceutical formulation of claim 3, wherein upon administration to a patient, an average free serum zonisamide Cmax value is at least about 5% less than an average free serum zonisamide Cmax value of a comparable immediate-release zonisamide under comparable conditions. ### Claim 11 (depends on 2) The pharmaceutical formulation of claim 2, further comprising bupropion. ### Claim 12 (depends on 11) The pharmaceutical formulation of claim 11, wherein said bupropion comprises a sustained-release bupropion. ### Claim 13 (depends on 2) The pharmaceutical formulation of claim 2, comprising sustained-release zonisamide beads that are configured to control the dissolution profile of said sustained-release zonisamide. ### Claim 14 (depends on 13) The pharmaceutical formulation of claim 13, wherein said sustained-release zonisamide beads comprise at least one of a filler and an excipient. ### Claim 15 (depends on 14) The pharmaceutical formulation of claim 14, wherein said excipient comprises at least one selected from a cellulose ether, methylcellulose, hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), corn starch, polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP) and cross-linked PVP. ### Claim 16 (depends on 14) The pharmaceutical formulation of claim 14, wherein said filler comprises at least one selected from acetyltriethyl citrate (ATEC), acetyltri-n-butyl citrate (ATBC), aspartame, lactose, alginates, calcium carbonate, carbopol, carrageenan, cellulose, cellulose acetate phthalate, croscarmellose sodium, crospovidone, dextrose, dibutyl sebacate, ethylcellulose, fructose, gellan gum, glyceryl behenate, guar gum, lactose, lauryl lactate, low-substituted hydroxypryopl cellulose (L-HPC), magnesium stearate, maltodextrin, maltose, mannitol, methylcellulose, microcrystalline cellulose, methacrylate, sodium carboxymethylcellulose, polyvinyl acetate phthalate (PVAP), povidone, shellac, sodium starch glycolate, sorbitol, starch, sucrose, triacetin, triethylcitrate, vegetable based fatty acid, xanthan gum, and xylitol. ### Claim 17 (depends on 13) The pharmaceutical formulation of claim 13, wherein said dissolution profile comprises at least one dissolution characteristic selected from: (a) less than about 65% of the zonisamide in the sustained-release zonisamide beads is dissolved within the first hour in a standard dissolution test, and (b) less than about 50% of the zonisamide in the sustained-release zonisamide beads is dissolved within the first hour in a standard dissolution test. ### Claim 18 (depends on 2) The pharmaceutical formulation of claim 2, configured in a dosage form selected from twice daily, once daily, once every two days, once every three days, once every four days, once every five days, once every six days, and once weekly. ### Claim 19 (depends on 1) A method of treatment comprising administering the pharmaceutical formulation of claim 1 to a patient in need thereof. ### Claim 20 (depends on 19) The method of claim 19, wherein the patient experiences a reduced risk of an adverse event associated with administering a comparable dosage of an immediate-release zonisamide. ### Claim at position 21 21-26. (canceled)