# US 10,307,419 B2 · Tablet comprising 7-[4-(4-benzo[b]thiopen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,307,419 B2 - Document ID: US10307419B2 - Status: Granted - Kind: B2 - Application number: 15/713,427 - Filed: 2017-09-22 - Published: 2018-01-11 - Granted: 2019-06-04 - Earliest claimed: 2011-10-14 - Assignees: Otsuka Pharmaceutical Co., Ltd. - Applicants: Otsuka Pharmaceutical Co., Ltd. - Inventors: Yoshiharu Inoue - Web page: https://patentgrep.com/patent/US10307419B2 ## CPC - A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin - A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/2813: {Inorganic compounds} - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - 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 This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl -piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability. The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4 -yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer, containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet. ## Claims ### Claim 1 A tablet comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, an excipient (a), a binder (b), a disintegrant (c), a lubricant (d), and a coating, wherein the uncoated tablet comprises: 0.05 to 25% by weight of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, 10 to 98.5% by weight of the excipient (a), which is at least one member selected from the group consisting of lactose, corn starch, and microcrystalline cellulose; 0.1 to 20% by weight of the binder (b), which is hydroxypropyl cellulose; 1 to 25% by weight of the disintegrant (c), which is at least one member selected from the group consisting of low-substituted hydroxypropyl cellulose, croscarmellose sodium, and sodium carboxymethyl starch; and 0.1 to 10% by weight of the lubricant (d), which is magnesium stearate; wherein said coating comprises hydroxypropyl methylcellulose, talc, and a colorant (e), the colorant (e) is present in an amount ranging from 0.1 to 50% by weight of the coating and comprises iron oxide and titanium oxide, and the coating substantially does not contain polyethylene glycol. ### Claim 2 (depends on 1) The tablet according to claim 1, wherein per 1 part by weight of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, the tablet comprises: 1 to 2000 parts by weight of the excipient (a); 0.01 to 100 parts by weight of the binder (b); 0.1 to 500 parts by weight of the disintegrant (c); and 0.01 to 50 parts by weight of the lubricant (d). ### Claim 3 (depends on 1) The tablet according to claim 1, which is obtained by forming, into a tablet, a granulated substance obtained through wet granulation. ### Claim 4 (depends on 1) The tablet according to claim 1, wherein the tablet does not contain povidone or crospovidone. ### Claim 5 (depends on 1) The tablet according to claim 1, wherein the excipient (a) is lactose, corn starch, and microcrystalline cellulose; and the disintegrant (c) is low-substituted hydroxypropyl cellulose. ### Claim 6 A method for producing a tablet, the method comprising the steps of: (1) granulating a mixture containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, an excipient (a), a binder (b), and a disintegrant (c), and further mixing thereto a lubricant (d); and (2) forming the obtained mixture into a tablet form; and (3) mixing a coating agent, a colorant (e), and a liquid medium to obtain a coating mixture, and coating the surface of the tablet form using the coating mixture to form the tablet, wherein the tablet comprises: 0.05 to 25% by weight of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, 10 to 98.5% by weight of the excipient (a), which is at least one member selected from the group consisting of lactose, corn starch, and microcrystalline cellulose; 0.1 to 20% by weight of the binder (b), which is hydroxypropyl cellulose; 1 to 25% by weight of the disintegrant (c), which is at least one member selected from the group consisting of low-substituted hydroxypropyl cellulose, croscarmellose sodium, and sodium carboxymethyl starch; and 0.1 to 10% by weight of the lubricant (d), which is magnesium stearate; the tablet further comprising a coating layer on the surface thereof, wherein said coating agent comprises hydroxypropyl methyl cellulose and talc, the colorant (e) is present in an amount ranging from 0.1 to 50% by weight of the coating mixture and comprises iron oxide and titanium oxide, and the coating mixture substantially does not contain polyethylene glycol. ### Claim 7 (depends on 6) The method for producing the tablet according to claim 6, wherein the excipient (a) is lactose, corn starch, and microcrystalline cellulose; and the disintegrant (c) is low-substituted hydroxypropyl cellulose.