Tablet comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1h-quinolin-2-one or a salt thereof

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.

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), and a lubricant (d), 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.   
     
     
         2 . 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).   
     
     
         3 . The tablet according to  claim 1 , which further comprises a coating layer on the surface thereof. 
     
     
         4 . The tablet according to  claim 3 , which further comprises the colorant (e) in the coating layer,
 wherein the colorant (e) contains an iron oxide, and   the tablet contains 0.1 to 50% by weight of the colorant (e) with respect to the weight of the coating layer.   
     
     
         5 . The tablet according to  claim 4 , wherein the coating substantially does not contain polyethylene glycol. 
     
     
         6 . The tablet according to  claim 1 , which is obtained by forming, into a tablet, a granulated substance obtained through wet granulation. 
     
     
         7 . The tablet according to  claim 1 , wherein the tablet does not contain povidone or crospovidone. 
     
     
         8 . 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. 
     
     
         9 . 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, 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.   
     
     
         10 . The method for producing the tablet according to  claim 9 , further comprising the step of:
 (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 coating layer,   wherein the colorant (e) contains an iron oxide, and   the tablet contains 0.1 to 50% by weight of the colorant (e) with respect to the weight of the coating layer.   
     
     
         11 . The method for producing the tablet according to  claim 10 , wherein the coating mixture substantially does not contain polyethylene glycol. 
     
     
         12 . The method for producing the tablet according to  claim 9 , wherein the excipient (a) is lactose, corn starch, and microcrystalline cellulose; and the disintegrant (c) is low-substituted hydroxypropyl cellulose.