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 excipient (a) is at least one member selected from the group consisting of lactose, corn starch, and microcrystalline cellulose;   the binder (b) is hydroxypropyl cellulose;   the disintegrant (c) is at least one member selected from the group consisting of low-substituted hydroxypropyl cellulose, croscarmellose sodium, and sodium carboxymethyl starch; and   the lubricant (d) is magnesium stearate.   
     
     
         2 . The tablet according to  claim 1 , wherein the tablet is an uncoated tablet comprising:
 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);   0.1 to 20% by weight of the binder (b);   1 to 25% by weight of the disintegrant (c); and   0.1 to 10% by weight of the lubricant (d), with respect to the weight of the uncoated tablet.   
     
     
         3 . The tablet according to  claim 1  or  2 , wherein per 1 part by weight of 7-[4-(4-benzo[b]thiophen-4-yl-piperasin-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 (to); 
 0.1 to 500 parts by weight of the disintegrant (c); and 
 0.01 to 50 parts by weight of the lubricant (d). 
 
     
     
         4 . The tablet according to  claim 1 , which further comprises a coating layer on the surface thereof. 
     
     
         5 . The tablet according to  claim 4 , 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.   
     
     
         6 . The tablet according to  claim 1  or  2 , which is obtained by forming, into a tablet, a granulated substance obtained through wet granulation. 
     
     
         7 . The tablet according to  claim 1  or  2 , wherein the tablet does not contain povidone or crospovidone. 
     
     
         8 . 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,   wherein the excipient (a) is at least one member selected from the group consisting of lactose, corn starch, and microcrystalline cellulose;   the binder (b) is hydroxypropyl cellulose;   the disintegrant (c) is at least one member selected from the group consisting of low-substituted hydroxypropyl cellulose, croscarmellose sodium, and sodium carboxymethyl starch; and   the lubricant (d) is magnesium stearate.   
     
     
         9 . The method for producing the tablet according to  claim 8 , 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 using the coating mixture.