TABLET COMPRISING 7-[4-(4-BENZO[ b ]THIOPHEN-4-YL-PIPERAZIN-1-YL) BUTOXY]-1H-QUINOLIN-2-ONE OR A SALT THEREOF

Description

hypromellose 2906, and hypromellose 2910),; other polysaccharidessuch as acacia, powdered acacia, agar, powdered agar, guar gum,tragacanth, powdered tragacanth, pullulan, and pectin; acrylicacid based polymer such as methacrylic acid copolymer L,5 methacrylic acid copolymer LD, methacrylic acid copolymer S,ethyl acrylate-methyl methacrylate copolymer dispersion,aminoalkyl methacrylate copolymer E, and aminoalkyl methacrylatecopolymer RS; sodium alginate; purified gelatin; hydrolyzedgelatin powder; carboxyvinyl polymer; copolyvidone; povidone;10 polyvinyl alcohol. These binders (b) may be used singly or in acombination of two or more. Among these, a cellulose derivativeis preferable, and hydroxypropyl cellulose is more preferable. Itshould be noted that, when povidone is contained as a binder (b),the obtained tablet tends to have reduced photostability and15 storage stability. Therefore, it is more preferable if thiscomponent is substantially not contained.

[0029] The binder (b) content is not particularly limited, andis preferably about 0.1 to 20% by weight with respect to the20 weight of the tablet (when the tablet is coated, the weight ofthe uncoated tablet), and more preferably about 0.5 to 5% byweight.

[0030] The binder (b) amount is not particularly limited, and25 is preferably about 0.01 to 100 parts by weight per 1 part byweight of Compound (I) or a salt thereof, and more preferablyabout 0.1 to 50 parts by weight. By setting the content andamount of the binder (b) as described above, the productivity anddisintegration ability can be improved.30

[0031] Examples of disintegrants (c) include starch or aderivative thereof such as wheat starch, corn starch, potatostarch, partially pregelatinized starch, sodium carboxymethylstarch, and hydroxypropyl starch; cellulose or a derivative35 thereof such as microcrystalline cellulose, carboxymethyl

Claims

1. A tablet comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt5 thereof as an active ingredient, an excipient (a), abinder (b), a disintegrant (c) and a lubricant (d),wherein the excipient (a) is at least one memberselected from the group consisting of lactose, cornstarch, and microcrystalline cellulose;10 the binder (b) is hydroxypropyl cellulose;the disintegrant (c) is at least one memberselected from the group consisting of low-substitutedhydroxypropyl cellulose, croscarmellose sodium, and sodiumcarboxymethyl starch; and15 the lubricant (d) is magnesium stearate.

2. The tablet according to claim 1, wherein thetablet is an uncoated tablet comprising:20 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);25 1 to 25% by weight of the disintegrant (c); and0.1 to 10% by weight of the lubricant (d), withrespect to the weight of the uncoated tablet.

3. 30 The tablet according to claim 1 or 2, whereinper 1 part by weight of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a saltthereof, the tablet comprises:1 to 2000 parts by weight of the excipient (a);35 0.01 to 100 parts by weight of the binder (b);0.1 to 500 parts by weight of the disintegrant(c); and0.01 to 50 parts by weight of the lubricant (d).5

4. The tablet according to any one of claims 1 to3, which further comprises a coating layer on the surfacethereof.10

5. The tablet according to claim 4, which furthercomprises the colorant (e) in the coating layer,wherein the colorant (e) contains an ironoxide, and15 the tablet contains 0.1 to 50% by weight of thecolorant (e) with respect to the weight of the coatinglayer.

6. 20 The tablet according to any one of claims 1 to5, wherein the tablet does not contain povidone orcrospovidone.

7. 25 A method for producing a tablet, the methodcomprising 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),30 and a disintegrant (c), and further mixing thereto alubricant (d); and(2) forming the obtained mixture into a tablet,wherein the excipient (a) is at least onemember selected from the group consisting of lactose, corn35 starch, and microcrystalline cellulose;the binder (b) is hydroxypropyl cellulose;the disintegrant (c) is at least one memberselected from the group consisting of low-substitutedhydroxypropyl cellulose, croscarmellose sodium, and sodium5 carboxymethyl starch; andthe lubricant (d) is magnesium stearate.

8. The method for producing the tablet according to10 claim 7, further comprising the step of:(3) mixing a coating agent, a colorant (e), anda liquid medium to obtain a coating mixture, and coatingthe surface of the tablet using the coating mixture.15

9. The method for producing the tablet according toclaim 7 or 8, wherein the granulating is performed throughwet granulation.

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