Tablet

A tablet and methyl technology, applied in the field of tablets, can solve problems such as increasing tablet size and decreasing patient compliance, achieve excellent productivity, prevent tablet surface damage, prevent tablet cracking and tablet compression problems Effect

Inactive Publication Date: 2012-07-04
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, higher compound (A) content in tablets increases tablet size and patient compliance, especially in infants and elderly patients who have difficulty swallowing

Method used

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Experimental program
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Embodiment approach

[0175] In particular, preferred embodiments of the tablet of the present invention include:

[0176] "Tablets each containing 50 mg of compound (A) (free form)";

[0177] "Tablets each containing 100 mg of Compound (A) (free form)"; and

[0178] "Tablets each containing 200 mg of compound (A) (free form)".

[0179] Compound (A) or a salt thereof may be used in combination with one or more other drugs (hereinafter sometimes referred to as "concomitant drug").

[0180] As a specific example, compound (A) or a salt thereof can be used in combination with one or more drugs (concomitant drugs) selected from the following: therapeutic agents for diabetes, therapeutic agents for diabetic complications, therapeutic agents for hyperlipidemia, anti-hyperlipidemia Blood pressure drugs, anti-obesity drugs, diuretics, anticoagulants, etc.

[0181]Examples of the diabetes therapeutic agent include insulin preparations (for example, animal insulin preparations extracted from bovine or por...

Embodiment 1

[0196] According to the prescription of Table 1, compound (A) succinate (monosuccinate), crystalline cellulose (PH-302), croscarmellose sodium, magnesium stearate and light silica Mix uniformly in a mixer (vertical granulator 50L, Powrex Corporation) and granulate with a roller compactor (Alexander). The resulting granulated product was granulated by a granulator (power mill P-3, Showa Kako Corporation) to obtain a granulated powder. Crystalline cellulose (KG-802), hydroxypropyl cellulose (HPC-L 100M; Nippon Soda Co., Ltd.) and magnesium stearate were added to the granulated powder, and mixed in a mixer (tumbler 60L , Showa Kako Corporation) was mixed to obtain granules for tableting. The granules were compressed to a weight of 110 mg in a rotary tableting machine (AQUARIOUS3-A, Kikusui Seisakusho Ltd.) with an 8×4.5 mm punch to obtain plain tablets. Titanium dioxide, ferric oxide, yellow iron oxide, and talc were dispersed in an aqueous solution of hydroxypropyl methylcellu...

Embodiment 2

[0200] According to the prescription of Table 2, compound (A) succinate (monosuccinate), crystalline cellulose (PH-302), croscarmellose sodium, magnesium stearate and light silica Mix uniformly in a mixer (vertical granulator 50L, Powrex Corporation) and granulate with a roller compactor (Alexander). The resulting granulated product was granulated by a granulator (power mill P-3, Showa Kako Corporation) to obtain a granulated powder. Crystalline cellulose (KG-802), hydroxypropyl cellulose (HPC-L 100M; Nippon Soda Co., Ltd.) and magnesium stearate were added to the granulated powder, and mixed in a mixer (tumbler 60L , Showa Kako Corporation) was mixed to obtain granules for tableting. The granules were compressed to a weight of 220 mg in a rotary tableting machine (AQUARIOUS3-A, Kikusui Seisakusho Ltd.) with a punch of 11×6 mm to obtain plain tablets. Titanium dioxide, ferric oxide, yellow iron oxide, and talc were dispersed in an aqueous solution of hydroxypropyl methylcell...

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Abstract

Disclosed is a high-dose tablet which contains 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)- pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active ingredient. Specifically disclosed is a tablet which contains the compound (A) or a salt thereof, and a fluidizer, with the content of the compound (A) being 35-50% by weight.

Description

technical field [0001] The present invention relates to 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1 A formulation of (2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (abbreviated as "compound (A)" in the present invention) or a salt thereof, a production method thereof, and the like. [Background of the invention] [0002] Compound (A) is a compound shown in the following formula: [0003] [0004] Compound (A) or a salt thereof is reported to be an inhibitor of dipeptidyl peptidase (DPP-IV), an enzyme that decomposes glucagon-like peptide-1 (GLP-1, a hormone that promotes insulin secretion) (US2005 / 0261271). [0005] In addition, a method comprising administering 1 to 250 mg of compound (A) or a salt thereof to a patient once a week has been reported (WO2008 / 033851). Oral administration of the compound (A) and its salt is recommended in view of making self-administration easier, and tablets, especially tablets for once-a-week administration, are re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K9/20A61K47/04A61K47/38
CPCA61K31/506A61K9/2077A61K9/2054A61P13/12A61P19/08A61P25/00A61P27/02A61P27/12A61P3/00A61P3/04A61P31/00A61P3/06A61P3/08A61P9/00A61P9/10A61P9/12A61P3/10A61K9/20A61K47/38A61K47/02
Inventor 村川佑介冈部贵幸
Owner TAKEDA PHARMA CO LTD
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