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Solid preparation comprising alogliptin and metformin hydrochloride

A technology of metformin hydrochloride and solid preparations, which can be applied to medical preparations containing active ingredients, pill delivery, coatings, etc., and can solve problems such as storage stability of the compound metformin that has not been reported

Active Publication Date: 2010-08-11
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, a formulation excellent in storage stability comprising compound (I) or a salt thereof and metformin hydrochloride has not been reported

Method used

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  • Solid preparation comprising alogliptin and metformin hydrochloride
  • Solid preparation comprising alogliptin and metformin hydrochloride
  • Solid preparation comprising alogliptin and metformin hydrochloride

Examples

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preparation example Construction

[0204] During the preparation of the coated tablet (A), it is preferable to form an inactive intermediate layer between the inner core and the outer layer to avoid direct contact between the inner core and the outer layer. The intermediate layer contains, for example, the above-mentioned coating base and coating additives. The intermediate layer preferably comprises an aqueous film coating base (preferably hydroxypropylmethylcellulose) and an opacifier and / or colorant (preferably talc).

[0205] In the above-mentioned coated tablet (A), the outer layer is formed at a ratio of preferably 0.1-100 parts by weight, more preferably 1-50 parts by weight, still more preferably 3-30 parts by weight, relative to 100 parts by weight of the inner core.

[0206] Moreover, in the above-mentioned coated tablet (A), the intermediate layer is formed at a ratio of preferably 0.1-30 parts by weight, more preferably 0.5-20 parts by weight, still more preferably 1-5 parts by weight, relative to 1...

preparation example 1

[0278] A mixture of benzoate (177.08 g), mannitol (262.5 g) and crystalline cellulose (31.25 g) of compound (I) was subjected to fluidized bed granulation (POWREX CORPORATION, model: LAB-1), while spraying An aqueous solution (292 g) of polyvinylpyrrolidone (29.18 g) was obtained to obtain granules containing compound (IA).

[0279] Separately, a mixture of metformin hydrochloride (463.0 g) and crystalline cellulose (11.11 g) was subjected to fluidized bed granulation (POWREX CORPORATION, model: LAB-1), while spraying an aqueous solution (259 g) of polyvinylpyrrolidone (25.93 g) To obtain granules containing metformin hydrochloride.

[0280] The above compound (IA)-containing granules (9.6 g), metformin hydrochloride-containing granules (432.2 g), crystalline cellulose (CEOLUS KG-802, 25.1 g), crospovidone (Kollidon CL-F, 24.63 g) Mixed with magnesium stearate (1.48 g) to obtain a powder mixture. The resulting powder mixture was tableted using a rotary tablet press (KIKUSUI ...

preparation example 2

[0283] A mixture of benzoate (347.01 g), mannitol (1428.6 g) and crystalline cellulose (122.48 g) of compound (I) was subjected to fluidized bed granulation (POWREX CORPORATION, model: FD-3S), while spraying Aqueous solution (1020 g) of polyvinylpyrrolidone (102.06 g) to obtain granules containing compound (IA).

[0284] Separately, a mixture of metformin hydrochloride (1851.9 g) and crystalline cellulose (44.44 g) was subjected to fluidized bed granulation (POWREX CORPORATION, model: FD-3S), while spraying an aqueous solution (1037 g) of polyvinylpyrrolidone (103.7 g) To obtain granules containing metformin hydrochloride.

[0285] The above compound (IA)-containing granules (58.8 g), metformin hydrochloride-containing granules (648 g), crystalline cellulose (CEOLUS KG-802, 39.6 g), crospovidone (Kollidon CL-F, 39.6 g) and Magnesium stearate (2.4 g) was mixed to obtain a powder mixture. The resulting powder mixture was tableted using a rotary tablet press (KIKUSUI SEISAKUSYO...

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Abstract

The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part:a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof.

Description

technical field [0001] The present invention relates to a solid preparation excellent in storage stability, a method for producing the same, and a method for stabilizing compound (I). The solid preparation contains 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4- Dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile (common name: alogliptin; hereinafter sometimes referred to as compound (I)) or a salt thereof and metformin hydrochloride. Background technique [0002] Compound (I) or a salt thereof used in the present invention has been reported as an inhibitor of dipeptidyl peptidase (DPP-IV), which degrades glucagon-like peptide-1 ( GLP-1), a hormone that enhances insulin secretion (WO2005 / 095381). [0003] There has been a report on the combined administration of compound (I) or a salt thereof used in the present invention and metformin hydrochloride (WO2007 / 033266). [0004] However, a preparation comprising compound (I) or a salt thereof and metformin hydrochloride ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/26A61K31/513A61K31/155A61K45/06
CPCA61K9/2018A61K9/2054A61K31/513A61K9/2853A61K9/2866A61K9/2077A61K9/2086A61K9/2027A61K9/209A61K45/06A61K31/155A61P3/10A61P3/04A61P3/06A61P9/00A61P9/10A61P9/12A61K2300/00
Inventor 山本一路小山博义
Owner TAKEDA PHARMA CO LTD
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