Solid preparation comprising alogliptin and metformin hydrochloride
AssigneeTakeda Pharmaceutical Company Limited
InventorsKazumichi Yamamoto, Hiroyoshi Koyama
Life of this patent
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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.
Claims26
A solid preparation comprising the following first part and second part;
- first part:
- a part comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile or a salt thereof and substantially free of metformin hydrochloride
- second part:
- a part comprising metformin hydrochloride and substantially free of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile and a salt thereof.
(canceled)
A method of stabilizing 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile or a salt thereof in a solid preparation comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile or a salt thereof, metformin hydrochloride and an additive, which comprises physically separating 2-[([6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile or a salt thereof from the metformin hydrochloride by the additive.
A method of producing a solid preparation, comprising a step of mixing the following first granule, second granule and additive and compression molding the mixture:
- first granule:
- a granule comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile or a salt thereof and substantially free of metformin hydrochloride
- second granule:
- a granule comprising metformin hydrochloride and substantially free of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile and a salt thereof.
Dependencies are inferred from the claim text.