JPWO2021117861A5 - - Google Patents

Claims (36)

(1) 84-95 wt% of imeglimin or a pharmaceutically acceptable salt thereof, and (2) one or more binders selected from the group consisting of hydroxypropyl cellulose, polyvinyl alcohol and hydroxypropyl methyl cellulose . A tablet containing 5.5 to 6.0 wt% and (3) a disintegrant and manufactured using the fluidized layer granulation method . (1) The tablet according to claim 1, which contains 88 to 95 wt% of imeglimin or a pharmaceutically acceptable salt thereof. (1) The tablet according to claim 1, which contains 90 to 95 wt% of imeglimin or a pharmaceutically acceptable salt thereof. (1) The tablet according to claim 1 or 2, which contains 90 to 92 wt% of imeglimin or a pharmaceutically acceptable salt thereof. (3) The tablet according to claim 1 or 2, which contains 0.2 to 7.5 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 5, which contains 0.2 to 5.0 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 6, which contains 0.2 to 4.0 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 7, which contains 0.2 to 3.0 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 8, which contains 0.2 to 2.0 wt% of a disintegrant. (3) The tablet according to claim 1 or 2, which contains 0.5 to 7.5 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 4 and 10, which contains 0.5 to 5.0 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 4, 10 and 11, which contains 0.5 to 4.0 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 4, 10 to 12, which contains 0.5 to 3.0 wt% of a disintegrant. (3) The tablet according to any one of claims 1 to 4, 10 to 13, which contains 0.5 to 2.0 wt% of a disintegrant. (2) Any one of claims 1 to 14 containing 4.5 to 6.0 wt% of one or more binders selected from the group consisting of hydroxypropyl cellulose, polyvinyl alcohol and hydroxypropyl methyl cellulose. The tablets described in the section. (2) Any one of claims 1 to 15 containing 4.5 to 5.5 wt% of one or more binders selected from the group consisting of hydroxypropyl cellulose, polyvinyl alcohol and hydroxypropyl methyl cellulose. The tablets described in the section. (2) Any one of claims 1 to 16 containing 4.8 to 5.5 wt% of one or more binders selected from the group consisting of hydroxypropyl cellulose, polyvinyl alcohol and hydroxypropyl methyl cellulose. The tablets described in the section. The tablet according to any one of claims 1 to 17 , wherein the hydroxypropyl cellulose has a viscosity of 2.0 to 400 mPa · s. The tablet according to any one of claims 1 to 18 , wherein the hydroxypropyl cellulose has a viscosity of 6.0 to 400 mPa · s. The tablet according to any one of claims 1 to 19 , wherein the polyvinyl alcohol has a viscosity of 3.4 to 9.2 mPa · s. The tablet according to any one of claims 1 to 20 , wherein the polyvinyl alcohol has a viscosity of 4.3 to 5.8 mPa · s. The tablet according to any one of claims 1 to 21 , wherein the viscosity of hydroxypropylmethyl cellulose is 4.0 to 12.0 mPa · s. The tablet according to any one of claims 1 to 22 , wherein the viscosity of hydroxypropylmethyl cellulose is 4.0 to 6.0 mPa · s. The tablet according to any one of claims 1 to 23 , wherein the viscosity of hydroxypropylmethyl cellulose is 4.5 to 6.0 mPa · s. Claims 1 to 18 include hydroxypropyl cellulose having a viscosity of 2.0 to 2.9 mPa · s in the range of 3.5 wt% or less and hydroxypropyl cellulose having a viscosity of 150 to 400 mPa · s in the range of 1.5 wt% or less. , 20-24 . The tablet according to any one of Items . (2) The tablet according to any one of claims 1 to 21 , 25 , wherein the binder is one or two selected from the group consisting of hydroxypropyl cellulose and polyvinyl alcohol. (2) The tablet according to any one of claims 1 to 19 and 22 to 25 , wherein the binder is one or two selected from the group consisting of hydroxypropyl cellulose and hydroxypropyl methyl cellulose. (2) The tablet according to any one of claims 1 to 19 and 25 to 27 , wherein the binder is hydroxypropyl cellulose. (3) The tablet according to any one of claims 1 to 28 , wherein the disintegrant is one or more selected from the group consisting of sodium croscarmellose, sodium starch glycolate and crospopidone. (3) The tablet according to any one of claims 1 to 29, wherein the disintegrant is sodium croscarmellose. (1) Imeglycin or a pharmaceutically acceptable salt thereof, (2) one or more binders selected from the group consisting of hydroxypropyl cellulose, polyvinyl alcohol and hydroxypropyl methyl cellulose, and (3) disintegrant. The method for producing a tablet according to claim 1 , which comprises a step of producing granulated granules containing the above-mentioned granules by using a fluidized layer granulation method. One or two selected from the group consisting of (2) hydroxypropyl cellulose, polyvinyl alcohol and hydroxypropyl methyl cellulose in a powder containing (1) imeglycin or a pharmaceutically acceptable salt thereof and (3) a disintegrant. The production method according to claim 31 , which comprises a step of adding the above binder and producing using the fluidized bed granulation method. The production method according to claim 31 or 32 , further comprising a tableting step or a film coating step. The production method according to claim 33 , wherein any of the fluidized bed granulation step, the tableting step, and the film coating step is manufactured with a production amount of 10 kg or more. The production method according to claim 33 , wherein any of the fluidized bed granulation step, the tableting step, and the film coating step is manufactured with a production amount of 30 kg or more. The production method according to claim 33 , wherein any of the fluidized bed granulation step, the tableting step, and the film coating step is manufactured with a production amount of 50 kg or more.