Novel Pyridine Compounds
US-2024316020-A1 · Sep 26, 2024 · US
US2018116965A1 · US · A1
| Field | Value |
|---|---|
| Publication number | US-2018116965-A1 |
| Application number | US-201615569682-A |
| Country | US |
| Kind code | A1 |
| Filing date | Apr 27, 2016 |
| Priority date | Apr 28, 2015 |
| Publication date | May 3, 2018 |
| Grant date | — |
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Disclosed is a pharmaceutical composition for oral administration, comprising 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, which is a compound having pH-dependent solubility, or a pharmaceutically acceptable salt thereof, and a cellulose derivative. In the pharmaceutical composition for oral administration, the solubility and absorbability of the drug are improved.
Opening claim text (preview).
1 . A pharmaceutical composition for oral administration, comprising 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, and a cellulose derivative. 2 . The pharmaceutical composition for oral administration according to claim 1 , wherein the cellulose derivative is hydroxypropyl cellulose and/or hypromellose. 3 . The pharmaceutical composition for oral administration according to claim 1 , wherein the cellulose derivative is hydroxypropyl cellulose and/or hypromellose. 4 . The pharmaceutical composition for oral administration according to claim 1 , wherein 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, and a cellulose derivative form a solid dispersion. 5 . The pharmaceutical composition for oral administration according to claim 1 , further comprising an effervescent substance. 6 . The pharmaceutical composition for oral administration according to claim 5 , wherein the effervescent substance is sodium hydrogen carbonate. 7 . The pharmaceutical composition for oral administration according to claim 1 , further comprising a disintegrating component. 8 . The pharmaceutical composition for oral administration according to claim 7 , wherein the disintegrating component is one member or two or more members selected from the group consisting of crystalline cellulose, calcium hydrogen phosphate hydrate, sodium starch glycolate, low-substituted hydroxypropyl cellulose, and croscarmellose sodium. 9 . The pharmaceutical composition for oral administration according to claim 7 , wherein the disintegrating component is one member or two or more members selected from the group consisting of crystalline cellulose, low-substituted hydroxypropyl cellulose, and croscarmellose sodium. 10 . The pharmaceutical composition for oral administration according to claim 7 , wherein the disintegrating component is crystalline cellulose and/or croscarmellose sodium. 11 . The pharmaceutical composition for oral administration according to claim 7 , wherein the disintegrating component is croscarmellose sodium. 12 . The pharmaceutical composition for oral administration according to claim 1 , wherein the content of the cellulose derivative is 10% by weight to 1000% by weight with respect to the weight of 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, or a pharmaceutically acceptable salt thereof. 13 . The pharmaceutical composition for oral administration according to claim 1 , wherein the pharmaceutical composition for oral administration is a tablet. 14 . The pharmaceutical composition for oral administration according to claim 1 , wherein the pharmaceutical composition for oral administration is a pharmaceutical composition for preventing and/or treating bladder or urinary tract diseases related to bladder contraction by a muscarinic M3 receptor. 15 . (canceled)
Effervescent (A61K9/0065 takes precedence) · CPC title
Inorganic compounds · CPC title
Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623) · CPC title
Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin · CPC title
Inorganic compounds · CPC title
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