Compositions controlling pH range of release and/or release rate
The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I) and (ii) at least one kind of ingredient selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer and/or a surfactant, as well as a production method thereof.
1 - 26 . (canceled)
27 . A method for controlling a pH range of release and/or a release rate of a thienotriazolodiazepine compound of the formula (I)
wherein X is a halogen, R 1 is C1-C4 alkyl, R 2 is C1-C4 alkyl, a is an integer of 1-4, R 3 is C1-C4 alkyl, C1-C4
hydroxyalkyl, C1-C4 alkoxy, phenyl optionally having substituent(s), or heteroaryl optionally having substituent(s), a pharmaceutically acceptable salt thereof or a hydrate thereof.
28 . The method of claim 27 , wherein the thienotriazolodiazepine compound of the formula (I) is
(S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide.
29 . The method of claim 27 , for treating an inflammatory disease in the neutral area in the gastrointestinal tract lumen.
30 . The method of claim 29 , wherein the inflammatory disease is ulcerative colitis or Crohn's disease.
31 . A method for administering a thienotriazolodiazepine compound of the formula (I)
wherein X is a halogen, R 1 is C1-C4 alkyl, R 2 is C1-C4 alkyl, a is an integer of 1-4, R 3 is C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl optionally having substituent(s), or heteroaryl optionally having substituent(s), a pharmaceutically acceptable salt thereof or a hydrate thereof, wherein a pH range of release and/or a release rate of the compound, the pharmaceutically acceptable salt thereof or the hydrate thereof is controlled in the body.
32 . The method of claim 31 , wherein the thienotriazolodiazepine compound of the formula (I) is
(S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide.
33 . The method of claim 31 , for treating an inflammatory disease in the neutral area in the gastrointestinal tract lumen.
34 . The method of claim 33 , wherein the inflammatory disease is ulcerative colitis or Crohn's disease.