US2003130268A1PendingUtilityA1

Compositions controlling pH range of release and /or release rate

45
Priority: Jun 16, 2000Filed: Dec 16, 2002Published: Jul 10, 2003
Est. expiryJun 16, 2020(expired)· nominal 20-yr term from priority
Inventors:Kazuyoshi SagaraTomoyuki OmuraHirofumi SamemotoHirotsugu Komatsu
A61P 29/00A61K 9/1676A61K 31/551A61K 31/5517A61K 9/2018A61P 1/04A61K 9/1635A61K 9/2059A61K 9/204A61K 9/146A61K 9/143A61K 9/1652A61K 9/2054A61K 47/38A61K 9/1641A61P 1/00
45
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Claims

Abstract

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.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A composition controlling a pH range of release and/or a release rate, which comprises (i) 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; 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.  
     
     
         2 . The composition controlling a pH range of release and/or a release rate of  claim 1 , wherein the ingredient is at least one kind selected from the group consisting of an enteric polymer and a water-insoluble polymer.  
     
     
         3 . The composition controlling a pH range of release and/or a release rate of  claim 1 , which further comprises a surfactant.  
     
     
         4 . The composition controlling a pH range of release and/or a release rate of  claim 1 , wherein the 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.  
     
     
         5 . The composition controlling a pH range of release and/or a release rate of  claim 1 , which is a therapeutic agent for an inflammatory disease in the neutral area in the gastrointestinal tract lumen.  
     
     
         6 . The composition controlling a pH range of release and/or a release rate of  claim 5 , wherein the inflammatory disease is ulcerative colitis or Crohn's disease.  
     
     
         7 . The composition controlling a pH range of release and/or a release rate of  claim 1 , which is a solid dispersion.  
     
     
         8 . A composition controlling a pH range of release and/or a release rate, which comprises the compound of the formula (I), a pharmaceutically acceptable salt thereof or a hydrate thereof, and a surfactant.  
     
     
         9 . The composition controlling a pH range of release and/or a release rate of  claim 8 , wherein the 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.  
     
     
         10 . The composition controlling a pH range of release and/or a release rate of  claim 8 , which is a therapeutic agent for an inflammatory disease in the neutral area in the gastrointestinal tract lumen.  
     
     
         11 . The composition controlling a pH range of release and/or a release rate of  claim 10 , wherein the inflammatory disease is ulcerative colitis or Crohn's disease.  
     
     
         12 . The composition controlling a pH range of release and/or a release rate of  claim 8 , which is a solid dispersion.  
     
     
         13 . A production method of a composition controlling a pH range of release and/or a release rate, which comprises dissolving or dispersing the compound of the formula (I), a pharmaceutically acceptable salt thereof or a hydrate thereof, and a polymer in a solvent, and evaporating the solvent.  
     
     
         14 . The method of  claim 13 , wherein the polymer is at least one kind selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer.  
     
     
         15 . The method of  claim 13 , wherein the polymer is at least one kind selected from the group consisting of an enteric polymer and a water-insoluble polymer.  
     
     
         16 . The method of  claim 13 , further comprising dissolving or dispersing a surfactant in the solvent.  
     
     
         17 . A production method of a composition controlling a pH range of release and/or a release rate, which comprises dissolving or dispersing the compound of the formula (I), a pharmaceutically acceptable salt thereof or a hydrate thereof, and a surfactant in a solvent, and evaporating the solvent.  
     
     
         18 . A composition controlling a pH range of release and/or a release rate, which is obtainable by the method of any of  claims 13  to  17 .  
     
     
         19 . The composition controlling a pH range of release and/or a release rate of  claim 18 , which is a solid dispersion.  
     
     
         20 . A production method of a composition controlling a pH range of release and/or a release rate, which comprises melting the compound of the formula (I), a pharmaceutically acceptable salt thereof or a hydrate thereof, dissolving or dispersing a polymer, and cooling for solidification.  
     
     
         21 . The method of  claim 20 , wherein the polymer is at least one kind selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer.  
     
     
         22 . The method of  claim 20 , wherein the polymer is at least one kind selected from the group consisting of an enteric polymer and a water-insoluble polymer.  
     
     
         23 . The method of  claim 20 , further comprising dissolving or dispersing a surfactant in the melt product.  
     
     
         24 . A production method of a composition controlling a pH range of release and/or a release rate, which comprises melting the compound of the formula (I), a pharmaceutically acceptable salt thereof or a hydrate thereof, dissolving or dispersing a surfactant, and cooling for solidification.  
     
     
         25 . A composition controlling a pH range of release and/or a release rate which is obtainable by the method of any of  claims 20  to  24 .  
     
     
         26 . The composition controlling a pH range of release and/or a release rate of  claim 25 , which is a solid dispersion.

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