US2017112830A1PendingUtilityA1

Suspension and cake composition containing carbostyryl derivative and silicone oil and/or silicone oil derivative

Assignee: OTSUKA PHARMA CO LTDPriority: Aug 24, 2010Filed: Nov 1, 2016Published: Apr 27, 2017
Est. expiryAug 24, 2030(~4.1 yrs left)· nominal 20-yr term from priority
Inventors:Shogo Hiraoka
A61P 25/18A61K 47/34A61K 9/19A61K 9/1641A61K 9/10A61K 31/496A61K 9/20A61K 9/16
44
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Claims

Abstract

A suspension and a cake composition are provided in which agglomeration of the active ingredient that is caused when silicone oil and/or silicone oil derivative is contained therein can be suppressed without a special treatment, such as sonication. The suspension contains, in a dispersion medium, an active ingredient of a specific mean primary particle size, and silicone oil and/or silicone oil derivative. The cake composition contains an active ingredient of a specific mean particle size, and silicone oil and/or silicone oil derivative.

Claims

exact text as granted — not AI-modified
1 . A method for preventing active ingredient particles from agglomerating in a suspension;
 the suspension containing an active ingredient and silicone oil and/or silicone oil derivative in a dispersion medium;   the active ingredient being at least one member selected from the group consisting of aripiprazole and a compound represented by structural formula (II):   
       
         
           
           
               
               
           
         
         the active ingredient being in a form of particles having a mean primary particle size of 0.1 μm or larger and smaller than 200 μm; 
         the method comprising mixing the active ingredient with the silicone oil and/or silicone oil derivative in a dispersion medium, in such a manner that the silicone oil and/or silicone oil derivative is contained in an amount of 0.001 to 0.2 weight parts relative to 100 weight parts of the active ingredient contained in the suspension. 
       
     
     
         2 . The method for preventing the active ingredient particles from agglomerating in the suspension according to  claim 1 , wherein the active ingredient is aripiprazole. 
     
     
         3 . The method for preventing the active ingredient particles from agglomerating in the suspension according to  claim 1 , wherein the active ingredient is the compound represented by structural formula (II): 
       
         
           
           
               
               
           
         
       
     
     
         4 . A suspension comprising an active ingredient and silicone oil and/or silicone oil derivative in a dispersion medium;
 the active ingredient being at least one member selected from the group consisting of aripiprazole and a compound represented by structural formula (II):   
       
         
           
           
               
               
           
         
         the active ingredient being in a form of particles and having a mean primary particle size of 0.1 μm or larger and smaller than 200 μm; and 
         the silicone oil and/or silicone oil derivative being contained in an amount of 0.001 to 0.2 weight parts relative to 100 weight parts of the active ingredient contained in the suspension. 
       
     
     
         5 . The suspension according to  claim 4 , wherein the active ingredient is aripiprazole. 
     
     
         6 . The suspension according to  claim 4 , wherein the active ingredient is the compound represented by structural formula (II): 
       
         
           
           
               
               
           
         
       
     
     
         7 . A cake composition comprising an active ingredient and silicone oil and/or silicone oil derivative;
 the active ingredient being at least one member selected from the group consisting of aripiprazole and a compound represented by structural formula (II):   
       
         
           
           
               
               
           
         
         the active ingredient being in a form of particles and having a mean particle size of 0.1 μm or larger and smaller than 200 μm; and 
         the silicone oil and/or silicone oil derivative being contained in an amount of 0.001 to 0.2 weight parts relative to 100 weight parts of the active ingredient contained in the cake composition. 
       
     
     
         8 . The cake composition according to  claim 7 , wherein the active ingredient is aripiprazole. 
     
     
         9 . The cake composition according to  claim 7 , wherein the active ingredient is the compound represented by structural formula (II):

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