Oral solid preparation comprising aripiprazole and method for producing oral solid preparation comprising aripiprazole

Abstract

[Object] An object of the present invention is to provide an oral solid preparation that can be produced in a simpler manner than conventional methods, that exhibits high bioavailability and high dissolubility even in persons having low stomach acid, and that can also ensure dissolubility after being allowed to stand for a certain period of time. Another object is to provide a simple method for producing the oral solid preparation. [Means for Achieving the Object] The present invention relates to an oral solid preparation comprising, as an active ingredient, a finely milled crystal obtained by milling an aripiprazole hydrate crystal, and a pharmaceutically acceptable carrier, the finely milled crystal having a mean particle size of 15 μm or less; and a method for producing an oral solid preparation comprising the steps of ( 1 ) milling an aripiprazole hydrate crystal into a finely milled crystal having a mean particle size of 15 μm or less, and ( 2 ) mixing the obtained finely milled crystal with a pharmaceutically acceptable carrier.

1 - 7 . (canceled) 
     
     
         8 . A method for treating schizophrenia, intractable (drug-resistant, chronic) schizophrenia with cognitive impairment and intractable (drug-resistant, chronic) schizophrenia without cognitive impairment; mania, acute mania bipolar disorder acute mania; bipolar disorder; depression, bipolar disorder depression; autism, Down's syndrome, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease, Parkinson's disease; panic, obsessive compulsive disorder (OCD), alcohol and drug dependency, vomiting, motion sickness, obesity, migraine, cognitive impairment; major depression, behavioral and psychological symptoms of dementia (BPSD), Tourette's syndrome, bulimia nervosa, and chronic pain/fibromyalgia/chronic fatigue syndrome,
 the method comprising orally administering to a patient in need thereof an oral solid preparation,   the oral solid preparation comprising a finely milled aripiprazole hydrate crystal and a pharmaceutically acceptable carrier,   the finely milled aripiprazole hydrate crystal having a mean particle size of 1 to 10 μm, and   the oral solid preparation being in the form of a tablet, flash-melt tablet, pill, powder, granule or capsule.   
     
     
         9 . The method according to  claim 8 , wherein the aripiprazole hydrate crystal is aripiprazole hydrate A,
 wherein the aripiprazole hydrate A has an endothermic curve comprising a small endothermic peak at about 71° C. and a gradual endothermic peak around 60-120° C. in a thermogravimetric/differential thermal analysis measured at a heating rate of 5° C /min.   
     
     
         10 . The method according to  claim 8 , wherein the finely milled aripiprazole hydrate crystal has a mean particle size of 1 to 5 μm. 
     
     
         11 . The method according to  claim 9 , wherein the finely milled aripiprazole hydrate crystal has a mean particle size of 1 to 5 μm. 
     
     
         12 . The method according to  claim 8 , wherein the finely milled aripiprazole hydrate crystal has a mean particle size of 2.5 to 10 μm. 
     
     
         13 . The method according to  claim 9 , wherein the finely milled aripiprazole hydrate crystal has a mean particle size of 2.5 to 10 μm. 
     
     
         14 . The method according to  claim 8 , wherein the oral solid preparation is in the form of a tablet, pill, granule, or capsule. 
     
     
         15 . The method according to  claim 9 , wherein the oral solid preparation is in the form of a tablet, pill, granule, or capsule.