Method for producing pulverized organic compound particle

Abstract

Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poor water solubility organic compound particle for medical use, which is characterized in that a poor water solubility organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poor water solubility organic compound particle for medical use, which is produced by such a production method.

1 - 12 . (canceled) 
     
     
         13 . Poorly water-soluble organic compound fine particles for medical use, which has a melting point or a decomposition point in the range of 80 to 350 degrees C., is crystalline and has an average diameter of 600 nm or less. 
     
     
         14 . Poorly water-soluble organic compound fine particles for medical use according to  claim 13 ,
 wherein content of fine particles of 0.2 micron or less in diameter in pulverized organic compound particles is 70% or more.   
     
     
         15 . Poorly water-soluble organic compound fine particles for medical use according to  claim 13 ,
 wherein 90% diameter of the poorly water-soluble organic compound fine particles for medical use is 600 nm or less.   
     
     
         16 . Poorly water-soluble organic compound fine particles for medical use according to  claim 13 ,
 wherein the poorly water-soluble organic compound includes no surface active agent.   
     
     
         17 . Poorly water-soluble organic compound fine particles for medical use according to  claim 13 ,
 wherein the poorly water-soluble organic compound is one or more organic compounds selected from the group consisting of nifedipine, nicardipine, nimodipine, dipyridamole, diisopyramide, prazosin hydrochloride, prednisolone, cortisone acetate, dexamethasone, betamethasone, beclometasone dipropionate, fluticasone propionate, budesonide, fluocinolone acetonide, indomethacin, naproxen, ketoprofen, 7-[(3,5-dimethoxy-4-hydroxycinnamoyl)amino]-3-octyloxy-4-hydroxy-1-methyl-2(1H)-quinolinone, phenyloin, phenacemide, ethotoin, primidone, diazepam, nitrazepam, clonazepam, digitoxin, spironolactone, triamterene, chlorthalidone, polythiazide, benzthiazide, griseofulvin, nalidixic acid, chloramphenicol, chlorzoxazone, phenprobamate, mequitazine, bisbentiamin, mitomycin C, bicalutamide, paclitaxel, ubenimex, dacarbazine, fluconazole, miconazole, rifampicin, triamcinolone acetonide, clemastine fumarate, pranlukast hydrate, zafirlukast, fenofibrate, dihydroxybenzophenone, dihydrocholesterol, beta-carotene, propyl gallate, cinnamic acid, saccharin, folic acid and maltol.