Method for producing fine particles of aripiprazole anhydride crystals b

Method for producing fine particles of aripiprazole anhydride crystals b

Disclosed herein is a method for producing fine particles of aripiprazole anhydride crystals B less than 50 µm in size, comprising the steps of: (a) heating and dissolving crude aripiprazole in a lower alcohol selected from the group consisting of methanol and ethanol, and subsequently cooling the r...

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Hauptverfasser: YANO KATSUHIKO, AOKI SATOSHI, BANDO TAKUJI, FUKANA MAKOTO
Format: Patent
Sprache:eng
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator YANO KATSUHIKO
AOKI SATOSHI
BANDO TAKUJI
FUKANA MAKOTO
description Disclosed herein is a method for producing fine particles of aripiprazole anhydride crystals B less than 50 µm in size, comprising the steps of: (a) heating and dissolving crude aripiprazole in a lower alcohol selected from the group consisting of methanol and ethanol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (b) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (c) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals to dry. In one embodiment the volume average particle size of the wet-milled crystals in step (b) is 15 to 20 µm. Aripiprazole is known as 7-{ 4-[4-(2,3-dichlorophenyl)-I-piperazinyl]butoxy} -3,4-dihydrocarbostyril or 7-{ 4-[4-(2,3-dichlorophenyl)-Ipiperazinyl]butoxy} -3,4-dihydro-2(IH)-quinolinone.
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In one embodiment the volume average particle size of the wet-milled crystals in step (b) is 15 to 20 µm. Aripiprazole is known as 7-{ 4-[4-(2,3-dichlorophenyl)-I-piperazinyl]butoxy} -3,4-dihydrocarbostyril or 7-{ 4-[4-(2,3-dichlorophenyl)-Ipiperazinyl]butoxy} -3,4-dihydro-2(IH)-quinolinone.</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2015</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20150828&amp;DB=EPODOC&amp;CC=NZ&amp;NR=620429A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20150828&amp;DB=EPODOC&amp;CC=NZ&amp;NR=620429A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>YANO KATSUHIKO</creatorcontrib><creatorcontrib>AOKI SATOSHI</creatorcontrib><creatorcontrib>BANDO TAKUJI</creatorcontrib><creatorcontrib>FUKANA MAKOTO</creatorcontrib><title>Method for producing fine particles of aripiprazole anhydride crystals b</title><description>Disclosed herein is a method for producing fine particles of aripiprazole anhydride crystals B less than 50 µm in size, comprising the steps of: (a) heating and dissolving crude aripiprazole in a lower alcohol selected from the group consisting of methanol and ethanol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (b) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (c) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals to dry. 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In one embodiment the volume average particle size of the wet-milled crystals in step (b) is 15 to 20 µm. Aripiprazole is known as 7-{ 4-[4-(2,3-dichlorophenyl)-I-piperazinyl]butoxy} -3,4-dihydrocarbostyril or 7-{ 4-[4-(2,3-dichlorophenyl)-Ipiperazinyl]butoxy} -3,4-dihydro-2(IH)-quinolinone.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Method for producing fine particles of aripiprazole anhydride crystals b
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