Method for producing fine particles of aripiprazole anhydride crystals B

US9278934B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9278934-B2
Application numberUS-201214128305-A
CountryUS
Kind codeB2
Filing dateJun 29, 2012
Priority dateJun 29, 2011
Publication dateMar 8, 2016
Grant dateMar 8, 2016

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Abstract

Official abstract text for this publication.

The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.

First claim

Opening claim text (preview).

The invention claimed is: 1. A method for producing fine particles of aripiprazole anhydride crystals B, the method comprising the steps of: (a) heating and dissolving crude aripiprazole in a lower alcohol, 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. 2. The production method according to claim 1 , wherein the volume average particle size of the obtained fine particles of aripiprazole anhydride crystals B is less than 50 μm. 3. The production method according to claim 1 or 2 , wherein the lower alcohol is methanol or ethanol. 4. The production method according to claim 3 , wherein the lower alcohol is ethanol. 5. The production method according to claim 4 , wherein the lower alcohol substantially contains no water. 6. The production method according to claim 5 , wherein the water content in the lower alcohol is less than 10 vol %. 7. The production method according to claim 6 , wherein the volume average particle size of the wet-milled crystals in step (b) is less than 50 μm. 8. The production method according to claim 7 , wherein the volume average particle size of the wet-milled crystals in step (b) is 15 to 20 μm. 9. The production method according to claim 1 or 2 , wherein the heating temperature in step (c) is in the range near the boiling point of the lower alcohol to about 125° C. 10. The production method according to claim 1 or 2 , wherein the lower alcohol is ethanol, and the heating temperature in step (c) is in the range of about 78 to 125° C.

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Classifications

  • Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title

  • C07D215/22Primary

    attached in position 2 or 4 · CPC title

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What does patent US9278934B2 cover?
The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcoh…
Who is the assignee on this patent?
Bando Takuji, Yano Katsuhiko, Fukana Makoto, and 2 more
What technology area does this patent fall under?
Primary CPC classification C07D215/22. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Mar 08 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).