AR046142A1 - PROCESO PARA FABRICAR ARIPIPRAZOL ESTERIL DE TAMANO DE PARTICULA PROMEDIO MENOR QUE 100 µM PERO MAYOR QUE 25 µM - Google Patents

PROCESO PARA FABRICAR ARIPIPRAZOL ESTERIL DE TAMANO DE PARTICULA PROMEDIO MENOR QUE 100 µM PERO MAYOR QUE 25 µM

Info

Publication number
AR046142A1
AR046142A1 ARP040103850A ARP040103850A AR046142A1 AR 046142 A1 AR046142 A1 AR 046142A1 AR P040103850 A ARP040103850 A AR P040103850A AR P040103850 A ARP040103850 A AR P040103850A AR 046142 A1 AR046142 A1 AR 046142A1
Authority
AR
Argentina
Prior art keywords
aripiprazole
particle size
jet
stream
solution
Prior art date
Application number
ARP040103850A
Other languages
English (en)
Inventor
Margaret Gleeson
Soojin Kim
Donald Kientzler
San Kiang
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34549310&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR046142(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR046142A1 publication Critical patent/AR046142A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/02—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of powders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/0004—Crystallisation cooling by heat exchange
    • B01D9/0009—Crystallisation cooling by heat exchange by direct heat exchange with added cooling fluid
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/005—Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/005—Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
    • B01D9/0054—Use of anti-solvent
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/0063—Control or regulation
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/0081—Use of vibrations, e.g. ultrasound
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
    • B01J2/02—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops
    • B01J2/06—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops in a liquid medium
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Thermal Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Un proceso para fabricar aripiprazol estéril que tiene un tamano de partícula promedio menor que 100 micrones pero preferentemente mayor que 25 micrones empleando un procedimiento de cristalización por chorros convergentes. El aripiprazol a granel resultante del tamano de partícula deseado puede ser utilizado para formar una formulación de aripiprazol secada por congelamiento, estéril, la cual durante la constitución con agua y la inyección intramuscular libera aripiprazol durante un período de al menos aproximadamente una semana y hasta aproximadamente ocho semanas. Reivindicación 1: Un proceso para preparar aripiprazol cristalino estéril de tamano de partícula pequeno deseado y de distribución estrecha de tamano de partícula caracterizado porque comprende: (a) proporcionar una corriente de chorro de una solución de aripiprazol en un solvente orgánico; (b) proporcionar una corriente de chorro de anti-solvente, el cual es capaz de iniciar la precipitación del aripiprazol de la solución; (c) provocar que la corriente de chorro de la solución de aripiprazol en el solvente y la corriente de chorro del anti-solvente choquen entre sí y se golpeen una contra la otra para crear una turbulencia elevada en su punto de impacto, cada corriente de chorro tiene una velocidad lineal suficiente para lograr un micromezclado de intensidad elevada de cada corriente previo a la nucleación, para producir una suspensión de cristales de monohidrato de aripiprazol; y (d) recuperar los cristales de monohidrato de aripiprazol de tamano de partícula pequeno deseado y de distribución estrecha de tamano de partícula. Reivindicación 15: Un proceso de preparación de aripiprazol estéril de tamano de partícula pequeno deseado y distribución estrecha de tamano, caracterizado porque comprende: (a) proporcionar una corriente de chorro de una solución de aripiprazol en etanol/agua calentada a una temperatura dentro del intervalo desde aproximadamente 70 hasta aproximadamente 85sC; (b) proporcionar una corriente de chorro de agua desionizada la cual está a una temperatura dentro del intervalo desde aproximadamente 2 hasta aproximadamente 40sC; (c) provocar que la corriente de chorro de la solución de aripiprazol en etanol y la corriente de chorro de agua, cada una a una velocidad de flujo dentro del intervalo desde aproximadamente 0,2 hasta aproximadamente 0,3 Kg/min, en donde son empleadas boquillas de chorro de diámetro interno de 0, 0508 cm (0,02 pulgadas), choquen entre sí para crear una turbulencia elevada en su punto de impacto para lograr un micromezclado de intensidad elevada de cada corriente previo a la nucleación, para formar una suspensión de cristales de monohidrato de aripiprazol; y (d) recuperar los cristales de monohidrato de aripiprazol que tienen un tamano de partícula promedio aproximadamente 95% menor que 100 micrones.
ARP040103850A 2003-10-23 2004-10-22 PROCESO PARA FABRICAR ARIPIPRAZOL ESTERIL DE TAMANO DE PARTICULA PROMEDIO MENOR QUE 100 µM PERO MAYOR QUE 25 µM AR046142A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US51388603P 2003-10-23 2003-10-23

Publications (1)

Publication Number Publication Date
AR046142A1 true AR046142A1 (es) 2005-11-23

Family

ID=34549310

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103850A AR046142A1 (es) 2003-10-23 2004-10-22 PROCESO PARA FABRICAR ARIPIPRAZOL ESTERIL DE TAMANO DE PARTICULA PROMEDIO MENOR QUE 100 µM PERO MAYOR QUE 25 µM

Country Status (16)

Country Link
US (3) US20050152981A1 (es)
EP (1) EP1675593B1 (es)
JP (1) JP4875984B2 (es)
KR (1) KR101121345B1 (es)
CN (1) CN1871007A (es)
AR (1) AR046142A1 (es)
AU (1) AU2004284904B2 (es)
BR (1) BRPI0415754A (es)
CA (1) CA2543248C (es)
CO (1) CO5670354A2 (es)
ES (1) ES2632499T3 (es)
IL (1) IL175008A (es)
MX (1) MXPA06004333A (es)
PE (1) PE20050810A1 (es)
TW (1) TWI371274B (es)
WO (1) WO2005041970A1 (es)

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US7714129B2 (en) * 2003-12-16 2010-05-11 Teva Pharmaceutical Industries Ltd. Methods of preparing anhydrous aripiprazole form II
EP1613598B1 (en) * 2003-12-16 2011-10-19 Teva Pharmaceutical Industries, Ltd. Methods of preparing aripiprazole crystalline forms
DE202005020539U1 (de) * 2004-02-05 2006-09-28 Teva Pharmaceutical Industries Ltd. Aripiprazol
US7507823B2 (en) * 2004-05-06 2009-03-24 Bristol-Myers Squibb Company Process of making aripiprazole particles
EP1812397A1 (en) * 2004-11-18 2007-08-01 Synthon B.V. Process of making crystalline aripiprazole
EP1933814A2 (en) * 2005-09-15 2008-06-25 Elan Pharma International Limited Nanoparticulate aripiprazole formulations
US8158152B2 (en) * 2005-11-18 2012-04-17 Scidose Llc Lyophilization process and products obtained thereby
JP2008537540A (ja) * 2005-12-22 2008-09-18 テバ ファーマシューティカル インダストリーズ リミティド アリピプラゾールの粒径を小さくする方法
US8420122B2 (en) 2006-04-28 2013-04-16 Merck Sharp & Dohme Corp. Process for the precipitation and isolation of 6,6-dimethyl-3-aza-bicyclo [3.1.0] hexane-amide compounds by controlled precipitation and pharmaceutical formulations containing same
SG172690A1 (en) * 2006-04-28 2011-07-28 Schering Corp Process for the precipitation and isolation of 6,6-dimethyl-3-aza-bicyclo [3.1.0] hexane-amide compounds by controlled precipitation and pharmaceutical formulations containing same
ES2401603T3 (es) * 2006-10-24 2013-04-23 Cambrex Charles City, Inc. Procedimiento para preparar aripiprazol anhidro de tipo l
CN101172966B (zh) * 2007-04-06 2012-08-29 重庆医药工业研究院有限责任公司 一种阿立哌唑微晶的制备方法
PL2170279T3 (pl) 2007-07-31 2018-05-30 Otsuka Pharmaceutical Co., Ltd. Sposoby wytwarzania zawiesiny arypiprazolu i liofilizowanej formulacji
GB0909154D0 (en) * 2008-09-25 2009-07-08 Nanomaterials Tech Pte Ltd A process for making particles for delivery of drug nanoparticles
DE102009008478A1 (de) * 2009-02-11 2010-08-19 PHAST Gesellschaft für pharmazeutische Qualitätsstandards mbH Vorrichtung und Verfahren zur Herstellung pharmazeutisch hochfeiner Partikel sowie zur Beschichtung solcher Partikel in Mikroreaktoren
CN101507908B (zh) * 2009-04-09 2010-12-01 北京化工大学 微通道套管式装置及其应用
PT2550092T (pt) * 2010-03-22 2018-11-13 Instillo Gmbh Método para produção de micro ou nanopartículas
CN101816913B (zh) * 2010-05-20 2015-10-21 吴传斌 一种微球制造方法及制造设备
MX344235B (es) 2010-08-24 2016-12-07 Otsuka Pharmaceutical Co Ltd * Suspension y composicion en torta que contiene un derivado de carbostirilo y aceite de silicona y/o un derivado de aceite de silicona.
CN107625728A (zh) 2010-10-18 2018-01-26 大日本住友制药株式会社 注射用缓释制剂
CN103327968B (zh) * 2011-01-24 2016-09-07 大塚制药株式会社 含有以阿立哌唑作为有效成分的块状组合物的医疗用器具、及以阿立哌唑作为有效成分的块状组合物
JO3410B1 (ar) * 2011-06-07 2019-10-20 Otsuka Pharma Co Ltd تركيبة أريبيبرازول مجفف بالتبريد
CN102850268B (zh) 2011-06-27 2015-07-15 上海中西制药有限公司 阿立哌唑ⅰ型微晶、阿立哌唑固体制剂及制备方法
WO2013000391A1 (zh) 2011-06-27 2013-01-03 上海中西制药有限公司 一种阿立哌唑药物制剂及其制备方法
JOP20200109A1 (ar) 2012-04-23 2017-06-16 Otsuka Pharma Co Ltd مستحضر قابل للحقن
US9732068B1 (en) * 2013-03-15 2017-08-15 GenSyn Technologies, Inc. System for crystalizing chemical compounds and methodologies for utilizing the same
AR096131A1 (es) 2013-04-30 2015-12-09 Otsuka Pharma Co Ltd Preparado oral sólido que comprende aripiprazol y un método para producir un preparado oral sólido que comprende aripiprazol
CA2959329C (en) * 2014-08-25 2023-06-27 Alkermes Pharma Ireland Limited Crystallization process of aripiprazole derivatives in extended release formulations for treatment of schizophrenia
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Also Published As

Publication number Publication date
CO5670354A2 (es) 2006-08-31
EP1675593B1 (en) 2017-05-31
US20130161848A1 (en) 2013-06-27
US9066848B2 (en) 2015-06-30
JP4875984B2 (ja) 2012-02-15
AU2004284904A1 (en) 2005-05-12
TWI371274B (en) 2012-09-01
TW200518783A (en) 2005-06-16
EP1675593A4 (en) 2007-04-25
IL175008A0 (en) 2006-08-20
MXPA06004333A (es) 2006-06-05
EP1675593A1 (en) 2006-07-05
CA2543248C (en) 2013-04-02
CA2543248A1 (en) 2005-05-12
US20110166352A1 (en) 2011-07-07
PE20050810A1 (es) 2005-09-25
KR20070090070A (ko) 2007-09-05
BRPI0415754A (pt) 2006-12-19
AU2004284904B2 (en) 2010-05-20
ES2632499T3 (es) 2017-09-13
US20050152981A1 (en) 2005-07-14
JP2007509153A (ja) 2007-04-12
CN1871007A (zh) 2006-11-29
WO2005041970A1 (en) 2005-05-12
IL175008A (en) 2014-11-30
KR101121345B1 (ko) 2012-03-09

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