CA2379005A1 - Forme faiblement hygroscopique d'aripiprazole et methodes de preparation - Google Patents

Forme faiblement hygroscopique d'aripiprazole et methodes de preparation Download PDF

Info

Publication number: CA2379005A1
Authority: CA; Canada
Prior art keywords: aripiprazole; hydrate; anhydride crystals; aripiprazole anhydride; crystals
Prior art date: 2001-09-25
Legal status (The legal status 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 status listed.): Abandoned

Application number

CA 2379005

Other languages

English (en)

Inventor

Yoshihiro Nishioka

Tsutomu Fujimura

Takuji Bando

Noriyuki Kobayashi

Makoto Ishigami

Youichi Taniguchi

Tsuyoshi Yabuuchi

Satoshi Aoki

Junichi Kawasaki

Kiyoshi Fujimoto

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Otsuka Pharmaceutical Co Ltd

Original Assignee

Otsuka Pharmaceutical Co Ltd

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.)

2001-09-25

Filing date

2002-03-27

Publication date

2003-03-25

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=19112920&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2379005(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2002-03-27 Application filed by Otsuka Pharmaceutical Co Ltd filed Critical Otsuka Pharmaceutical Co Ltd

2002-09-18 Priority to ARP020103511A priority Critical patent/AR033485A1/es

2002-09-20 Priority to PE2008001435A priority patent/PE20090124A1/es

2002-09-20 Priority to PE2002000922A priority patent/PE20030445A1/es

2002-09-20 Priority to MYPI20023512A priority patent/MY138669A/en

2002-09-23 Priority to TW091121771A priority patent/TWI318572B/zh

2002-09-23 Priority to TW098116881A priority patent/TWI332839B/zh

2002-09-25 Priority to KR10-2004-7007990A priority patent/KR100530731B1/ko

2002-09-25 Priority to CNA2008101254086A priority patent/CN101423493A/zh

2002-09-25 Priority to CA2713466A priority patent/CA2713466C/fr

2002-09-25 Priority to PT08000360T priority patent/PT1927357E/pt

2002-09-25 Priority to UAA200612812 priority patent/UA84764C2/uk

2002-09-25 Priority to EP08000359A priority patent/EP1927356B1/fr

2002-09-25 Priority to DK08000357.7T priority patent/DK1927355T3/da

2002-09-25 Priority to CN2008101254071A priority patent/CN101423492B/zh

2002-09-25 Priority to CN201410053920.XA priority patent/CN103751119A/zh

2002-09-25 Priority to DK08000359.3T priority patent/DK1927356T3/da

2002-09-25 Priority to CN201710019464.0A priority patent/CN106692151A/zh

2002-09-25 Priority to LTEP08000358.5T priority patent/LT1925308T/lt

2002-09-25 Priority to IL15383802A priority patent/IL153838A0/xx

2002-09-25 Priority to PL393607A priority patent/PL393607A1/pl

2002-09-25 Priority to AT04002427T priority patent/ATE464050T1/de

2002-09-25 Priority to CN2008101254103A priority patent/CN101434574B/zh

2002-09-25 Priority to CN201610186509.9A priority patent/CN105832677A/zh

2002-09-25 Priority to AT08000357T priority patent/ATE465736T1/de

2002-09-25 Priority to PT08000359T priority patent/PT1927356E/pt

2002-09-25 Priority to CN02801754A priority patent/CN1463191A/zh

2002-09-25 Priority to EP08000358.5A priority patent/EP1925308B1/fr

2002-09-25 Priority to GEAP2002005101 priority patent/GEP20053457B/en

2002-09-25 Priority to DE60236231T priority patent/DE60236231D1/de

2002-09-25 Priority to ES04002427.5T priority patent/ES2343179T5/es

2002-09-25 Priority to CA002688860A priority patent/CA2688860A1/fr

2002-09-25 Priority to CNA2008101254118A priority patent/CN101434575A/zh

2002-09-25 Priority to AT08000359T priority patent/ATE465737T1/de

2002-09-25 Priority to SI200230906T priority patent/SI1927357T1/sl

2002-09-25 Priority to DK04002427.5T priority patent/DK1419776T4/en

2002-09-25 Priority to ES08000360T priority patent/ES2343602T3/es

2002-09-25 Priority to DE60236383T priority patent/DE60236383D1/de

2002-09-25 Priority to SI200230903T priority patent/SI1419776T2/sl

2002-09-25 Priority to CN2009101474911A priority patent/CN101574348B/zh

2002-09-25 Priority to CN2009101474930A priority patent/CN101579344B/zh

2002-09-25 Priority to CN201610811822.7A priority patent/CN106420627A/zh

2002-09-25 Priority to CN201410053617.XA priority patent/CN103751118A/zh

2002-09-25 Priority to CNA2005100785991A priority patent/CN1699346A/zh

2002-09-25 Priority to JP2002279085A priority patent/JP3760264B2/ja

2002-09-25 Priority to RU2003101334/15A priority patent/RU2259366C2/ru

2002-09-25 Priority to SI200230337T priority patent/SI1330249T1/sl

2002-09-25 Priority to PT80003585T priority patent/PT1925308T/pt

2002-09-25 Priority to PCT/JP2002/009858 priority patent/WO2003026659A1/fr

2002-09-25 Priority to DK08000360.1T priority patent/DK1927357T3/da

2002-09-25 Priority to CN201310728318.7A priority patent/CN103755632B/zh

2002-09-25 Priority to ES08000358.5T priority patent/ES2596354T3/es

2002-09-25 Priority to CN201310191361.4A priority patent/CN103288727B/zh

2002-09-25 Priority to CN201410053619.9A priority patent/CN103751093A/zh

2002-09-25 Priority to AT02782507T priority patent/ATE322269T1/de

2002-09-25 Priority to EP08000360A priority patent/EP1927357B1/fr

2002-09-25 Priority to PT02782507T priority patent/PT1330249E/pt

2002-09-25 Priority to CN2013100996412A priority patent/CN103191118A/zh

2002-09-25 Priority to EP04002427.5A priority patent/EP1419776B2/fr

2002-09-25 Priority to CN201510615759.5A priority patent/CN105267151A/zh

2002-09-25 Priority to CA2689051A priority patent/CA2689051C/fr

2002-09-25 Priority to PT04002427T priority patent/PT1419776E/pt

2002-09-25 Priority to CN2012100054661A priority patent/CN102579446A/zh

2002-09-25 Priority to PL393598A priority patent/PL221521B1/pl

2002-09-25 Priority to EP02782507A priority patent/EP1330249B1/fr

2002-09-25 Priority to AU2002334413A priority patent/AU2002334413C1/en

2002-09-25 Priority to MXPA03000440A priority patent/MXPA03000440A/es

2002-09-25 Priority to CN201410466919.XA priority patent/CN104306337A/zh

2002-09-25 Priority to KR10-2003-7000818A priority patent/KR100490222B1/ko

2002-09-25 Priority to EP16169141.5A priority patent/EP3081216A1/fr

2002-09-25 Priority to CN201510333215.XA priority patent/CN104945321A/zh

2002-09-25 Priority to AT08000360T priority patent/ATE467416T1/de

2002-09-25 Priority to CN200910266341A priority patent/CN101792415A/zh

2002-09-25 Priority to ES08000357T priority patent/ES2343219T3/es

2002-09-25 Priority to UA2003010503A priority patent/UA80802C2/xx

2002-09-25 Priority to DK08000358.5T priority patent/DK1925308T3/en

2002-09-25 Priority to PL360900A priority patent/PL225415B1/pl

2002-09-25 Priority to CA2689052A priority patent/CA2689052C/fr

2002-09-25 Priority to PL417178A priority patent/PL230869B1/pl

2002-09-25 Priority to CN2008101254090A priority patent/CN101434573B/zh

2002-09-25 Priority to CN200610006215XA priority patent/CN1817882B/zh

2002-09-25 Priority to SI200230905T priority patent/SI1927355T1/sl

2002-09-25 Priority to CN2009101474907A priority patent/CN101574347B/zh

2002-09-25 Priority to PL393603A priority patent/PL221536B1/pl

2002-09-25 Priority to CA2688934A priority patent/CA2688934C/fr

2002-09-25 Priority to CA2426921A priority patent/CA2426921C/fr

2002-09-25 Priority to ES02782507T priority patent/ES2261750T3/es

2002-09-25 Priority to ES08000359T priority patent/ES2343220T3/es

2002-09-25 Priority to HU0600141A priority patent/HUP0600141A3/hu

2002-09-25 Priority to DE60236229T priority patent/DE60236229D1/de

2002-09-25 Priority to PL393596A priority patent/PL393596A1/pl

2002-09-25 Priority to EP08000357A priority patent/EP1927355B1/fr

2002-09-25 Priority to CN2009101474926A priority patent/CN101579343B/zh

2002-09-25 Priority to PL393601A priority patent/PL219565B1/pl

2002-09-25 Priority to DK02782507T priority patent/DK1330249T3/da

2002-09-25 Priority to DE60235995T priority patent/DE60235995D1/de

2002-09-25 Priority to CA2688915A priority patent/CA2688915C/fr

2002-09-25 Priority to PT08000357T priority patent/PT1927355E/pt

2002-09-25 Priority to CN201610811281.8A priority patent/CN106420640A/zh

2002-09-25 Priority to BR0205391-8A priority patent/BR0205391A/pt

2002-09-25 Priority to US10/333,244 priority patent/US20040058935A1/en

2002-09-25 Priority to PL393608A priority patent/PL219564B1/pl

2002-09-25 Priority to SI200230904T priority patent/SI1927356T1/sl

2002-09-25 Priority to CN201410468156.2A priority patent/CN104306374A/zh

2002-09-25 Priority to DE60210409T priority patent/DE60210409T2/de

2003-01-07 Priority to IL153838A priority patent/IL153838A/en

2003-01-17 Priority to NO20030247A priority patent/NO328134B1/no

2003-03-25 Publication of CA2379005A1 publication Critical patent/CA2379005A1/fr

2004-04-22 Priority to HK16111449.6A priority patent/HK1223043A1/zh

2004-04-22 Priority to HK15103617.0A priority patent/HK1203060A1/xx

2004-04-22 Priority to HK15103616.1A priority patent/HK1203059A1/xx

2004-05-26 Priority to JP2004156130A priority patent/JP3750023B2/ja

2005-11-25 Priority to JP2005341187A priority patent/JP4614870B2/ja

2006-09-08 Priority to ARP060103919A priority patent/AR056503A2/es

2006-12-14 Priority to HK06113738.4A priority patent/HK1092808B/xx

2007-04-26 Priority to US11/790,603 priority patent/US20070213343A1/en

2007-04-26 Priority to US11/790,604 priority patent/US8399469B2/en

2007-04-26 Priority to US11/790,605 priority patent/US8017615B2/en

2007-04-26 Priority to US11/790,606 priority patent/US7910589B2/en

2007-04-30 Priority to US11/797,024 priority patent/US20070203151A1/en

2007-04-30 Priority to US11/797,030 priority patent/US20070203152A1/en

2007-04-30 Priority to US11/797,019 priority patent/US20070203150A1/en

2007-12-27 Priority to IL188455A priority patent/IL188455A0/en

2008-04-02 Priority to NO20081626A priority patent/NO336264B1/no

2008-04-02 Priority to NO20081632A priority patent/NO336262B1/no

2008-04-02 Priority to NO20081631A priority patent/NO336263B1/no

2008-04-02 Priority to NO20081633A priority patent/NO20081633L/no

2008-04-02 Priority to NO20081627A priority patent/NO336265B1/no

2009-04-28 Priority to NO20091689A priority patent/NO336679B1/no

2009-08-21 Priority to ARP090103228A priority patent/AR073111A2/es

2009-08-21 Priority to HK09107688.3A priority patent/HK1129889B/xx

2009-08-21 Priority to HK09107690.9A priority patent/HK1129891B/xx

2010-01-21 Priority to HK10100649.3A priority patent/HK1136960B/xx

2010-01-21 Priority to HK10100650.9A priority patent/HK1136961B/xx

2010-01-21 Priority to HK10100635.9A priority patent/HK1136958B/xx

2010-01-21 Priority to HK10100638.6A priority patent/HK1136959B/xx

2010-03-24 Priority to IL204707A priority patent/IL204707A/en

2010-04-23 Priority to CL2010000405A priority patent/CL2010000405A1/es

2010-06-11 Priority to CY20101100529T priority patent/CY1110208T1/el

2010-06-11 Priority to CY20101100531T priority patent/CY1110070T1/el

2010-06-11 Priority to CY20101100530T priority patent/CY1110212T1/el

2010-07-05 Priority to ARP100102387A priority patent/AR077635A2/es

2010-07-05 Priority to CY20101100614T priority patent/CY1110244T1/el

2011-06-23 Priority to US13/067,750 priority patent/US8642760B2/en

2011-06-29 Priority to US13/067,838 priority patent/US8901303B2/en

2011-08-25 Priority to US13/217,636 priority patent/US8703772B2/en

2012-01-13 Priority to US13/350,117 priority patent/US8580796B2/en

2012-05-21 Priority to US13/476,758 priority patent/US8901130B2/en

2012-05-21 Priority to US13/476,773 priority patent/US8703773B2/en

2012-08-15 Priority to ARP120102986A priority patent/AR087544A2/es

2013-01-25 Priority to US13/749,753 priority patent/US8993761B2/en

2013-04-23 Priority to IL225902A priority patent/IL225902A0/en

2013-10-09 Priority to US14/049,777 priority patent/US9359302B2/en

2013-12-31 Priority to HK13114439.5A priority patent/HK1187048B/xx

2014-04-08 Priority to PH12014500782A priority patent/PH12014500782A1/en

2014-09-19 Priority to HK14109483.9A priority patent/HK1196128B/xx

2014-09-22 Priority to IL234770A priority patent/IL234770A0/en

2014-10-06 Priority to NO20141193A priority patent/NO337844B1/no

2015-02-18 Priority to US14/624,595 priority patent/US10150735B2/en

2015-11-13 Priority to HK15111240.8A priority patent/HK1210468A1/xx

2016-03-23 Priority to HK16103439.5A priority patent/HK1215397A1/zh

2016-05-09 Priority to US15/149,522 priority patent/US20160251315A1/en

2016-11-03 Priority to CY20161101119T priority patent/CY1118195T1/el

2018-10-24 Priority to US16/169,255 priority patent/US20190225584A1/en

2019-12-18 Priority to US16/718,281 priority patent/US20200123110A1/en

2021-01-28 Priority to US17/160,716 priority patent/US20210395204A1/en

Status Abandoned legal-status Critical Current

Links

229960004372 aripiprazole Drugs 0.000 title claims abstract description 271
CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 title claims abstract description 133
238000000034 method Methods 0.000 title claims abstract description 93
238000002360 preparation method Methods 0.000 title claims abstract description 36
239000008186 active pharmaceutical agent Substances 0.000 title claims description 55
229940088679 drug related substance Drugs 0.000 title claims description 55
239000013078 crystal Substances 0.000 claims abstract description 167
-1 aripiprazole anhydride Chemical class 0.000 claims abstract description 144
238000010438 heat treatment Methods 0.000 claims description 83
239000002245 particle Substances 0.000 claims description 35
238000001228 spectrum Methods 0.000 claims description 34
238000000634 powder X-ray diffraction Methods 0.000 claims description 30
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 29
239000003826 tablet Substances 0.000 claims description 29
238000003801 milling Methods 0.000 claims description 28
150000008064 anhydrides Chemical class 0.000 claims description 16
239000003937 drug carrier Substances 0.000 claims description 16
239000007787 solid Substances 0.000 claims description 16
239000003814 drug Substances 0.000 claims description 14
229940079593 drug Drugs 0.000 claims description 12
201000000980 schizophrenia Diseases 0.000 claims description 12
238000010521 absorption reaction Methods 0.000 claims description 9
238000004455 differential thermal analysis Methods 0.000 claims description 9
238000002411 thermogravimetry Methods 0.000 claims description 8
208000028698 Cognitive impairment Diseases 0.000 claims description 6
208000010877 cognitive disease Diseases 0.000 claims description 6
238000000113 differential scanning calorimetry Methods 0.000 claims description 5
208000020925 Bipolar disease Diseases 0.000 claims description 4
206010026749 Mania Diseases 0.000 claims description 4
208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 4
230000001684 chronic effect Effects 0.000 claims description 4
208000024827 Alzheimer disease Diseases 0.000 claims description 3
208000019901 Anxiety disease Diseases 0.000 claims description 3
230000036506 anxiety Effects 0.000 claims description 3
208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 2
206010003805 Autism Diseases 0.000 claims description 2
208000020706 Autistic disease Diseases 0.000 claims description 2
201000010374 Down Syndrome Diseases 0.000 claims description 2
206010019233 Headaches Diseases 0.000 claims description 2
208000008589 Obesity Diseases 0.000 claims description 2
208000018737 Parkinson disease Diseases 0.000 claims description 2
201000001880 Sexual dysfunction Diseases 0.000 claims description 2
206010044688 Trisomy 21 Diseases 0.000 claims description 2
206010047700 Vomiting Diseases 0.000 claims description 2
238000004458 analytical method Methods 0.000 claims description 2
239000003085 diluting agent Substances 0.000 claims description 2
231100000869 headache Toxicity 0.000 claims description 2
201000003152 motion sickness Diseases 0.000 claims description 2
230000004770 neurodegeneration Effects 0.000 claims description 2
208000015122 neurodegenerative disease Diseases 0.000 claims description 2
235000020824 obesity Nutrition 0.000 claims description 2
231100000872 sexual dysfunction Toxicity 0.000 claims description 2
208000019116 sleep disease Diseases 0.000 claims description 2
230000008673 vomiting Effects 0.000 claims description 2
208000024891 symptom Diseases 0.000 claims 4
230000001747 exhibiting effect Effects 0.000 claims 2
239000007935 oral tablet Substances 0.000 claims 2
229940096978 oral tablet Drugs 0.000 claims 2
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
208000035475 disorder Diseases 0.000 claims 1
239000000203 mixture Substances 0.000 description 63
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 40
238000009472 formulation Methods 0.000 description 38
235000019359 magnesium stearate Nutrition 0.000 description 20
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 19
IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 18
239000000843 powder Substances 0.000 description 17
IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 16
238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 14
239000004615 ingredient Substances 0.000 description 12
WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 11
229960000913 crospovidone Drugs 0.000 description 11
235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 11
229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 11
229920002472 Starch Polymers 0.000 description 8
239000008107 starch Substances 0.000 description 8
235000019698 starch Nutrition 0.000 description 8
238000002844 melting Methods 0.000 description 7
230000008018 melting Effects 0.000 description 7
239000002904 solvent Substances 0.000 description 7
HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 7
239000000969 carrier Substances 0.000 description 6
239000008187 granular material Substances 0.000 description 6
238000012545 processing Methods 0.000 description 6
239000000126 substance Substances 0.000 description 6
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 5
239000000378 calcium silicate Substances 0.000 description 5
229910052918 calcium silicate Inorganic materials 0.000 description 5
OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 5
230000018044 dehydration Effects 0.000 description 5
238000006297 dehydration reaction Methods 0.000 description 5
239000008101 lactose Substances 0.000 description 5
239000000725 suspension Substances 0.000 description 5
WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 4
108010011485 Aspartame Proteins 0.000 description 4
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
108010010803 Gelatin Proteins 0.000 description 4
244000007021 Prunus avium Species 0.000 description 4
235000010401 Prunus avium Nutrition 0.000 description 4
235000014441 Prunus serotina Nutrition 0.000 description 4
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 4
TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 4
239000000619 acesulfame-K Substances 0.000 description 4
239000000605 aspartame Substances 0.000 description 4
235000010357 aspartame Nutrition 0.000 description 4
IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 4
229960003438 aspartame Drugs 0.000 description 4
HEBKCHPVOIAQTA-NGQZWQHPSA-N d-xylitol Chemical compound OC[C@H](O)C(O)[C@H](O)CO HEBKCHPVOIAQTA-NGQZWQHPSA-N 0.000 description 4
238000005516 engineering process Methods 0.000 description 4
239000008273 gelatin Substances 0.000 description 4
229920000159 gelatin Polymers 0.000 description 4
235000019322 gelatine Nutrition 0.000 description 4
235000011852 gelatine desserts Nutrition 0.000 description 4
239000007788 liquid Substances 0.000 description 4
HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 4
239000000243 solution Substances 0.000 description 4
235000002906 tartaric acid Nutrition 0.000 description 4
239000011975 tartaric acid Substances 0.000 description 4
239000000811 xylitol Substances 0.000 description 4
235000010447 xylitol Nutrition 0.000 description 4
229960002675 xylitol Drugs 0.000 description 4
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 3
239000005995 Aluminium silicate Substances 0.000 description 3
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
244000299461 Theobroma cacao Species 0.000 description 3
235000005764 Theobroma cacao ssp. cacao Nutrition 0.000 description 3
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229910052749 magnesium Inorganic materials 0.000 description 1
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DHRRIBDTHFBPNG-UHFFFAOYSA-L magnesium dichloride hexahydrate Chemical compound O.O.O.O.O.O.[Mg+2].[Cl-].[Cl-] DHRRIBDTHFBPNG-UHFFFAOYSA-L 0.000 description 1
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229910000027 potassium carbonate Inorganic materials 0.000 description 1
229910000160 potassium phosphate Inorganic materials 0.000 description 1
235000011009 potassium phosphates Nutrition 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
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229940113147 shellac Drugs 0.000 description 1
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235000010413 sodium alginate Nutrition 0.000 description 1
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229940005550 sodium alginate Drugs 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
235000002639 sodium chloride Nutrition 0.000 description 1
235000009518 sodium iodide Nutrition 0.000 description 1
239000007901 soft capsule Substances 0.000 description 1
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239000007940 sugar coated tablet Substances 0.000 description 1
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235000012222 talc Nutrition 0.000 description 1
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YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
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239000008158 vegetable oil Substances 0.000 description 1
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NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1

Landscapes

Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Saccharide Compounds (AREA)

CA 2379005 2001-09-25 2002-03-27 Forme faiblement hygroscopique d'aripiprazole et methodes de preparation Abandoned CA2379005A1 (fr)

Priority Applications (164)

Application Number	Priority Date	Filing Date	Title
ARP020103511A AR033485A1 (es)	2001-09-25	2002-09-18	Sustancia medicinal de aripiprazol de baja higroscopicidad y proceso para la preparacion de la misma
PE2008001435A PE20090124A1 (es)	2001-09-25	2002-09-20	Composicion farmaceutica que comprende cristales de aripiprazol b de baja higroscopicidad y procedimiento de preparacion de la misma
PE2002000922A PE20030445A1 (es)	2001-09-25	2002-09-20	Sustancia medicinal de aripiprazol de baja higroscopicidad y proceso para la preparacion de la misma
MYPI20023512A MY138669A (en)	2001-09-25	2002-09-20	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
TW091121771A TWI318572B (en)	2001-09-25	2002-09-23	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
TW098116881A TWI332839B (en)	2001-09-25	2002-09-23	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
KR10-2004-7007990A KR100530731B1 (ko)	2001-09-25	2002-09-25	저흡습성 아리피프라졸 약물 물질 및 이의 제조 방법
CNA2008101254086A CN101423493A (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
CA2713466A CA2713466C (fr)	2001-09-25	2002-09-25	Substance pharmaceutique d'aripiprazole faiblement hygroscopique et methodes de preparation associees
PT08000360T PT1927357E (pt)	2001-09-25	2002-09-25	Substância de fármaco aripiprazole (cristal e) com baixa higroscopicidade e processos para a sua preparação
UAA200612812 UA84764C2 (en)	2001-09-25	2002-09-25	Low hygroscopic aripiprazole drug substance and process for the preparation thereof
EP08000359A EP1927356B1 (fr)	2001-09-25	2002-09-25	Médicament à base d'aripiprazole (crystal D) de faible hygroscopie et son procédé de préparation
DK08000357.7T DK1927355T3 (da)	2001-09-25	2002-09-25	Medikamentsubstans med lav hygroskopisk aripiprazol (krystal F) og fremgangsmåder til fremstilling deraf
CN2008101254071A CN101423492B (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
CN201410053920.XA CN103751119A (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
DK08000359.3T DK1927356T3 (da)	2001-09-25	2002-09-25	Medikamentsubstans med lav hygroskopisk aripiprazol (krystal D) og fremgangsmåder til fremstilling deraf
CN201710019464.0A CN106692151A (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
LTEP08000358.5T LT1925308T (lt)	2001-09-25	2002-09-25	Kietas peroralinis aripiprazolio farmacinis preparatas ir jo gavimo būdai
IL15383802A IL153838A0 (en)	2001-09-25	2002-09-25	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
PL393607A PL393607A1 (pl)	2001-09-25	2002-09-25	Sposób wytwarzania granulek farmaceutycznego stałego preparat doustnego i sposób wytwarzania farmaceutycznego stałego preparatu doustnego oraz farmaceutyczny stały preparat doustny
AT04002427T ATE464050T1 (de)	2001-09-25	2002-09-25	Aripiprazole wirkstoff mit niedriger hygroskopie und verfahren zu ihrer herstellung
CN2008101254103A CN101434574B (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
CN201610186509.9A CN105832677A (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
AT08000357T ATE465736T1 (de)	2001-09-25	2002-09-25	Gering hygroskopische aripiprazol-substanz (kristal f) und herstellungsverfahren
PT08000359T PT1927356E (pt)	2001-09-25	2002-09-25	Substância de fármaco aripiprazole (cristal d) com baixa higroscopicidade e processos para a sua preparação
CN02801754A CN1463191A (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
EP08000358.5A EP1925308B1 (fr)	2001-09-25	2002-09-25	Préparation pharmaceutique orale solide d'aripiprazole et ses procédés de préparation
GEAP2002005101 GEP20053457B (en)	2001-09-25	2002-09-25	Low Hygroscopic Aripiprazole Drug Substance and Processes for Preparation Thereof
DE60236231T DE60236231D1 (de)	2001-09-25	2002-09-25	Gering hygroskopische Aripiprazol-Substanz (Kristal D) und Herstellungsverfahren
ES04002427.5T ES2343179T5 (es)	2001-09-25	2002-09-25	Sustancia farmacéutica de aripiprazol con higroscopicidad reducida y método de preparación de la misma
CA002688860A CA2688860A1 (fr)	2001-09-25	2002-09-25	Substance pharmaceutique d'aripiprazole faiblement hygroscopique et methodes de preparation associees
CNA2008101254118A CN101434575A (zh)	2001-09-25	2002-09-25	低吸湿性阿立哌唑药物及其制备方法
AT08000359T ATE465737T1 (de)	2001-09-25	2002-09-25	Gering hygroskopische aripiprazol-substanz (kristal d) und herstellungsverfahren
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JP2001-290645		2001-09-25

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CA2379005A1 true CA2379005A1 (fr)	2003-03-25

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Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CA 2379005 Abandoned CA2379005A1 (fr)	2001-09-25	2002-03-27	Forme faiblement hygroscopique d'aripiprazole et methodes de preparation

Country Status (5)

Country	Link
CA (1)	CA2379005A1 (fr)
EC (1)	ECSP034434A (fr)
GE (1)	GEP20053457B (fr)
UA (4)	UA84924C2 (fr)
ZA (1)	ZA200300113B (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US8039621B2 (en)	2006-10-24	2011-10-18	Cambrex Charles City, Inc.	Process for preparing anhydrous Aripirazole type I

2002
- 2002-03-27 CA CA 2379005 patent/CA2379005A1/fr not_active Abandoned
- 2002-09-25 UA UAA200612816A patent/UA84924C2/ru unknown
- 2002-09-25 UA UAA200612801A patent/UA86235C2/uk unknown
- 2002-09-25 GE GEAP2002005101 patent/GEP20053457B/en unknown
- 2002-09-25 UA UAA200612815A patent/UA84923C2/ru unknown
- 2002-09-25 ZA ZA200300113A patent/ZA200300113B/en unknown
- 2002-09-25 UA UAA200612803A patent/UA85235C2/ru unknown
2003
- 2003-01-17 EC ECSP034434 patent/ECSP034434A/es unknown

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US8039621B2 (en)	2006-10-24	2011-10-18	Cambrex Charles City, Inc.	Process for preparing anhydrous Aripirazole type I

Also Published As

Publication number	Publication date
ECSP034434A (es)	2003-04-25
UA84924C2 (ru)	2008-12-10
GEP20053457B (en)	2005-02-25
ZA200300113B (en)	2004-08-06
UA85235C2 (ru)	2009-01-12
UA86235C2 (uk)	2009-04-10
UA84923C2 (ru)	2008-12-10

Legal Events

Date	Code	Title	Description
2005-03-29	FZDE	Dead

Publication	Publication Date	Title
EP1330249B1 (fr)	2006-04-05	Substance pharmaceutique d'aripiprazole faiblement hygroscopique et methodes de preparation associees
AU2002334413A1 (en)	2003-06-26	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
CA2379005A1 (fr)	2003-03-25	Forme faiblement hygroscopique d'aripiprazole et methodes de preparation
US8703772B2 (en)	2014-04-22	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
NZ523313A (en)	2006-05-26	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof

CA2379005A1 - Forme faiblement hygroscopique d'aripiprazole et methodes de preparation - Google Patents

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Priority Applications (164)

Applications Claiming Priority (2)

Publications (1)

Family

ID=19112920

Family Applications (1)

Country Status (5)

Cited By (1)

Cited By (1)

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