EA200500040A1 - Фармацевтическая композиция, содержащая стабилизированную аморфную форму донепезил гидрохлорида - Google Patents
Фармацевтическая композиция, содержащая стабилизированную аморфную форму донепезил гидрохлоридаInfo
- Publication number
- EA200500040A1 EA200500040A1 EA200500040A EA200500040A EA200500040A1 EA 200500040 A1 EA200500040 A1 EA 200500040A1 EA 200500040 A EA200500040 A EA 200500040A EA 200500040 A EA200500040 A EA 200500040A EA 200500040 A1 EA200500040 A1 EA 200500040A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- hydrochloride
- pharmaceutical composition
- droened
- stabilized
- amorphic form
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 title abstract 2
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 abstract 2
- 229960003135 donepezil hydrochloride Drugs 0.000 abstract 2
- XWAIAVWHZJNZQQ-UHFFFAOYSA-N donepezil hydrochloride Chemical compound [H+].[Cl-].O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 XWAIAVWHZJNZQQ-UHFFFAOYSA-N 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 2
- PAMIQIKDUOTOBW-UHFFFAOYSA-N 1-methylpiperidine Chemical compound CN1CCCCC1 PAMIQIKDUOTOBW-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 229960003530 donepezil Drugs 0.000 abstract 1
- 238000010952 in-situ formation Methods 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000006641 stabilisation Effects 0.000 abstract 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
Abstract
Настоящее изобретение относится к стабилизированным фармацевтическим композициям, содержащим аморфную форму 1-бензил-4-((5,6-диметокси-1-инданон)-2-ил)метилпиперидин (донепезил) гидрохлорида и к способу стабилизации этого соединения. Фармацевтическую композицию получают путем получения донепезил гидрохлорида in situ и внесения полученного раствора в смесь фармацевтически приемлемых наполнителей. Аморфную форму донепезил гидрохлорида стабилизируют путем добавления ингибитора кристаллизации к раствору или к смеси фармацевтически приемлемых наполнителей.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SI200200155A SI21223A (sl) | 2002-06-19 | 2002-06-19 | Farmacevtska formulacija s stabiliziranim amorfnim donepezilijevim kloridom |
PCT/SI2003/000019 WO2004000317A1 (en) | 2002-06-19 | 2003-06-18 | Pharmaceutical composition containing stabilised amorphous form of donepezil hydrochloride |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200500040A1 true EA200500040A1 (ru) | 2005-06-30 |
EA012904B1 EA012904B1 (ru) | 2010-02-26 |
Family
ID=29778199
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200500040A EA012904B1 (ru) | 2002-06-19 | 2003-06-18 | Фармацевтическая композиция, содержащая стабилизированную аморфную форму донепезил гидрохлорида |
Country Status (15)
Country | Link |
---|---|
EP (1) | EP1513528B1 (ru) |
AT (1) | ATE431739T1 (ru) |
AU (1) | AU2003279102A1 (ru) |
CY (1) | CY1109314T1 (ru) |
DE (1) | DE60327696D1 (ru) |
DK (1) | DK1513528T3 (ru) |
EA (1) | EA012904B1 (ru) |
ES (1) | ES2326529T3 (ru) |
HR (1) | HRP20041198B1 (ru) |
PL (1) | PL212584B1 (ru) |
PT (1) | PT1513528E (ru) |
RS (1) | RS51824B (ru) |
SI (2) | SI21223A (ru) |
UA (1) | UA86573C2 (ru) |
WO (1) | WO2004000317A1 (ru) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL150509A (en) | 2002-07-01 | 2007-07-04 | Joseph Kaspi | Pharmaceutical preparations containing donafazil hydrochloride |
IL154370A0 (en) * | 2003-02-10 | 2003-09-17 | Chemagis Ltd | Solid amorphous mixtures, processes for the preparation thereof and pharmaceutical compositions containing the same |
CA2552221A1 (en) * | 2003-12-31 | 2005-07-21 | Actavis Group Hf | Donepezil formulations |
US8980894B2 (en) | 2004-03-25 | 2015-03-17 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the treatment of asymptomatic (occult) heart failure |
EP1579862A1 (en) | 2004-03-25 | 2005-09-28 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the reduction of heart size in mammals suffering from heart failure |
KR20070083679A (ko) | 2004-09-29 | 2007-08-24 | 케마지스 리미티드 | 약학적으로 순수한 비정질 도네페닐 염산염의 제조를 위한정제된 도네페질 말레산염의 용도 |
DE602005011326D1 (de) * | 2004-10-19 | 2009-01-08 | Krka Tovarna Zdravil D D | Feste pharmazeutische zusammensetzung mit donepezilhydrochlorid |
WO2006063025A1 (en) * | 2004-12-07 | 2006-06-15 | Nektar Therapeutics | Stable non-crystalline formulation comprising donepezil |
US20060122226A1 (en) | 2004-12-08 | 2006-06-08 | Itai Adin | Crystalline forms of Donepezil base |
MX2007007836A (es) | 2004-12-27 | 2007-08-20 | Eisai R&D Man Co Ltd | Metodo para estabilizar un farmaco anti-demencia. |
JP2007015934A (ja) * | 2005-07-05 | 2007-01-25 | Meiko Shoji Kk | 温感クリーム化粧料 |
DE102005060377A1 (de) | 2005-12-16 | 2007-06-21 | Ratiopharm Gmbh | Pharmazeutische Zusammensetzung enthaltend Donepezilhydrochlorid, Tablette hieraus und Verfahren zu deren Herstellung |
EP1920785A1 (en) | 2006-11-07 | 2008-05-14 | Boehringer Ingelheim Vetmedica Gmbh | Liquid preparation comprising a complex of pimobendan and cyclodextrin |
DE102007037932A1 (de) | 2007-08-11 | 2009-02-12 | Alfred E. Tiefenbacher Gmbh & Co.Kg | Donepezilhydrochlorid in amorpher Form enthaltende Tablette |
DE102009041839A1 (de) * | 2009-09-18 | 2011-03-24 | Dolorgiet Gmbh & Co. Kg | Donepezil-haltige Tabletten |
EP2366378A1 (en) | 2010-03-01 | 2011-09-21 | Dexcel Pharma Technologies Ltd. | Sustained-release donepezil formulations |
WO2011151359A1 (en) | 2010-06-02 | 2011-12-08 | Noscira, S.A. | Combined treatment with a cholinesterase inhibitor and a thiadiazolidinedione derivative |
EP2502620A1 (en) | 2011-03-24 | 2012-09-26 | Krka Tovarna Zdravil, D.D., Novo Mesto | Solid pharmaceutical composition comprising donepezil |
WO2013135852A1 (en) | 2012-03-15 | 2013-09-19 | Boehringer Ingelheim Vetmedica Gmbh | Pharmaceutical tablet formulation for the veterinary medical sector, method of production and use thereof |
MX373040B (es) | 2013-07-19 | 2020-05-26 | Boehringer Ingelheim Vetmedica Gmbh | Composicion farmaceutica acuosa liquida que contiene derivados de ciclodextrina eterificada con conservador. |
EP2925305B1 (en) | 2013-12-04 | 2016-07-27 | Boehringer Ingelheim Vetmedica GmbH | Improved pharmaceutical compositions of pimobendan |
EP3380079A4 (en) * | 2015-11-25 | 2019-08-21 | Patheon Development Services Inc. | AMORPHOUS DISPERSION GRANULES AND PHARMACEUTICAL FORMS FOR ORAL USE |
US10537570B2 (en) | 2016-04-06 | 2020-01-21 | Boehringer Ingelheim Vetmedica Gmbh | Use of pimobendan for the reduction of heart size and/or the delay of onset of clinical symptoms in patients with asymptomatic heart failure due to mitral valve disease |
KR102372630B1 (ko) * | 2019-05-15 | 2022-03-14 | 주식회사 대웅제약 | 고함량의 도네페질 또는 그의 염을 포함하는 경피흡수제제 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2525108B1 (fr) * | 1982-04-19 | 1989-05-12 | Elan Corp Ltd | Medicaments a haut degre de solubilite et procede pour leur obtention |
DK1019374T3 (da) * | 1996-06-07 | 2003-04-07 | Eisai Co Ltd | Polymorfe og Donepezil-hydrochlorid og fremstillingsfremgangsmåde |
ES2310164T3 (es) * | 1999-02-10 | 2009-01-01 | Pfizer Products Inc. | Dispositivo de liberacion controlada por la matriz. |
JP5767429B2 (ja) * | 1999-11-12 | 2015-08-19 | アッヴィ・インコーポレイテッド | 固体分散剤中の結晶化阻害剤 |
-
2002
- 2002-06-19 SI SI200200155A patent/SI21223A/sl not_active IP Right Cessation
-
2003
- 2003-06-18 ES ES03741747T patent/ES2326529T3/es not_active Expired - Lifetime
- 2003-06-18 PL PL372116A patent/PL212584B1/pl unknown
- 2003-06-18 EP EP03741747A patent/EP1513528B1/en not_active Expired - Lifetime
- 2003-06-18 DK DK03741747T patent/DK1513528T3/da active
- 2003-06-18 PT PT03741747T patent/PT1513528E/pt unknown
- 2003-06-18 SI SI200331643T patent/SI1513528T1/sl unknown
- 2003-06-18 AU AU2003279102A patent/AU2003279102A1/en not_active Abandoned
- 2003-06-18 RS YU110604A patent/RS51824B/en unknown
- 2003-06-18 UA UAA200500514A patent/UA86573C2/ru unknown
- 2003-06-18 AT AT03741747T patent/ATE431739T1/de active
- 2003-06-18 HR HRP20041198AA patent/HRP20041198B1/hr not_active IP Right Cessation
- 2003-06-18 WO PCT/SI2003/000019 patent/WO2004000317A1/en not_active Application Discontinuation
- 2003-06-18 DE DE60327696T patent/DE60327696D1/de not_active Expired - Lifetime
- 2003-06-18 EA EA200500040A patent/EA012904B1/ru not_active IP Right Cessation
-
2009
- 2009-08-17 CY CY20091100878T patent/CY1109314T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
PL212584B1 (pl) | 2012-10-31 |
EP1513528B1 (en) | 2009-05-20 |
ES2326529T3 (es) | 2009-10-14 |
DK1513528T3 (da) | 2009-09-07 |
UA86573C2 (ru) | 2009-05-12 |
SI1513528T1 (sl) | 2009-10-31 |
ATE431739T1 (de) | 2009-06-15 |
HRP20041198A2 (en) | 2005-04-30 |
RS110604A (en) | 2007-02-05 |
PT1513528E (pt) | 2009-08-18 |
AU2003279102A1 (en) | 2004-01-06 |
EP1513528A1 (en) | 2005-03-16 |
PL372116A1 (en) | 2005-07-11 |
EA012904B1 (ru) | 2010-02-26 |
HRP20041198B1 (hr) | 2013-05-31 |
DE60327696D1 (de) | 2009-07-02 |
RS51824B (en) | 2012-02-29 |
SI21223A (sl) | 2003-12-31 |
CY1109314T1 (el) | 2014-07-02 |
WO2004000317A1 (en) | 2003-12-31 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
|
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |