JP2004522798A - メトプロロールを含有する微粒子を製造する方法 - Google Patents
メトプロロールを含有する微粒子を製造する方法 Download PDFInfo
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- JP2004522798A JP2004522798A JP2002571033A JP2002571033A JP2004522798A JP 2004522798 A JP2004522798 A JP 2004522798A JP 2002571033 A JP2002571033 A JP 2002571033A JP 2002571033 A JP2002571033 A JP 2002571033A JP 2004522798 A JP2004522798 A JP 2004522798A
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- metoprolol
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0100824A SE0100824D0 (sv) | 2001-03-09 | 2001-03-09 | Method III to obtain microparticles |
| PCT/SE2002/000401 WO2002072074A1 (en) | 2001-03-09 | 2002-03-06 | Method to prepare microparticles metoprolol that contain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004522798A true JP2004522798A (ja) | 2004-07-29 |
| JP2004522798A5 JP2004522798A5 (enExample) | 2005-12-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002571033A Pending JP2004522798A (ja) | 2001-03-09 | 2002-03-06 | メトプロロールを含有する微粒子を製造する方法 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20040116392A1 (enExample) |
| EP (1) | EP1370245B1 (enExample) |
| JP (1) | JP2004522798A (enExample) |
| KR (1) | KR20030081507A (enExample) |
| CN (1) | CN1236761C (enExample) |
| AT (1) | ATE295153T1 (enExample) |
| AU (1) | AU2002235102B2 (enExample) |
| BR (1) | BR0207919A (enExample) |
| CA (1) | CA2440167A1 (enExample) |
| DE (1) | DE60204125T2 (enExample) |
| ES (1) | ES2240691T3 (enExample) |
| HU (1) | HUP0303450A2 (enExample) |
| IL (1) | IL157777A0 (enExample) |
| IS (1) | IS6937A (enExample) |
| MX (1) | MXPA03008088A (enExample) |
| NO (1) | NO20033967L (enExample) |
| NZ (1) | NZ528168A (enExample) |
| PL (1) | PL363972A1 (enExample) |
| PT (1) | PT1370245E (enExample) |
| RU (1) | RU2292878C2 (enExample) |
| SE (1) | SE0100824D0 (enExample) |
| UA (1) | UA75909C2 (enExample) |
| WO (1) | WO2002072074A1 (enExample) |
| ZA (1) | ZA200306880B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0100823D0 (sv) * | 2001-03-09 | 2001-03-09 | Astrazeneca Ab | Method I to obtain microparticles |
| US20060159756A1 (en) * | 1999-09-10 | 2006-07-20 | Brita Sjoblom | Method to obtain microparticles containing an H+,K+-ATP-ASE inhibitor |
| SE0100822D0 (sv) * | 2001-03-09 | 2001-03-09 | Astrazeneca Ab | Method II to obtain microparticles |
| US8006685B2 (en) * | 2002-07-05 | 2011-08-30 | Turbochef Technologies, Inc. | Re-circulating oven with gas clean-up |
| EP1915137B8 (de) | 2005-08-10 | 2013-09-11 | ADD Advanced Drug Delivery Technologies, Ltd. | Orales präparat mit kontrollierter freisetzung |
| US20070053983A1 (en) * | 2005-09-06 | 2007-03-08 | Girish Jain | Extended release compositions of metoprolol succinate |
| NZ574427A (en) * | 2006-07-28 | 2011-11-25 | Zaklady Farmaceutyczne Polpharma S A | Extended release pharmaceutical formulation of metoprolol and process for its preparation |
| ES2753148T3 (es) * | 2007-02-23 | 2020-04-07 | Glatt Air Techniques Inc | Método para determinar el peso del recubrimiento que va a ser aplicado para formar una forma de dosificación de liberación controlada |
| CN101269056B (zh) * | 2007-03-19 | 2010-05-19 | 天津药物研究院 | 一种美托洛尔盐类口服脉冲微丸制剂 |
| NZ584521A (en) * | 2007-10-10 | 2011-03-31 | Avantor Performance Mat Inc | Directly compressible high functionality granular microcrystalline cellulose based excipient, manufacturing process and use thereof |
| US20100055180A1 (en) * | 2007-10-10 | 2010-03-04 | Mallinckrodt Baker, Inc. | Directly Compressible Granular Microcrystalline Cellulose Based Excipient, Manufacturing Process and Use Thereof |
| CN102641257A (zh) * | 2012-03-31 | 2012-08-22 | 内蒙古医学院 | 阿替洛尔缓释微囊及其制备方法 |
| RU2585023C1 (ru) * | 2014-12-18 | 2016-05-27 | Общество с ограниченной ответственностью "Нанолек" | Способ гранулирования |
| CN104739805B (zh) * | 2015-04-09 | 2017-12-19 | 邸蓉 | 制备琥珀酸美托洛尔缓释微丸的复相乳液法 |
| WO2019183470A2 (en) | 2018-03-22 | 2019-09-26 | Incarda Therapeutics, Inc. | A novel method to slow ventricular rate |
| CN115252913A (zh) * | 2022-08-02 | 2022-11-01 | 赛诺神畅医疗科技有限公司 | 一种血管给药涂层及其制备方法和应用 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US653014A (en) * | 1899-10-06 | 1900-07-03 | Ashley & Bailey Company | Process of silkifying cotton. |
| SE354851B (enExample) * | 1970-02-18 | 1973-03-26 | Haessle Ab | |
| SE418247B (sv) * | 1975-11-17 | 1981-05-18 | Haessle Ab | Sett att framstella kroppar med reglerad frigoring av en aktiv komponent |
| DE3565475D1 (en) * | 1984-04-07 | 1988-11-17 | Bayer Ag | Process and apparatus for the production of granules |
| IE58110B1 (en) * | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| SE450087B (sv) * | 1985-10-11 | 1987-06-09 | Haessle Ab | Korn med kontrollerad frisettning av farmaceutiskt aktiva emnen som anbringats teckande pa ett kompakt olosligt kernmaterial |
| SE455836B (sv) * | 1985-10-11 | 1988-08-15 | Haessle Ab | Beredning med kontrollerad frisettning innehallande ett salt av metoprolol samt metod for framstellning av denna beredning |
| DE3909455A1 (de) * | 1989-03-22 | 1990-09-27 | Hoechst Ag | Verfahren zur herstellung von wasserdispergierbaren granulaten |
| FR2725623A1 (fr) * | 1994-10-18 | 1996-04-19 | Flamel Tech Sa | Microcapsules medicamenteuses et/ou nutritionnelles pour administration per os |
| AU6824996A (en) * | 1995-08-17 | 1997-03-12 | Dyer, Alison Margaret | Controlled release products |
| DE19613395A1 (de) * | 1996-04-03 | 1997-10-09 | Basf Ag | Granulate hygroskopischer, wasserlöslicher Produkte |
| US6096339A (en) * | 1997-04-04 | 2000-08-01 | Alza Corporation | Dosage form, process of making and using same |
| US5891474A (en) * | 1997-01-29 | 1999-04-06 | Poli Industria Chimica, S.P.A. | Time-specific controlled release dosage formulations and method of preparing same |
| DE19733094A1 (de) * | 1997-07-31 | 1999-02-04 | Merck Patent Gmbh | Formulierung auf der Basis von Ascorbinsäure mit verbesserter Farbstabilität |
| WO1999018935A1 (de) * | 1997-10-15 | 1999-04-22 | Merck Patent Gmbh | Herstellung eines direkt verpressbaren tablettierhilfsstoffes |
| EP0987020A1 (en) * | 1998-09-04 | 2000-03-22 | Pharma Pass LLC | Metoprolol composition and processes for manufacturing the same |
| US6395300B1 (en) * | 1999-05-27 | 2002-05-28 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
| US20060159756A1 (en) * | 1999-09-10 | 2006-07-20 | Brita Sjoblom | Method to obtain microparticles containing an H+,K+-ATP-ASE inhibitor |
| SE0100823D0 (sv) * | 2001-03-09 | 2001-03-09 | Astrazeneca Ab | Method I to obtain microparticles |
| TWI354568B (en) * | 2000-09-20 | 2011-12-21 | Jagotec Ag | Insoluble drug particle compositions with improved |
| SE0100822D0 (sv) * | 2001-03-09 | 2001-03-09 | Astrazeneca Ab | Method II to obtain microparticles |
-
2001
- 2001-03-09 SE SE0100824A patent/SE0100824D0/xx unknown
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2002
- 2002-03-06 IL IL15777702A patent/IL157777A0/xx unknown
- 2002-03-06 CA CA002440167A patent/CA2440167A1/en not_active Abandoned
- 2002-03-06 JP JP2002571033A patent/JP2004522798A/ja active Pending
- 2002-03-06 DE DE60204125T patent/DE60204125T2/de not_active Expired - Fee Related
- 2002-03-06 ES ES02701873T patent/ES2240691T3/es not_active Expired - Lifetime
- 2002-03-06 AU AU2002235102A patent/AU2002235102B2/en not_active Ceased
- 2002-03-06 PL PL02363972A patent/PL363972A1/xx not_active Application Discontinuation
- 2002-03-06 WO PCT/SE2002/000401 patent/WO2002072074A1/en not_active Ceased
- 2002-03-06 MX MXPA03008088A patent/MXPA03008088A/es active IP Right Grant
- 2002-03-06 HU HU0303450A patent/HUP0303450A2/hu unknown
- 2002-03-06 RU RU2003127739/15A patent/RU2292878C2/ru not_active IP Right Cessation
- 2002-03-06 BR BR0207919-4A patent/BR0207919A/pt not_active IP Right Cessation
- 2002-03-06 PT PT02701873T patent/PT1370245E/pt unknown
- 2002-03-06 AT AT02701873T patent/ATE295153T1/de not_active IP Right Cessation
- 2002-03-06 US US10/469,907 patent/US20040116392A1/en not_active Abandoned
- 2002-03-06 NZ NZ528168A patent/NZ528168A/en unknown
- 2002-03-06 EP EP02701873A patent/EP1370245B1/en not_active Expired - Lifetime
- 2002-03-06 KR KR10-2003-7011782A patent/KR20030081507A/ko not_active Abandoned
- 2002-03-06 CN CNB028095901A patent/CN1236761C/zh not_active Expired - Fee Related
- 2002-06-03 UA UA2003098380A patent/UA75909C2/uk unknown
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2003
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- 2003-09-03 ZA ZA200306880A patent/ZA200306880B/en unknown
- 2003-09-08 NO NO20033967A patent/NO20033967L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| DE60204125T2 (de) | 2006-01-19 |
| ATE295153T1 (de) | 2005-05-15 |
| ZA200306880B (en) | 2004-12-03 |
| PT1370245E (pt) | 2005-08-31 |
| EP1370245A1 (en) | 2003-12-17 |
| ES2240691T3 (es) | 2005-10-16 |
| IS6937A (is) | 2003-09-03 |
| NO20033967L (no) | 2003-10-28 |
| IL157777A0 (en) | 2004-03-28 |
| RU2292878C2 (ru) | 2007-02-10 |
| EP1370245B1 (en) | 2005-05-11 |
| NO20033967D0 (no) | 2003-09-08 |
| NZ528168A (en) | 2005-01-28 |
| DE60204125D1 (de) | 2005-06-16 |
| BR0207919A (pt) | 2004-04-27 |
| UA75909C2 (en) | 2006-06-15 |
| US20040116392A1 (en) | 2004-06-17 |
| MXPA03008088A (es) | 2003-12-12 |
| HK1059737A1 (en) | 2004-07-16 |
| CN1507345A (zh) | 2004-06-23 |
| SE0100824D0 (sv) | 2001-03-09 |
| PL363972A1 (en) | 2004-11-29 |
| HUP0303450A2 (hu) | 2004-01-28 |
| CA2440167A1 (en) | 2002-09-19 |
| AU2002235102B2 (en) | 2006-08-31 |
| RU2003127739A (ru) | 2005-03-10 |
| KR20030081507A (ko) | 2003-10-17 |
| WO2002072074A1 (en) | 2002-09-19 |
| CN1236761C (zh) | 2006-01-18 |
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