KR20150027840A - 타펜타돌의 적정 - Google Patents
타펜타돌의 적정 Download PDFInfo
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- KR20150027840A KR20150027840A KR20157003922A KR20157003922A KR20150027840A KR 20150027840 A KR20150027840 A KR 20150027840A KR 20157003922 A KR20157003922 A KR 20157003922A KR 20157003922 A KR20157003922 A KR 20157003922A KR 20150027840 A KR20150027840 A KR 20150027840A
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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Applications Claiming Priority (3)
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|---|---|---|---|
| EP07008218A EP1985292A1 (en) | 2007-04-23 | 2007-04-23 | Titration of tapentadol |
| EP07008218.5 | 2007-04-23 | ||
| PCT/EP2008/003178 WO2008128740A1 (en) | 2007-04-23 | 2008-04-21 | Titration of tapentadol |
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| KR1020097024357A Division KR20100017267A (ko) | 2007-04-23 | 2008-04-21 | 타펜타돌의 적정 |
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| KR1020177037810A Division KR102078999B1 (ko) | 2007-04-23 | 2008-04-21 | 타펜타돌의 적정 |
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| KR20150027840A true KR20150027840A (ko) | 2015-03-12 |
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| KR1020177037810A Active KR102078999B1 (ko) | 2007-04-23 | 2008-04-21 | 타펜타돌의 적정 |
| KR1020097024357A Ceased KR20100017267A (ko) | 2007-04-23 | 2008-04-21 | 타펜타돌의 적정 |
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| KR1020177037810A Active KR102078999B1 (ko) | 2007-04-23 | 2008-04-21 | 타펜타돌의 적정 |
| KR1020097024357A Ceased KR20100017267A (ko) | 2007-04-23 | 2008-04-21 | 타펜타돌의 적정 |
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| EP (5) | EP1985292A1 (enExample) |
| JP (4) | JP5933176B2 (enExample) |
| KR (3) | KR20150027840A (enExample) |
| CN (1) | CN101730530B (enExample) |
| AT (1) | ATE534378T1 (enExample) |
| AU (1) | AU2008241013B2 (enExample) |
| CA (1) | CA2683786C (enExample) |
| CY (1) | CY1112320T1 (enExample) |
| DK (1) | DK2148670T3 (enExample) |
| ES (1) | ES2378255T3 (enExample) |
| HR (1) | HRP20120147T1 (enExample) |
| IL (1) | IL201479A (enExample) |
| MX (1) | MX2009011444A (enExample) |
| NZ (1) | NZ580415A (enExample) |
| PL (1) | PL2148670T3 (enExample) |
| PT (1) | PT2148670E (enExample) |
| RU (1) | RU2472497C2 (enExample) |
| SI (1) | SI2148670T1 (enExample) |
| WO (1) | WO2008128740A1 (enExample) |
| ZA (1) | ZA200907355B (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1985292A1 (en) * | 2007-04-23 | 2008-10-29 | Grünenthal GmbH | Titration of tapentadol |
| WO2010096045A1 (en) * | 2008-10-30 | 2010-08-26 | Nectid, Inc. | Novel and potent tapentadol dosage forms |
| US8870876B2 (en) * | 2009-02-13 | 2014-10-28 | Tarsus Medical Inc. | Methods and devices for treating hallux valgus |
| US8277459B2 (en) | 2009-09-25 | 2012-10-02 | Tarsus Medical Inc. | Methods and devices for treating a structural bone and joint deformity |
| US8652141B2 (en) | 2010-01-21 | 2014-02-18 | Tarsus Medical Inc. | Methods and devices for treating hallux valgus |
| US20130116333A1 (en) * | 2010-05-05 | 2013-05-09 | Ratiopharm Gmbh | Solid tapentadol in non-crystalline form |
| US8696719B2 (en) | 2010-06-03 | 2014-04-15 | Tarsus Medical Inc. | Methods and devices for treating hallux valgus |
| CA2795923C (en) * | 2010-06-30 | 2018-10-16 | Gruenenthal Gmbh | Tapentadol for use in the treatment of irritable bowel syndrome |
| MX341072B (es) * | 2010-07-23 | 2016-08-05 | Grünenthal Gmbh * | Sales o co-cristales de 3-(3-dimetilamino-1-etil-2-metil-propil)-f enol. |
| CN101948397A (zh) * | 2010-09-07 | 2011-01-19 | 天津泰普药品科技发展有限公司 | 镇痛药他喷他多重要中间体的制备方法 |
| EP3597182A1 (en) | 2011-03-04 | 2020-01-22 | Grünenthal GmbH | Aqueous pharmaceutical formulation of tapentadol for oral administration |
| CN103501775A (zh) * | 2011-03-04 | 2014-01-08 | 格吕伦塔尔有限公司 | 他喷他多的胃肠外给药 |
| AU2012224954C1 (en) | 2011-03-04 | 2017-04-06 | Grünenthal GmbH | Semisolid aqueous pharmaceutical composition containing tapentadol |
| SI2694049T1 (sl) | 2011-04-05 | 2019-01-31 | Gruenenthal Gmbh | Tapentadol za preprečevanje razvoja kronične bolečine |
| JP6040219B2 (ja) * | 2011-04-05 | 2016-12-07 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 三叉神経因性痛に伴う疼痛の治療用タペンタドール |
| HUE049308T2 (hu) | 2011-04-29 | 2020-09-28 | Gruenenthal Gmbh | Tapentadol alkalmazása depresszió és szorongás megelõzésére és kezelésére |
| EP2968182B8 (en) * | 2013-03-15 | 2018-07-25 | SpecGx LLC | Abuse deterrent solid dosage form for immediate release with functional score |
| EP2845625A1 (en) * | 2013-09-04 | 2015-03-11 | Grünenthal GmbH | Tapentadol for use in the treatment of fibromyalgia and chronic fatigue syndrome |
| CN107847471A (zh) | 2015-03-27 | 2018-03-27 | 格吕伦塔尔有限公司 | 他喷他多肠胃外给药的稳定制剂 |
| AU2016266432B2 (en) * | 2015-05-26 | 2020-10-22 | Laboratorio Medinfar-Produtos Farmacêuticos, S.A. | Compositions for use in treating Parkinson's disease and related disorders |
| WO2017148595A1 (en) | 2016-02-29 | 2017-09-08 | Grünenthal GmbH | Titration of cebranopadol |
| PE20190908A1 (es) | 2016-09-23 | 2019-06-26 | Gruenenthal Chemie | Formulacion estable para la administracion parenteral de tapentadol |
| WO2021185804A1 (en) | 2020-03-16 | 2021-09-23 | Grünenthal GmbH | Scored tablet |
| CA3213818A1 (en) * | 2021-03-17 | 2022-09-22 | Actelion Pharmaceuticals Ltd | Pharmaceutical dosage system |
| WO2022234076A1 (en) * | 2021-05-07 | 2022-11-10 | Grünenthal GmbH | Tapentadol for treating neuropathic pain in covid-19 patients |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4783337A (en) | 1983-05-11 | 1988-11-08 | Alza Corporation | Osmotic system comprising plurality of members for dispensing drug |
| US4612008A (en) * | 1983-05-11 | 1986-09-16 | Alza Corporation | Osmotic device with dual thermodynamic activity |
| US4765989A (en) | 1983-05-11 | 1988-08-23 | Alza Corporation | Osmotic device for administering certain drugs |
| JPS6327805A (ja) | 1986-07-21 | 1988-02-05 | Sumitomo Electric Ind Ltd | 光フアイバの接続用部材及びそれを用いた接続方法 |
| DE4426245A1 (de) * | 1994-07-23 | 1996-02-22 | Gruenenthal Gmbh | 1-Phenyl-3-dimethylamino-propanverbindungen mit pharmakologischer Wirkung |
| US6339105B1 (en) * | 1999-10-12 | 2002-01-15 | Ortho-Mcneil Pharmaceutical, Inc. | Analgesic regimen |
| PE20030527A1 (es) | 2001-10-24 | 2003-07-26 | Gruenenthal Chemie | Formulacion farmaceutica con liberacion retardada que contiene 3-(3-dimetilamino-1-etil-2-metil-propil) fenol o una sal farmaceuticamente aceptable del mismo y tabletas para administracion oral que la contienen |
| PT1572167E (pt) | 2002-12-13 | 2008-10-03 | Euro Celtique Sa | Regime posológico de buprenorfina papa analgesia |
| US7413749B2 (en) * | 2003-03-11 | 2008-08-19 | Purdue Pharma L.P. | Titration dosing regimen for controlled release tramadol |
| DE102007019417A1 (de) * | 2007-04-23 | 2008-11-13 | Grünenthal GmbH | Tapentadol zur Schmerzbehandlung bei Arthrose |
| EP1985292A1 (en) * | 2007-04-23 | 2008-10-29 | Grünenthal GmbH | Titration of tapentadol |
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