CA2345638A1 - Formes posologiques a administration par voie orale contenant le compose (2s,3s,5r)-2-(3,5-difluorophenyl)-3,5-dimethyl-2-morpholinol et une quantite stabilisante efficace d'acide alginique - Google Patents
Formes posologiques a administration par voie orale contenant le compose (2s,3s,5r)-2-(3,5-difluorophenyl)-3,5-dimethyl-2-morpholinol et une quantite stabilisante efficace d'acide alginique Download PDFInfo
- Publication number
- CA2345638A1 CA2345638A1 CA002345638A CA2345638A CA2345638A1 CA 2345638 A1 CA2345638 A1 CA 2345638A1 CA 002345638 A CA002345638 A CA 002345638A CA 2345638 A CA2345638 A CA 2345638A CA 2345638 A1 CA2345638 A1 CA 2345638A1
- Authority
- CA
- Canada
- Prior art keywords
- oral dosage
- dosage form
- discrete oral
- discrete
- alginic acid
- Prior art date
- 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
Links
- 239000000783 alginic acid Substances 0.000 title claims abstract description 29
- 235000010443 alginic acid Nutrition 0.000 title claims abstract description 29
- 229920000615 alginic acid Polymers 0.000 title claims abstract description 29
- 229960001126 alginic acid Drugs 0.000 title claims abstract description 29
- 150000004781 alginic acids Chemical class 0.000 title claims abstract description 29
- 230000000087 stabilizing effect Effects 0.000 title claims abstract description 4
- OZGPVYJHWWPEFT-RGNHYFCHSA-N manifaxine Chemical compound C[C@@H]1N[C@H](C)CO[C@@]1(O)C1=CC(F)=CC(F)=C1 OZGPVYJHWWPEFT-RGNHYFCHSA-N 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title description 18
- 238000009472 formulation Methods 0.000 title description 6
- 239000006186 oral dosage form Substances 0.000 claims abstract description 46
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims abstract description 13
- 229960002715 nicotine Drugs 0.000 claims abstract description 13
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims abstract description 13
- 150000003839 salts Chemical class 0.000 claims abstract description 13
- 239000012453 solvate Substances 0.000 claims abstract description 10
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 20
- -1 (2S,3S,SR)-2-(3,5-difluorophenyl)-3,5-dimethyl-2-morpholinol Chemical compound 0.000 claims description 11
- 239000000945 filler Substances 0.000 claims description 10
- 235000019359 magnesium stearate Nutrition 0.000 claims description 10
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- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical group N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 7
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- 230000002265 prevention Effects 0.000 claims description 4
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- 239000008101 lactose Substances 0.000 claims description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 3
- 239000008117 stearic acid Substances 0.000 claims description 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
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- UKMSUNONTOPOIO-UHFFFAOYSA-M behenate Chemical compound CCCCCCCCCCCCCCCCCCCCCC([O-])=O UKMSUNONTOPOIO-UHFFFAOYSA-M 0.000 claims 1
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- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 description 5
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- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Chemical class OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
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- 229940049706 benzodiazepine Drugs 0.000 description 3
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
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- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 description 2
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
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- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
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- 235000010323 ascorbic acid Nutrition 0.000 description 1
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Classifications
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Cosmetics (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
L'invention concerne des formes posologiques discrètes à administration par voie orale, généralement des comprimés ou des gélules, contenant le composé (2S,3S,5R)-2-(3,5-difluorophényl)-3,5-diméthyl-2-morpholinol ou un sel ou solvate physiologiquement acceptable de ce composé, ou un solvate dudit sel, et une quantité stabilisante efficace d'acide alginique. Ces formes posologiques sont utiles pour prévenir ou traiter l'hypercinésie avec déficit de l'attention ou la dépression, ou pour traiter l'accoutumance à des produits contenant de la nicotine, en particulier des produits contenant du tabac, afin d'aider, par exemple, un patient à s'arrêter de fumer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10211298P | 1998-09-28 | 1998-09-28 | |
| US60/102,112 | 1998-09-28 | ||
| PCT/EP1999/007117 WO2000018406A1 (fr) | 1998-09-28 | 1999-09-24 | Formes posologiques a administration par voie orale contenant le compose (2s,3s,5r)-2-(3,5-difluorophenyl)-3,5-dimethyl-2-morpholinol et une quantite stabilisante efficace d'acide alginique |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2345638A1 true CA2345638A1 (fr) | 2000-04-06 |
Family
ID=22288187
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002345638A Abandoned CA2345638A1 (fr) | 1998-09-28 | 1999-09-24 | Formes posologiques a administration par voie orale contenant le compose (2s,3s,5r)-2-(3,5-difluorophenyl)-3,5-dimethyl-2-morpholinol et une quantite stabilisante efficace d'acide alginique |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP1117407A1 (fr) |
| JP (1) | JP2002525328A (fr) |
| KR (1) | KR20010075385A (fr) |
| CN (1) | CN1328459A (fr) |
| AR (1) | AR022673A1 (fr) |
| AU (1) | AU6087399A (fr) |
| BR (1) | BR9914096A (fr) |
| CA (1) | CA2345638A1 (fr) |
| CZ (1) | CZ20011142A3 (fr) |
| HU (1) | HUP0103459A2 (fr) |
| IL (1) | IL142054A0 (fr) |
| MA (1) | MA26693A1 (fr) |
| NO (1) | NO20011555L (fr) |
| PE (1) | PE20001087A1 (fr) |
| PL (1) | PL346877A1 (fr) |
| TR (1) | TR200100863T2 (fr) |
| WO (1) | WO2000018406A1 (fr) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1220673A2 (fr) * | 1999-10-13 | 2002-07-10 | Glaxo Group Limited | Methode destinee au traitement de l'obesite |
| DE102008047910A1 (de) | 2008-09-19 | 2010-03-25 | Molkerei Meggle Wasserburg Gmbh & Co. Kg | Tablettierhilfsstoff auf Laktose- und Cellulosebasis |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4597969A (en) * | 1982-04-05 | 1986-07-01 | Merck Sharp & Dohme | Stabilization of unstable drugs or food supplements |
| GB8924528D0 (en) * | 1989-10-31 | 1989-12-20 | Wellcome Found | Heterocyclic pharmaceutical compounds,preparation and use |
-
1999
- 1999-09-23 MA MA25782A patent/MA26693A1/fr unknown
- 1999-09-24 CZ CZ20011142A patent/CZ20011142A3/cs unknown
- 1999-09-24 CA CA002345638A patent/CA2345638A1/fr not_active Abandoned
- 1999-09-24 KR KR1020017003874A patent/KR20010075385A/ko not_active Withdrawn
- 1999-09-24 AR ARP990104841A patent/AR022673A1/es unknown
- 1999-09-24 JP JP2000571924A patent/JP2002525328A/ja active Pending
- 1999-09-24 EP EP99947420A patent/EP1117407A1/fr not_active Withdrawn
- 1999-09-24 PL PL99346877A patent/PL346877A1/xx unknown
- 1999-09-24 WO PCT/EP1999/007117 patent/WO2000018406A1/fr not_active Ceased
- 1999-09-24 HU HU0103459A patent/HUP0103459A2/hu unknown
- 1999-09-24 BR BR9914096-9A patent/BR9914096A/pt not_active IP Right Cessation
- 1999-09-24 IL IL14205499A patent/IL142054A0/xx unknown
- 1999-09-24 CN CN99813675A patent/CN1328459A/zh active Pending
- 1999-09-24 AU AU60873/99A patent/AU6087399A/en not_active Abandoned
- 1999-09-24 TR TR2001/00863T patent/TR200100863T2/xx unknown
- 1999-09-27 PE PE1999000976A patent/PE20001087A1/es not_active Application Discontinuation
-
2001
- 2001-03-27 NO NO20011555A patent/NO20011555L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| NO20011555D0 (no) | 2001-03-27 |
| JP2002525328A (ja) | 2002-08-13 |
| PE20001087A1 (es) | 2000-10-20 |
| CN1328459A (zh) | 2001-12-26 |
| WO2000018406A1 (fr) | 2000-04-06 |
| CZ20011142A3 (cs) | 2001-09-12 |
| MA26693A1 (fr) | 2004-12-20 |
| AR022673A1 (es) | 2002-09-04 |
| HUP0103459A2 (hu) | 2002-01-28 |
| AU6087399A (en) | 2000-04-17 |
| TR200100863T2 (tr) | 2001-07-23 |
| NO20011555L (no) | 2001-03-27 |
| PL346877A1 (en) | 2002-03-11 |
| KR20010075385A (ko) | 2001-08-09 |
| IL142054A0 (en) | 2002-03-10 |
| BR9914096A (pt) | 2001-07-31 |
| EP1117407A1 (fr) | 2001-07-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |