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RU2004131870A - Фармацевтический препарат, содержащий оксикодон и налоксон - Google Patents

Фармацевтический препарат, содержащий оксикодон и налоксон Download PDF

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Publication number
RU2004131870A
RU2004131870A RU2004131870/15A RU2004131870A RU2004131870A RU 2004131870 A RU2004131870 A RU 2004131870A RU 2004131870/15 A RU2004131870/15 A RU 2004131870/15A RU 2004131870 A RU2004131870 A RU 2004131870A RU 2004131870 A RU2004131870 A RU 2004131870A
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drug according
naloxone
oxycodone
contained
preparation
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RU2004131870/15A
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RU2295344C2 (ru
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Бианка БРЕГМАНН (DE)
Бианка БРЕГМАНН
Зилке МЮХЛАУ (DE)
Зилке МЮХЛАУ
Кристоф ШПИТЦЛЕЙ (DE)
Кристоф ШПИТЦЛЕЙ
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Еуро-Селтик С.А. (Lu)
Еуро-Селтик С.А.
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Priority claimed from DE10215131A external-priority patent/DE10215131A1/de
Priority claimed from DE10215067A external-priority patent/DE10215067A1/de
Application filed by Еуро-Селтик С.А. (Lu), Еуро-Селтик С.А. filed Critical Еуро-Селтик С.А. (Lu)
Publication of RU2004131870A publication Critical patent/RU2004131870A/ru
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, 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
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Emergency Medicine (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Nutrition Science (AREA)
  • Inorganic Chemistry (AREA)
  • Physiology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medical Treatment And Welfare Office Work (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (30)

1. Стабильный при хранении фармацевтический препарат, содержащий оксикодон и налоксон в практически ненабухающей диффузионной матрице, включающей этилцеллюлозу, характеризующийся тем, что активные соединения высвобождаются из препарата длительно, неизменно и независимо друг от друга.
2. Препарат по п.1, отличающийся тем, что оксикодон и/или налоксон содержатся в виде их фармацевтически приемлемых производных с такой же активностью, например, свободных оснований или солей.
3. Препарат по п.2, отличающийся тем, что оксикодон и/или налоксон содержатся в виде их гидрохлорида, сульфата, бисульфата, тартрата, нитрата, цитрата, битартрата, фосфата, малата, малеата, гидробромида, гидроиодида, фумарата или сукцината.
4. Препарат по одному из предыдущих пунктов, отличающийся тем, что оксикодон содержится в избытке по отношению к налоксону, содержащемуся в единичной дозе.
5. Препарат по п.1, отличающийся тем, что налоксон содержится в количестве от 1 до 50 мг.
6. Препарат по п.1, отличающийся тем, что оксикодон содержится в количестве от 10 до 150 мг, предпочтительно от 10 до 80 мг.
7. Препарат по п.1, отличающийся тем, что оксикодон и налоксон содержатся в весовом отношении, равном максимально 25:1, предпочтительно максимально 20:1, 15:1, особенно предпочтительно 5:1, 4:1, 3:1, 2:1 или 1:1.
8. Препарат по п.1, отличающийся тем, что он содержит практически не набухающую и не разрушающуюся диффузионную матрицу.
9. Препарат по п.1, отличающийся тем, что диффузионная матрица содержит, по меньшей мере, этилцеллюлозу и, по меньшей мере, один жирный спирт в качестве компонентов, которые существенно влияют на характер высвобождения активных соединений.
10. Препарат по п.1, отличающийся тем, что препарат содержит обычные наполнители и добавки, особенно смазывающие агенты, агенты, облегчающие текучесть, пластификаторы.
11. Препарат по п.10, отличающийся тем, что он содержит в качестве смазывающего агента стеарат магния, стеарат кальция, и/или лаурат кальция, и/или жирные кислоты, предпочтительно, стеариновую кислоту.
12. Препарат по п.10, отличающийся тем, что в качестве добавок, способствующих текучести, он содержит высокодисперсную двуокись кремния, предпочтительно Aerosil®, тальк, кукурузный крахмал, окись магния и стеарат магния и/или кальция.
13. Стабильный при хранении фармацевтический препарат, содержащий оксикодон и налоксон в практически ненабухающей диффузионной матрице, характеризующийся тем, что характеристики высвобождения матрицы зависят от этилцеллюлозы и, по меньшей мере, одного жирного спирта, и препарат содержит оксикодон и налоксон в весовом отношении максимально 25:1, предпочтительно максимально 20:1, 15:1, особенно предпочтительно 5:1, 4:1, 3:1, 2:1 или 1:1.
14. Препарат по п.13, отличающийся тем, что оксикодон и налоксон содержатся в виде их фармацевтически приемлемых производных с равной активностью, например свободных оснований или солей.
15. Препарат по п.14, отличающийся тем, что оксикодон и налоксон содержатся в виде гидрохлорида, сульфата, бисульфата, тартрата, нитрата, цитрата, битартрата, фосфата, малата, малеата, гидробромида, гидроиодида, фумарата или сукцината.
16. Препарат по п.13, отличающийся тем, что оксикодон содержится в единичной дозе в избытке по отношению к налоксону.
17. Препарат по п.13, отличающийся тем, что налоксон содержится в количестве от 1 до 50 мг.
18. Препарат по п.13, отличающийся тем, что оксикодон содержится в количестве от 10 до 150 мг, предпочтительно от 10 до 80 мг.
19. Препарат по п.13, отличающийся тем, что препарат содержит практически не набухающую и не разрушающуюся диффузионную матрицу.
20. Препарат по п.19, отличающийся тем, что диффузионная матрица включает, по меньшей мере, этилцеллюлозу и, по меньшей мере, один жирный спирт в качестве компонентов, которые существенно влияют на характер высвобождения активных соединений.
21. Препарат по п.13, отличающийся тем, что жирные спирты включают лауриловый, миристиловый, стеариловый, цетостеа-риловый и/или цетиловый спирты, особенно предпочтительно стеариловый спирт.
22. Препарат по п.13, отличающийся тем, что он содержит обычные наполнители и добавки, особенно, смазывающие агенты, агенты, способствующие текучести, пластификаторы.
23. Препарат по п.22, отличающийся тем, что он в качестве смазывающих агентов содержит стеарат магния, стеарат кальция и/или лаурат кальция и/или жирные кислоты, предпочтительно стеариновую кислоту.
24. Препарат по п.22, отличающийся тем, что он содержит в качестве добавок, способствующих текучести, высокодисперсную двуокись кремния, предпочтительно Aerosil®, тальк, кукурузный крахмал, окись магния и стеарат магния и/или кальция.
25. Препарат по п.1 или 13, отличающийся тем, что вместо этилцеллюлозы он содержит коммерчески доступные полимерные смеси, которые включают этилцеллюлозу, предпочтительно Surelease® E-7-7050.
26. Препарат по п.1 или 13, характеризующийся тем, что он получен для орального, назального, ректального введения или для введения путем ингаляции.
27. Препарат по п.1 или 13, отличающийся тем, что он является таблеткой, пилюлей, капсулой, гранулой или порошком.
28. Препарат по п.1 или 13, отличающийся тем, что он или его предшественник получены методом гранулирования с укрупнением или измельчением.
29. Препарат по п.1 или 13, отличающийся тем, что он или его предшественники получены методом экструзии.
30. Препарат по п.1 или 13, отличающийся тем, что он может храниться в течение, по меньшей мере, двух лет в стандартных условиях при 60%-ной относительной влажности и температуре 25°С.
RU2004131870/15A 2002-04-05 2003-04-04 Фармацевтический препарат, содержащий оксикодон и налоксон RU2295344C2 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10215131A DE10215131A1 (de) 2002-04-05 2002-04-05 Matrix zur verzögerten, gleichbleibenden und unabhängigen Freisetzung von Wirkstoffen
DE10215131.8 2002-04-05
DE10215067.2 2002-04-05
DE10215067A DE10215067A1 (de) 2002-04-05 2002-04-05 Lagerstabiles pharmazeutisches Präparat, das Oxycodon und Naloxon umfasst

Publications (2)

Publication Number Publication Date
RU2004131870A true RU2004131870A (ru) 2005-05-27
RU2295344C2 RU2295344C2 (ru) 2007-03-20

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RU2004131870/15A RU2295344C2 (ru) 2002-04-05 2003-04-04 Фармацевтический препарат, содержащий оксикодон и налоксон
RU2004130845/15A RU2297225C2 (ru) 2002-04-05 2003-04-04 Матрица, обеспечивающая пролонгированное, инвариантное и независимое высвобождение активных соединений
RU2006128796/15A RU2342935C2 (ru) 2002-04-05 2006-08-08 Фармацевтическая композиция для лечения вызываемых опиоидами побочных эффектов и идиопатических синдромов

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