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DK1126826T6 - Multipartikel-modificeret-frigivelsessammensætning af methylphenidat - Google Patents

Multipartikel-modificeret-frigivelsessammensætning af methylphenidat Download PDF

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Publication number
DK1126826T6
DK1126826T6 DK99956822.3T DK99956822T DK1126826T6 DK 1126826 T6 DK1126826 T6 DK 1126826T6 DK 99956822 T DK99956822 T DK 99956822T DK 1126826 T6 DK1126826 T6 DK 1126826T6
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DK
Denmark
Prior art keywords
methylphenidate
modified release
composition
component
release
Prior art date
Application number
DK99956822.3T
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English (en)
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DK1126826T5 (da
DK1126826T3 (da
Inventor
John G Devane
Paul Stark
Niall M M Fanning
Singh Rekhi Gurvinder
Original Assignee
Alkermes Pharma Ireland Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22312931&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK1126826(T6) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Alkermes Pharma Ireland Ltd filed Critical Alkermes Pharma Ireland Ltd
Publication of DK1126826T3 publication Critical patent/DK1126826T3/da
Publication of DK1126826T5 publication Critical patent/DK1126826T5/da
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Publication of DK1126826T6 publication Critical patent/DK1126826T6/da

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K9/50Microcapsules 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
    • A61K9/5084Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4458Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (30)

1. Multipartikel-modificeret-frigivelsessammensætning, der indeholder methylphenidat og har en første-komponent, der omfatter en førstepopulation af methylphenidat-indeholdende-partikler og mindst en efterfølgende-komponent, hvor hver efterfølgende-komponent omfatter en efterfølgende-population af methylphenidat-indeholdende-partikler; hvori den mindst ene efterfølgende-population af methylphenidat-indeholdende-partikler yderligere omfatter en modificeret-frigivelsescoating eller, alternativt eller yderligere, et modificeret-frigivelses-matrixmateriale, så at sammensætningen efter oral levering til et individ leverer methylphenidaten på en pulserende måde, for at danne perioder med høje blodplasmakoncentrationer af methylphenidat spredt med perioder med lave blodplasmakoncentrationer af methylphenidat, hvori perioderne med lave blodplasmakoncentrationer tilvejebringer udvaskning af methylphenidat.
2. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori sammensætningen omfatter en første-komponent og en efterfølgende-komponent.
3. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 2, hvori den første-komponent omfatter en øjeblikkelig-frigivelseskomponent og den efterfølgende-komponent er en modificeret-frigivelseskomponent.
4. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 3, hvori den modificerede-frigivelseskomponent omfatter partikler, der har modificeret-frigivelsescoating.
5. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 3, hvori den modificerede-frigivelseskomponent omfatter et modificeret-frigivelses-matrixmateriale.
6. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori methylphenidaten hovedsagelig omfatter en optisk ren enantiomer eller en blanding, racemat eller på anden vis, af enantiomerer.
7. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori mindst en af de første- og efterfølgende-komponenter yderligere omfatter en forøger.
8. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori mængden af methylphenidat indeholdt i de første- og efterfølgende-komponenter er den samme eller forskellige.
9. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 8, hvori mængden af methylphenidat indeholdt i hver komponent er fra 0,1 mg til 500 mg.
10. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori methylphenidaten er i form af et farmaceutisk acceptabelt salt deraf en enantiomer eller blandinger deraf eller blandinger deraf.
11. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori de første- og efterfølgende-populationer af methylphenidat-indeholdende-partikler har forskellige in v/Yro-opløsningsprofiler.
12. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori den første-komponent er en øjeblikkelig-frigivelseskomponent og i den mindst ene efterfølgende-komponent er en modificeret-frigivelseskomponent.
13. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 12, som ved brug hovedsagelig frigiver hele methylphenidaten fra den førstepopulation af methylphenidat-indeholdende-partikler før frigivelse af methylphenidaten fra den efterfølgende-population af methylphenidat-indeholdende-partikler.
14. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 1, hvori in-v/vO-frigivelsen af methylphenidaten i et individ efterligner /n-v/vo-frigivelsen af methylphenidat indgivet i form af to eller flere doser af øjeblikkelig- frigivelsesformer af methylphenidat.
15. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 10, hvori in- v/Vo-frigivelsen af methylphenidaten i et individ efterligner in-vivo-frigivelsen af methylphenidat indgivet i form af to eller flere doser af øjeblikke-lig-frigivelsesformer af methylphenidat.
16. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 13, hvori den gennemsnittelige in v/Vo-opløsningsprofil målt i USP-Type-l-apparat (100 rpm) i 0,01 N HCI, pH 2,0 og 37 °C er sådan at ca. 50 til 100 % af methylphenidaten indeholdt i den første-population af methylphenidat-indeholdende-partikler er frigivet indenfor fire timer af indgivelse af sammensætningen og ca. 30 til 100 % af methylphenidaten indeholdt i den efterfølgende-population af methylphenidat-indeholdende-partikler er frigivet mellem fire og otte timer efter indgivelse af sammensætningen.
17. Multipartikel-modificeret-frigivelsessammensætning ifølge krav 13, hvori den gennemsnittelige in v/Vo-opløsningsprofil målt i USP-Type-l-apparat (100 rpm) i 0,01 N HCI, pH 2,0 og 37 °C er sådan at ca. 80 til 100 % af methylphenidaten indeholdt i den første population af methylphenidat- indeholdende-partikler er frigivet indenfor fire timer af indgivelse af sammensætningen og ca. 60 til 100 % af methylphenidaten indeholdt i den efterfølgende population af methylphenidat-indeholdende-partikler er frigivet mellem fire og otte timer efter indgivelse af sammensætningen.
18. Fast oral-dosisform, der omfatter en multipartikel-modificeret- frigivelsessammensætning ifølge krav 1.
19. Fast oral dosisform ifølge krav 18, der omfatter en blanding af første- og efterfølgende-methylphenidat-indeholdende-partikler fyldt ind i hårde gelatine- eller bløde gelatine kapsler.
20. Fast oral dosisform ifølge krav 18, hvori de første- og efterfølgende-komponenter komprimeres adskilt og uafhængigt til mini-tabletter og fyldt ind i hårde- eller bløde gelatine kapsler.
21. Fast oraldosisform ifølge krav 18, hvori den første-komponent er komprimeret til det første lag af en multilagstablet og den mindst ene efterfølgende-komponent er komprimeret til et efterfølgende lag af multilagstabletten.
22. Fast oral dosisform ifølge krav 18, hvori de første- og efterfølgende-komponenter er inkorporeret i en hurtig-opløsende-dosisform.
23. Fast oraldosisform ifølge krav 22, hvori den hurtig-opløsende-dosisform er en hurtigsmeltende tablet dosisform.
24. Anvendelse af en multipartikel-modificeret-frigivelsessammensætning ifølge krav 1 i fremstillingen af et medikament til behandling af opmærksomhedsforstyrrelsessygdom.
25. Anvendelse af en multipartikel-modificeret-frigivelsessammensætning ifølge krav 10 i fremstillingen af et medikament til behandling af opmærksomhedsforstyrrelsessygdom.
26. Anvendelse ifølge krav 24 eller 25, hvori sygdommen er kendetegnet ved opbygning af patienttolerance til methylphenidat indgivet i behandlingen af tilstanden.
27. Sammensætningen ifølge krav 3, hvori den modificerede- frigivelseskomponent omfatter en pH-afhængig-polymercoating, som frigiver en puls af methylphenidat fra den modificerede-frigivelseskomponent efter af en forsinkelsestid.
28. Sammensætningen ifølge krav 27, hvori den pH-afhængige-polymercoating omfatter methacrylat-copolymerer.
29. Sammensætningen ifølge krav 27, hvori den pH-afhængige-polymercoating omfatter en blanding af methacrylat og ammoniomethacrylat-copolymerer i et forhold tilstrækkeligt til at opnår en puls af aktiv ingrediens fra den modificerede- frigivelseskomponent efter af en forsinkelsestid.
30. Sammensætningen ifølge krav 29, hvori forholdet af methacrylat til am-moniomethacrylat-copolymerer is 1:1.
DK99956822.3T 1998-11-02 1999-11-01 Multipartikel-modificeret-frigivelsessammensætning af methylphenidat DK1126826T6 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10672698P 1998-11-02 1998-11-02
PCT/US1999/025632 WO2000025752A1 (en) 1998-11-02 1999-11-01 Multiparticulate modified release composition

Publications (3)

Publication Number Publication Date
DK1126826T3 DK1126826T3 (da) 2009-01-19
DK1126826T5 DK1126826T5 (da) 2018-10-22
DK1126826T6 true DK1126826T6 (da) 2019-06-24

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DK99956822.3T DK1126826T6 (da) 1998-11-02 1999-11-01 Multipartikel-modificeret-frigivelsessammensætning af methylphenidat

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US (7) US6228398B1 (da)
EP (3) EP1126826B3 (da)
JP (2) JP4613275B2 (da)
KR (3) KR100812832B1 (da)
CN (2) CN100444830C (da)
AR (1) AR021858A1 (da)
AT (1) ATE411011T3 (da)
AU (4) AU770645B2 (da)
BR (1) BRPI9914977B8 (da)
CA (2) CA2348871C (da)
CO (1) CO5261536A1 (da)
CY (1) CY1110421T1 (da)
CZ (1) CZ303495B6 (da)
DE (1) DE69939748D1 (da)
DK (1) DK1126826T6 (da)
ES (1) ES2313797T7 (da)
HK (1) HK1050487A1 (da)
HU (1) HU230454B1 (da)
ID (1) ID29852A (da)
IL (4) IL142896A0 (da)
MX (1) MXPA01004381A (da)
MY (1) MY122159A (da)
NO (1) NO343240B1 (da)
NZ (1) NZ511442A (da)
PE (1) PE20001322A1 (da)
PL (1) PL205109B1 (da)
PT (1) PT1126826E (da)
RU (1) RU2236847C2 (da)
SK (1) SK287674B6 (da)
TR (1) TR200101216T2 (da)
WO (1) WO2000025752A1 (da)

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