HRP20100127T1 - Višečestični oblici - Google Patents

Višečestični oblici Download PDF

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Publication number
HRP20100127T1
HRP20100127T1 HR20100127T HRP20100127T HRP20100127T1 HR P20100127 T1 HRP20100127 T1 HR P20100127T1 HR 20100127 T HR20100127 T HR 20100127T HR P20100127 T HRP20100127 T HR P20100127T HR P20100127 T1 HRP20100127 T1 HR P20100127T1
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HR
Croatia
Prior art keywords
multiparticle
oxycodone
forms according
pharmaceutical composition
plasticizer
Prior art date
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HR20100127T
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English (en)
Inventor
Walden Malcolm
Hayes Geoff
Mohammad Hassan
Tamber Harjit
Whitelock Steve
Martinelli Vincenzo
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Euro-Celtique S.A.
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Priority claimed from GB0315137A external-priority patent/GB0315137D0/en
Priority claimed from GB0403102A external-priority patent/GB0403102D0/en
Priority claimed from GB0413454A external-priority patent/GB0413454D0/en
Application filed by Euro-Celtique S.A. filed Critical Euro-Celtique S.A.
Publication of HRP20100127T1 publication Critical patent/HRP20100127T1/hr

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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
    • A61K9/14Particulate 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
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • 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
    • A61K9/14Particulate 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
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Organic Chemistry (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Processes Of Treating Macromolecular Substances (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Manufacturing Of Micro-Capsules (AREA)

Abstract

Ekstrudirani iz otopine, višečestični oblici sa kontroliranim oslobađanjem, naznačeni time što sadrže (a) oksikodon, (b) amonijev metakrilat kopolimer netopljiv u vodi, (c) plastifikator, (d) lubrikant i (e) modifikator vodopropusnosti, pri čemu je navedeni modifikator vodopropusnosti vodopropusan amonijev metakrilat kopolimer ili hidroksipropil metilceluloza. Patent sadrži još 26 patentnih zahtjeva.

Claims (27)

1. Ekstrudirani iz otopine, višečestični oblici sa kontroliranim oslobađanjem, naznačeni time što sadrže (a) oksikodon, (b) amonijev metakrilat kopolimer netopljiv u vodi, (c) plastifikator, (d) lubrikant i (e) modifikator vodopropusnosti, pri čemu je navedeni modifikator vodopropusnosti vodopropusan amonijev metakrilat kopolimer ili hidroksipropil metilceluloza.
2. Višečestični oblici prema patentnom zahtjevu 1, naznačeni time što je oksikodon prisutan kao farmaceutski prihvatljiva sol.
3. Višečestični oblici prema patentnom zahtjevu 2, naznačeni time što je oksikodon prisutan kao oksikodon hidroklorid.
4. Višečestični oblici prema bilo kojem od patentnih zahtjeva 1 do 3, naznačeni time što je plastifikator izabran od cetil alkohola, stearil alkohola, cetostearil alkohola, sorbitola, saharoze, visoke molekularne težine - polietilen glikola, dibutil sebacata, tributil citrata, trietil citrata, propilen glikola i polietilen glikola niske molekularne težine.
5. Višečestični oblici prema patentnom zahtjevu 4, naznačeni time što je plastifikator stearil alkohol.
6. Višečestični oblici prema patentnom zahtjevu 4, naznačeni time što je plastifikator polietilen glikol visoke molekularne težine.
7. Višečestični oblici prema bilo kojem od patentnih zahtjeva 1 do 6, naznačeni time što je lubrikant izabran od gliceril behenata, talka i silikon dioksida.
8. Višečestični oblici prema patentnom zahtjevu 7, naznačeni time što je lubrikant gliceril behenat.
9. Višečestični oblici prema bilo kojem od patentnih zahtjeva 1 do 6, naznačeni time što je lubrikant stearinska kiselina ili stearat sol.
10. Višečestični oblici prema bilo kojem od patentnih zahtjeva 1 do 9, naznačeni time što je modifikator vodopropusnosti vodopropusni amonijev metakrilat kopolimer.
11. Višečestični oblici prema bilo kojem od patentnih zahtjeva 1 do 10, naznačeni time što je modifikator vodopropusnosti - Eudragit RL PO.
12. Višečestični oblici prema bilo kojem od patentnih zahtjeva 1 do 11, naznačeni time što su postotne količine sastojaka (a) do (e) kao što su navedene u slijedećoj tabeli, na temelju ukupne težine pet sastojaka: oksikodon kao hidroklorid 3 do 50 netopljivi amonijev metakrilat kopolimer 25 do 85 plastifikator 1 do 30 lubrikant 1 do 25 modifikator vodopropusnosti 1 do 40.
13. Višečestični oblici prema patentnom zahtjevu 12, naznačeni time što su postotne količine sastojaka (a) do (e) kao što su navedene u slijedećoj tabeli, na temelju ukupne težine pet sastojaka: oksikodon kao hidroklorid 5 do 40 netopljjivi amonijev metakrilat kopolimer 35 do 75 plastifikator 3 do 25 lubrikant 2 do 25 modifikator vodopropusnosti 1 do 30.
14. Višečestični oblici prema patentnom zahtjevu 12, naznačeni time što su procentne količine sastojaka (a) do (e) kao što su navedene u slijedećoj tabeli, na osnovu ukupne težine pet sastojaka: oksikodon kao hidroklorid 7.5 do 35 netopljiv amonijev metakrilat kopolimer 50 do 65 plastifikator 5 do 15 lubrikant 2 do 25 modifikator vodopropusnosti 1 do 20.
15. Višečestični oblici prema patentnom zahtjevu 1, naznačeni time što sadrže oksikodon, Eudragit RS PO, stearil alkohol, gliceril behenat i Eudragit RL PO.
16. Farmaceutska kompozicija u obliku jedinične doze, naznačena time što sadrži višečestične oblike prema bilo kojem od prethodnih patentnih zahtjeva.
17. Farmaceutska kompozicija prema patentnom zahtjevu 16, naznačena time što jedinična doza osigurava dozu oksikodona koja je dovoljna da osigura analgeziju humanom pacijentu.
18. Farmaceutska kompozicija prema patentnom zahtjevu 17, naznačena time što je bioekvivalentna OxyContin® tabletama.
19. Farmaceutska kompozicija prema patentnom zahtjevu 17 ili 18, naznačena time što je dovoljna doza oksikodona 5 do 400 mg.
20. Farmaceutska kompozicija prema patentnom zahtjevu 19, naznačena time što je jedinična doza oksikodona 5 mg, 10 mg, 20 mg, 40 mg, 80 mg ili 160 mg.
21. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 16 do 20, naznačena time što je u obliku kapsule sa punjenjem od navedenih višečestičnih oblika.
22. Farmaceutska kompozicija prema patentnom zahtjevu 21, naznačena time što su višečestični oblici punjeni u tvrde želatinozne kapsule, pri čemu svaka od tih kapsula sadrži jediničnu dozu.
23. Farmaceutska kompozicija prema patentnom zahtjevu 22, naznačena time što je težina punjenja u kapsuli u opsegu od 120 do 500 mg.
24. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 16 do 23, naznačena time što je namjenjena za primjenu u intervalima od 12 sati.
25. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 16, 17 i 19 do 23, naznačena time što je namjenjena za primjenu u intervalima od 24 sata.
26. Postupak za pripremu višečestičnih oblika prema patentnom zahtjevu 1 naznačen time što sadrži pripremu mješavine koja sadrži (a) oksikodon, (b) amonijev metakrilat kopolimer koji je netopljiv u vodi, (c) plastifikator, (d) lubrikant i (e) modifikator vodopropusnosti, pri čemu je navedeni modifikator vodopropusnosti vodopropusan amonijev metakrilat kopolimer ili hidroksipropil metilceluloza; i ekstruziju mješavine.
27. Farmaceutska kompozicija naznačena time što sadrži višečestične oblike prema bilo kojem od patentnih zahtjeva 1 do 15 i višečestične oblike antagonista oksikodona.
HR20100127T 2003-06-27 2010-03-08 Višečestični oblici HRP20100127T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0315137A GB0315137D0 (en) 2003-06-27 2003-06-27 Multiparticulates
GB0403102A GB0403102D0 (en) 2004-02-12 2004-02-12 Multiparticulates
GB0413454A GB0413454D0 (en) 2004-06-16 2004-06-16 Multiparticulates
PCT/GB2004/002705 WO2005000310A1 (en) 2003-06-27 2004-06-23 Multiparticulates

Publications (1)

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HRP20100127T1 true HRP20100127T1 (hr) 2010-04-30

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ID=33556051

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HR20100127T HRP20100127T1 (hr) 2003-06-27 2010-03-08 Višečestični oblici
HRP20140635TT HRP20140635T1 (hr) 2003-06-27 2014-07-04 Multiäśestice

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EP (2) EP1644002B1 (hr)
JP (2) JP5348841B2 (hr)
KR (1) KR101116518B1 (hr)
AR (1) AR044935A1 (hr)
AT (1) ATE453394T1 (hr)
AU (1) AU2004251481B2 (hr)
BR (1) BRPI0411901B1 (hr)
CA (1) CA2530385C (hr)
CY (2) CY1109917T1 (hr)
DE (1) DE602004024888D1 (hr)
DK (2) DK1889621T3 (hr)
EA (1) EA013424B1 (hr)
ES (2) ES2490598T3 (hr)
HR (2) HRP20100127T1 (hr)
IL (1) IL172730A (hr)
MX (1) MXPA05013799A (hr)
MY (1) MY176831A (hr)
NO (1) NO20060443L (hr)
NZ (1) NZ544181A (hr)
PE (1) PE20050286A1 (hr)
PL (2) PL1889621T3 (hr)
PT (2) PT1889621E (hr)
SI (2) SI1889621T1 (hr)
TW (1) TWI357815B (hr)
WO (1) WO2005000310A1 (hr)

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CN1741792A (zh) * 2003-01-24 2006-03-01 控制递送系统有限公司 经眼部递送肾上腺素能剂的持续释放系统和方法
TWI357815B (en) * 2003-06-27 2012-02-11 Euro Celtique Sa Multiparticulates

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