HRP20110863T1 - Oblik produljenog oslobađanja paliperidona - Google Patents

Oblik produljenog oslobađanja paliperidona Download PDF

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Publication number
HRP20110863T1
HRP20110863T1 HR20110863T HRP20110863T HRP20110863T1 HR P20110863 T1 HRP20110863 T1 HR P20110863T1 HR 20110863 T HR20110863 T HR 20110863T HR P20110863 T HRP20110863 T HR P20110863T HR P20110863 T1 HRP20110863 T1 HR P20110863T1
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Croatia
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tablet
release
cellulose
paliperidone
polymer
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HR20110863T
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English (en)
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Fox Michael
Di Capua Simona
Reinberg Ronny
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Teva Pharmaceutical Industries Ltd.
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Publication of HRP20110863T1 publication Critical patent/HRP20110863T1/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
    • A61K9/20Pills, 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K9/2072Pills, 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61K9/167Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2072Pills, 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
    • 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
    • A61K9/2072Pills, 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
    • A61K9/2081Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5036Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/5073Microcapsules 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 having two or more different coatings optionally including drug-containing subcoatings
    • 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
    • A61K9/5073Microcapsules 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 having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078Microcapsules 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 having two or more different coatings optionally including drug-containing subcoatings with drug-free core

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Tableta paliperidona s produljenim oslobađanjem u obliku uložene tablete koja obuhvaća: (a) uloženu jezgru koja sadrži neobloženi paliperidon i barem jedan polimer koji može odgoditi oslobađanje paliperidona iz uložene jezgre i koji može nabubriti kada se navlaži; i (b) vanjski sloj koji sadrži farmaceutsku pomoćnu tvar koja je u biti netopljiva u vodi, pri čemu vanjski sloj samo djelomično okružuje uloženu jezgru. Patent sadrži još 14 patentnih zahtjeva.

Claims (15)

1. Tableta paliperidona s produljenim oslobađanjem u obliku uložene tablete koja obuhvaća: (a) uloženu jezgru koja sadrži neobloženi paliperidon i barem jedan polimer koji može odgoditi oslobađanje paliperidona iz uložene jezgre i koji može nabubriti kada se navlaži; i (b) vanjski sloj koji sadrži farmaceutsku pomoćnu tvar koja je u biti netopljiva u vodi, pri čemu vanjski sloj samo djelomično okružuje uloženu jezgru.
2. Tableta s produljenim oslobađanjem prema zahtjevu 1, gdje se barem jedan polimer za jezgru tablete izabire iz grupe koja obuhvaća polivinilpirolidon, poli(etilen oksid), polisaharide, hidrofilne derivate celuloze, metilcelulozu, etil celulozu, hidroksipropil metilcelulozu, hidroksietil celulozu, hidroksipropil celulozu, hidroksietil metilcelulozu, karboksi metilcelulozu i natrij karboksi metilcelulozu, poželjno se taj barem jedan polimer za jezgru tablete izabire iz grupe koja obuhvaća metil celulozu, etil celulozu, hidroksipropilmetilcelulozu, hidroksietil celulozu, hidroksipropil celulozu, hidroksietil metilcelulozu, karboksi metilcelulozu i natrij karboksi metilcelulozu, poželjnije se taj barem jedan polimer za jezgru tablete izabire iz grupe koja obuhvaća poli(etilen oksid) i hidroksipropil metilcelulozu.
3. Tableta s produljenim oslobađanjem prema zahtjevu 1 ili zahtjevu 2, pri čemu je farmaceutska pomoćna tvar za vanjski sloj, i koja je u biti netopljiva u vodi, farmaceutski prihvatljivi polimer koji je u biti netopljiv u vodi, poželjno se taj farmaceutski prihvatljivi polimer koji je u biti netopljiv u vodi izabire iz grupe koja obuhvaća kationske kopolimere etilakrilata i metilakrilata s kvartarnim amonijevim skupinama, etilakrilat metilmetakrilat kopolimer s neutralnim esterskim skupinama, estere celuloze, etere celuloze i esteretere celuloze, etil celuloze kao što su celuloza acetat, celuloza diacetat, celuloza triacetat i poliesterske polimere, poli(ε-kaprolakton)e, poli(alkilen glikol adipat)e, poli(etilen glikol adipat), poli(propilen glikol adipat) i poli(butilen glikol adipat), polivinil acetat te njihove mješavine i kopolimere.
4. Tableta s produljenim oslobađanjem prema zahtjevu 3, gdje je farmaceutski prihvatljivi polimer, koji je u biti netopljiv u vodi, etil celuloza.
5. Tableta s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 3, gdje je uložena jezgra u obliku tablete ili komprimiranog umetka.
6. Tableta s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 3, gdje jezgra i/ili vanjski sloj nezavisno dalje sadrže barem jednu drugu farmaceutsku pomoćnu tvar.
7. Tableta s produljenim oslobađanjem prema zahtjevu 6, gdje se ta barem jedna druga farmaceutski pomoćna tvar izabire iz grupe koja obuhvaća farmaceutski prihvatljiva punila, nosače, modifikatore pH, sredstva za kliženje, lubrikante, veziva, boje i arome.
8. Tableta s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 7, gdje jezgra sadrži paliperidon u količini od oko 1-3% w/w, punilo oko 2-5% w/w, modifikator pH oko 5-15% w/w, polimer koji regulira oslobađanje oko 5-20% w/w, lubrikant oko 0-1% w/w i sredstvo za kliženje oko 0-1% w/w; a vanjski sloj sadrži polimer koji regulira oslobađanje u količini od oko 50-90% w/w, boju oko 0-1% w/w i lubrikant oko 0-1% w/w.
9. Tableta s produljenim oslobađanjem prema zahtjevu 8, gdje uložena jezgra sadrži paliperidon u količini od oko 1-3% w/w, STARLAC oko 2-5% w/w, magnezijev karbonat USP oko 5-15% w/w, poli(etilen oksid) oko 5-20% w/w, stearinsku kiselinu NF oko 0-1% w/w i silicijev dioksid NF oko 0-1% w/w; a vanjski sloj sadrži etil celulozu u količini od oko 50-90% w/w, žuti željezov oksid NF oko 0-1% w/w i stearinsku kiselinu NF oko 0-1% w/w.
10. Postupak izrade tablete s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 9, koji obuhvaća (1) miješanje paliperidona i barem jednog polimera koji odgađa oslobađanje paliperidona i koji može nabubriti kada se navlaži; i (2) djelomično pokrivanje smjese iz koraka (1) s vanjskim slojem koji sadrži farmaceutsku pomoćnu tvar koja je u biti netopljiva u vodi, da se dobije tableta s produljenim oslobađanjem u obliku djelomično obložene tablete.
11. Postupak prema zahtjevu 10, gdje se mješavina iz koraka (1) komprimira u umetak ili tabletu prije koraka (2).
12. Postupak prema zahtjevu 10, gdje se mješavina iz koraka (1) komprimira u umetak ili tabletu prije koraka (2); umetak ili tableta se miješa s barem jednim polimerom, koji odgađa oslobađanje paliperidona i koji može nabubriti kada se navlaži, radi formiranja smjese; i smjesa se komprimira u tabletu prije koraka (2).
13. Postupak prema bilo kojem od zahtjeva 10 do 12, gdje se punilo, modifikator pH, sredstvo za kliženje i/ili lubrikant dodaju u koraku (1).
14. Postupak prema zahtjevu 11 ili 12, gdje se umetak ili tableta nastali kompresijom melju prije miješanja s barem jednim polimerom, koji odgađa oslobađanje paliperidona i koji može nabubriti kada se navlaži, radi formiranja smjese koja se komprimira u tabletu prije koraka (2).
15. Postupak prema bilo kojem od zahtjeva 10 do 14, gdje se proizvod iz koraka (2) komprimira da se dobije umetnuta tableta.
HR20110863T 2007-08-21 2011-11-21 Oblik produljenog oslobađanja paliperidona HRP20110863T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US93559707P 2007-08-21 2007-08-21
PCT/US2008/010014 WO2009025859A1 (en) 2007-08-21 2008-08-21 Paliperidone sustained release formulation

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US (1) US20090087487A1 (hr)
EP (1) EP2079446B1 (hr)
AT (1) ATE530170T1 (hr)
ES (1) ES2374200T3 (hr)
HR (1) HRP20110863T1 (hr)
PL (1) PL2079446T3 (hr)
PT (1) PT2079446E (hr)
WO (1) WO2009025859A1 (hr)

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WO2010009900A1 (en) * 2008-07-25 2010-01-28 Krka, D.D. Novo Mesto Paliperidone composition comprising solid matrix particles
EP2161019A1 (en) * 2008-09-05 2010-03-10 KRKA, D.D., Novo Mesto Prolonged release multiparticulate pharmaceutical composition comprising paliperidone
WO2010089775A2 (en) * 2009-02-05 2010-08-12 Getz Pharma Research Improved drug dosage form for controlled delivery of one or more pharmaceutically active agent
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PL2079446T3 (pl) 2012-04-30
US20090087487A1 (en) 2009-04-02
ES2374200T3 (es) 2012-02-14
ATE530170T1 (de) 2011-11-15
EP2079446A1 (en) 2009-07-22
WO2009025859A1 (en) 2009-02-26
PT2079446E (pt) 2011-12-23
EP2079446B1 (en) 2011-10-26

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