HRP20120134T1 - Stabilni i lako topivljivi pripravci kandesartan-cileksetila, dobiveni vlažnim granuliranjem - Google Patents

Stabilni i lako topivljivi pripravci kandesartan-cileksetila, dobiveni vlažnim granuliranjem Download PDF

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Publication number
HRP20120134T1
HRP20120134T1 HR20120134T HRP20120134T HRP20120134T1 HR P20120134 T1 HRP20120134 T1 HR P20120134T1 HR 20120134 T HR20120134 T HR 20120134T HR P20120134 T HRP20120134 T HR P20120134T HR P20120134 T1 HRP20120134 T1 HR P20120134T1
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HR
Croatia
Prior art keywords
preparation
candesartan
cilexetil
surfactant
active drug
Prior art date
Application number
HR20120134T
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English (en)
Inventor
Gindullis Frank
Simoes Sergio
Gabriel Leitão da Silva Alberto
Original Assignee
Helm Ag
Bluepharma
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by Helm Ag, Bluepharma filed Critical Helm Ag
Publication of HRP20120134T1 publication Critical patent/HRP20120134T1/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
    • A61K9/2004Excipients; 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
    • 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
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/2022Organic 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
    • A61K9/14Particulate 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
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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

Abstract

Postupak dobivanja vlažno granuliranog pripravka kandesartan-cileksetila i/ili njegovih solvata ili hidrata, naznačen time što se sastoji u: a) kombiniranju kandesartan-cileksetila ili njegovih solvata ili hidrata s vodenom otopinom koja sadrži natrijev dokusat kao prvi surfaktant, te s natrijevim lauril-sulfatom kao drugim surfaktantom, tako da se kandesartan-cileksetil homogeno dispergira u otopini; b) kombiniranju navedene disperzije iz koraka (a) s najmanje jednom farmaceutskom pomoćnom tvari, po mogućnosti laktozom i/ili preželatiniranim škrobom i/ili kalcij-karboksimetilcelulozom i/ili hidroksipropilcelulozom, uz smicanje kako bi se dobilo vlažne granule; c) izbornom rešetanju i prosijavanju navedenih vlažnih granula; d) sušenju navedenih granula; e) izbornom umiješavanju drugih pomoćnih tvari; if) izbornom oblikovanju pripravka u oblike jedinica doziranja. Patent sadrži još 9 patentnih zahtjeva.

Claims (10)

1. Postupak dobivanja vlažno granuliranog pripravka kandesartan-cileksetila i/ili njegovih solvata ili hidrata, naznačen time što se sastoji u: a) kombiniranju kandesartan-cileksetila ili njegovih solvata ili hidrata s vodenom otopinom koja sadrži natrijev dokusat kao prvi surfaktant, te s natrijevim lauril-sulfatom kao drugim surfaktantom, tako da se kandesartan-cileksetil homogeno dispergira u otopini; b) kombiniranju navedene disperzije iz koraka (a) s najmanje jednom farmaceutskom pomoćnom tvari, po mogućnosti laktozom i/ili preželatiniranim škrobom i/ili kalcij-karboksimetilcelulozom i/ili hidroksipropilcelulozom, uz smicanje kako bi se dobilo vlažne granule; c) izbornom rešetanju i prosijavanju navedenih vlažnih granula; d) sušenju navedenih granula; e) izbornom umiješavanju drugih pomoćnih tvari; i f) izbornom oblikovanju pripravka u oblike jedinica doziranja.
2. Postupak u skladu s patentnim zahtjevom 1, naznačen time što se upotrebljava vodenu otopinu prvog surfaktanta, gdje je navedeni surfaktant prisutan u koncentraciji od otprilike 1 % do 20% (tež./tež.), po mogućnosti od 2% do 8 % (tež./tež.).
3. Postupak dobivanja oblika jedinice doziranja koji sadrži kandesartan-cileksetil i/ili njegove solvate ili hidrate i najmanje jedan drugi aktivni lijek, naznačen time što se pripravak kojeg se dobiva postupkom u skladu s patentnim zahtjevima 1 i 2 kombinira s najmanje jednim drugim aktivnim lijekom i izborno dodatnim pomoćnim tvarima.
4. Postupak u skladu s patentnim zahtjevom 3, naznačen time što navedeni drugi aktivni lijek se dodaje u otopinu iz koraka (a) i/ili u smjesu iz koraka (b) i/ili u granule iz koraka (e) kako bi se kombiniralo pripravak s navedenim drugim aktivnim lijekom.
5. Vlažno granulirani farmaceutski pripravak kandesartan-cileksetila i/ili njegovih solvata ili hidrata, naznačen time što sadrži: a) kandesartan-cileksetil, ili njegove solvate ili hidrate, predobrađen vodenom otopinom natrijevog dokusata kao prvogm surfaktanta, te natrijevim lauril-sulfatom kao drugim surfaktantom; i b) najmanje jednu farmaceutski prihvatljivu pomoćnu tvar, dobivenu postupkom u skladu s bilo kojim od patentnih zahtjeva 1 do 4.
6. Vlažno granulirani farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što se farmaceutski prihvatljivu pomoćnu tvar bira između celuloza i celuloznih derivata, laktoze, škrobovi i škrobnih derivata, ciklodekstrina, polidekstroza, ili smjesa navedenih tvari, a po mogućnosti je se bira između hidroksipropilceluloze, laktoze i kalcij-karboksimetilceluloze, te preželatiniranog škroba.
7. Oblik jedinice doziranja kojeg se dobiva iz vlažno granuliranog pripravka u skladu s patentnim zahtjevom 5 ili 6, naznačen time što je navedeni oblik jedinice doziranja tableta ili kapsula, gdje je po mogućnosti navedeni oblik doziranja obložen.
8. Vlažno granulirani farmaceutski pripravak u skladu s patentnim zahtjevom 5 ili 6, naznačen time što je navedena kombinacija surfaktanata prisutna u rasponu koncentracija od otprilike 0,1% do 10 % (tež./tež.) navedenog pripravka, po mogućnosti u rasponu od 0,5% do 5 % (tež./tež.) navedenog pripravka.
9. Vlažno granulirani farmaceutski pripravak u skladu s patentnim zahtjevom 5 ili 6, naznačen time što navedeni pripravak također sadrži najmanje jedan aktivni lijek uz kandesartan-cileksetil.
10. Vlažno granulirani farmaceutski pripravak u skladu s patentnim zahtjevom 9, naznačen time što se navedeni dodatni aktivni lijek bira iz skupina diuretika, po mogućnosti hidroklortiazida, antihipertenzivnih sredstava, po mogućnosti amlodipina i njegovih soli, te inhibitora reduktaze, po mogućnosti atorvastatina i njegovih soli.
HR20120134T 2008-09-17 2012-02-10 Stabilni i lako topivljivi pripravci kandesartan-cileksetila, dobiveni vlažnim granuliranjem HRP20120134T1 (hr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08016396A EP2165702B1 (en) 2008-09-17 2008-09-17 Stable and readily dissolved compositions of candesartan cilexetil prepared with wet granulation

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HRP20120134T1 true HRP20120134T1 (hr) 2012-03-31

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Country Status (8)

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EP (1) EP2165702B1 (hr)
AT (1) ATE533474T1 (hr)
DK (1) DK2165702T3 (hr)
ES (1) ES2377552T3 (hr)
HR (1) HRP20120134T1 (hr)
PL (1) PL2165702T3 (hr)
PT (1) PT2165702E (hr)
SI (1) SI2165702T1 (hr)

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JP5917844B2 (ja) * 2011-06-24 2016-05-18 日本ケミファ株式会社 カンデサルタンシレキセチル製剤
PL236001B1 (pl) 2012-12-21 2020-11-30 Adamed Spolka Z Ograniczona Odpowiedzialnoscia Złożona kompozycja farmaceutyczna zawierająca kandesartan cyleksetylu oraz amlodypinę, sposób jej wytwarzania oraz jednostkowa postać dawkowania zawierająca tę kompozycję
EP2952187A4 (en) * 2013-01-30 2016-08-17 Sawai Seiyaku Kk PHARMACEUTICAL COMPOSITION WITH CANDESARTAN CILEXETIL
KR101710441B1 (ko) * 2015-12-28 2017-02-28 신풍제약주식회사 안정성 및 용출성이 향상된 정제
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JP2018141011A (ja) * 2018-05-24 2018-09-13 日本ケミファ株式会社 カンデサルタン シレキセチル製剤
KR20230000506A (ko) * 2021-06-24 2023-01-03 주식회사 종근당 칸데사르탄, 암로디핀 및 아트로바스타틴을 포함하는 약제학적 복합제제

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Publication number Publication date
ES2377552T3 (es) 2012-03-28
EP2165702A1 (en) 2010-03-24
PT2165702E (pt) 2012-02-07
EP2165702B1 (en) 2011-11-16
SI2165702T1 (sl) 2012-05-31
ATE533474T1 (de) 2011-12-15
DK2165702T3 (da) 2012-03-05
PL2165702T3 (pl) 2012-04-30

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