HRP20200046T1 - Formulacije apiksabana - Google Patents

Formulacije apiksabana Download PDF

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Publication number
HRP20200046T1
HRP20200046T1 HRP20200046TT HRP20200046T HRP20200046T1 HR P20200046 T1 HRP20200046 T1 HR P20200046T1 HR P20200046T T HRP20200046T T HR P20200046TT HR P20200046 T HRP20200046 T HR P20200046T HR P20200046 T1 HRP20200046 T1 HR P20200046T1
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HR
Croatia
Prior art keywords
tablet
apixaban
tablets
mixing
less
Prior art date
Application number
HRP20200046TT
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English (en)
Inventor
Jatin Patel
Charles Frost
Jingpin Jia
Chandra Vema-Varapu
Original Assignee
Bristol-Myers Squibb Holdings Ireland Unlimited Company
Pfizer Inc.
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43901603&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20200046(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol-Myers Squibb Holdings Ireland Unlimited Company, Pfizer Inc. filed Critical Bristol-Myers Squibb Holdings Ireland Unlimited Company
Publication of HRP20200046T1 publication Critical patent/HRP20200046T1/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
    • 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
    • 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
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • 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
    • A61K9/20Pills, 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
    • A61K9/2013Organic 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
    • 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
    • A61K9/2095Tabletting 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
    • 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
    • A61K9/4833Encapsulating processes; Filling of capsules
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring

Claims (10)

1. Tableta koja sadrži do 5 mg kristalnih čestica apiksabana koje imaju D90 manji od 89 µm, kao što je mjereno rasipanjem laserske svjetlosti, i farmaceutski prihvatljiv razblaživač ili nosač, gdje formulacija pokazuje svojstva otapanja takva da se količina lijeka koja je ekvivalentna sa najmanje 77% otapa u roku od 30 minuta, pri čemu se test otapanja izvodi u vodenom mediju puferiranom na pH opseg 1 do 7.4 i kontroliran je na 37° C.
2. Tableta kao što je definirano u patentnom zahtjevu 1, gdje (a) rezultat je utvrđen kao prosjek od 6 tableta; i/ili (b) test otapanja je izveden u 900 mL medija za otapanje koji sadrži 0.05 M natrij fosfata pri pH 6.8 sa 0.05% SDS na 37 °C upotrebom USP aparata 2 (lopatice) pri brzini rotacije od 75 o/min i uzorci su analizirani za apiksaban pomoću HPLC na 280 nm.
3. Tableta kao što je definirano u patentnom zahtjevu 1 ili 2, gdje navedena kompozicija sadrži oblik N-1 apiksabana.
4. Tableta kao što je definirano u bilo kojem od patentnih zahtjeva 1 do 3, gdje je apiksaban u obliku kristalnih čestica koje imaju D90 manji od 50 µm, D90 manji od 30 µm ili D90 manji od 25 µm kao što je mjereno rasipanjem laserske svjetlosti.
5. Tableta kao što je definirano u bilo kojem od patentnih zahtjeva 1 do 4, gdje je apiksaban u obliku kristalnih čestica koje imaju srednju vrijednost veličine čestice manju od 89 µm kao što je mjereno rasipanjem laserske svjetlosti.
6. Tableta za upotrebu u liječenju tromboembolijskog poremećaja, gdje tableta je tableta kao što je definirano u jednom od patentnih zahtjeva 1 do 5.
7. Tableta za upotrebu u liječenju tromboembolijskog poremećaja kao što je definirano u patentnom zahtjevu 6, gdje je tableta administrirana oralno dva puta dnevno.
8. Postupak proizvodnje tableta apiksabana, gdje svaka tableta ima kompoziciju koja sadrži do 5 mg kristalnih čestica apiksabana i farmaceutski prihvatljiv razblaživač ili nosač, koji obuhvaća korake: (1) miješanja sirovih materijala potrebno prije granulacije; (2) granulacija sirovih materijala iz koraka (1) primjenom procesa suhe granulacije, pri čemu čestice apiksabana imaju D90 manji od 89 µm kao što je mjereno sa rasipanjem laserske svjetlosti; (3) miješanja granula određene veličine iz koraka (2) sa ekstragranularnim sirovim materijalima; (4) komprimiranja smjese iz koraka (3) u tablete; i (5) oblaganja filmom tableta iz koraka (4), gdje formulacija pokazuje svojstva otapanja takva da se količina lijeka koja je ekvivalentna sa najmanje 77% otapa u roku od 30 minuta, pri čemu se test otapanja izvodi u vodenom mediju puferiranom na pH opseg 1 do 7.4 i kontroliran je na 37° C.
9. Postupak proizvodnje tableta apiksabana kao što je definirano u patentnom zahtjevu 8, pri čemu su svojstva otapanja utvrđena kao prosjek od 6 tableta.
10. Postupak proizvodnje tableta apiksabana kao što je definirano u patentnom zahtjevu 8 ili 9 koji obuhvaća korake: (1) miješanja sirovih materijala, sa apiksabanom kontrolirane veličine čestica; (2) uključivanja intragranularnih dijelova vezujućeg sredstva, sredstva za raspadanje i drugih punilaca u smjesu iz koraka (1); (3) granulacije materijala iz koraka (2) korištenjem postupka suhe granulacije koji obuhvaća: (a) uklanjanje grudica iz intragranularnog lubrikanta upotrebom pogodnog sita ili mlina; (b) dodavanje lubrikanta smjesi iz koraka (2) i miješanje; (c) sabijanje ovlažene smjese u trake gustoće u opsegu od 1.1 do 1.2 g/cm3 i formiranje do dane veličine sabijenih traka upotrebom valjak kompaktora; (4) miješanja granula određene veličine iz koraka (3) i ekstragranularnog sredstva za raspadanje u odgovarajućoj mješalici; (5) uklanjanja grudica iz ekstragranularnog lubrikanta upotrebom pogodnog sita/mlina i miješanje sa granulama iz koraka (4); (6) komprimiranja smjese iz (5) u tablete; (7) oblaganja filmom tableta iz koraka (6).
HRP20200046TT 2010-02-25 2020-01-13 Formulacije apiksabana HRP20200046T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30805610P 2010-02-25 2010-02-25
EP17175864.2A EP3246021B1 (en) 2010-02-25 2011-02-24 Apixaban formulations

Publications (1)

Publication Number Publication Date
HRP20200046T1 true HRP20200046T1 (hr) 2020-03-20

Family

ID=43901603

Family Applications (5)

Application Number Title Priority Date Filing Date
HRP20160179TT HRP20160179T1 (hr) 2010-02-25 2016-02-19 Formulacije apiksabana
HRP20190430TT HRP20190430T8 (hr) 2010-02-25 2019-03-05 Formulacije apiksabana
HRP20192064TT HRP20192064T1 (hr) 2010-02-25 2019-11-15 Formulacije apiksabana
HRP20192069TT HRP20192069T1 (hr) 2010-02-25 2019-11-18 Formulacije apiksabana
HRP20200046TT HRP20200046T1 (hr) 2010-02-25 2020-01-13 Formulacije apiksabana

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Application Number Title Priority Date Filing Date
HRP20160179TT HRP20160179T1 (hr) 2010-02-25 2016-02-19 Formulacije apiksabana
HRP20190430TT HRP20190430T8 (hr) 2010-02-25 2019-03-05 Formulacije apiksabana
HRP20192064TT HRP20192064T1 (hr) 2010-02-25 2019-11-15 Formulacije apiksabana
HRP20192069TT HRP20192069T1 (hr) 2010-02-25 2019-11-18 Formulacije apiksabana

Country Status (31)

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US (5) US9326945B2 (hr)
EP (7) EP3662899A1 (hr)
JP (4) JP5846647B2 (hr)
KR (4) KR20210124532A (hr)
CN (3) CN109602716A (hr)
AU (1) AU2011220775B2 (hr)
BR (1) BR112012021337A8 (hr)
CA (1) CA2791171C (hr)
CO (1) CO6640207A2 (hr)
CY (5) CY1117434T1 (hr)
DK (5) DK2538925T3 (hr)
ES (5) ES2757603T3 (hr)
HK (5) HK1180248A1 (hr)
HR (5) HRP20160179T1 (hr)
HU (4) HUE047140T2 (hr)
IL (3) IL309564A (hr)
IN (1) IN2012DN06587A (hr)
LT (4) LT3251660T (hr)
MX (3) MX353145B (hr)
NZ (1) NZ601738A (hr)
PE (3) PE20160042A1 (hr)
PL (5) PL3017811T3 (hr)
PT (5) PT3257500T (hr)
RS (5) RS59810B1 (hr)
RU (1) RU2685724C2 (hr)
SG (2) SG10201501349VA (hr)
SI (5) SI2538925T1 (hr)
SM (1) SMT201600049B (hr)
TR (1) TR201903195T4 (hr)
WO (1) WO2011106478A2 (hr)
ZA (1) ZA201205807B (hr)

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