HRP20160880T4 - Formulacija obložene tablete i postupak - Google Patents

Formulacija obložene tablete i postupak Download PDF

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Publication number
HRP20160880T4
HRP20160880T4 HRP20160880TT HRP20160880T HRP20160880T4 HR P20160880 T4 HRP20160880 T4 HR P20160880T4 HR P20160880T T HRP20160880T T HR P20160880TT HR P20160880 T HRP20160880 T HR P20160880T HR P20160880 T4 HRP20160880 T4 HR P20160880T4
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HR
Croatia
Prior art keywords
coating
tablet
coated tablet
polymer
coating layer
Prior art date
Application number
HRP20160880TT
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English (en)
Inventor
Divyakant Desai
Bing I. Li
Original Assignee
Astrazeneca Ab
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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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34971747&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20160880(T4) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of HRP20160880T1 publication Critical patent/HRP20160880T1/hr
Publication of HRP20160880T4 publication Critical patent/HRP20160880T4/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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K9/20Pills, 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (16)

1. Obložena tableta naznačena time da sadrži jezgru tablete i a) unutrašnji brtveni sloj premaza obložen oko jezgre tablete, koji sadrži formulaciju polimera za oblaganje koji sadrži polimer baziran na polivinilalkoholu (PVA); b) drugi sloj premaza obložen oko unutrašnjeg brtvenog premaza jezgre tablete, te drugi sloj premaza sadrži saksagliptin ili njegovu farmaceutski prihvatljivu sol, te formulacija polimera za oblaganje sadrži polimer baziran na PVA; i c) vanjski zaštitni sloj premaza obložen oko drugog sloja premaza jezgre tablete, navedeni vanjski zaštitni sloj premaza sadrži formulaciju sloja premaza koja sadrži polimer baziran na PVA.
2. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da navedeni drugi sloj premaza se sastoji od 0.1 do 70% težinski saksagliptina ili njegove farmaceutski prihvatljive soli i od 30 do 99.5% težinski polimera za oblaganje, u odnosu na težinu drugog sloja premaza.
3. Obložena tableta kako je definirano u zahtjevu 2 naznačena time da formulacija polimera za oblaganje u drugom sloju premaza je najmanje 2 mg s jezgrom tablete od 200 mg, i saksagliptin ili njegova farmaceutski prihvatljiva sol je najmanje 0.2 mg s tabletom od 200 mg.
4. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da je polimer baziran na PVA u drugom sloju premaza isti kao polimer baziran na PVA u drugim slojevima premaza.
5. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da se polimer baziran na PVA sastoji od polivinil alkohola.
6. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da je u drugom sloju premaza saksagliptin ili njegova farmaceutski prihvatljiva sol prisutan u količini koja je u rasponu od 0.2 do 140 mg i polimer za oblaganje je prisutan u količini koja je u rasponu od 2 do 140 mg, i u svakom od unutrašnjem brtvećem sloju premaza i vanjskom zaštitnom sloju premaza, polimer za oblaganje je prisutan u količini koja je u rasponu od 1 do 100 mg.
7. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da se jezgra tablete sastoji od jednog ili više punila, proizvoljno jednog ili više vezivnih sredstava, proizvoljno jednog ili više sredstava za razgradnju i proizvoljno jednog ili više lubrikanata za tabletiranje.
8. Obložena tableta kako je definirano u zahtjevu 7 naznačena time da se jezgra tablete sastoji od mikrokristalinične celuloze, laktoza monohidrata, kroskarmeloza natrija, te magnezijevog stearata.
9. Obložena tableta kako je definirano u zahtjevu 1; naznačena time da svaki sloj premaza sadrži sredstvo za plastificiranje.
10. Obložena tableta kako je definirano u zahtjevu 9, naznačena time da sredstvo za plastificiranje je poli(etilen glikol).
11. Obložena tableta kako je definirano u zahtjevu 1, naznačena time da se početna tableta koristi umjesto jezgre tablete.
12. Obložena tableta kako je definirano u zahtjevu 11, naznačena time da početna tableta je tableta drugog lijeka.
13. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da ima slijedeći sastav:
14. Obložena tableta kako je definirano u zahtjevu 1 naznačena time da se za 5 mg potencije drugi sloj premaza sastoji od 5 mg saksagliptina ili njegove farmaceutski prihvatljive soli i 5 mg premaza na bazi polimera i za 2.5 mg potencije drugi sloj premaza se sastoji od 2.5 mg saksagliptina ili njegove farmaceutski prihvatljive soli i 20 mg premaza na bazi polimera.
15. Postupak za pripremanje obložene tablete kako je definirano u zahtjevu 1 naznačen time da sadrži: a) osiguravanje jezgre tablete; b) prevlačenje tablete s formulacijom unutrašnjeg brtvenog sloja premaza koja sadrži najmanje jedan polimer za prevlačenje koji je baziran na PVA; c) sušenje obložene tablete da se na njoj stvori unutrašnji brtveni premaz; d) oblaganje tako obložene tablete sa formulacijom drugog sloja premaza koja sadrži medikament koji je saksagliptin ili njegova farmaceutski prihvatljiva sol i najmanje jedan polimer za prevlačenje baziran na PVA; e) sušenje tako obložene tablete da se na njoj stvori drugi sloj premaza; i f) oblaganje tako obložene tablete sa formulacijom trećeg vanjskog zaštitnog sloja premaza koja sadrži najmanje jedan polimer za prevlačenje baziran na PVA; i g) sušenje tako obložene tablete da se oblikuje obložena tablete prema izumu.
16. Postupak kako je definirano u zahtjevu 15 naznačen time da se slojevi premaza primjenjuju kao suspenzija od najmanje jednog polimera za prevlačenje koji je baziran na PVA.
HRP20160880TT 2004-05-28 2016-07-15 Formulacija obložene tablete i postupak HRP20160880T4 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US57531904P 2004-05-28 2004-05-28
EP05756474.2A EP1753406B2 (en) 2004-05-28 2005-05-26 Coated tablet formulation and method
PCT/US2005/018692 WO2005117841A1 (en) 2004-05-28 2005-05-26 Coated tablet formulation and method

Publications (2)

Publication Number Publication Date
HRP20160880T1 HRP20160880T1 (hr) 2016-09-23
HRP20160880T4 true HRP20160880T4 (hr) 2020-01-10

Family

ID=34971747

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20160880TT HRP20160880T4 (hr) 2004-05-28 2016-07-15 Formulacija obložene tablete i postupak
HRP20161210TT HRP20161210T4 (hr) 2004-05-28 2016-09-21 Formulacija obložene tablete i postupak

Family Applications After (1)

Application Number Title Priority Date Filing Date
HRP20161210TT HRP20161210T4 (hr) 2004-05-28 2016-09-21 Formulacija obložene tablete i postupak

Country Status (33)

Country Link
US (4) US7951400B2 (hr)
EP (3) EP1753406B2 (hr)
JP (1) JP4901727B2 (hr)
KR (2) KR101290925B1 (hr)
CN (2) CN102895208B (hr)
AR (2) AR049062A1 (hr)
AU (1) AU2005249467B2 (hr)
BR (1) BRPI0510419B8 (hr)
CA (1) CA2568391C (hr)
CY (2) CY1117813T1 (hr)
DK (2) DK2298288T4 (hr)
ES (3) ES2754573T3 (hr)
GE (1) GEP20094639B (hr)
HK (2) HK1094951A1 (hr)
HR (2) HRP20160880T4 (hr)
HU (2) HUE029446T2 (hr)
IL (2) IL179454A (hr)
LT (1) LT2298288T (hr)
ME (2) ME02516B (hr)
MX (1) MXPA06013711A (hr)
MY (1) MY147639A (hr)
NO (1) NO343907B1 (hr)
NZ (1) NZ551591A (hr)
PE (1) PE20060425A1 (hr)
PL (2) PL1753406T5 (hr)
PT (2) PT1753406E (hr)
RS (2) RS55174B2 (hr)
RU (1) RU2372894C2 (hr)
SI (3) SI2298288T2 (hr)
TW (2) TWI415635B (hr)
UA (1) UA88168C2 (hr)
WO (1) WO2005117841A1 (hr)
ZA (1) ZA200609541B (hr)

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