HRP20131088T1 - Äśvrsti farmaceutski pripravci s fiksnom dozom koji sadrže irbesartan i amlodipin, njihova priprava i terapijska primjena - Google Patents

Äśvrsti farmaceutski pripravci s fiksnom dozom koji sadrže irbesartan i amlodipin, njihova priprava i terapijska primjena Download PDF

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Publication number
HRP20131088T1
HRP20131088T1 HRP20131088AT HRP20131088T HRP20131088T1 HR P20131088 T1 HRP20131088 T1 HR P20131088T1 HR P20131088A T HRP20131088A T HR P20131088AT HR P20131088 T HRP20131088 T HR P20131088T HR P20131088 T1 HRP20131088 T1 HR P20131088T1
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Croatia
Prior art keywords
irbesartan
amlodipine
preparation
preparation according
tablet
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HRP20131088AT
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English (en)
Inventor
Praveen Khullar
Vinay Kolhe
Amol Kulkarni
Shirishbay Patel
Yashwant Phadke
D. Saravanan
Mansing Shingte
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Sanofi
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Application filed by Sanofi filed Critical Sanofi
Publication of HRP20131088T1 publication Critical patent/HRP20131088T1/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
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • 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
    • A61K9/2095Tabletting 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/282Organic compounds, e.g. fats
    • 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
    • A61K9/5084Mixtures 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (15)

1. Stabilni čvrsti oralni farmaceutski pripravak s fiksnom dozom u obliku jednoslojne tablete koja sadrži irbesartan, amlodipin-besilat i farmaceutski prihvatljive pomoćne tvari, naznačen time što je irbesartan fizički odvojen od amlodipin-besilata i što je irbesartan u obliku obloženih granula uklopljen u ekstragranularni matriks koji sadrži amlodipin-besilat.
2. Pripravak u skladu s patentnim zahtjevom 1, naznačen time što je tableta obložena filmom.
3. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 2, naznačen time što irbesartan čini između 20% i 70%, težinski, od ukupnog pripravka.
4. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što amlodipin-besilat čini između 1% i 20%, težinski, od ukupnog pripravka.
5. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen timen što farmaceutski prihvatljive pomoćne tvari se bira iz skupine koju čine razrjeđivač, sredstvo za raspadanje, sredstvo protiv prijanjanja, vezivo, mazivo i njihova smjesa.
6. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što navedeni čvrsti pripravak ne sadrži laktozu.
7. Čvrsti pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time se što količina irbesartana kreće između 150 mg i 300 mg od ukupne težine tablete, po mogućnosti 300 mg ili 150 mg.
8. Čvrsti pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što se količina amlodipin-besilata kreće između 5mg i 10 mg od ukupne težine tablete, po mogućnosti 7 mg ili 14 mg.
9. Čvrsti pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 8 u obliku tablete, naznačen time što je ukupna težina tablete između 400 mg i 600 mg, po mogućnosti 500 mg.
10. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što sadrži manje od 1,50% (tež./tež.) od ukupnih nečistoća za amlodipin i manje od 0,50% (tež./tež.) od ukupnih nečistoća za irbesartan nakon 6 mjeseci na 40 °C/75% relativne vlažnosti.
11. Postupak priprave stabilnog oralnog farmaceutskog pripravka u obliku jednoslojne tablete koja sadrži irbesartan i amlodipin-besilat, naznačen time što se postupak sastoji u koracima: i) granuliranja irbesartana i jedne ili više farmaceutski prihvatljivih pomoćnih tvari, s vodenom otopinom koja sadrži vezivo, kako bi se dobilo granule; ii) sušenja granula; iii) odvojenog miješanja amlodipin-besilata s farmaceutski prihvatljivim pomoćnim tvarima; iv) miješanje granula koje sadrže irbesartan iz koraka ii) sa smjesom koja sadrži amlodipin-besilat iz koraka iii); v) dodavanja maziva u smjesu iz koraka iv); izborno nakon koraka prije dodavanja maziva; i vi) komprimiranja smjese u tablete.
12. Postupak u skladu s patentnim zahtjevom 11, naznačen time što skupina farmaceutski prihvatljivih pomoćnih tvari upotrijebljenih u koraku i) i iii) postupka ne sadrži laktozu.
13. Postupak u skladu s bilo kojim od patentnih zahtjeva 11 do 12, naznačen time što se korak prije dodavanja maziva sastoji u miješanju smjese iz koraka iv) u trajanju od 10 do 25 minuta, po mogućnosti 20 minuta prije provođenja koraka dodavanja maziva.
14. Upotreba irbesartana i amlodipin-besilata u proizvodnji medikamenta za liječenje hipertenzije, naznačena time što je navedeni medikament u stabilnom čvrstom pripravku s fiksnom dozom u skladu s bilo kojim od patentnih zahtjeva 1 do 10.
15. Upotreba u skladu s patentnim zahtjevom 14, naznačena time što predstavlja liječenje pacijenata s hipertenzijom koja nije pod dovoljnom kontrolom amlodipinom kao monoterapijom blokatorom kalcijskih kanala (CCB) ili irbesartanom kao antagonistom receptora angiotenzina II (ARB).
HRP20131088AT 2009-06-30 2013-11-14 Äśvrsti farmaceutski pripravci s fiksnom dozom koji sadrže irbesartan i amlodipin, njihova priprava i terapijska primjena HRP20131088T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1341DE2009 2009-06-30
PCT/IB2009/007027 WO2011001202A1 (en) 2009-06-30 2009-09-17 Solid pharmaceutical fixed dose compositions comprising irbesartan and amlodipine, their preparation and their therapeutic application

Publications (1)

Publication Number Publication Date
HRP20131088T1 true HRP20131088T1 (hr) 2013-12-20

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US (1) US9173848B2 (hr)
EP (1) EP2448561B1 (hr)
JP (1) JP5763063B2 (hr)
KR (1) KR101667081B1 (hr)
CN (2) CN106176745A (hr)
AR (1) AR077284A1 (hr)
AU (1) AU2009349125B2 (hr)
BR (1) BRPI0925315B8 (hr)
CA (1) CA2766884C (hr)
CL (1) CL2011003371A1 (hr)
CO (1) CO6480972A2 (hr)
CR (1) CR20110704A (hr)
CY (1) CY1114933T1 (hr)
DK (1) DK2448561T3 (hr)
DO (1) DOP2011000406A (hr)
EA (1) EA021317B1 (hr)
EC (1) ECSP11011559A (hr)
ES (1) ES2435240T3 (hr)
GT (1) GT201100337A (hr)
HK (1) HK1169309A1 (hr)
HR (1) HRP20131088T1 (hr)
IL (1) IL217229A (hr)
MA (1) MA33463B1 (hr)
MX (1) MX2011014005A (hr)
MY (1) MY152951A (hr)
NI (1) NI201100227A (hr)
NZ (1) NZ597317A (hr)
PE (1) PE20121131A1 (hr)
PL (1) PL2448561T3 (hr)
PT (1) PT2448561E (hr)
RS (1) RS53087B (hr)
SG (1) SG177426A1 (hr)
SI (1) SI2448561T1 (hr)
SM (1) SMT201400011B (hr)
TN (1) TN2011000651A1 (hr)
TW (1) TWI476191B (hr)
UA (1) UA103688C2 (hr)
UY (1) UY32749A (hr)
WO (1) WO2011001202A1 (hr)
ZA (1) ZA201109541B (hr)

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TWI402083B (zh) * 2006-12-26 2013-07-21 Daiichi Sankyo Co Ltd 固形製劑及其安定化方法

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WO2011001202A1 (en) 2011-01-06
CO6480972A2 (es) 2012-07-16
ZA201109541B (en) 2013-03-27
EA201270087A1 (ru) 2012-07-30
UA103688C2 (uk) 2013-11-11
MA33463B1 (fr) 2012-07-03
GT201100337A (es) 2014-05-20
CL2011003371A1 (es) 2012-07-27
AU2009349125B2 (en) 2016-05-19
NZ597317A (en) 2014-05-30
US9173848B2 (en) 2015-11-03
NI201100227A (es) 2012-03-28
CA2766884A1 (en) 2011-01-06
AU2009349125A1 (en) 2012-01-19
TWI476191B (zh) 2015-03-11
CN102573804A (zh) 2012-07-11
AR077284A1 (es) 2011-08-17
CA2766884C (en) 2016-08-23
CY1114933T1 (el) 2016-12-14
DK2448561T3 (da) 2013-11-25
EP2448561B1 (en) 2013-08-14
KR20120102579A (ko) 2012-09-18
PT2448561E (pt) 2013-11-21
CR20110704A (es) 2012-06-15
JP2012532118A (ja) 2012-12-13
ES2435240T3 (es) 2013-12-17
KR101667081B1 (ko) 2016-10-17
UY32749A (es) 2011-01-31
SMT201400011B (it) 2014-03-07
DOP2011000406A (es) 2012-04-15
US20120171288A1 (en) 2012-07-05
MX2011014005A (es) 2012-04-30
TN2011000651A1 (en) 2013-05-24
SI2448561T1 (sl) 2013-12-31
JP5763063B2 (ja) 2015-08-12
TW201111368A (en) 2011-04-01
RS53087B (en) 2014-06-30
SG177426A1 (en) 2012-02-28
IL217229A (en) 2016-10-31
BRPI0925315B8 (pt) 2021-05-25
PE20121131A1 (es) 2012-09-04
BRPI0925315B1 (pt) 2019-10-08
MY152951A (en) 2014-12-15
PL2448561T3 (pl) 2014-01-31
EP2448561A1 (en) 2012-05-09
ECSP11011559A (es) 2012-01-31
IL217229A0 (en) 2012-07-31
EA021317B1 (ru) 2015-05-29
HK1169309A1 (en) 2013-01-25
CN106176745A (zh) 2016-12-07

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