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HRP20151321T1 - Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih - Google Patents

Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih Download PDF

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Publication number
HRP20151321T1
HRP20151321T1 HRP20151321TT HRP20151321T HRP20151321T1 HR P20151321 T1 HRP20151321 T1 HR P20151321T1 HR P20151321T T HRP20151321T T HR P20151321TT HR P20151321 T HRP20151321 T HR P20151321T HR P20151321 T1 HRP20151321 T1 HR P20151321T1
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HR
Croatia
Prior art keywords
pharmaceutical form
epalrestat
modified
diabetic
release pharmaceutical
Prior art date
Application number
HRP20151321TT
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English (en)
Inventor
Isabel Kalofonos
Judy Caron
William Martin-Doyle
Original Assignee
Bionevia Pharmaceuticals Inc.
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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Application filed by Bionevia Pharmaceuticals Inc. filed Critical Bionevia Pharmaceuticals Inc.
Publication of HRP20151321T1 publication Critical patent/HRP20151321T1/hr

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    • 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • 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
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • 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
    • 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
    • A61K9/20Pills, 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (15)

1. Farmaceutski oblik s prilagođenim otpuštanjem, koji sadrži: epalrestat ili njegov farmaceutski prikladan derivat; polimer koji bubri u vodi i pH je neovisan; anionski polimer koji nije na bazi celuloze i koji bubri u vodi; i sredstvo na bazi saharida koje prilagođava brzinu otpuštanja.
2. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, koji, (i) kada se daje bolesniku u redovnom režimu doziranja, daje relativno ravan profil koncentracije epalrestata u plazmi u stanju ravnoteže, pri čemu nema bitnih pikova ili valova u relativno ravnom profilu koncentracije u plazmi i minimalna koncentracija epalrestata u plazmi u relativno ravnom profilu koncentracije u plazmi jest dovoljna da omogući terapijski učinak u bolesnika; ili (ii) kada se daje bolesniku u redovnom režimu doziranja, daje relativno ravan profil koncentracije epalrestata u plazmi u stanju ravnoteže tako da je srednji omjer Cmin/Cmax epalrestata tijekom intervala doziranja oko 0,55 do oko 1,0 i Cmin jest dovoljan da omogući terapijski učinak; ili (iii) jest oblik za doziranje jednom ili dva puta dnevno, daje bolesniku terapijski učinak kroz oko 12 do oko 24 sata i relativno ravan profil koncentracije epalrestata u plazmi u stanju ravnoteže tako da minimalna koncentracija epalrestata u plazmi tijekom intervala doziranja iznosi oko 55% maksimalne koncentracije u plazmi tijekom intervala doziranja.
3. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje se polimer koji bubri u vodi i pH je neovisan izabire iz grupe koja obuhvaća hipromelozu, hidroksipropil etil celuloze, hidroksipropil celulozu, hidroksietil celulozu, metil celulozu i njihove kombinacije.
4. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje se anionski polimer koji nije na bazi celuloze i koji bubri u vodi izabire iz grupe koja obuhvaća anionske derivate agara; anionske derivate guar gume; anionske derivate karuba gume; anionske derivate ksantan gume; anionske derivate alginina; anionske derivate polisaharida manoze i galaktoze, ili kitosana; anionske derivate modificiranog škroba i njihove kombinacije.
5. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje je sredstvo na bazi saharida koje prilagođava brzinu otpuštanja poliolski spoj.
6. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 5, gdje se poliolski spoj izabire između arabitola, ksilitola, ribitola, manitola, sorbitola, dulcitola, fucitola, iditola, izomalta, maltitola i laktitiola.
7. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, koji je u matriksnoj formi, kao što je oralna tableta.
8. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje je težinski omjer polimera koji bubri u vodi i pH je neovisan prema anionskom polimeru koji nije na bazi celuloze i koji bubri u vodi od oko 2,5 : 1 do oko 1,5 : 1.
9. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje je epalrestat ili njegov farmaceutski prikladan derivat u količini od oko 30% do oko 45% težine.
10. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje epalrestat ili njegov farmaceutski prikladan derivat jest kolin hidrogen diepalrestat ili betain hidrogen diepalrestat.
11. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, za uporabu u postupku koji obuhvaća primjenu bolesniku jednom ili dva puta dnevno.
12. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, za uporabu u postupku liječenja dijabetesa ili dijabetičke komplikacije kod subjekta kojem je to potrebno.
13. Farmaceutski oblik s prilagođenim otpuštanjem za uporabu prema zahtjevu 12, koja obuhvaća primjenu bolesniku jednom ili dva puta dnevno.
14. Farmaceutski oblik s prilagođenim otpuštanjem za uporabu prema zahtjevu 12, gdje se dijabetička komplikacija izabire iz grupe koju čine dijabetička neuropatija, dijabetička nefropatija, dijabetička kardiomiopatija, dijabetička retinopatija, dijabetička gastropareza, katarakte, čirevi stopala, dijabetička makroangiopatija, dijabetička mikroangiopatija, visoka razina glukoze u krvi, visoke razine HbA1c i njihove kombinacije.
15. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, za uporabu u postupku inhibicije aldoza reduktaze kod subjekta kojem je to potrebno; ili za uporabu kardiozaštite kod subjekta kojem je to potrebno.
HRP20151321TT 2011-01-20 2015-12-03 Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih HRP20151321T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161434637P 2011-01-20 2011-01-20
EP12736674.8A EP2665477B1 (en) 2011-01-20 2012-01-20 Modified release compositions of epalrestat or a derivative thereof and methods for using the same
PCT/US2012/022094 WO2012100208A1 (en) 2011-01-20 2012-01-20 Modified release compositions of epalrestat or a derivative thereof and methods for using the same

Publications (1)

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HRP20151321T1 true HRP20151321T1 (hr) 2016-01-29

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HRP20151321TT HRP20151321T1 (hr) 2011-01-20 2015-12-03 Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih

Country Status (15)

Country Link
US (2) US9566269B2 (hr)
EP (2) EP3042654A1 (hr)
CY (1) CY1117483T1 (hr)
DK (1) DK2665477T3 (hr)
ES (1) ES2555927T3 (hr)
HK (1) HK1191569A1 (hr)
HR (1) HRP20151321T1 (hr)
HU (1) HUE026715T2 (hr)
PL (1) PL2665477T3 (hr)
PT (1) PT2665477E (hr)
RS (1) RS54447B1 (hr)
RU (2) RU2017124629A (hr)
SI (1) SI2665477T1 (hr)
SM (1) SMT201500307B (hr)
WO (1) WO2012100208A1 (hr)

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EP2665477A1 (en) 2013-11-27
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