HRP20191559T1 - Farmaceutski pripravci za liječenje infekcije bakterijom helicobacter pylori - Google Patents

Farmaceutski pripravci za liječenje infekcije bakterijom helicobacter pylori Download PDF

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Publication number
HRP20191559T1
HRP20191559T1 HRP20191559T HRP20191559T1 HR P20191559 T1 HRP20191559 T1 HR P20191559T1 HR P20191559 T HRP20191559 T HR P20191559T HR P20191559 T1 HRP20191559 T1 HR P20191559T1
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capsule according
dose
preparation
release
amoxicillin
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Gilead Raday
Guy Goldberg
Patrick Gosselin
Reza Fathi
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Redhill Biopharma Ltd
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Application filed by Redhill Biopharma Ltd filed Critical Redhill Biopharma Ltd
Publication of HRP20191559T1 publication Critical patent/HRP20191559T1/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
    • A61K9/48Preparations 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
    • A61K9/4808Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
    • 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
    • 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
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • 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
    • 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4747Quinolines; Isoquinolines spiro-condensed
    • 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
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4891Coated capsules; Multilayered drug free capsule shells
    • 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
    • A61K9/5026Organic 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
    • A61K9/48Preparations 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)

Claims (23)

1. Kapsula koja sadrži: (1) pripravak prve doze s trenutnim otpuštanjem u obliku komprimiranih minitableta, pripravak prve doze s trenutnim otpuštanjem koji se sastoji od najmanje dva antibiotika te (2) pripravak druge doze s odgođenim otpuštanjem u obliku komprimiranih minitableta, pripravak druge doze s odgođenim otpuštanjem koji se sastoji od inhibitora protonske pumpe i obloge, naznačen time što je, kada se testira u uređaju s košaricom, obloga pripravka druge doze s odgođenim otpuštanjem osmišljena tako da ispunjava kriterije profila otapanja u dvofaznom testu u uređaju s košaricom: (a) otpuštanje najviše 10 % prema težini inhibitora protonske pumpe tijekom 120 minuta u kiseloj fazi s 900 ml 0,1 N HCl pri 100 o/min te (b) otpuštanje najmanje 75 % prema težini inhibitora protonske pumpe tijekom 45 minuta u 900 ml fosfatnog pufera pH vrijednosti 6,8 pri 100 o/min nakon primjene kiseline.
2. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što obloga u pripravku druge doze odgađa otpuštanje inhibitora protonske pumpe sa 120 na najmanje 240 minuta nakon peroralne primjene.
3. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što pripravak prve doze sadrži amoksicilin i ansamicin ili farmaceutski prihvatljive soli ili njihove solvate.
4. Kapsula u skladu s patentnim zahtjevom 3, naznačena time što ansamicin sadrži rifampicin, rifabutin, farmaceutski prihvatljive soli ili njihove solvate ili kombinacije navedenog.
5. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što u pripravku druge doze inhibitor protonske pumpe sadrži omeprazol, pantoprazol, lansoprazol, ilaprazol, dekslansoprazol, esomeprazol ili rabeprazol, farmaceutski prihvatljive soli ili njihove solvate ili kombinacije navedenog.
6. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što pripravak druge doze sadrži tvar koja odgađa otpuštanje.
7. Kapsula u skladu s patentnim zahtjevom 6, naznačena time što se tvar koja odgađa otpuštanje sastoji od natrijeva alginata, gliceril monostearata, gliceril distearata, akrilnih kiselina, celuloza ili kombinacija navedenog.
8. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što se najmanje 70 % prema težini barem dvaju antibiotika otpušta između 5 i 120 minuta nakon peroralne primjene te se najmanje 70 % prema težini protonskog inhibitora otpušta između 120 i 240 minuta nakon peroralne primjene.
9. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što se sastoji od rifabutina, amoksicilina i omeprazola.
10. Kapsula u skladu s patentnim zahtjevom 9, naznačena time što omjer amoksicilina i rifabutina iznosi između 10 do 40 prema težini.
11. Kapsula u skladu s patentnim zahtjevom 9, naznačena time što omjer amoksicilina i omeprazola iznosi između 20 do 40 prema težini.
12. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što se pripravak prve i druge doze dodatno sastoje od punila, sredstva za raspadanje, veziva, površinski aktivne tvari, alkalizirajućeg sredstva, maziva ili kombinacija navedenog.
13. Kapsula u skladu s patentnim zahtjevom 12, naznačena time što se punilo sastoji od laktoze, celuloze, škroba, kalcijevih fosfata, kalcijeva karbonata, šećera ili kombinacija navedenog.
14. Kapsula u skladu s patentnim zahtjevom 12 ili patentnim zahtjevom 13, naznačena time što se sredstvo za raspadanje sastoji od kroskarmeloza-natrija, karboksimetil-celuloze, natrijeva škrob glikolata, krospovidona ili kombinacija navedenog.
15. Kapsula u skladu s bilo kojim patentnim zahtjevom od 12 do 14, naznačena time što se vezivo sastoji od škroba, celuloze, polivinilpirolidona, ksantan gume, alginske kiseline, agara ili kombinacija navedenog.
16. Kapsula u skladu s bilo kojim patentnim zahtjevom od 12 do 15, naznačena time što se površinski aktivna tvar sastoji od natrijeva lauril-sulfata, polioksietilen polioksipropilen glikola, polietilen glikola, polipropilen glikola, polivinil kaprolaktama--polivinil acetata--polietilen glikola, makrogolglicerol hidroksistearata ili kombinacija navedenog.
17. Kapsula u skladu s bilo kojim patentnim zahtjevom od 12 do 16, naznačena time što se alkalizirajuće sredstvo sastoji od meglumina, kalcijeva karbonata, natrijeva sulfata, natrijeva bikarbonata ili kombinacija navedenog.
18. Kapsula u skladu s bilo kojim patentnim zahtjevom od 12 do 17, naznačena time što se mazivo sastoji od magnezijeva stearata, silicijeva dioksida, talka, stearinske kiseline, natrijeva stearil fumarata, gliceril behenata ili kombinacija navedenog.
19. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što se pripravak prve doze sastoji od 250 mg amoksicilina i 12,5 mg rifabutina ili farmaceutski prihvatljivih soli ili njihovih solvata i što se pripravak druge doze sastoji od 10 mg omeprazola ili farmaceutski prihvatljivih soli ili njihovih solvata.
20. Kapsula u skladu s patentnim zahtjevom 1, naznačena time što se pripravak druge doze sastoji od vanjskog zaštitnog sloja, enterične obloge i unutrašnjeg zaštitnog sloja.
21. Kapsula u skladu s patentnim zahtjevom 1 za primjenu u liječenju infekcije bakterijom H. pylori u domaćinu, naznačena time što se kapsula primjenjuje na domaćinu tri puta dnevno.
22. Kapsula u skladu s patentnim zahtjevom 21, naznačena time što se svakodnevno primjenjuje 3000 mg amoksicilina, 120 mg omeprazola i 150 mg rifabutina.
23. Kapsula u skladu s patentnim zahtjevom 21, naznačena time što se svakodnevno primjenjuje do 4500 mg amoksicilina i do 300 mg rifabutina.
HRP20191559 2013-02-13 2019-08-29 Farmaceutski pripravci za liječenje infekcije bakterijom helicobacter pylori HRP20191559T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361764401P 2013-02-13 2013-02-13
US201361764385P 2013-02-13 2013-02-13
EP14751025.9A EP2956149B1 (en) 2013-02-13 2014-02-12 Pharmaceutical compositions for the treatment of helicobacter pylori
PCT/US2014/016071 WO2014127025A1 (en) 2013-02-13 2014-02-12 Pharmaceutical compositions for the treatment of helicobacter pylori

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HRP20191559T1 true HRP20191559T1 (hr) 2019-11-29

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US (7) US9050263B2 (hr)
EP (1) EP2956149B1 (hr)
JP (1) JP6494529B2 (hr)
KR (1) KR102062357B1 (hr)
CN (2) CN105163743A (hr)
AU (1) AU2014216373B2 (hr)
BR (1) BR112015019264B1 (hr)
CA (1) CA2900763C (hr)
CL (1) CL2015002253A1 (hr)
CY (1) CY1122113T1 (hr)
DK (1) DK2956149T3 (hr)
ES (1) ES2744406T3 (hr)
HK (1) HK1217645A1 (hr)
HR (1) HRP20191559T1 (hr)
HU (1) HUE052411T2 (hr)
IL (1) IL240387B (hr)
MX (1) MX368536B (hr)
NZ (1) NZ711754A (hr)
PH (1) PH12015501783B1 (hr)
PL (1) PL2956149T3 (hr)
PT (1) PT2956149T (hr)
RU (1) RU2671400C2 (hr)
SG (1) SG11201506318QA (hr)
SI (1) SI2956149T1 (hr)
UA (1) UA120249C2 (hr)
WO (1) WO2014127025A1 (hr)

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