HRP20240525T1 - Pripravak na bazi lipida za oralnu primjenu antagonista bradikininskog b2-receptora - Google Patents

Pripravak na bazi lipida za oralnu primjenu antagonista bradikininskog b2-receptora Download PDF

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Publication number
HRP20240525T1
HRP20240525T1 HRP20240525TT HRP20240525T HRP20240525T1 HR P20240525 T1 HRP20240525 T1 HR P20240525T1 HR P20240525T T HRP20240525T T HR P20240525TT HR P20240525 T HRP20240525 T HR P20240525T HR P20240525 T1 HRP20240525 T1 HR P20240525T1
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Croatia
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weight
propylene glycol
liquid pharmaceutical
pharmaceutical preparation
liquid
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HRP20240525TT
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English (en)
Inventor
Christoph Gibson
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Pharvaris Gmbh
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Publication of HRP20240525T1 publication Critical patent/HRP20240525T1/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
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • 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
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • A61K9/4816Wall or shell material
    • A61K9/4825Proteins, e.g. gelatin
    • 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
    • A61P7/10Antioedematous agents; Diuretics
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (15)

1. Tekući farmaceutski pripravak za oralnu primjenu koji sadrži antagonist bradikininskog (BK) B2 receptora koji ima kemijsku strukturu u skladu s Formulom 1, ili njegov stereoizomer, sol ili solvat: [image] pri čemu je R deuterij ili vodik; pri čemu je antagonist BK B2 receptora otopljen u tekućem nosaču koji sadrži propilen glikol monokaprilat, polioksil ricinusovo ulje i propilen glikol.
2. Tekući farmaceutski pripravak prema zahtjevu 1, naznačen time što je antagonist BK B2 receptora spoj u skladu s Formulom 1, ili njegova sol ili solvat, pri čemu je R deuterij.
3. Tekući farmaceutski pripravak prema zahtjevu 1 ili 2, naznačen time što je količina propilen glikol monokaprilata u tekućem nosaču 40-60 tež.%, temeljeno na težini tekućeg nosača.
4. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što količina polioksilnog ricinusovog ulja u tekućem nosaču iznosi 30-50 tež.%, temeljeno na težini tekućeg nosača.
5. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je količina propilen glikola 2,5-15 tež.%, temeljeno na težini tekućeg nosača.
6. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je propilen glikol monokaprilat propilen glikol monokaprilat tipa II (USP/NF).
7. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je polioksil ricinusovo ulje polioksil 40 hidrogenirano ricinusovo ulje (USP/NF).
8. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je sadržaj propilen glikol monokaprilata 50 tež.%, sadržaj polioksilnog ricinusovog ulja je 40 tež.%, a sadržaj propilen glikola je 10 tež.% , na temelju kombinirane težine propilen glikol monokaprilata, polioksil ricinusovog ulja i propilen glikola u tekućem nosaču.
9. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što ima sadržaj antagonista BK B2 receptora u rasponu od 5 mg do 100 mg po g, kao što je od 5 mg do 65 mg po g, ili kao što je od 20 mg do 70 mg po g tekućeg farmaceutskog pripravka.
10. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što uglavnom sadrži: (a) temeljeno na ukupnoj težini tekućeg farmaceutskog pripravka, 0,5 do 6,5 tež.%, kao što je 5 tež.%, spoja u skladu s Formulom 1, ili njegovog stereoizomera, soli ili solvata, pri čemu je R deuterij; (b) temeljeno na ukupnoj težini tekućeg farmaceutskog pripravka, 93,5 do 99,5 tež.% tekućeg nosača, pri čemu navedeni tekući nosač uglavnom sadrži: (i) 50 dijelova (težinski) propilen glikol monokaprilata, kao što je propilen glikol monokaprilat tipa II (USP/NF); (ii) 40 dijelova (težinski) polioksilnog ricinusovog ulja, kao što je 40 udjela hidrogeniranog ricinusovog ulja (USP/NF); (iii) 5 do 10 dijelova (težinski) propilen glikola; i izborno (iv) do 5 dijelova (težinski) vode; i izborno (c) ostatak je jedna ili više dodatnih pomoćnih tvari otopljenih ili raspršenih u tekućem nosaču.
11. Kapsula za oralnu primjenu, naznačena time što sadrži tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva.
12. Kapsula prema zahtjevu 11, naznačena time što je kapsula meka kapsula.
13. Meka kapsula prema zahtjevu 12, naznačena time što sadrži stijenku kapsule koja sadrži želatinu, vodu i najmanje jedan plastifikator odabran između propilen glikola, glicerola, sorbitola, sorbitana, smjesa plastifikatora na bazi sorbitola, ili bilo koje njihove kombinacije.
14. Tekući farmaceutski pripravak prema bilo kojem od zahtjeva 1 do 10, ili kapsula prema bilo kojem od zahtjeva 11 do 13, za upotrebu u akutnom ili kroničnom liječenju subjekta koji pati od bolesti ili stanja koje reagira na modulaciju BK B2 receptora.
15. Tekući farmaceutski pripravak za upotrebu prema zahtjevu 14, ili kapsula za upotrebu prema zahtjevu 14, naznačena time što je bolest ili stanje koje reagira na modulaciju BK B2 receptora edem, kao što je nasljedni angioedem.
HRP20240525TT 2021-08-05 2022-08-05 Pripravak na bazi lipida za oralnu primjenu antagonista bradikininskog b2-receptora HRP20240525T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP21189990 2021-08-05
PCT/EP2022/072049 WO2023012322A1 (en) 2021-08-05 2022-08-05 Lipid-based composition for oral administration of bradykinin b2-receptor antagonists
EP22760986.4A EP4203919B1 (en) 2021-08-05 2022-08-05 Lipid-based composition for oral administration of bradykinin b2-receptor antagonists

Publications (1)

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HRP20240525T1 true HRP20240525T1 (hr) 2024-07-05

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US (1) US20240350418A1 (hr)
EP (1) EP4203919B1 (hr)
JP (1) JP2024528195A (hr)
KR (1) KR20240039185A (hr)
CN (1) CN118076342A (hr)
AU (1) AU2022323749A1 (hr)
BR (1) BR112024002215A2 (hr)
CA (1) CA3227476A1 (hr)
CO (1) CO2024001171A2 (hr)
DK (1) DK4203919T3 (hr)
ES (1) ES2978563T3 (hr)
FI (1) FI4203919T3 (hr)
HR (1) HRP20240525T1 (hr)
HU (1) HUE066306T2 (hr)
IL (1) IL310321A (hr)
LT (1) LT4203919T (hr)
MX (1) MX2024001711A (hr)
PL (1) PL4203919T3 (hr)
PT (1) PT4203919T (hr)
RS (1) RS65427B1 (hr)
SI (1) SI4203919T1 (hr)
TW (1) TW202320774A (hr)
WO (1) WO2023012322A1 (hr)

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CN117224522B (zh) * 2023-11-15 2024-02-23 北京协和药厂有限公司 药物组合物及其制备方法、药物制剂

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ES2218554T3 (es) 1994-10-27 2004-11-16 Fujisawa Pharmaceutical Co., Ltd. Piridopirimidonas, quinolinas y n-heterociclos condensados que son antagonistas de bradiquinina.
FR2737892B1 (fr) 1995-08-17 1997-10-24 Fournier Ind & Sante Nouveaux composes de benzenesulfonamide, procede de preparation et utilisation en therapeutique
GB9602029D0 (en) 1996-02-01 1996-04-03 Fujisawa Pharmaceutical Co New heterocyclic compounds
DE19609827A1 (de) 1996-03-13 1997-09-18 Hoechst Ag Aminoalkyl- und Acylaminoalkylether, Verfahren zu deren Herstellung und ihre Verwendung als Bradykinin-Rezeptorantagonisten
DE19610784A1 (de) 1996-03-19 1997-09-25 Hoechst Ag Fluoralkyl- und Fluoralkoxysubstituierte heterocyclische Bradykinin-Antagonisten, Verfahren zu ihrer Herstellung und ihre Verwendung
AUPN952696A0 (en) 1996-04-29 1996-05-23 Fujisawa Pharmaceutical Co., Ltd. New heterocyclic compounds
DE19712960A1 (de) 1997-03-27 1998-10-01 Hoechst Ag Benzyloxy-substituierte, anellierte N-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Bradykininrezeptorantagonisten
CA2319730A1 (en) 1998-06-08 1999-12-16 Advanced Medicine, Inc. Bradykinin antagonists
CA2364178C (en) 2000-12-05 2006-01-10 Yasuhiro Katsu N-benzenesulfonyl l-proline compounds as bradykinin antagonists
TW200824686A (en) * 2006-10-31 2008-06-16 Wyeth Corp Formulations of phospholipase enzyme inhibitors
TWI407960B (zh) 2007-03-23 2013-09-11 Jerini Ag 小分子緩激肽b2受體調節劑
AR073304A1 (es) 2008-09-22 2010-10-28 Jerini Ag Moduladores del receptor de bradiquinina b2 de molecula pequena
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FI4203919T3 (fi) 2024-05-03
CA3227476A1 (en) 2023-02-09
CN118076342A (zh) 2024-05-24
MX2024001711A (es) 2024-03-05
KR20240039185A (ko) 2024-03-26
EP4203919B1 (en) 2024-01-31
LT4203919T (lt) 2024-05-10
EP4203919A1 (en) 2023-07-05
IL310321A (en) 2024-03-01
TW202320774A (zh) 2023-06-01
PL4203919T3 (pl) 2024-06-10
WO2023012322A1 (en) 2023-02-09
CO2024001171A2 (es) 2024-05-20
RS65427B1 (sr) 2024-05-31
BR112024002215A2 (pt) 2024-04-30
ES2978563T3 (es) 2024-09-16
SI4203919T1 (sl) 2024-08-30
PT4203919T (pt) 2024-04-23
AU2022323749A1 (en) 2024-02-08
US20240350418A1 (en) 2024-10-24
HUE066306T2 (hu) 2024-07-28
DK4203919T3 (da) 2024-04-29
JP2024528195A (ja) 2024-07-26

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