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HRP20230566T1 - Liposomalna formulacija za podmazivanje zglobova - Google Patents

Liposomalna formulacija za podmazivanje zglobova Download PDF

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Publication number
HRP20230566T1
HRP20230566T1 HRP20230566TT HRP20230566T HRP20230566T1 HR P20230566 T1 HRP20230566 T1 HR P20230566T1 HR P20230566T T HRP20230566T T HR P20230566TT HR P20230566 T HRP20230566 T HR P20230566T HR P20230566 T1 HRP20230566 T1 HR P20230566T1
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Croatia
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range
joint
dmpc
composition according
membrane
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HRP20230566TT
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Yechezkel Barenholz
Yaniv DOLEV
Keren TURJEMAN
Gadi Sarfati
Maty Ayal-Hershkovitz
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Moebius Medical Ltd.
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Publication of HRP20230566T1 publication Critical patent/HRP20230566T1/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
    • A61K9/10Dispersions; Emulsions
    • A61K9/127Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K9/0012Galenical 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
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L27/00Materials for grafts or prostheses or for coating grafts or prostheses
    • A61L27/50Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L27/00Materials for grafts or prostheses or for coating grafts or prostheses
    • A61L27/50Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
    • A61L27/54Biologically active materials, e.g. therapeutic substances
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/20Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials
    • A61L2300/22Lipids, fatty acids, e.g. prostaglandins, oils, fats, waxes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2400/00Materials characterised by their function or physical properties
    • A61L2400/06Flowable or injectable implant compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2400/00Materials characterised by their function or physical properties
    • A61L2400/10Materials for lubricating medical devices
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2430/00Materials or treatment for tissue regeneration
    • A61L2430/06Materials or treatment for tissue regeneration for cartilage reconstruction, e.g. meniscus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2430/00Materials or treatment for tissue regeneration
    • A61L2430/24Materials or treatment for tissue regeneration for joint reconstruction

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (15)

1. Farmaceutski sastav koji sadrži: neionsko sredstvo za toničnost koje sadrži poliol manitol; i liposome koji sadrže najmanje jednu membranu koja sadrži najmanje jedan fosfolipid (PL) odabran među glicerofosfolipidima (GPL), pri čemu navedeni GPL ima dva ugljikovodična lanca C12-C18, koji su isti ili različiti, i sfingomijelin (SM) koji ima ugljikovodični lanac C12-C18 pri čemu najmanje jedna membrana ima temperaturu faznog prijelaza unutar raspona od 20 °C do 39 °C; pri čemu je farmaceutski sastav u osnovi bez dodatnog farmaceutski aktivnog sredstva.
2. Sastav prema patentnom zahtjevu 1: i.) koji sadrži tekući medij u kojem su suspendirani liposomi, pri čemu je navedeni tekući medij odabran između pufera i vode po izboru, pri čemu je navedeni pufer odabran između histidinskog pufera i fosfatno puferirane fiziološke otopine po izboru; ii.) pri čemu je manitol prisutan u farmaceutskom sastavu u masenom postotku unutar raspona od 0,1 % (m/m) do 7 % (m/m); iii.) koji ima osmolalnost unutar raspona od 200 do 600 mOsm, koji po izboru ima osmolalnost od 300 mOsm, i/ili; iv.) koji ima pH-vrijednost unutar raspona od 5 – 8
3. Sastav prema patentnom zahtjevu 1, pri čemu je maseni omjer liposoma i manitola unutar raspona od 6 : 1 do 2 : 1.
4. Sastav prema bilo kojem od patentnih zahtjeva 1 do 3, pri čemu: i.) su navedeni liposomi multilamelarne vezikule (MLV); ii.) navedeni GPL sadrži dva acilna lanca C14, C15, C16ili C18, i/ili; iii.) najmanje jedan od navedenih ugljikovodičnih lanaca je zasićeni ugljikovodični lanac, pri čemu su po izboru dva ugljikovodična lanca zasićena.
5. Sastav prema bilo kojem od patentnih zahtjeva 1 do 4, pri čemu je navedeni PL fosfatidilkolin (PC).
6. Sastav prema patentnom zahtjevu 5, pri čemu najmanje jedna navedena membrana sadrži 1,2-dimiristoil-sn-glicero-3-fosfokolin (DMPC).
7. Sastav prema patentnom zahtjevu 6, pri čemu najmanje jedna navedena membrana sadrži PC odabran iz skupine koja se sastoji od 1,2-dipalmitoil-sn-glicero-3-fosfokolina (DPPC), 1,2-dipentadekanoil-sn-glicero- 3-fosfokolina (C15), 1,2-distearoil-sn-glicero-3-fosfokolina (DSPC) i SM koji ima ugljikovodični lanac C16 (D-eritro C16).
8. Sastav prema patentnom zahtjevu 7, pri čemu: i.) je molski udio DMPC-a u najmanje jednoj membrani unutar raspona od 10 % do 75 %; ii.) da najmanje jedna navedena membrana sadrži DMPC i DPPC, pri čemu je molski postotni omjer DMPC-a i DPPC-a unutar raspona od 25 : 75 do 70 : 30 po izboru, pri čemu je molski postotni omjer DMPC-a i DPPC-a 45 : 55, po izboru; iii.) najmanje jedna navedena membrana sadrži DMPC i C15, pri čemu je molski postotni omjer DMPC-a i C15 unutar raspona od 25 : 75 do 45 : 55, po izboru; iv.) najmanje jedna navedena membrana sadrži DMPC i DSPC, pri čemu je molski postotni omjer DMPC-a i DSPC-a 75 : 25, po izboru; i/ili v.) najmanje jedna navedena membrana sadrži DMPC i D-eritro C16, pri čemu je molski postotni omjer DMPC-a i D-eritro C16 unutar raspona od 10 : 90 do 25 : 75, po izboru.
9. Sastav prema patentnom zahtjevu 5, pri čemu najmanje jedna navedena membrana sadrži C15.
10. Sastav prema bilo kojem od patentnih zahtjeva 1 do 9, pri čemu: i.) je ukupna koncentracija PL-a unutar raspona od 50 do 300 mM; ii.) su fosfolipidi prisutni u farmaceutskom sastavu u masenom postotku unutar raspona od 0,5 % (m/m) do 30 % (m/m) ukupne mase farmaceutskog sastava; iii.) liposomi imaju srednji promjer između 0,5 µm i 10 µm; iv.) najmanje jedna membrana ima temperaturu faznog prijelaza od 30 °C do 35 °C; v.) je temperatura zgloba unutar raspona od 1 °C do 15 °C iznad navedene temperature faznog prijelaza; i/ili vi.) u osnovi ne sadrži hijaluronsku kiselinu.
11. Sastav prema patentnom zahtjevu 1, pri čemu sadrži liposome MLV čije se membrane sastoje od DMPC-a i DPPC-a; manitol; i histidinski pufer, pri čemu je DMPC prisutan u farmaceutskom sastavu u masenom postotku unutar raspona od 1 % (m/m) do 10 % (m/m), DPPC je prisutan u masenom postotku unutar raspona od 2 % (m/m) do 12 % (m/m), a manitol je prisutan u masenom postotku unutar raspona od 1 % (m/m) do 7 % (m/m), od ukupne mase farmaceutskog sastava.
12. Sastav prema bilo kojem od patentnih zahtjeva 1 do 11, pri čemu: i.) jedna dozna jedinica farmaceutskog sastava sadrži od 20 mg do 350 mg manitola i od 50 mg do 1000 mg fosfolipida: ii.) je u obliku parenteralnog farmaceutskog sastava koji sadrži suspenziju liposoma; i/ili iii.) je sastav u obliku primjerenom za primjenu koji je odabran iz skupine koja se sastoji od intraartikularne injekcije, artroskopske primjene i kirurške primjene.
13. Sastav prema bilo kojem od patentnih zahtjeva 1 do 12, za upotrebu u liječenju, upravljanju ili prevenciji poremećaja zgloba ili stanja ili simptoma koji proizlaze iz poremećaja zgloba, ili za sprječavanje trošenja zgloba, pri čemu je navedeni poremećaj zgloba ili stanje odabrano iz skupine koja se sastoji od artritisa, osteoartritisa, osteoartritisa u bolesnika s reumatoidnim artritisom, traumatske ozljede zgloba, ukočenog zgloba, sportske ozljede, traumatske ozljede u pogledu osteoartritisa (OA), zgloba nakon artrocenteze, artroskopske kirurgije, otvorene operacije zgloba, zamjene zgloba i psorijatičnog artritisa, po izboru.
14. Sastav prema bilo kojem od patentnih zahtjeva 1 do 13, za upotrebu za smanjenje boli u zglobu koljena u bolesnika s osteoartritisom.
15. Farmaceutski sastav koji sadrži: neionsko sredstvo za toničnost koje sadrži poliol manitol; i liposome koji sadrže najmanje jednu membranu koja sadrži najmanje jedan fosfolipid (PL) odabran među glicerofosfolipidima (GPL), pri čemu navedeni GPL ima dva ugljikovodična lanca C12-C18, koji su isti ili različiti, i sfingomijelin (SM) koji ima ugljikovodični lanac C12-C18, pri čemu najmanje jedna membrana ima temperaturu faznog prijelaza unutar raspona od 20 °C do 39 °C; farmaceutski sastav u osnovi je bez dodatnog farmaceutski aktivnog sredstva, za upotrebu u liječenju boli ili iritacije u zglobu u osobe koja ima poremećaj zgloba, pri čemu zglob ima temperaturu zgloba koja je iznad temperature faznog prijelaza.
HRP20230566TT 2017-08-22 2018-08-21 Liposomalna formulacija za podmazivanje zglobova HRP20230566T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762548429P 2017-08-22 2017-08-22
EP18847493.6A EP3672653B1 (en) 2017-08-22 2018-08-21 Liposomal formulation for joint lubrication
PCT/IL2018/050923 WO2019038763A1 (en) 2017-08-22 2018-08-21 LIPOSOMAL FORMULATION FOR JOINT LUBRICATION

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HRP20230566T1 true HRP20230566T1 (hr) 2023-08-18

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US (3) US11123293B2 (hr)
EP (2) EP3672653B1 (hr)
JP (2) JP7082336B2 (hr)
KR (2) KR102607729B1 (hr)
CN (2) CN114601799B (hr)
AU (3) AU2018319594B2 (hr)
BR (1) BR112020003767B1 (hr)
CA (2) CA3219776A1 (hr)
DK (1) DK3672653T3 (hr)
EA (1) EA202090476A1 (hr)
ES (1) ES2948715T3 (hr)
FI (1) FI3672653T3 (hr)
HR (1) HRP20230566T1 (hr)
HU (1) HUE062030T2 (hr)
IL (3) IL301801B2 (hr)
LT (1) LT3672653T (hr)
MA (1) MA49959B1 (hr)
MX (2) MX2020002041A (hr)
MY (1) MY197149A (hr)
PH (1) PH12020500331A1 (hr)
PL (1) PL3672653T3 (hr)
PT (1) PT3672653T (hr)
SG (1) SG11202000773QA (hr)
SI (1) SI3672653T1 (hr)
WO (1) WO2019038763A1 (hr)

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