HRP20221208T1 - Depot sustav koji sadrži glatiramer acetat - Google Patents

Depot sustav koji sadrži glatiramer acetat Download PDF

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Publication number
HRP20221208T1
HRP20221208T1 HRP20221208TT HRP20221208T HRP20221208T1 HR P20221208 T1 HRP20221208 T1 HR P20221208T1 HR P20221208T T HRP20221208T T HR P20221208TT HR P20221208 T HRP20221208 T HR P20221208T HR P20221208 T1 HRP20221208 T1 HR P20221208T1
Authority
HR
Croatia
Prior art keywords
glatiramer acetate
pharmaceutical preparation
water
pharmaceutically acceptable
microparticles
Prior art date
Application number
HRP20221208TT
Other languages
English (en)
Inventor
Ehud Marom
Shai Rubnov
Original Assignee
Mapi Pharma Limited
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.)
Filing date
Publication date
Application filed by Mapi Pharma Limited filed Critical Mapi Pharma Limited
Publication of HRP20221208T1 publication Critical patent/HRP20221208T1/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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10Peptides having 12 to 20 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • 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
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • 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
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K9/1682Processes
    • 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
    • A61K9/5031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • 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
    • A61K9/5089Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/02Peptides of undefined number of amino acids; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis

Claims (14)

1. Postupak proizvodnje parenteralne farmaceutskog pripravka s produljenim djelovanjem koji sadrži glatiramer acetat i farmaceutski prihvatljiv biorazgradivi nosač odabran između skupine koja sadrži poli(D,L-laktid) (PLA) i poli(D,L-laktid-ko-glikolid) (PLGA); taj postupak sadrži korake: (i) raspršivanja koncentriranog otapala glatiramer acetata u nekom otapalu farmaceutski prihvatljivog biorazgradivog nosača u isparljivom organskom otapalu koji se može uroniti u vodu, čime se dobija emulzija vode u ulju, (ii) raspršivanje navedene emulzije vode u ulju u kontinuiranoj vanjskoj vodenastoj fazi koja sadrži surfaktant da bi se stvorile kapljice dvostruke emulzije vode u ulju u vodi, (iii) isparavanje navedenog organskog otapala, čime se dobivaju mikročestice u krutom obliku, (iv) prikupljanje navedenih mikročestica filtriranjem ili centrifugiranjem.
2. Postupak sukladno patentnom zahtjevu 1, nadalje sadrži korak (v) pranja navedenih prikupljenih mikročestica s pročišćenom vodom.
3. Postupak sukladno patentnom zahtjevu 1 ili 2, nadalje sadrži korak (vi) liofilizacije navedenih prikupljenih mikročestica.
4. Postupak sukladno patentnom zahtjevu 3, nadalje sadrži korak (vii) rekonstituiranja navedenih liofiliziranih mikročestica.
5. Postupak sukladno patentnom zahtjevu 1 do 4, pri čemu je taj farmaceutski prihvatljiv biorazgradivi nosač PLGA.
6. Postupak sukladno patentnom zahtjevu 1 do 5, pri čemu je surfaktant odabran između skupine koja sadrži polivinil alkohol (PVA), polisorbat, kopolimere bloka polietilen oksida polipropilen oksida i celuloznog estera.
7. Postupak sukladno patentnom zahtjevu 1 do 6, pri čemu je liofilizacija navedenih mikročetica uz prisutnost krioprotektanta, poželjno manitola.
8. Parenteralni farmaceutski pripravak s dugim djelovanjem koje sadrži glatiramer acetat i farmaceutski prihvatljiv biorazgradivi nosač je odabran između skupine koja sadrži poli(D,L-laktid) (PLA) i poli(D,L-laktid-ko-glikolid) (PLGA) koji se može dobiti postupkom sukladno bilo kojem od patentnih zahtjeva 1 do 7.
9. Farmaceutski pripravak sukladno patentnom zahtjevu 8, pri čemu je farmaceutski prihvatljiv biorazgradiv nosač PLGA.
10. Farmaceutski pripravak sukladno patentnom zahtjevu 8 ili 9, pri čemu glatiramer acetat sadrži L-alanin, L-glutarnu kiselinu, L-lizin, i L-tirozin u molarnim odnosima od 0,14 glutarne kiseline, 0,43 alanina, 0,10 tirozina i 0,33 lizina.
11. Farmaceutski pripravak sukladno patentnim zahtjevima 8 do 10, koja je pohranjen u obliku podobnom za implantaciju na medicinski prihvatljivom mjestu kod subjekta kojem je potrebna i/ili koja je pogodna za raspored doziranja odjednom svaka 2 tjedna do jednom mjesečno.
12. Farmaceutski pripravak sukladno patentnom zahtjevu 8 do 11 radi liječenja multiple skleroze.
13. Farmaceutski pripravak za uporabu u liječenju multiple skleroze sukaldno patentnom zahtjevu 12, pri čemu taj pripravak osigurava jednaku ili superironu terapijsku učinkovitost za komercijalno dostupne dnevne injektibilne oblike doze glatiramer acetata, sa smanjenom učestalošću i/ili ozbiljnošću neželjenih učinaka na lokalnoj i/ili sistemskoj razini; i pri čemu taj pripravak nadalje osigurava produljeno otpuštanje ili produljen učinak glatiramera kod subjekta u usporedbi s pretežito sličnom dozom formulacije s neposrednim otpuštanjem glatiramer acetata.
14. Farmaceutski pripravak za uporabu u liječenje multiple skleroze sukladno patentnom zahtjevu 12 ili 13, pri čemu se taj glatiramer acetat daje u kombinaciji s najmanje jednim drugim aktivnim sastojkom.
HRP20221208TT 2010-01-04 2010-08-19 Depot sustav koji sadrži glatiramer acetat HRP20221208T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29192810P 2010-01-04 2010-01-04
EP18205308.2A EP3536333B1 (en) 2010-01-04 2010-08-19 Depot system comprising glatiramer acetate

Publications (1)

Publication Number Publication Date
HRP20221208T1 true HRP20221208T1 (hr) 2022-12-09

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HRP20221208TT HRP20221208T1 (hr) 2010-01-04 2010-08-19 Depot sustav koji sadrži glatiramer acetat
HRP20182076TT HRP20182076T1 (hr) 2010-01-04 2018-12-10 Sustav s kontroliranim otpuštanjem koji obuhvaća glatiramer acetat

Family Applications After (1)

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HRP20182076TT HRP20182076T1 (hr) 2010-01-04 2018-12-10 Sustav s kontroliranim otpuštanjem koji obuhvaća glatiramer acetat

Country Status (20)

Country Link
US (1) US8796226B2 (hr)
EP (2) EP2398488B1 (hr)
JP (2) JP5916622B2 (hr)
CN (3) CN107661490B (hr)
AU (1) AU2010337822B2 (hr)
BR (1) BR112012016459B1 (hr)
CA (1) CA2784394C (hr)
CY (1) CY1120975T1 (hr)
DK (2) DK3536333T3 (hr)
ES (2) ES2699692T3 (hr)
HK (2) HK1245667A1 (hr)
HR (2) HRP20221208T1 (hr)
HU (2) HUE040390T2 (hr)
LT (2) LT2398488T (hr)
MX (2) MX2020003805A (hr)
PL (2) PL2398488T3 (hr)
PT (2) PT2398488T (hr)
SI (1) SI2398488T1 (hr)
TR (1) TR201818858T4 (hr)
WO (1) WO2011080733A1 (hr)

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Publication number Publication date
LT3536333T (lt) 2022-11-10
HUE040390T2 (hu) 2019-03-28
AU2010337822B2 (en) 2016-03-17
PL2398488T3 (pl) 2019-03-29
EP2398488A1 (en) 2011-12-28
CA2784394A1 (en) 2011-07-07
CA2784394C (en) 2016-12-13
JP2013516403A (ja) 2013-05-13
CN107184954A (zh) 2017-09-22
PT3536333T (pt) 2022-11-11
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