HRP20211853T1 - Sastavi in situ injekcijskih biorazgradivih implantata - Google Patents

Sastavi in situ injekcijskih biorazgradivih implantata Download PDF

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Publication number
HRP20211853T1
HRP20211853T1 HRP20211853TT HRP20211853T HRP20211853T1 HR P20211853 T1 HRP20211853 T1 HR P20211853T1 HR P20211853T T HRP20211853T T HR P20211853TT HR P20211853 T HRP20211853 T HR P20211853T HR P20211853 T1 HRP20211853 T1 HR P20211853T1
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Croatia
Prior art keywords
composition
range
polymer
water
drug
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HRP20211853TT
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English (en)
Inventor
Ibon Guierro Aduriz
María Teresa GÓMEZ OCHOA
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Laboratorios Farmaceuticos Rovi, S.A.
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Application filed by Laboratorios Farmaceuticos Rovi, S.A. filed Critical Laboratorios Farmaceuticos Rovi, S.A.
Publication of HRP20211853T1 publication Critical patent/HRP20211853T1/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
    • A61K9/0002Galenical 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
    • 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)

Claims (13)

1. Injekcijski sterilan depo za intramuskularnu primjenu sadrži: biokompatibilan polimer, koji je polimer ili kopolimer na osnovi mliječne kiseline i/ili mliječne kiseline plus glikolne kiseline s monomernim omjerom mliječne i glikolne kiseline u rasponu od 48 : 52 do 100 : 0 i inherentnom viskoznošću u rasponu od 0,25 – 0,48 dl/g izmjerenom pri 25 °C u kloroformu koncentracije 0,1 %, te se sastoji od krajnjih alkilnih ili alkilno-esterskih skupina; otapalo koje se miješa s vodom, s dipolnim momentom od približno 3,7 – 4,5 D i dielektričnom konstantom između 30 i 50, koja je dimetilsulfoksid (DMSO), i lijek s topljivošću u vodi manjom od 2 mg/ml, odabran iz skupine koja se sastoji od fentanila, risperidona, olanzapina i letrozola, samostalno ili u bilo kojoj međusobnoj kombinaciji; naznačen time što viskoznost polimerne otopine, koja se sastoji od polimera i DMSO-a je u rasponu 0,20 – 7,0 Pa s, pri čemu se navedena viskoznost polimerne otopine mjeri pri 25 °C.
2. Sastav injekcijskog depoa prema zahtjevu 1, sadrži i u vodi topljivo sredstvo za modificiranje pH.
3. Sastav injekcijskog depoa prema zahtjevu 2 u kojem se u vodi topljivo sredstvo za modificiranje pH sastoji od Mg(OH)2 u molarnom omjeru lijeka : Mg(OH)2 između 2 : 3 i 2 : 5.
4. Sastav injekcijskog depoa prema bilo kojem od prethodnih zahtjeva 1 – 3 sterilan je kao gotov proizvod a u njemu je lijek i/ili biokompatibilan polimer steriliziran zračenjem u rasponu od 5 – 25 kGy.
5. Sastav injekcijskog depoa prema bilo kojem od prethodnih zahtjeva 1 – 4, u kojem viskoznost polimerne otopine polimera i DMSO-a u rasponu između 0,7 i 7,0 Pa s.
6. Sastav injekcijskog depoa prema bilo kojem od prethodnih zahtjeva 1 – 5 za uporabu u liječenju kroničnih ljudskih bolesti.
7. Sastav prema zahtjevu 6 kad je kronična bolest shizofrenija ili bipolarni poremećaj.
8. Uporaba sastava prema bilo kojem od prethodnih zahtjeva 1 – 5 u proizvodnji lijeka za liječenje kroničnih ljudskih bolesti.
9. Farmaceutski komplet prikladan za stvaranje in situ biorazgradivog implantata u tijelu, a čiji je sastav prema bilo kojem od zahtjeva 1 – 5, pri čemu se lijek i biokompatibilan polimer nalaze u prvom spremniku, a otapalo koje se miješa s vodom nalazi se u drugom, odvojenom spremniku.
10. Farmaceutski komplet prema zahtjevu 9, u kojem je barem jedan od prvih i drugih spremnika štrcaljka, bočica, uređaj ili uložak, za jednokratnu uporabu ili ne.
11. Farmaceutski komplet prema zahtjevu 10, iz kojega su spremnici spojivi priključnim uređajem.
12. Farmaceutski komplet prema bilo kojem od zahtjeva 9 do 11, u kojem je sadržaj barem jednog prvog i drugog spremnika liofiliziran.
13. Farmaceutski komplet prema bilo kojem od zahtjeva 9 do 12, čiji je sadržaj barem jednog prvog i drugog spremnika sterilizira zračenjem u rasponu od 5 – 25 kGy.
HRP20211853TT 2010-05-31 2010-05-31 Sastavi in situ injekcijskih biorazgradivih implantata HRP20211853T1 (hr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10382153.4A EP2394663B1 (en) 2010-05-31 2010-05-31 Compositions for injectable in-situ biodegradable implants

Publications (1)

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HRP20211853T1 true HRP20211853T1 (hr) 2022-03-04

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HRP20211853TT HRP20211853T1 (hr) 2010-05-31 2010-05-31 Sastavi in situ injekcijskih biorazgradivih implantata
HRP20230890TT HRP20230890T1 (hr) 2010-05-31 2011-05-31 Metode za pripremu injektabilnih depo sastava

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US (2) US10058504B2 (hr)
EP (2) EP2394663B1 (hr)
JP (1) JP5923493B2 (hr)
CN (1) CN102933234A (hr)
BR (1) BR112012030707A2 (hr)
CA (1) CA2800641C (hr)
CY (1) CY1124783T1 (hr)
DK (1) DK2582395T3 (hr)
EA (1) EA024211B1 (hr)
ES (2) ES2897976T3 (hr)
FI (1) FI2582395T3 (hr)
HR (2) HRP20211853T1 (hr)
HU (3) HUE057236T2 (hr)
LT (2) LT2394663T (hr)
MX (1) MX346167B (hr)
PL (2) PL2394663T3 (hr)
PT (2) PT2394663T (hr)
RS (2) RS64451B1 (hr)
SI (2) SI2394663T1 (hr)
WO (1) WO2011151356A2 (hr)
ZA (1) ZA201209394B (hr)

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PT2394663T (pt) 2021-11-26
PL2394663T3 (pl) 2022-02-21
PT2582395T (pt) 2023-08-18
US20130177603A1 (en) 2013-07-11
LT2394663T (lt) 2022-02-10
RS53205B (en) 2014-06-30
JP5923493B2 (ja) 2016-05-24
US10058504B2 (en) 2018-08-28
LT2582395T (lt) 2023-08-10
HUE057236T2 (hu) 2022-04-28
US10195138B2 (en) 2019-02-05
CA2800641A1 (en) 2011-12-08
HUE063623T2 (hu) 2024-01-28
RS64451B1 (sr) 2023-09-29
DK2582395T3 (da) 2023-08-07
CY1124783T1 (el) 2022-11-25
EP2582395B1 (en) 2023-05-10
EP2394663B1 (en) 2021-10-13
CN102933234A (zh) 2013-02-13
PL2582395T3 (pl) 2023-08-21
SI2394663T1 (sl) 2022-02-28
HRP20230890T1 (hr) 2023-11-10
US20180318208A1 (en) 2018-11-08
ES2897976T3 (es) 2022-03-03
WO2011151356A3 (en) 2012-03-22
BR112012030707A2 (pt) 2016-11-01
CA2800641C (en) 2018-05-22
ES2950857T3 (es) 2023-10-16
MX2012013867A (es) 2013-01-24
ZA201209394B (en) 2013-08-28
FI2582395T3 (fi) 2023-08-08
SI2582395T1 (sl) 2023-10-30
MX346167B (es) 2017-03-08
EP2394663A1 (en) 2011-12-14
JP2013527213A (ja) 2013-06-27
EA201201570A1 (ru) 2013-09-30
WO2011151356A2 (en) 2011-12-08
HUE054922T2 (hu) 2021-10-28
EP2582395A2 (en) 2013-04-24
EA024211B1 (ru) 2016-08-31

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