HRP20161549T1 - Injektabilni farmaceutski pripravci koji sadrže antipsihotik koji je netopljiv u vodi, sorbitan laurat i polisorbat 20 - Google Patents

Injektabilni farmaceutski pripravci koji sadrže antipsihotik koji je netopljiv u vodi, sorbitan laurat i polisorbat 20 Download PDF

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Publication number
HRP20161549T1
HRP20161549T1 HRP20161549TT HRP20161549T HRP20161549T1 HR P20161549 T1 HRP20161549 T1 HR P20161549T1 HR P20161549T T HRP20161549T T HR P20161549TT HR P20161549 T HRP20161549 T HR P20161549T HR P20161549 T1 HRP20161549 T1 HR P20161549T1
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preparation
weight
polysorbate
composition according
approximately
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HRP20161549TT
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Magali B. Hickey
Jason M. Perry
Daniel R. Deaver
Julius F. Remenar
Jennifer Vandiver
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Alkermes Pharma Ireland Limited
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Application filed by Alkermes Pharma Ireland Limited filed Critical Alkermes Pharma Ireland Limited
Publication of HRP20161549T1 publication Critical patent/HRP20161549T1/hr

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    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further 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
    • 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • 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
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (23)

1. Farmaceutski pripravak koji sadrži: (a) spoj A-7 [image] (b) sorbitan laurat; (c) polisorbat 20; i (d) vodeni nosač; pri čemu pripravak formira vodenu, flokuliranu, injektabilnu suspenziju.
2. Pripravak prema zahtjevu 1, pri čemu pripravak sadrži komponente (b) i (c) u odnosu koji rezultira flokulama koje sadrže komponentu (a), pri čemu se flokule talože do visine koja je veća od unaprijed određene visine sedimenta, tako da se komponente (a), (b) i (c) mogu resuspendirati radi injektiranja.
3. Pripravak prema zahtjevu 2, pri čemu visina sedimenta ima najmanje povećanje visine sedimenta od 20 do 80% u usporedbi sa neflokuliranom kompozicijom poslije 24 sata neometanog mirovanja.
4. Pripravak prema zahtjevu 2, pri čemu se komponente (a), (b) i (c) mogu resuspendirati radi injektiranja protresanjem rukom između 1-60 sekundi.
5. Pripravak prema bilo kojem od prethodnih zahtjeva, pri čemu je odnos komponenata (b) do (c) takav da se pripravak može injektirati uz korištenje igle veličine od 20 do 25 G.
6. Pripravak prema zahtjevu 2, pri čemu (a), (b), i (c) formiraju flokule koje imaju slijedeće veličine: Dv[10]: 2-10 μm, Dv[50]: 10-30 μm, i Dv[90]: manje od 65 μmM.
7. Pripravak prema bilo kojem od prethodnih zahtjeva, pri čemu je odnos komponenata (b) prema (c) približno od 5 do 2, težinski.
8. Pripravak prema bilo kojem od prethodnih zahtjeva, koji sadrži oko 0.2 - 1 težinskih postotaka sorbitan laurata.
9. Pripravak prema zahtjevu 1, koji sadrži oko 0,05 - 0,8 težinskih postotaka polisorbata 20.
10. Pripravak prema zahtjevu 1, koji sadrži oko 0,1 - 0,3 težinskih postotaka polisorbata 20.
11. Pripravak prema bilo kojem od prethodnih zahtjeva, koji sadrži približno 15 - 35 težinskih postotaka spoja A-7.
12. Pripravak prema bilo kom od prethodnih zahtjeva, koji sadrži približno 20 - 30 težinskih postotaka spoja A-7.
13. Injektabilni farmaceutski pripravak koji sadrži: (a) spoj A-7: [image] pri čemu je komponenta (a) u težinskom odnosu približno od 15 - 35%; (b) sorbitan laurat u težinskom odnosu približno od 0,2 - 1% (c) polisorbat 20 u težinskom odnosu približno od 0,05 - 0,8%; i (d) vodeni nosač.
14. Injektabilni pripravak koja sadrži: (a) spoj A-7: [image] (b) sorbitan laurat; (c) polisorbat 20; i (d) vodeni nosač.
15. Pripravak prema zahtjevu 14, pri čemu je pripravak formuliran za modulaciju reakcije tkiva povezane sa davanjem antipsihotika netopljivog u vodi.
16. Pripravak prema zahtjevu 15, pri čemu je modulacija reakcije tkiva smanjenje iritacije na mestu injekcije.
17. Pripravak prema bilo kjeom od zahtjeva 1 do 16 za primjenu u metodi liječenja poremećaja središnjeg živčanog sustava.
18. Pripravak za primjenu prema zahtjevu 17, pri čemu je poremećaj psihotično stanje.
19. Pripravak za primjenu prema zahtjevu 18, pri čemu je psihotično stanje shiizofrenija ili shiizofreniformne bolesti.
20. Farmaceutski pripravak koja sadrži: (a) 24 - 30 težinskih postotaka spoja A-7: [image] (b) 0,2 - 1 težinskih postotaka sorbitan laurata; (c) 0,1 - 0,3 težinskih postotaka polisorbata 20; i (d) vodeni nosač.
21. Pripravak prema bilo kojem od zahtjeva 1, 13, 14 ili 20, pri čemu je vodeni nosač pufer.
22. Pripravak prema zahtjevu 21, pri čemu je pufer fosfatni, citratni, tartratni ili acetatni pufer.
23. Pripravak prema zahtjevu 21 ili 22, pri čemu je vodeni nosač fosfatna puferirana slana otopina.
HRP20161549TT 2011-03-18 2016-11-22 Injektabilni farmaceutski pripravci koji sadrže antipsihotik koji je netopljiv u vodi, sorbitan laurat i polisorbat 20 HRP20161549T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161454008P 2011-03-18 2011-03-18
PCT/US2012/029625 WO2012129156A1 (en) 2011-03-18 2012-03-19 Pharmaceutical compositions comprising sorbitan esters
EP12712189.5A EP2685979B1 (en) 2011-03-18 2012-03-19 Injectable pharmaceutical compositions comprising a water-insoluble anti-psychotic, sorbitan laurate and polysorbate 20

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HRP20161549T1 true HRP20161549T1 (hr) 2016-12-30

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HRP20240285TT HRP20240285T1 (hr) 2011-03-18 2012-03-19 Farmaceutski pripravci koji sadrže sorbitan estere
HRP20161549TT HRP20161549T1 (hr) 2011-03-18 2016-11-22 Injektabilni farmaceutski pripravci koji sadrže antipsihotik koji je netopljiv u vodi, sorbitan laurat i polisorbat 20

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US (7) US9034867B2 (hr)
EP (3) EP2685979B1 (hr)
JP (3) JP6138703B2 (hr)
CN (3) CN107252414B (hr)
AU (4) AU2012231160B2 (hr)
BR (1) BR112013023847B1 (hr)
CA (1) CA2830511C (hr)
CY (1) CY1118252T1 (hr)
DK (2) DK2685979T3 (hr)
ES (2) ES2972387T3 (hr)
FI (1) FI3156056T3 (hr)
HR (2) HRP20240285T1 (hr)
HU (2) HUE032109T2 (hr)
IL (4) IL296695B1 (hr)
LT (2) LT2685979T (hr)
MX (1) MX358344B (hr)
PL (2) PL2685979T3 (hr)
PT (2) PT2685979T (hr)
RS (2) RS65237B1 (hr)
RU (2) RU2627469C2 (hr)
SI (2) SI2685979T1 (hr)
SM (1) SMT201600423B (hr)
WO (1) WO2012129156A1 (hr)

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