HRP20151357T1 - Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa - Google Patents

Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa Download PDF

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Publication number
HRP20151357T1
HRP20151357T1 HRP20151357TT HRP20151357T HRP20151357T1 HR P20151357 T1 HRP20151357 T1 HR P20151357T1 HR P20151357T T HRP20151357T T HR P20151357TT HR P20151357 T HRP20151357 T HR P20151357T HR P20151357 T1 HRP20151357 T1 HR P20151357T1
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Croatia
Prior art keywords
composition according
formula
particles
pharmaceutical composition
compound
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HRP20151357TT
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English (en)
Inventor
Joanna M. Koziara
Mark M. Menning
Reza Oliyai
Robert G. Strickley
Richard Yu
Brian P. Kearney
Anita A. Mathias
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Gilead Sciences, Inc.
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Application filed by Gilead Sciences, Inc. filed Critical Gilead Sciences, Inc.
Publication of HRP20151357T1 publication Critical patent/HRP20151357T1/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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K9/1611Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (22)

1. Kompozicija se sastoji od mnoštva čestica čvrstog nosača gdje svaka od njih sadrži silicij dioksid i gdje svaka ima površinu i/ili pore; i spoj formule (I): [image] ili njegovu farmaceutski prihvatljivu sol u porama ili na površini čestica čvrstog nosača.
2. Kompozicija prema patentnom zahtjevu 1 gdje čestice silicij dioksida imaju srednju vrijednost presjeka čestica od 10 do 120 mikrona i BET površinu od 40 do 400 m2/g.
3. Kompozicija prema patentnom zahtjevu 2 gdje su čestice silicij dioksida hidrofilna pirogena silika .
4. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 3 gdje postotak težine spoja u formuli (I) iznosi do 50% ± 10% čestica čvrstog nosača.
5. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 4 gdje spoj formule (I) ima obogaćenu koncentraciju od 99 ± 1% stereoizomera formule (Ia): [image]
6. Metoda sadrži kombinirani spoj formule (I): [image] odgovarajućeg rastvarača, i mnoštva čestica čvrstog nosača od kojih svaka sadrži silicij dioksid kako bi se dobila mješavina.
7. Tableta sadrži: 1) spoj formule (I): [image] ili njegovu farmaceutski prihvatljivu sol i 2) mnoštvo čestica čvrstog nosača od kojih svaka sadrži silicij dioksid.
8. Tableta prema patentnom zahtjevu 7 gdje mnoštvo čestica čvrstog nosača sadrži mnoštvo silika čestica od kojih svaka ima površinu i pore, i koje imaju srednju vrijednost presjeka čestica 10 do 120 μm i BET površinu od 40 do 400 m2/g.
9. Tableta prema patentnim zahtjevima 7 ili 8 koja dalje sadrži drugi terapeutski agens.
10. Tableta prema patentnom zahtjevu 7 koja dalje sadrži 3) mikrokristalnu celulozu; 4) hidroksipropil celulozu; 5) natrij kroskarmelozu; i 6) magnezij stearat.
11. Tableta prema bilo kojem od patentnih zahtjeva od 7 do 10 gdje spoj formule (I) ima obogaćenu koncentraciju od 99 ± 1% stereoizomera formule (Ia): [image]
12. Farmaceutska kompozicija sadrži kvaternarnu kombinaciju spoja formule (Ia)/tenofovir disoproksil fumarat/emtricitabin/elvitegravir, i mnoštvo čestica čvrstog nosača od kojih svaka sadrži silicij dioksid, gdje je spoj formule (Ia): [image]
13. Farmaceutska kompozicija prema patentnom zahtjevu 12 gdje čestice silicij dioksida imaju srednju vrijednost presjeka čestica od 10 do 120 μm i BET površinu od 40 to 400 m2/g.
14. Farmaceutska kompozicija prema patentnom zahtjevu 13 gdje su čestice silicij dioksida hidrofilna pirogena silika.
15. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 14 gdje čestice silicij dioksida imaju srednju vrijednost presjeka zrna od 20 do 40 μm.
16. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 15 gdje čestice silicij dioksida imaju BET površinu od najmanje 150 m2/g.
17. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 16 gdje je spoj formule (Ia) obloženo u porama i na površini čestica silicij dioksida.
18. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 17 gdje odnos težine spoja formule (Ia) do težine čestica silicij dioksida iznosi 1 ± 0.05%.
19. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 13 do 18 koja je formulirana kao tableta.
20. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 5, tableta prema bilo kojem od patentnih zahtjeva od 7 do 11, ili farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 19 za upotrebu pri medicinskoj terapiji.
21. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 5, tableta prema bilo kojem od patentnih zahtjeva od 7 do 11, ili farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 19 za upotrebu u liječenju virusnih infekcija.
22. Kompozicija za upotrebu kako je naznačeno u patentnom zahtjevu 21, ili tableta za upotrebu kako je naznačeno u patentnom zahtjevu 21, ili farmaceutska kompozicija za upotrebu kako je naznačeno u patentnom zahtjevu 21, gdje je virusna infekcija HIV.
HRP20151357TT 2008-05-02 2015-12-09 Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa HRP20151357T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US4993508P 2008-05-02 2008-05-02
US15065209P 2009-02-06 2009-02-06
US15065509P 2009-02-06 2009-02-06
PCT/US2009/042607 WO2009135179A2 (en) 2008-05-02 2009-05-01 The use of solid carrier particles to improve the processability of a pharmaceutical agent
EP09739981.0A EP2296633B1 (en) 2008-05-02 2009-05-01 The use of solid carrier particles to improve the processability of a pharmaceutical agent

Publications (1)

Publication Number Publication Date
HRP20151357T1 true HRP20151357T1 (hr) 2016-01-29

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ID=40809930

Family Applications (1)

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HRP20151357TT HRP20151357T1 (hr) 2008-05-02 2015-12-09 Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa

Country Status (27)

Country Link
US (1) US10039718B2 (hr)
EP (2) EP3006032A1 (hr)
JP (2) JP5722213B2 (hr)
KR (2) KR101784647B1 (hr)
CN (3) CN102123700A (hr)
AP (1) AP3089A (hr)
AU (3) AU2009242451C1 (hr)
BR (1) BRPI0911871A8 (hr)
CA (1) CA2720856C (hr)
CO (1) CO6321225A2 (hr)
CY (1) CY1117067T1 (hr)
DK (1) DK2296633T3 (hr)
EA (2) EA201591353A1 (hr)
EC (1) ECSP10010636A (hr)
ES (1) ES2553897T3 (hr)
HK (2) HK1153670A1 (hr)
HR (1) HRP20151357T1 (hr)
HU (1) HUE026380T2 (hr)
IL (2) IL208614A (hr)
MX (2) MX2010011963A (hr)
NZ (1) NZ588978A (hr)
PL (1) PL2296633T3 (hr)
PT (1) PT2296633E (hr)
SG (2) SG190618A1 (hr)
SI (1) SI2296633T1 (hr)
WO (1) WO2009135179A2 (hr)
ZA (1) ZA201008007B (hr)

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