RU2009148985A - Стабилизированные аморфные формы иматиниба мезилата - Google Patents

Стабилизированные аморфные формы иматиниба мезилата Download PDF

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RU2009148985A
RU2009148985A RU2009148985/15A RU2009148985A RU2009148985A RU 2009148985 A RU2009148985 A RU 2009148985A RU 2009148985/15 A RU2009148985/15 A RU 2009148985/15A RU 2009148985 A RU2009148985 A RU 2009148985A RU 2009148985 A RU2009148985 A RU 2009148985A
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pharmaceutical composition
capsule
composition according
imatinib mesylate
mass
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RU2489149C2 (ru
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Элизабете ГОНКАЛВЕШ (CH)
Элизабете ГОНКАЛВЕШ
Оскар КАЛЬБ (CH)
Оскар Кальб
Михаэль МУТЦ (DE)
Михаэль Мутц
Вольфганг ВИРТ (CH)
Вольфганг ВИРТ
Джей Партибан ЛАКШМАН (US)
Джей Партибан Лакшман
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Новартис АГ (CH)
Новартис Аг
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    • 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
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
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    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof
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    • 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
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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    • A61P35/00Antineoplastic agents
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    • A61K9/00Medicinal preparations characterised by special physical form
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    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material
    • A61K9/4825Proteins, e.g. gelatin

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Abstract

1. Фармацевтическая композиция, содержащая активный агент, стабилизирующий аморфную форму иматиниба мезилата, и аморфный и иматиниба мезилат, необязательно, вместе с, по меньшей мере, одним фармацевтически приемлемым носителем, в которой активный агент выбран из твердых дисперсий, циклодекстриновых комплексов и продуктов совместного измельчения с выбранными эксципиентами. ! 2. Фармацевтическая композиция по п.1, в которой активный агент представляет собой твердую дисперсию. ! 3. Фармацевтическая композиция по п.1, в которой активный агент представляет собой циклодекстриновый комплекс. ! 4. Фармацевтическая композиция по одному из пп.1-3, представляющая собой капсулу. ! 5. Фармацевтическая композиция по п.4, представляющая собой капсулу, содержащую количество стабилизированного аморфного иматиниба мезилата, соответствующее 50 и 200 мг иматиниба мезилата. ! 6. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой оболочка содержит желатин. ! 7. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой оболочка содержит диоксид титана. ! 8. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой оболочка содержит красный оксид железа. ! 9. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой соотношение массы содержимого капсулы и массы оболочки капсулы составляет между около 100:25 и 100:50. ! 10. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой соотношение массы содержимого капсулы и массы оболочки капсулы составляет между около 100:30 и 100:40. ! 11. Фармацевтическая композиция по одному из пп.1-3, представляющая собой табле�

Claims (12)

1. Фармацевтическая композиция, содержащая активный агент, стабилизирующий аморфную форму иматиниба мезилата, и аморфный и иматиниба мезилат, необязательно, вместе с, по меньшей мере, одним фармацевтически приемлемым носителем, в которой активный агент выбран из твердых дисперсий, циклодекстриновых комплексов и продуктов совместного измельчения с выбранными эксципиентами.
2. Фармацевтическая композиция по п.1, в которой активный агент представляет собой твердую дисперсию.
3. Фармацевтическая композиция по п.1, в которой активный агент представляет собой циклодекстриновый комплекс.
4. Фармацевтическая композиция по одному из пп.1-3, представляющая собой капсулу.
5. Фармацевтическая композиция по п.4, представляющая собой капсулу, содержащую количество стабилизированного аморфного иматиниба мезилата, соответствующее 50 и 200 мг иматиниба мезилата.
6. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой оболочка содержит желатин.
7. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой оболочка содержит диоксид титана.
8. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой оболочка содержит красный оксид железа.
9. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой соотношение массы содержимого капсулы и массы оболочки капсулы составляет между около 100:25 и 100:50.
10. Фармацевтическая композиция по п.5, представляющая собой капсулу, в которой соотношение массы содержимого капсулы и массы оболочки капсулы составляет между около 100:30 и 100:40.
11. Фармацевтическая композиция по одному из пп.1-3, представляющая собой таблетку.
12. Фармацевтическая композиция по п.11, представляющая собой таблетку, содержащую количество стабилизированного аморфного иматиниба мезилата, соответствующее 100, 400 или 800 мг иматиниба мезилата.
RU2009148985/15A 2007-06-07 2008-06-05 Стабилизированные аморфные формы иматиниба мезилата RU2489149C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP07109816.4 2007-06-07
EP07109816A EP2000139A1 (en) 2007-06-07 2007-06-07 Stabilized amorphous forms of imatinib mesylate
US97419707P 2007-09-21 2007-09-21
US60/974,197 2007-09-21
PCT/US2008/065838 WO2008154262A1 (en) 2007-06-07 2008-06-05 Stabilized amorphous forms of imatinib mesylate

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RU2009148985A true RU2009148985A (ru) 2011-08-20
RU2489149C2 RU2489149C2 (ru) 2013-08-10

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US (4) US20100178336A1 (ru)
EP (2) EP2000139A1 (ru)
JP (2) JP5380440B2 (ru)
KR (2) KR101454086B1 (ru)
CN (2) CN101678023A (ru)
AR (1) AR067328A1 (ru)
AU (1) AU2008262059B2 (ru)
BR (1) BRPI0812442A2 (ru)
CA (1) CA2687741A1 (ru)
CL (1) CL2008001658A1 (ru)
CO (1) CO6241118A2 (ru)
CY (1) CY1113178T1 (ru)
DK (1) DK2305263T3 (ru)
ES (1) ES2391625T3 (ru)
HK (1) HK1150764A1 (ru)
IL (2) IL202157A0 (ru)
MX (1) MX2009013272A (ru)
MY (1) MY148878A (ru)
NZ (3) NZ598428A (ru)
PL (1) PL2305263T3 (ru)
PT (1) PT2305263E (ru)
RU (1) RU2489149C2 (ru)
SG (1) SG182175A1 (ru)
SI (1) SI2305263T1 (ru)
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WO (1) WO2008154262A1 (ru)
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