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RU2019140298A - Комбинация, ее применение и способы лечения с использованием указанной комбинации - Google Patents

Комбинация, ее применение и способы лечения с использованием указанной комбинации Download PDF

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Publication number
RU2019140298A
RU2019140298A RU2019140298A RU2019140298A RU2019140298A RU 2019140298 A RU2019140298 A RU 2019140298A RU 2019140298 A RU2019140298 A RU 2019140298A RU 2019140298 A RU2019140298 A RU 2019140298A RU 2019140298 A RU2019140298 A RU 2019140298A
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Prior art keywords
sodium
dolutegravir
rilpivirine hydrochloride
layer
starch glycolate
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RU2019140298A
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English (en)
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RU2019140298A3 (ru
RU2755710C2 (ru
Inventor
Кеннет Черчилль КЭМПБЕЛЛ
Урбейн Альфонс С. ДЕЛАЕТ
Джеймс М. ГУДРИЧ
Жюльетт Сеголен ГАКЬЕР
Томас ЛОГЕРИ
Доминик Ж. ЛИМЕ
Джон С. ПОТТЭДЖ
Людовик Силвэйн Марк РЕНО
Тревор Р. СКОТТ
Кристиан СЕЙЛЕР
Мэри ВУДВОРД
Original Assignee
Вайв Хелткер Компани
Янссен Сайенсиз Айэлэнд Анлимитед Компани
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Publication date
Priority claimed from GBGB1717131.5A external-priority patent/GB201717131D0/en
Priority claimed from GBGB1719377.2A external-priority patent/GB201719377D0/en
Priority claimed from GBGB1806490.7A external-priority patent/GB201806490D0/en
Application filed by Вайв Хелткер Компани, Янссен Сайенсиз Айэлэнд Анлимитед Компани filed Critical Вайв Хелткер Компани
Publication of RU2019140298A3 publication Critical patent/RU2019140298A3/ru
Publication of RU2019140298A publication Critical patent/RU2019140298A/ru
Application granted granted Critical
Publication of RU2755710C2 publication Critical patent/RU2755710C2/ru

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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
    • A61K9/209Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • 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
    • A61K31/5365Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/5395Heterocyclic 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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
    • 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
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • 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)
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  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (15)

1. Многослойная таблетка для лечения ВИЧ-инфекции, содержащая
а) долутегравир натрия; и
б) гидрохлорид рилпивирина,
где долутегравир натрия и гидрохлорид рилпивирина присутствуют в отдельных слоях.
2. Таблетка по п. 1, где указанная двухслойная таблетка содержит примерно 50 мг долутегравира натрия, в эквиваленте свободной кислоты, и примерно 25 мг гидрохлорида рилпивирина, в эквиваленте свободного основания.
3. Таблетка по п. 1, дополнительно содержащая оболочку.
4. Таблетка по п. 1, где долутегравир натрия присутствует в первом слое, содержащем
ингредиент масса (мг) интрагранулярные долутегравир натрия 52,62 D-маннит 145,38 микрокристаллическая целлюлоза 60,00 повидон К29/32 15,00 крахмалгликолят натрия 15,00 очищенная вода q.s. экстрагранулярные крахмалгликолят натрия 6,00 стеарилфумарат натрия 6,00
и гидрохлорид рилпивирина присутствует во втором слое, содержащем
ингредиент масса (мг) гидрохлорид рилпивирина 27,50 моногидрат лактозы 55,145 кроскармеллоза натрия 1,10 повидон К30 3,25 полисорбат 20 0,35 очищенная вода q.s. D-маннит 57,755 силикатизированная
микрокристаллическая целлюлоза
40,00
крахмалгликолят натрия 12,90 стеарат магния 2,00
5. Двухслойная таблетка для лечения ВИЧ инфекции, содержащая первый слой, содержащий долутегравир натрия; и второй слой, содержащий гидрохлорид рилпивирина; где указанная двухслойная таблетка содержит примерно 50 мг эквивалента свободной кислоты долутегравира натрия, и примерно 25 мг эквивалента свободного основания гидрохлорида рилпивирина; и где указанный первый слой и указанный второй слой непосредственно контактируют друг с другом; где первый слой содержит
ингредиент масса (мг) интрагранулярные долутегравир натрия 52,62 D-маннит 145,38 микрокристаллическая целлюлоза 60,00 повидон К29/32 15,00 крахмалгликолят натрия 15,00 очищенная вода q.s. экстрагранулярные крахмалгликолят натрия 6,00 стеарилфумарат натрия 6,00
и второй слой содержит
ингредиент масса (мг) гидрохлорид рилпивирина 27,50 моногидрат лактозы 55,145 кроскармеллоза натрия 1,10 повидон К30 3,25 полисорбат 20 0,35 очищенная вода q.s. D-маннит 57,755 силикатизированная микрокристаллическая целлюлоза 40,00 крахмалгликолят натрия 12,90 стеарат магния 2,00.
6. Способ лечения ВИЧ-инфекции у пациента, включающий введение указанному пациенту таблетки по любому из пп. 1-5.
RU2019140298A 2017-06-30 2018-06-27 Комбинация, ее применение и способы лечения с использованием указанной комбинации RU2755710C2 (ru)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US201762527169P 2017-06-30 2017-06-30
US62/527,169 2017-06-30
US201762535290P 2017-07-21 2017-07-21
US62/535,290 2017-07-21
GBGB1717131.5A GB201717131D0 (en) 2017-10-18 2017-10-18 Novel formulation
GB1717131.5 2017-10-18
US201762589576P 2017-11-22 2017-11-22
GBGB1719377.2A GB201719377D0 (en) 2017-11-22 2017-11-22 Novel formulation
US62/589,576 2017-11-22
GB1719377.2 2017-11-22
GB1806490.7 2018-04-20
GBGB1806490.7A GB201806490D0 (en) 2018-04-20 2018-04-20 Novel formulation
PCT/IB2018/054769 WO2019003150A2 (en) 2017-06-30 2018-06-27 ASSOCIATION, USES AND THERAPEUTIC DIAGRAMS

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RU2019140298A3 RU2019140298A3 (ru) 2021-07-30
RU2019140298A true RU2019140298A (ru) 2021-07-30
RU2755710C2 RU2755710C2 (ru) 2021-09-20

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KR (1) KR102722927B1 (ru)
CN (1) CN110958883A (ru)
AU (1) AU2018291076B2 (ru)
BR (1) BR112019027915A2 (ru)
CA (1) CA3067147A1 (ru)
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TW (1) TWI830703B (ru)
WO (1) WO2019003150A2 (ru)

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AU2018291076B2 (en) 2021-01-21
AU2018291076A1 (en) 2020-01-23
US20200113838A1 (en) 2020-04-16
JP2020525520A (ja) 2020-08-27
RU2019140298A3 (ru) 2021-07-30
KR102722927B1 (ko) 2024-10-28
BR112019027915A2 (pt) 2020-07-14
CA3067147A1 (en) 2019-01-03
WO2019003150A2 (en) 2019-01-03
WO2019003150A3 (en) 2019-02-21
TW201919586A (zh) 2019-06-01
EP3645003A2 (en) 2020-05-06
RU2755710C2 (ru) 2021-09-20
CN110958883A (zh) 2020-04-03
TWI830703B (zh) 2024-02-01
KR20200024259A (ko) 2020-03-06
JP7287906B2 (ja) 2023-06-06
EP3645003A4 (en) 2021-03-10
US12011506B2 (en) 2024-06-18

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