RU2018105494A - Улучшенные системы доставки наночастиц - Google Patents

Улучшенные системы доставки наночастиц Download PDF

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RU2018105494A
RU2018105494A RU2018105494A RU2018105494A RU2018105494A RU 2018105494 A RU2018105494 A RU 2018105494A RU 2018105494 A RU2018105494 A RU 2018105494A RU 2018105494 A RU2018105494 A RU 2018105494A RU 2018105494 A RU2018105494 A RU 2018105494A
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Russia
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composition according
therapeutic agent
nanoparticles
composition
prodrug
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RU2018105494A
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English (en)
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RU2018105494A3 (ru
Inventor
Леон ВАН
Винни ЛУИ
Пол ТАРДИ
Лоренс МАЙЕР
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Селатор Фармасьютикалз, Инк.
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Publication of RU2018105494A publication Critical patent/RU2018105494A/ru
Publication of RU2018105494A3 publication Critical patent/RU2018105494A3/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
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5146Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • A61K9/5153Polyesters, e.g. poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5192Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Optics & Photonics (AREA)
  • Nanotechnology (AREA)
  • Physics & Mathematics (AREA)
  • Botany (AREA)
  • Dermatology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (17)

1. Фармацевтический состав, включающий набор фармацевтических составов, содержащих наночастицы, где указанные наночастицы имеют средний диаметр менее 80 нм, и содержат:
а) по меньшей мере два терапевтических агента, каждый терапевтический агент соединен через линкер с гидрофобной частью для формирования пролекарства, и
b) амфифильный стабилизатор, содержащий гидрофобную часть и гидрофильную часть, в котором массовое соотношение гидрофобной части к гидрофильной части находится в диапазоне 8:5-12:5 и в котором гидрофобная часть имеет молекулярную массу 8 кДа - 15 кДа.
2. Состав по п. 1, в котором указанный амфифильный стабилизатор представляет собой диблок-сополимер.
3. Состав по п. 1, в котором в указанном амфифильном стабилизаторе гидрофобная часть содержит полимолочную кислоту (PLA) или сополимер молочной и гликолевой кислот (PLGA), и гидрофильная часть содержит полиэтиленгликоль (PEG).
4. Состав по п. 1, в котором по меньшей мере два терапевтических агента включены в одну и ту же наночастицу.
5. Состав по п. 1, в котором один терапевтический агент представляет собой таксан, и другой терапевтический агент представляет собой HSP ингибитор, или где один терапевтический агент представляет собой PI3K/AKT/mTOR ингибитор, и другой терапевтический агент представляет собой RAS/RAF/MEK/ERK ингибитор.
6. Состав по п. 1, в котором в каждом из указанных пролекарств, гидрофобная часть представляет собой холестерин и/или линкер представляет собой дигликолевую кислоту.
7. Состав по п. 1, в котором указанные наночастицы формируются путем смешивания водной фазы и органической фазы, указанная органическая фаза содержит указанный сополимер и указанное пролекарство.
8. Состав по п. 7, в котором указанное смешивание проводится путем быстрого смешивания струйных потоков, один из которых содержит водную фазу и другой содержит органическую фазу.
9. Состав по п. 1, в котором указнные наночастицы имеют средний диаметр 20-80 нм.
10. Состав по п. 1, который дополнительно содержит третий терапевтический агент.
11. Состав по п. 10, в котором указанный третий терапевтический агент поставляется как пролекарство и инкапсулирован в указанные наночастицы.
12. Способ введения комбинации двух или больше терапевтических агентов, способ, который содержит введение к субьекту состава по п. 1.
13. Способ по п. 12, в котором указанное введение осуществляется путем парентерального введения.
14. Способ по п. 13, в котором субъект является человеком или не принадлежащим к человеческому роду млекопитающим или птицей.
15. Способ получения состава по п. 1, способ, который содержит быстрое смешивание водной фазы с органической фазой, содержащей указанный сополимер и указанное пролекарство.
RU2018105494A 2015-07-15 2016-07-14 Улучшенные системы доставки наночастиц RU2018105494A (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562192973P 2015-07-15 2015-07-15
US62/192,973 2015-07-15
US201562252396P 2015-11-06 2015-11-06
US62/252,396 2015-11-06
PCT/US2016/042330 WO2017011685A1 (en) 2015-07-15 2016-07-14 Improved nanoparticle delivery systems

Publications (2)

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RU2018105494A true RU2018105494A (ru) 2019-08-15
RU2018105494A3 RU2018105494A3 (ru) 2019-12-17

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US (3) US10285951B2 (ru)
EP (1) EP3322404A4 (ru)
JP (2) JP2018521068A (ru)
KR (1) KR20180029242A (ru)
CN (1) CN107920985B (ru)
AU (2) AU2016294617B2 (ru)
BR (1) BR112018000217A2 (ru)
CA (1) CA2991062C (ru)
CO (1) CO2018000146A2 (ru)
HK (1) HK1251159A1 (ru)
IL (1) IL256797B (ru)
MA (1) MA42458A (ru)
MX (1) MX2018000611A (ru)
RU (1) RU2018105494A (ru)
SG (1) SG10201912394VA (ru)
WO (1) WO2017011685A1 (ru)
ZA (1) ZA201800130B (ru)

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WO2019178443A1 (en) * 2018-03-16 2019-09-19 University Of Massachusetts Yeast cell wall particle encapsulation of biodegradable pro-payloads
KR102088663B1 (ko) * 2018-03-20 2020-03-13 한국세라믹기술원 친수성 및 소수성 약물의 동시 전달을 위한 온도민감성 나노스펀지 플랫폼 및 이의 용도
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JP2024511067A (ja) 2021-03-19 2024-03-12 トレインド セラピューティクス ディスカバリー,インコーポレーテッド 訓練された免疫を調節するための化合物およびその使用方法

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US20210052508A1 (en) 2021-02-25
SG10201912394VA (en) 2020-02-27
MA42458A (fr) 2018-05-23
JP2018521068A (ja) 2018-08-02
RU2018105494A3 (ru) 2019-12-17
JP2022033751A (ja) 2022-03-02
KR20180029242A (ko) 2018-03-20
CN107920985B (zh) 2022-03-01
HK1251159A1 (zh) 2019-01-25
US20190209484A1 (en) 2019-07-11
US20180207104A1 (en) 2018-07-26
US10285951B2 (en) 2019-05-14
CO2018000146A2 (es) 2018-04-19
BR112018000217A2 (pt) 2018-09-04
EP3322404A4 (en) 2019-03-20
EP3322404A1 (en) 2018-05-23
MX2018000611A (es) 2018-09-06
CA2991062C (en) 2023-06-20
IL256797A (en) 2018-06-28
IL256797B (en) 2021-05-31
CN107920985A (zh) 2018-04-17
ZA201800130B (en) 2018-12-19
US11413253B2 (en) 2022-08-16
WO2017011685A1 (en) 2017-01-19
AU2021286353A1 (en) 2022-01-20
AU2016294617B2 (en) 2021-09-16
AU2016294617A1 (en) 2018-01-25
CA2991062A1 (en) 2017-01-19

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