EA201070626A1 - Система доставки лекарственного средства для введения водорастворимого катионного и амфифильного фармацевтически активного вещества - Google Patents

Система доставки лекарственного средства для введения водорастворимого катионного и амфифильного фармацевтически активного вещества

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Publication number
EA201070626A1
EA201070626A1 EA201070626A EA201070626A EA201070626A1 EA 201070626 A1 EA201070626 A1 EA 201070626A1 EA 201070626 A EA201070626 A EA 201070626A EA 201070626 A EA201070626 A EA 201070626A EA 201070626 A1 EA201070626 A1 EA 201070626A1
Authority
EA
Eurasian Patent Office
Prior art keywords
methyl ester
sodium salt
sdl
retinoylcysteic acid
water
Prior art date
Application number
EA201070626A
Other languages
English (en)
Other versions
EA018559B1 (ru
Inventor
Джулиан Алексов
Игорь Локот
Original Assignee
Ардениа Инвестментс, Лтд.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Ардениа Инвестментс, Лтд. filed Critical Ардениа Инвестментс, Лтд.
Publication of EA201070626A1 publication Critical patent/EA201070626A1/ru
Publication of EA018559B1 publication Critical patent/EA018559B1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules 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
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/5123—Organic compounds, e.g. fats, sugars
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/232—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/541—Organic ions forming an ion pair complex with the pharmacologically or therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate 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
    • A61K9/145—Intimate 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 compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nanotechnology (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

В настоящем изобретении предложена система доставки лекарственного средства (СДЛ) для введения водорастворимого катионного и амфифильного фармацевтически активного вещества (ФАВ), при этом указанная СДЛ содержит аморфные частицы размером <100 нм плохо растворимого в воде комплекса ФАВ с натриевой солью метилового эфира N-полностью-транс-ретиноилцистеиновой кислоты и/или натриевой солью метилового эфира N-13-цис-ретиноилцистеиновой кислоты, при этом указанные частицы заключены внутри наночастиц, образованных натриевой солью метилового эфира N-полностью-транс-ретиноилцистеиновой кислоты и/или натриевой солью метилового эфира N-13-цис-ретиноилцистеиновой кислоты, причем массовое отношение натриевой соли метилового эфира N-полностью-транс-ретиноилцистеиновой кислоты и/или натриевой соли метилового эфира N-13-цис-ретиноилцистеиновой кислоты к указанному комплексу составляет от примерно 0.5:1 до примерно 20:1. Также предложена фармацевтическая композиция, содержащая указанную СДЛ, способы получения указанной СДЛ и указанной фармацевтической композиции, а также применение указанной СДЛ и фармацевтической композиции для лечения рака.
EA201070626A 2007-12-19 2008-12-18 Система доставки лекарственного средства для введения водорастворимого катионного и амфифильного фармацевтически активного вещества EA018559B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/SE2007/001128 WO2009078755A1 (en) 2007-12-19 2007-12-19 Drug delivery system for administration of a water soluble, cationic and amphiphilic pharmaceutically active substance
PCT/SE2008/051517 WO2009078804A1 (en) 2007-12-19 2008-12-18 Drug delivery system for administration of a water soluble, cationic and amphiphilic pharmaceutically active substance

Publications (2)

Publication Number Publication Date
EA201070626A1 true EA201070626A1 (ru) 2010-12-30
EA018559B1 EA018559B1 (ru) 2013-08-30

Family

ID=40795733

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Application Number Title Priority Date Filing Date
EA201070626A EA018559B1 (ru) 2007-12-19 2008-12-18 Система доставки лекарственного средства для введения водорастворимого катионного и амфифильного фармацевтически активного вещества

Country Status (23)

Country Link
US (1) US8324274B2 (ru)
EP (1) EP2231193B1 (ru)
JP (1) JP5466174B2 (ru)
KR (1) KR101616135B1 (ru)
CN (1) CN101945671B (ru)
AU (1) AU2008339101B2 (ru)
BR (1) BRPI0821739B8 (ru)
CA (1) CA2709268C (ru)
CY (1) CY1121145T1 (ru)
DK (1) DK2231193T3 (ru)
EA (1) EA018559B1 (ru)
ES (1) ES2689509T3 (ru)
HR (1) HRP20181517T1 (ru)
HU (1) HUE039695T2 (ru)
LT (1) LT2231193T (ru)
MX (1) MX2010006906A (ru)
MY (1) MY150820A (ru)
NZ (1) NZ586858A (ru)
PL (1) PL2231193T3 (ru)
PT (1) PT2231193T (ru)
SI (1) SI2231193T1 (ru)
WO (2) WO2009078755A1 (ru)
ZA (1) ZA201004992B (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009078756A1 (en) 2007-12-19 2009-06-25 Ardenia Investments, Ltd. Drug delivery system for administration of a water soluble, cationic and amphiphilic pharmaceutically active substance
WO2009078754A1 (en) * 2007-12-19 2009-06-25 Ardenia Investments, Ltd. Drug delivery system for administration of poorly water soluble pharmaceutically active substances
CN112239418B (zh) * 2019-07-18 2023-07-07 上海现代药物制剂工程研究中心有限公司 视黄醇类化合物及其钠盐的制备方法
CN112321465B (zh) 2019-07-18 2023-06-06 上海现代药物制剂工程研究中心有限公司 一种含苯基化合物、其中间体、制备方法及应用

Family Cites Families (16)

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US6197809B1 (en) * 1998-12-23 2001-03-06 Ardenia Investments Ltd. Compounds for the treatment of cancer
JP4643009B2 (ja) * 1999-03-11 2011-03-02 アーデニア・インベストメンツ・リミテッド 癌治療のための新規化合物
US6656504B1 (en) 1999-09-09 2003-12-02 Elan Pharma International Ltd. Nanoparticulate compositions comprising amorphous cyclosporine and methods of making and using such compositions
SE0101702D0 (sv) * 2001-05-15 2001-05-15 Ardenia Investments Ltd Novel potentiating compounds
KR100566911B1 (ko) * 2001-06-25 2006-04-03 주식회사 삼양사 약물 전달체용 음이온기-함유 양친성 블록 공중합체 및 그의 양이온성 약물과의 복합체
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JP2004010479A (ja) * 2002-06-03 2004-01-15 Japan Science & Technology Corp ブロック共重合体とアンスラサイクリン系抗癌剤を含む新規固型製剤及びその製造法
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CN105288630A (zh) * 2005-02-18 2016-02-03 阿布拉科斯生物科学有限公司 治疗剂的组合和给予方式以及联合治疗
BRPI0615292A8 (pt) 2005-08-31 2018-03-06 Abraxis Bioscience Llc composições e métodos para preparação de fármacos de má solubilidade em água com estabilidade aumentada
WO2009078756A1 (en) 2007-12-19 2009-06-25 Ardenia Investments, Ltd. Drug delivery system for administration of a water soluble, cationic and amphiphilic pharmaceutically active substance
WO2009078754A1 (en) 2007-12-19 2009-06-25 Ardenia Investments, Ltd. Drug delivery system for administration of poorly water soluble pharmaceutically active substances

Also Published As

Publication number Publication date
CN101945671A (zh) 2011-01-12
JP5466174B2 (ja) 2014-04-09
BRPI0821739A2 (pt) 2015-06-16
KR20100099290A (ko) 2010-09-10
EP2231193B1 (en) 2018-07-18
AU2008339101A1 (en) 2009-06-25
AU2008339101B2 (en) 2015-08-06
SI2231193T1 (sl) 2018-12-31
PT2231193T (pt) 2018-11-02
LT2231193T (lt) 2018-11-12
EP2231193A4 (en) 2014-12-03
HUE039695T2 (hu) 2019-01-28
CA2709268C (en) 2016-02-09
HRP20181517T1 (hr) 2018-11-30
JP2011507840A (ja) 2011-03-10
PL2231193T3 (pl) 2019-01-31
DK2231193T3 (en) 2018-10-22
CA2709268A1 (en) 2009-06-25
CN101945671B (zh) 2012-08-22
MX2010006906A (es) 2010-11-10
WO2009078804A1 (en) 2009-06-25
EA018559B1 (ru) 2013-08-30
ES2689509T3 (es) 2018-11-14
US8324274B2 (en) 2012-12-04
BRPI0821739B1 (pt) 2021-03-02
BRPI0821739B8 (pt) 2021-05-25
MY150820A (en) 2014-02-28
WO2009078755A1 (en) 2009-06-25
NZ586858A (en) 2012-06-29
CY1121145T1 (el) 2020-05-29
EP2231193A1 (en) 2010-09-29
ZA201004992B (en) 2011-03-30
US20110236472A1 (en) 2011-09-29
KR101616135B1 (ko) 2016-04-27

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