JP6158513B2 - タクソール／ステロイド化合物 - Google Patents

タクソール／ステロイド化合物 Download PDF

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Publication number
JP6158513B2
JP6158513B2 JP2012535616A JP2012535616A JP6158513B2 JP 6158513 B2 JP6158513 B2 JP 6158513B2 JP 2012535616 A JP2012535616 A JP 2012535616A JP 2012535616 A JP2012535616 A JP 2012535616A JP 6158513 B2 JP6158513 B2 JP 6158513B2
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Prior art keywords
taxol
steroid
compound
cholesterol
oil
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JP2012535616A
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Japanese (ja)
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JP2013509360A5 (enExample
JP2013509360A (ja
Inventor
玉玲 対
玉玲 対
学軍 夏
学軍 夏
瑞芳 郭
瑞芳 郭
鵬宵 張
鵬宵 張
翠萍 周
翠萍 周
仁芸 汪
仁芸 汪
篶嘉 金
篶嘉 金
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Institute of Materia Medica, CAMS&PUMC
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Institute of Materia Medica, CAMS&PUMC
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    • 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
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • 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
    • A61K9/14—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
    • 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
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dispersion Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Epoxy Compounds (AREA)
JP2012535616A 2009-10-29 2010-10-28 タクソール／ステロイド化合物 Active JP6158513B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN200910236960.7A CN102048725B (zh) 2009-10-29 2009-10-29 紫杉醇胆固醇复合物
CN200910236960.7 2009-10-29
PCT/CN2010/078202 WO2011050735A1 (zh) 2009-10-29 2010-10-28 紫杉醇/类固醇复合物

Publications (3)

Publication Number Publication Date
JP2013509360A JP2013509360A (ja) 2013-03-14
JP2013509360A5 JP2013509360A5 (enExample) 2017-01-12
JP6158513B2 true JP6158513B2 (ja) 2017-07-12

Family

ID=43921347

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012535616A Active JP6158513B2 (ja) 2009-10-29 2010-10-28 タクソール／ステロイド化合物

Country Status (9)

Country Link
US (1) US20130150335A1 (enExample)
EP (1) EP2494956A4 (enExample)
JP (1) JP6158513B2 (enExample)
KR (1) KR20120091258A (enExample)
CN (2) CN102048725B (enExample)
AU (1) AU2010312017B2 (enExample)
BR (1) BR112012010149A2 (enExample)
CA (1) CA2779316C (enExample)
WO (1) WO2011050735A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102048688B (zh) * 2009-10-29 2014-03-05 中国医学科学院药物研究所 以胆固醇复合物为中间载体的紫杉醇亚微乳
EP2679225A1 (de) * 2012-06-26 2014-01-01 Universitätsklinikum Freiburg Pharmazeutische Zusammensetzung mit synergistischer Wirkung von direkten Katalaseinhibitoren und zur Katalasezerstörung führenden Modulatoren des NO-Stoffwechsels oder der extrazellulären Superoxidanionenproduktion
AU2018283411B2 (en) 2017-06-16 2021-04-29 Sorse Technology Corporation Preparing stable liquid emulsion forms of plant extract
CN108272747B (zh) * 2018-03-16 2020-02-18 武汉百纳礼康生物制药有限公司 一种非那雄胺溶致液晶凝胶制剂前体及其制备方法
BR112021005104A2 (pt) 2018-10-16 2021-06-08 US Nano Food & Drug INC formulação de injeção intratumoral
JP2023520975A (ja) 2020-04-13 2023-05-23 ユーエス・ナノ・フード・アンド・ドラッグ・インコーポレーテッド 塩基性化学療法腫瘍内注射製剤
KR102789632B1 (ko) * 2021-04-01 2025-04-01 에스엔제이 파마 인크 생활성물질의 경구용 나노입자 및 이의 제조방법
CN115177589B (zh) * 2021-04-07 2024-02-06 中国医学科学院药物研究所 一种紫杉醇脑靶向脂质体和其制备方法及应用
CN115463110B (zh) * 2021-06-10 2023-12-15 中国医学科学院药物研究所 一种胆酸修饰的口服紫杉醇纳米粒、其制备方法及应用
CN115737654B (zh) * 2021-09-03 2025-11-21 成都瑞沐生物医药科技有限公司 一种滴眼给药预防和/或治疗白内障的眼用制剂
CN116196283A (zh) * 2021-11-30 2023-06-02 深圳玖星制药有限公司 一种注射用紫杉烷类药物脂质体冻干粉剂的制备方法及原料组方
CN117482052A (zh) * 2023-11-29 2024-02-02 中国药科大学 一种口服紫杉醇三元递药系统及其制备方法与应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5616330A (en) * 1994-07-19 1997-04-01 Hemagen/Pfc Stable oil-in-water emulsions incorporating a taxine (taxol) and method of making same
US5827533A (en) * 1997-02-06 1998-10-27 Duke University Liposomes containing active agents aggregated with lipid surfactants
CN1116875C (zh) * 2000-10-19 2003-08-06 南京振中生物工程有限公司 紫杉醇脂质组合物及其制备方法
US20090110739A1 (en) * 2007-05-15 2009-04-30 University Of North Texas Health Science Center At Forth Worth Targeted cancer chemotherapy using synthetic nanoparticles
CN101396343B (zh) * 2007-09-26 2011-12-07 中国医学科学院药物研究所 以脂质复合物为中间载体的紫杉醇亚微乳
CN102048688B (zh) * 2009-10-29 2014-03-05 中国医学科学院药物研究所 以胆固醇复合物为中间载体的紫杉醇亚微乳

Also Published As

Publication number Publication date
CN102811706B (zh) 2015-05-06
CN102048725A (zh) 2011-05-11
US20130150335A1 (en) 2013-06-13
EP2494956A9 (en) 2013-04-17
HK1179513A1 (zh) 2013-10-04
JP2013509360A (ja) 2013-03-14
CN102048725B (zh) 2014-07-16
CA2779316C (en) 2016-05-03
WO2011050735A1 (zh) 2011-05-05
CA2779316A1 (en) 2011-05-05
EP2494956A4 (en) 2013-10-23
KR20120091258A (ko) 2012-08-17
AU2010312017B2 (en) 2014-07-17
EP2494956A1 (en) 2012-09-05
AU2010312017A1 (en) 2012-06-21
CN102811706A (zh) 2012-12-05
BR112012010149A2 (pt) 2018-03-20

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