CN102048725B - 紫杉醇胆固醇复合物 - Google Patents

紫杉醇胆固醇复合物 Download PDF

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Publication number
CN102048725B
CN102048725B CN200910236960.7A CN200910236960A CN102048725B CN 102048725 B CN102048725 B CN 102048725B CN 200910236960 A CN200910236960 A CN 200910236960A CN 102048725 B CN102048725 B CN 102048725B
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China
Prior art keywords
paclitaxel
cholesterol
complex
taxol
preparation
Prior art date
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CN200910236960.7A
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English (en)
Chinese (zh)
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CN102048725A (zh
Inventor
刘玉玲
夏学军
郭瑞芳
汪仁芸
王洪亮
金笃嘉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beijing Wuhebao Pharmaceutical Co ltd
Original Assignee
Institute of Materia Medica of CAMS and PUMC
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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Priority to CN200910236960.7A priority Critical patent/CN102048725B/zh
Application filed by Institute of Materia Medica of CAMS and PUMC filed Critical Institute of Materia Medica of CAMS and PUMC
Priority to BR112012010149-8A priority patent/BR112012010149A2/pt
Priority to CA2779316A priority patent/CA2779316C/en
Priority to JP2012535616A priority patent/JP6158513B2/ja
Priority to EP10826098.5A priority patent/EP2494956A4/en
Priority to HK13106587.1A priority patent/HK1179513B/xx
Priority to AU2010312017A priority patent/AU2010312017B2/en
Priority to US13/505,173 priority patent/US20130150335A1/en
Priority to CN201080059671.5A priority patent/CN102811706B/zh
Priority to PCT/CN2010/078202 priority patent/WO2011050735A1/zh
Priority to KR1020127013922A priority patent/KR20120091258A/ko
Publication of CN102048725A publication Critical patent/CN102048725A/zh
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Publication of CN102048725B publication Critical patent/CN102048725B/zh
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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
    • 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
    • A61K31/56—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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (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)
CN200910236960.7A 2009-10-29 2009-10-29 紫杉醇胆固醇复合物 Active CN102048725B (zh)

Priority Applications (11)

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
CN201080059671.5A CN102811706B (zh) 2009-10-29 2010-10-28 紫杉醇/类固醇复合物
JP2012535616A JP6158513B2 (ja) 2009-10-29 2010-10-28 タクソール／ステロイド化合物
EP10826098.5A EP2494956A4 (en) 2009-10-29 2010-10-28 Paclitaxel / STEROID COMPLEX
HK13106587.1A HK1179513B (en) 2009-10-29 2010-10-28 Paclitaxel/steroidal complex
AU2010312017A AU2010312017B2 (en) 2009-10-29 2010-10-28 Paclitaxel/steroidal complex
BR112012010149-8A BR112012010149A2 (pt) 2009-10-29 2010-10-28 composto de paclitaxel / esteroidal
CA2779316A CA2779316C (en) 2009-10-29 2010-10-28 Paclitaxel/steroidal compound
PCT/CN2010/078202 WO2011050735A1 (zh) 2009-10-29 2010-10-28 紫杉醇/类固醇复合物
KR1020127013922A KR20120091258A (ko) 2009-10-29 2010-10-28 파클리탁셀/스테로이드 복합체
US13/505,173 US20130150335A1 (en) 2009-10-29 2010-10-28 Paclitaxel/steroidal complex

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
CN102048725A CN102048725A (zh) 2011-05-11
CN102048725B true CN102048725B (zh) 2014-07-16

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CN200910236960.7A Active CN102048725B (zh) 2009-10-29 2009-10-29 紫杉醇胆固醇复合物
CN201080059671.5A Active CN102811706B (zh) 2009-10-29 2010-10-28 紫杉醇/类固醇复合物

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Country Status (9)

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

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
US11273105B2 (en) * 2017-06-16 2022-03-15 Sorse Technology Corporation Method for preparing solid 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
KR20210078505A (ko) 2018-10-16 2021-06-28 유에스 나노 푸드 앤 드럭 인코포레이티드 종양내 주사 제형
WO2021211294A1 (en) 2020-04-13 2021-10-21 US Nano Food & Drug INC Basic chemotherapeutic intratumour injection formulation
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1291474A (zh) * 2000-10-19 2001-04-18 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
CN101396343A (zh) * 2007-09-26 2009-04-01 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
US20090110739A1 (en) * 2007-05-15 2009-04-30 University Of North Texas Health Science Center At Forth Worth Targeted cancer chemotherapy using synthetic nanoparticles

Family Cites Families (3)

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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
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1291474A (zh) * 2000-10-19 2001-04-18 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
CN101396343A (zh) * 2007-09-26 2009-04-01 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
CN101396346A (zh) * 2007-09-26 2009-04-01 中国医学科学院药物研究所 紫杉醇脂质复合物

Also Published As

Publication number Publication date
EP2494956A9 (en) 2013-04-17
CN102811706A (zh) 2012-12-05
CN102811706B (zh) 2015-05-06
AU2010312017B2 (en) 2014-07-17
JP6158513B2 (ja) 2017-07-12
CN102048725A (zh) 2011-05-11
US20130150335A1 (en) 2013-06-13
KR20120091258A (ko) 2012-08-17
EP2494956A1 (en) 2012-09-05
JP2013509360A (ja) 2013-03-14
WO2011050735A1 (zh) 2011-05-05
CA2779316C (en) 2016-05-03
EP2494956A4 (en) 2013-10-23
HK1179513A1 (zh) 2013-10-04
BR112012010149A2 (pt) 2018-03-20
CA2779316A1 (en) 2011-05-05
AU2010312017A1 (en) 2012-06-21

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Effective date of registration: 20161019

Address after: 102600 Zhongguancun Daxing District science and Technology Park Daxing biomedical industry base, Fu Fu Street, No. 30

Patentee after: Beijing Wehand-Bio Pharmaceutical Co., Ltd.

Address before: 100050 Beijing city Xuanwu District Xiannongtan Street No. 1

Patentee before: Institute of Materia Medica of Chinese Academy of Medical Sciences

CP03 Change of name, title or address

Address after: 102600 30 Tianfu street, Daxing biomedical industry base, Zhongguancun Science and Technology Park, Daxing District, Beijing

Patentee after: Beijing wuhebao Pharmaceutical Co.,Ltd.

Address before: 102600 No.30 Tianfu street, Daxing biomedical industry base, Zhongguancun Science and Technology Park, Daxing District, Beijing

Patentee before: BEIJING WEHAND-BIO PHARMACEUTICAL Co.,Ltd.

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