WO2008139804A1 - 徐放性の陰荷電基を持つ低分子薬物含有ナノ粒子 - Google Patents

徐放性の陰荷電基を持つ低分子薬物含有ナノ粒子 Download PDF

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Publication number
WO2008139804A1
WO2008139804A1 PCT/JP2008/057167 JP2008057167W WO2008139804A1 WO 2008139804 A1 WO2008139804 A1 WO 2008139804A1 JP 2008057167 W JP2008057167 W JP 2008057167W WO 2008139804 A1 WO2008139804 A1 WO 2008139804A1
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Prior art keywords
low
negatively charged
charged group
poly
containing nanoparticle
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PCT/JP2008/057167
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English (en)
French (fr)
Inventor
Tsutomu Ishihara
Yutaka Mizushima
Toru Mizushima
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Ltt Bio-Pharma Co., Ltd.
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Application filed by Ltt Bio-Pharma Co., Ltd. filed Critical Ltt Bio-Pharma Co., Ltd.
Priority to CN2008800158427A priority Critical patent/CN101678113B/zh
Priority to KR1020097025625A priority patent/KR101513318B1/ko
Priority to EP08740264A priority patent/EP2156848A4/en
Priority to US12/597,969 priority patent/US20100129456A1/en
Priority to JP2009514038A priority patent/JP5248487B2/ja
Publication of WO2008139804A1 publication Critical patent/WO2008139804A1/ja

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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
    • A61K9/48—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
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • A61K9/5153—Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K9/5192—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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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)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Nanotechnology (AREA)
  • Optics & Photonics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

　効率的にターゲッティングし、薬物徐放性に優れ、かつ肝臓集積を低減することにより副作用を軽減させた低分子薬物含有ナノ粒子を提供することであり、陰荷電基を持つ低分子薬物を金属イオンにより疎水化し、これをポリＬ－乳酸又はポリ（Ｌ－乳酸／グリコール酸）共重合体、及びポリＤＬ－又はＬ－乳酸－ポリエチレングリコールブロック共重合体又はポリ（ＤＬ－又はＬ－乳酸／グリコール酸）－ポリエチレングリコールブロック共重合体と作用させることにより得られる陰荷電基を持つ低分子薬物含有ナノ粒子である。
PCT/JP2008/057167 2007-05-14 2008-04-11 徐放性の陰荷電基を持つ低分子薬物含有ナノ粒子 WO2008139804A1 (ja)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CN2008800158427A CN101678113B (zh) 2007-05-14 2008-04-11 缓释性的含有带负电荷基团的低分子药物的纳米粒子
KR1020097025625A KR101513318B1 (ko) 2007-05-14 2008-04-11 서방성의 음하전기를 갖는 저분자 약물 함유 나노 입자
EP08740264A EP2156848A4 (en) 2007-05-14 2008-04-11 NANOPARTICLE CONTAINING A LOW MOLECULAR WEIGHT DRUG HAVING A NEGATIVELY PROLONGED RELEASE GROUP
US12/597,969 US20100129456A1 (en) 2007-05-14 2008-04-11 Sustained-release nanoparticle containing low-molecular-weight drug with negatively charged group
JP2009514038A JP5248487B2 (ja) 2007-05-14 2008-04-11 徐放性の陰荷電基を持つ低分子薬物含有ナノ粒子

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007128059 2007-05-14
JP2007-128059 2007-05-14

Publications (1)

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WO2008139804A1 true WO2008139804A1 (ja) 2008-11-20

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Country Status (6)

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US (1) US20100129456A1 (ja)
EP (1) EP2156848A4 (ja)
JP (1) JP5248487B2 (ja)
KR (1) KR101513318B1 (ja)
CN (1) CN101678113B (ja)
WO (1) WO2008139804A1 (ja)

Cited By (19)

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WO2011049036A1 (ja) * 2009-10-19 2011-04-28 株式会社Ｌｔｔバイオファーマ 低分子薬物含有ナノ粒子
WO2011084518A2 (en) 2009-12-15 2011-07-14 Bind Biosciences, Inc. Therapeutic polymeric nanoparticles comprising corticosteroids and methods of making and using same
US8206747B2 (en) 2008-06-16 2012-06-26 Bind Biosciences, Inc. Drug loaded polymeric nanoparticles and methods of making and using same
US8211473B2 (en) 2009-12-11 2012-07-03 Bind Biosciences, Inc. Stable formulations for lyophilizing therapeutic particles
WO2012111627A1 (ja) 2011-02-18 2012-08-23 株式会社Ｌｔｔバイオファーマ プロスタグランジンｉ２誘導体を含有するナノ粒子
US8318211B2 (en) 2008-06-16 2012-11-27 Bind Biosciences, Inc. Therapeutic polymeric nanoparticles comprising vinca alkaloids and methods of making and using same
WO2013035579A1 (ja) * 2011-09-05 2013-03-14 株式会社Ｌｔｔバイオファーマ 薬物を封入した肝臓集積性ナノ粒子
US8518963B2 (en) 2009-12-15 2013-08-27 Bind Therapeutics, Inc. Therapeutic polymeric nanoparticle compositions with high glass transition temperature or high molecular weight copolymers
US8563041B2 (en) 2008-12-12 2013-10-22 Bind Therapeutics, Inc. Therapeutic particles suitable for parenteral administration and methods of making and using same
US8613951B2 (en) 2008-06-16 2013-12-24 Bind Therapeutics, Inc. Therapeutic polymeric nanoparticles with mTor inhibitors and methods of making and using same
KR20140086740A (ko) 2012-12-28 2014-07-08 주식회사 종근당 음이온성 약리학적 활성물질의 서방성 지질 초기제제 및 이를 포함하는 약제학적 조성물
JP2015505855A (ja) * 2011-12-14 2015-02-26 ザ・ジョンズ・ホプキンス・ユニバーシティー 粘膜浸透が増強されたかまたは炎症が低減されたナノ粒子
JP2015525245A (ja) * 2012-04-23 2015-09-03 ナノジェン ファーマシューティカルズ ポリマーナノ粒子およびその調整のプロセス
US9198874B2 (en) 2008-12-15 2015-12-01 Bind Therapeutics, Inc. Long circulating nanoparticles for sustained release of therapeutic agents
JP2017524712A (ja) * 2014-08-13 2017-08-31 ザ・ジョンズ・ホプキンス・ユニバーシティー 角膜同種移植片拒絶および新血管形成を予防するためのグルココルチコイドを負荷したナノ粒子
US9877923B2 (en) 2012-09-17 2018-01-30 Pfizer Inc. Process for preparing therapeutic nanoparticles
US9895378B2 (en) 2014-03-14 2018-02-20 Pfizer Inc. Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using the same
US10047072B2 (en) 2013-09-16 2018-08-14 Astrazeneca Ab Therapeutic polymeric nanoparticles and methods of making and using same
US11484507B2 (en) 2016-11-02 2022-11-01 Hillstream Biopharma, Inc. Polymeric nanoparticles providing nucleic acids encoding TNF-α

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JP5131971B2 (ja) * 2005-12-26 2013-01-30 株式会社Ｌｔｔバイオファーマ 水溶性非ペプチド性低分子薬物含有ナノ粒子
US9327037B2 (en) 2011-02-08 2016-05-03 The Johns Hopkins University Mucus penetrating gene carriers
KR101494594B1 (ko) 2011-08-30 2015-02-23 주식회사 종근당 약리학적 활성물질의 서방성 지질 초기제제 및 이를 포함하는 약제학적 조성물
TWI641396B (zh) 2011-09-23 2018-11-21 Bvw控股公司 醫療共聚物
JP2016529284A (ja) 2013-08-27 2016-09-23 ノースイースタン ユニバーシティ ナノ粒子薬物デリバリシステムおよび、癌および神経外傷の治療方法
US10335500B2 (en) 2014-05-12 2019-07-02 The Johns Hopkins University Highly stable biodegradable gene vector platforms for overcoming biological barriers
JP2018533574A (ja) * 2015-10-30 2018-11-15 ファイザー・インク 治療剤を含む治療用ナノ粒子ならびにそれを作製および使用する方法
WO2022154463A1 (ko) * 2021-01-15 2022-07-21 랩인큐브 주식회사 금속유기 복합입자 및 금속유기 복합입자를 포함하는 조성물

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Cited By (59)

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CN101678113B (zh) 2012-05-30
KR101513318B1 (ko) 2015-04-17
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