WO2008099800A1 - 放射性画像診断剤の製造方法 - Google Patents

放射性画像診断剤の製造方法 Download PDF

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Publication number
WO2008099800A1
WO2008099800A1 PCT/JP2008/052231 JP2008052231W WO2008099800A1 WO 2008099800 A1 WO2008099800 A1 WO 2008099800A1 JP 2008052231 W JP2008052231 W JP 2008052231W WO 2008099800 A1 WO2008099800 A1 WO 2008099800A1
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solution
radioactive
labeled
organic compound
imaging agent
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PCT/JP2008/052231
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English (en)
French (fr)
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Daisaku Nakamura
Soichi Nakamura
Masahito Toyama
Akio Hayashi
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Nihon Medi-Physics Co., Ltd.
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Application filed by Nihon Medi-Physics Co., Ltd. filed Critical Nihon Medi-Physics Co., Ltd.
Priority to JP2008558082A priority Critical patent/JP5258583B2/ja
Priority to CN200880008655.6A priority patent/CN101636183B/zh
Priority to CA2678020A priority patent/CA2678020C/en
Priority to KR1020097017131A priority patent/KR101485445B1/ko
Priority to EP08711095.3A priority patent/EP2119458B9/en
Priority to US12/526,667 priority patent/US8343459B2/en
Priority to ES08711095T priority patent/ES2421886T3/es
Publication of WO2008099800A1 publication Critical patent/WO2008099800A1/ja
Priority to HK10104126.7A priority patent/HK1138504A1/xx
Priority to US13/565,204 priority patent/US8658132B2/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C229/48Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0402Organic compounds carboxylic acid carriers, fatty acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0404Lipids, e.g. triglycerides; Polycationic carriers
    • A61K51/0406Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/001Acyclic or carbocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00Purification; Separation; Stabilisation; Use of additives
    • C07B63/04Use of additives
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)

Abstract

【課題】放射性ハロゲン標識アミノ酸化合物を有効成分とする放射性画像診断剤において、該有効成分の放射線分解を抑制し、より安定性を高め得る組成を有したものの製造方法を提供する。 【解決手段】放射性ハロゲン標識アミノ酸化合物を含有した溶液を調製する放射性フッ素標識有機化合物溶液調製工程と、前記放射性フッ素標識有機化合物を含有した溶液を希釈して放射能濃度を調整する希釈工程とを含む放射性画像診断剤の製造方法において、前記放射性フッ素標識有機化合物溶液調製工程後、前記希釈工程前に、前記放射性フッ素標識有機化合物を含有した溶液に酸を加える酸添加工程を含み、前記酸添加工程において添加する酸の量が、希釈工程後の液のpHを2.0から5.9とするのに十分な量、例えば、希釈工程後の液1Lに対して0.40~2.8mmol相当であることを特徴とする方法を用いる。
PCT/JP2008/052231 2007-02-13 2008-02-12 放射性画像診断剤の製造方法 WO2008099800A1 (ja)

Priority Applications (9)

Application Number Priority Date Filing Date Title
JP2008558082A JP5258583B2 (ja) 2007-02-13 2008-02-12 放射性画像診断剤の製造方法
CN200880008655.6A CN101636183B (zh) 2007-02-13 2008-02-12 放射性诊断显像剂的制备方法
CA2678020A CA2678020C (en) 2007-02-13 2008-02-12 Method for production of radiation diagnostic imaging agent
KR1020097017131A KR101485445B1 (ko) 2007-02-13 2008-02-12 방사성 화상진단제의 제조 방법
EP08711095.3A EP2119458B9 (en) 2007-02-13 2008-02-12 Method for production of radiation diagnostic imaging agent
US12/526,667 US8343459B2 (en) 2007-02-13 2008-02-12 Method for production of radiation diagnostic imaging agent
ES08711095T ES2421886T3 (es) 2007-02-13 2008-02-12 Método para producción de un agente de representación de imágenes de diagnóstico por radiación
HK10104126.7A HK1138504A1 (en) 2007-02-13 2010-04-28 Method for production of radiation diagnostic imaging agent
US13/565,204 US8658132B2 (en) 2007-02-13 2012-08-02 Method for production of radiation diagnostic imaging agent

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007031692 2007-02-13
JP2007-031692 2007-02-13

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/526,667 A-371-Of-International US8343459B2 (en) 2007-02-13 2008-02-12 Method for production of radiation diagnostic imaging agent
US13/565,204 Division US8658132B2 (en) 2007-02-13 2012-08-02 Method for production of radiation diagnostic imaging agent

Publications (1)

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WO2008099800A1 true WO2008099800A1 (ja) 2008-08-21

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Country Status (10)

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US (2) US8343459B2 (ja)
EP (1) EP2119458B9 (ja)
JP (1) JP5258583B2 (ja)
KR (1) KR101485445B1 (ja)
CN (1) CN101636183B (ja)
CA (1) CA2678020C (ja)
ES (1) ES2421886T3 (ja)
HK (1) HK1138504A1 (ja)
TW (1) TWI406674B (ja)
WO (1) WO2008099800A1 (ja)

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EP2106808A1 (en) * 2006-12-21 2009-10-07 Nihon Medi-Physics Co., Ltd. Radioactive diagnostic imaging agent
WO2010120368A2 (en) 2009-04-15 2010-10-21 Lantheus Medical Imaging, Inc. Stabilization of radiopharmaceutical compositions using ascorbic acid
JP2015500865A (ja) * 2011-12-21 2015-01-08 ジーイー・ヘルスケア・リミテッド クエン酸緩衝液中の18f−フルシクロビン組成物
JP2015530985A (ja) * 2012-08-09 2015-10-29 ジーイー・ヘルスケア・リミテッド 18f−フルシクロビンの製造
JP2021512070A (ja) * 2018-01-24 2021-05-13 エーシー・イミューン・エス・アー Pet画像化のための診断用組成物、診断用組成物を製造するための方法及び診断におけるその使用
US11077216B2 (en) 2014-06-30 2021-08-03 Ge Healthcare Limited Formulation and method of synthesis
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US11504430B2 (en) 2010-12-29 2022-11-22 Ge Healthcare Limited Eluent solution
US20130004414A1 (en) * 2011-06-30 2013-01-03 General Electric Company Devices and methods for reducing radiolysis of radioisotopes
US20130005958A1 (en) * 2011-06-30 2013-01-03 General Electric Company Devices and methods for reducing radiolysis of radioisotopes
GB201209082D0 (en) * 2012-05-24 2012-07-04 Ge Healthcare Ltd Purification method
GB2561122B (en) * 2012-12-21 2019-07-17 Ge Healthcare Ltd Composition comprising [18F]-Fluciclovine
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Cited By (16)

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EP2106808A1 (en) * 2006-12-21 2009-10-07 Nihon Medi-Physics Co., Ltd. Radioactive diagnostic imaging agent
EP2106808A4 (en) * 2006-12-21 2013-02-27 Nihon Mediphysics Co Ltd RADIOACTIVE DIAGNOSTIC IMAGING AGENT
US8790620B2 (en) 2006-12-21 2014-07-29 Nihon Medi-Physics Co., Ltd. Radioactive diagnostic imaging agent
WO2009059977A1 (en) * 2007-11-07 2009-05-14 Ge Healthcare Bv Stabilization of radiopharmaceuticals
WO2010120368A2 (en) 2009-04-15 2010-10-21 Lantheus Medical Imaging, Inc. Stabilization of radiopharmaceutical compositions using ascorbic acid
JP2012524064A (ja) * 2009-04-15 2012-10-11 ランセウス メディカル イメージング, インコーポレイテッド アスコルビン酸による放射性医薬組成物の安定化
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EP2119458A4 (en) 2010-03-24
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CA2678020A1 (en) 2008-08-21
EP2119458A1 (en) 2009-11-18
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TW200833362A (en) 2008-08-16
CA2678020C (en) 2015-03-24
CN101636183A (zh) 2010-01-27
JP5258583B2 (ja) 2013-08-07
EP2119458B9 (en) 2013-08-21
US8658132B2 (en) 2014-02-25
US8343459B2 (en) 2013-01-01
US20100119448A1 (en) 2010-05-13
HK1138504A1 (en) 2010-08-27
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CN101636183B (zh) 2014-03-19
TWI406674B (zh) 2013-09-01
US20120301399A1 (en) 2012-11-29

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