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WO2008143239A1 - 結晶性微粉化粒子 - Google Patents

結晶性微粉化粒子 Download PDF

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Publication number
WO2008143239A1
WO2008143239A1 PCT/JP2008/059194 JP2008059194W WO2008143239A1 WO 2008143239 A1 WO2008143239 A1 WO 2008143239A1 JP 2008059194 W JP2008059194 W JP 2008059194W WO 2008143239 A1 WO2008143239 A1 WO 2008143239A1
Authority
WO
WIPO (PCT)
Prior art keywords
particle diameter
crystalline particles
crystalline
cumulative frequency
volume distribution
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/JP2008/059194
Other languages
English (en)
French (fr)
Inventor
Masahiro Akimoto
Toshikazu Komagata
Motohiro Shiraki
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.)
Toray Industries Inc
Original Assignee
Toray Industries Inc
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.)
Filing date
Publication date
Application filed by Toray Industries Inc filed Critical Toray Industries Inc
Priority to US12/601,150 priority Critical patent/US8198446B2/en
Priority to CA2687955A priority patent/CA2687955C/en
Priority to ES08752990.5T priority patent/ES2627217T3/es
Priority to CN2008800255821A priority patent/CN101965187B/zh
Priority to JP2009515238A priority patent/JP5564943B2/ja
Priority to EP08752990.5A priority patent/EP2156837B1/en
Priority to AU2008254037A priority patent/AU2008254037B2/en
Priority to KR1020097024379A priority patent/KR101546398B1/ko
Publication of WO2008143239A1 publication Critical patent/WO2008143239A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K9/1682—Processes
    • A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
    • 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
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

N-(17-シクロプロピルメチル-4,5α-エポキシ-3,14-ジヒドロキシ-モルヒナン-6β-イル)-フタルイミド又はその薬剤的に許容される塩の結晶性粒子が開示されている。該結晶性粒子は、粒子径が小さい方の粒子から累積して体積分布の累積頻度が50%に達する点の粒子径（D50）が1～30μmの範囲内であり、粒子径が小さい方の粒子から累積して体積分布の累積頻度が90%に達する点の粒子径（D90）が90μm以下の粒子径分布をもち、結晶化度が80%以上である。該結晶性粒子によれば、該化合物の保存安定性を確保しつつ、原薬の生物学的利用能を高めることができる。
PCT/JP2008/059194 2007-05-21 2008-05-20 結晶性微粉化粒子 Ceased WO2008143239A1 (ja)

Priority Applications (8)

Application Number Priority Date Filing Date Title
US12/601,150 US8198446B2 (en) 2007-05-21 2008-05-20 Crystalline micropowder particles
CA2687955A CA2687955C (en) 2007-05-21 2008-05-20 Crystalline micropowder particles
ES08752990.5T ES2627217T3 (es) 2007-05-21 2008-05-20 Partículas micropulverizadas cristalinas
CN2008800255821A CN101965187B (zh) 2007-05-21 2008-05-20 结晶性微粉化粒子
JP2009515238A JP5564943B2 (ja) 2007-05-21 2008-05-20 結晶性微粉化粒子
EP08752990.5A EP2156837B1 (en) 2007-05-21 2008-05-20 Crystalline micropowder particles
AU2008254037A AU2008254037B2 (en) 2007-05-21 2008-05-20 Crystalline micropowder particles
KR1020097024379A KR101546398B1 (ko) 2007-05-21 2008-05-20 결정성 미분화 입자

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-133691 2007-05-21
JP2007133691 2007-05-21

Publications (1)

Publication Number Publication Date
WO2008143239A1 true WO2008143239A1 (ja) 2008-11-27

Family

ID=40031936

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/059194 Ceased WO2008143239A1 (ja) 2007-05-21 2008-05-20 結晶性微粉化粒子

Country Status (9)

Country Link
US (1) US8198446B2 (ja)
EP (1) EP2156837B1 (ja)
JP (1) JP5564943B2 (ja)
KR (1) KR101546398B1 (ja)
CN (1) CN101965187B (ja)
AU (1) AU2008254037B2 (ja)
CA (1) CA2687955C (ja)
ES (1) ES2627217T3 (ja)
WO (1) WO2008143239A1 (ja)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013119527A (ja) * 2011-12-07 2013-06-17 Tokuyama Corp 溶解性および安定性の向上した難溶性医薬品原体及びその製造方法
JP2016106139A (ja) * 2016-03-07 2016-06-16 株式会社トクヤマ 溶解性および安定性の向上した難溶性医薬品原体及びその製造方法
JP2017081983A (ja) * 2009-04-24 2017-05-18 イシューティカ ピーティーワイ リミテッド 商業的規模での封入ナノ粒子の製造
JP2022003029A (ja) * 2020-06-23 2022-01-11 東和薬品株式会社 ゾニサミド原薬粒子およびその用途
JP7669325B2 (ja) 2022-05-10 2025-04-28 北京遠大九和薬業有限公司 化合物及びフマル酸の結晶形態、医薬組成物及びコロナウイルス誘発性疾患の治療方法

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114105839B (zh) * 2020-08-27 2025-02-14 湖北舒邦药业有限公司 一种原料药的前处理方法及其组合物
CN115887234B (zh) * 2021-09-30 2025-08-01 黄冈美丰化工科技有限公司 2-(4-n,n-二乙基氨基-2-羟基苯甲酰基)苯甲酸正己基酯粒子及其制备方法
JP2024071268A (ja) * 2022-11-14 2024-05-24 株式会社リガク 結晶化度測定装置、結晶化度測定方法及びプログラム

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004033457A1 (ja) 2002-10-09 2004-04-22 Toray Industries, Inc. 頻尿もしくは尿失禁の治療または予防剤および含窒素環状置換基を有するモルヒナン誘導体
WO2005094826A1 (ja) 2004-03-30 2005-10-13 Toray Industries, Inc. 止痒剤
WO2006049248A1 (ja) 2004-11-04 2006-05-11 Toray Industries, Inc. 鎮痛剤
WO2007055184A1 (ja) 2005-11-09 2007-05-18 Toray Industries, Inc. 機能性腸障害の治療または予防剤
WO2007072749A1 (ja) 2005-12-21 2007-06-28 Toray Industries, Inc. 鎮咳剤

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000000492A1 (en) * 1998-06-26 2000-01-06 Chugai Seiyaku Kabushiki Kaisha FINE POWDER OF L-α-AMINOADIPIC ACID DERIVATIVE, ORAL SOLID PREPARATIONS CONTAINING THE SAME, AND METHOD FOR TREATMENT OF BULK POWDERS
IL154457A0 (en) * 2000-08-14 2003-09-17 Teva Pharma Mircronized torsemide
JP3939601B2 (ja) * 2001-06-20 2007-07-04 株式会社アクティバスファーマ キノリノン誘導体医薬組成物及びその製造方法
BRPI0408403A (pt) * 2003-03-21 2006-03-21 Dsm Ip Assets Bv pó cristalino de triidrato de amoxicilina

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004033457A1 (ja) 2002-10-09 2004-04-22 Toray Industries, Inc. 頻尿もしくは尿失禁の治療または予防剤および含窒素環状置換基を有するモルヒナン誘導体
WO2005094826A1 (ja) 2004-03-30 2005-10-13 Toray Industries, Inc. 止痒剤
WO2006049248A1 (ja) 2004-11-04 2006-05-11 Toray Industries, Inc. 鎮痛剤
WO2007055184A1 (ja) 2005-11-09 2007-05-18 Toray Industries, Inc. 機能性腸障害の治療または予防剤
WO2007072749A1 (ja) 2005-12-21 2007-06-28 Toray Industries, Inc. 鎮咳剤

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SAGAWA Y.: "Iyakuhin Seizai Gijutsu", CMC PUBLISHING CO., LTD., 25 July 2002 (2002-07-25), pages 5 - 10, 25 - 34, XP008118275 *
SIMON C., TETRAHEDRON, vol. 50, 1994, pages 9757

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017081983A (ja) * 2009-04-24 2017-05-18 イシューティカ ピーティーワイ リミテッド 商業的規模での封入ナノ粒子の製造
JP2013119527A (ja) * 2011-12-07 2013-06-17 Tokuyama Corp 溶解性および安定性の向上した難溶性医薬品原体及びその製造方法
JP2016106139A (ja) * 2016-03-07 2016-06-16 株式会社トクヤマ 溶解性および安定性の向上した難溶性医薬品原体及びその製造方法
JP2022003029A (ja) * 2020-06-23 2022-01-11 東和薬品株式会社 ゾニサミド原薬粒子およびその用途
JP7745371B2 (ja) 2020-06-23 2025-09-29 東和薬品株式会社 ゾニサミド原薬粒子およびその用途
JP7669325B2 (ja) 2022-05-10 2025-04-28 北京遠大九和薬業有限公司 化合物及びフマル酸の結晶形態、医薬組成物及びコロナウイルス誘発性疾患の治療方法

Also Published As

Publication number Publication date
JP5564943B2 (ja) 2014-08-06
EP2156837A4 (en) 2012-12-05
EP2156837A1 (en) 2010-02-24
AU2008254037B2 (en) 2013-10-17
US8198446B2 (en) 2012-06-12
KR20100056424A (ko) 2010-05-27
JPWO2008143239A1 (ja) 2010-08-12
ES2627217T3 (es) 2017-07-27
CN101965187B (zh) 2012-11-21
CA2687955A1 (en) 2008-11-27
KR101546398B1 (ko) 2015-08-26
CA2687955C (en) 2015-06-30
AU2008254037A1 (en) 2008-11-27
EP2156837B1 (en) 2017-04-26
US20100160634A1 (en) 2010-06-24
CN101965187A (zh) 2011-02-02

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