CN105308101B - 具有s形释放曲线的聚丙交酯-聚乙交酯微粒的制备 - Google Patents

具有s形释放曲线的聚丙交酯-聚乙交酯微粒的制备 Download PDF

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Publication number
CN105308101B
CN105308101B CN201480034979.2A CN201480034979A CN105308101B CN 105308101 B CN105308101 B CN 105308101B CN 201480034979 A CN201480034979 A CN 201480034979A CN 105308101 B CN105308101 B CN 105308101B
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phase
particle
risperidone
polymer
organic solvent
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CN105308101A (zh
Inventor
E·卡拉瓦斯
E·科特里斯
S·海蒂都尔
T·曼特尔丽萨
G·帕帕尼古拉乌
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Pharmathen SA
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Pharmathen SA
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J13/00Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
    • B01J13/02Making microcapsules or microballoons
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08JWORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
    • C08J3/00Processes of treating or compounding macromolecular substances
    • C08J3/12Powdering or granulating
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08JWORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
    • C08J3/00Processes of treating or compounding macromolecular substances
    • C08J3/12Powdering or granulating
    • C08J3/14Powdering or granulating by precipitation from solutions
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08JWORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
    • C08J2300/00Characterised by the use of unspecified polymers
    • C08J2300/16Biodegradable polymers
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08JWORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
    • C08J2367/00Characterised by the use of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Derivatives of such polymers
    • C08J2367/04Polyesters derived from hydroxy carboxylic acids, e.g. lactones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN201480034979.2A 2013-06-20 2014-06-18 具有s形释放曲线的聚丙交酯-聚乙交酯微粒的制备 Active CN105308101B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EPPCT/EP2013/001821 2013-06-20
EP2013001821 2013-06-20
PCT/EP2014/001652 WO2014202214A1 (en) 2013-06-20 2014-06-18 Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile

Publications (2)

Publication Number Publication Date
CN105308101A CN105308101A (zh) 2016-02-03
CN105308101B true CN105308101B (zh) 2018-10-23

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US (1) US9943484B2 (enExample)
JP (1) JP6464154B2 (enExample)
CN (1) CN105308101B (enExample)
AU (1) AU2014283692B2 (enExample)
CA (1) CA2916301C (enExample)
DK (1) DK3010962T4 (enExample)
ES (1) ES2640486T5 (enExample)
FI (1) FI3010962T4 (enExample)
HU (1) HUE036141T2 (enExample)
LT (1) LT3010962T (enExample)
PT (1) PT3010962T (enExample)
RU (1) RU2658004C2 (enExample)
SA (1) SA515370296B1 (enExample)
WO (1) WO2014202214A1 (enExample)
ZA (1) ZA201509354B (enExample)

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ES2774359T3 (es) 2014-07-30 2020-07-20 Merck Patent Gmbh Composición que puede comprimirse directamente que contiene celulosa microcristalina
JP2016102093A (ja) * 2014-11-28 2016-06-02 ニプロ株式会社 塩基性の求核化合物を含有するマイクロカプセルの製造方法
ES2960753T3 (es) 2015-09-21 2024-03-06 Teva Pharmaceuticals Int Gmbh Formulaciones de olanzapina de liberación sostenida
JP2020511483A (ja) 2017-03-20 2020-04-16 テバ・ファーマシューティカルズ・インターナショナル・ゲーエムベーハーTeva Pharmaceuticals International GmbH 徐放性オランザピン製剤
KR102047983B1 (ko) * 2017-11-30 2019-11-22 주식회사 지투지바이오 안전성 및 저장 안정성이 향상된 생분해성 미립구의 제조방법
GR1009870B (el) * 2019-07-09 2020-11-12 Φαρματεν Α.Β.Ε.Ε. Φαρμακευτικο σκευασμα που περιλαμβανει ενα ατυπο αντιψυχωσικο φαρμακο και μεθοδος παρασκευης αυτου
JP7550474B2 (ja) * 2019-12-31 2024-09-13 広州帝奇医薬技術有限公司 第3級アミン医薬組成物の工業化バッチ調製方法
EP4125823A1 (en) 2020-03-30 2023-02-08 Biological E Limited Risperidone microspheres, process for their prepartion and uses thereof
KR102259589B1 (ko) * 2020-11-30 2021-06-02 (주)인벤티지랩 미소구체 제조 시스템 및 미소구체 제조 방법
EP4277661A1 (en) 2021-01-18 2023-11-22 Anton Frenkel Pharmaceutical dosage form
KR20230157365A (ko) * 2021-02-24 2023-11-16 오크우드 레버러토리즈, 엘엘씨 루라시돈을 포함하는 마이크로스피어 제제 및 이의 제조 및 사용 방법
CN118284414A (zh) 2021-07-06 2024-07-02 M·哈斯莱顿 血清素再摄取抑制剂戒断综合征的治疗
GR1010327B (el) * 2021-10-06 2022-10-17 Φαρματεν Α.Β.Ε.Ε., Παρατεταμενης αποδεσμευσης ενεσιμο φαρμακευτικο σκευασμα λεβοθυροξινης και μεθοδος παρασκευης αυτου
WO2025135778A1 (ko) * 2023-12-18 2025-06-26 주식회사 포스테라헬스사이언스 약물의 특성에 따른 활성형 미립자의 제조 방법, 이의 제조 방법으로 제조된 활성형 미립자 및 상기 활성형 미립자를 이용한 약물을 포함하는 장기 지속 제형의 제조 방법
WO2025207396A1 (en) * 2024-03-27 2025-10-02 Avidence Therapeutics, Inc. Microsphere-based injectable rofecoxib formulation

Citations (2)

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Publication number Priority date Publication date Assignee Title
CN1226821A (zh) * 1996-05-07 1999-08-25 阿尔克迈斯控制医疗第二公司 微颗粒
WO2000040221A1 (en) * 1998-12-30 2000-07-13 Alkermes Controlled Therapeutics Inc. Ii Preparation of microparticles having a selected release profile

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US5478564A (en) * 1990-02-22 1995-12-26 Teva Pharmaceutical Industries, Ltd. Preparation of microparticles for controlled release of water-soluble substances
US5288496A (en) 1990-05-15 1994-02-22 Stolle Research & Development Corporation Growth promoters for animals
BR9607752B1 (pt) * 1996-01-24 2009-05-05 formulação farmacêutica de microcápsula de liberação controlada.
US6264987B1 (en) 2000-05-19 2001-07-24 Alkermes Controlled Therapeutics Inc. Ii Method for preparing microparticles having a selected polymer molecular weight
US7690026B2 (en) * 2005-08-22 2010-03-30 Microsoft Corporation Distributed single sign-on service

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
CN1226821A (zh) * 1996-05-07 1999-08-25 阿尔克迈斯控制医疗第二公司 微颗粒
WO2000040221A1 (en) * 1998-12-30 2000-07-13 Alkermes Controlled Therapeutics Inc. Ii Preparation of microparticles having a selected release profile

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Publication number Publication date
RU2658004C2 (ru) 2018-06-19
RU2016101418A (ru) 2017-07-25
HUE036141T2 (hu) 2018-06-28
AU2014283692B2 (en) 2017-04-27
SA515370296B1 (ar) 2017-10-12
ES2640486T3 (es) 2017-11-03
US20160143851A1 (en) 2016-05-26
JP6464154B2 (ja) 2019-02-06
CA2916301C (en) 2020-01-07
DK3010962T3 (en) 2017-10-23
FI3010962T4 (fi) 2023-05-04
WO2014202214A1 (en) 2014-12-24
ES2640486T5 (es) 2023-04-28
US9943484B2 (en) 2018-04-17
JP2017507895A (ja) 2017-03-23
PT3010962T (pt) 2017-09-05
CN105308101A (zh) 2016-02-03
AU2014283692A1 (en) 2016-01-21
DK3010962T4 (da) 2023-04-17
CA2916301A1 (en) 2014-12-24
ZA201509354B (en) 2017-07-26
LT3010962T (lt) 2017-09-25

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