JP6338573B2 - 多形体組成物、その製造方法及びその使用 - Google Patents

多形体組成物、その製造方法及びその使用 Download PDF

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Publication number
JP6338573B2
JP6338573B2 JP2015511680A JP2015511680A JP6338573B2 JP 6338573 B2 JP6338573 B2 JP 6338573B2 JP 2015511680 A JP2015511680 A JP 2015511680A JP 2015511680 A JP2015511680 A JP 2015511680A JP 6338573 B2 JP6338573 B2 JP 6338573B2
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Prior art keywords
nimodipine
polymer
range
formulation
release
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JP2015522534A5 (https=
JP2015522534A (ja
Inventor
アール ロッホ マクドナルド
アール ロッホ マクドナルド
カーラ アール ディヴィス
カーラ アール ディヴィス
ケヴィン バートン
ケヴィン バートン
ゲイリー ウィンチェスター
ゲイリー ウィンチェスター
アンジェラ アール ステラ
アンジェラ アール ステラ
パリッサ ヘシュマティ
パリッサ ヘシュマティ
Original Assignee
エッジ セラピューティクス インコーポレイテッド
エッジ セラピューティクス インコーポレイテッド
エヴォニック コーポレイション
エヴォニック コーポレイション
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Publication of JP2015522534A5 publication Critical patent/JP2015522534A5/ja
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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
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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 macromolecular compounds
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015511680A 2012-05-09 2013-05-09 多形体組成物、その製造方法及びその使用 Expired - Fee Related JP6338573B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261644523P 2012-05-09 2012-05-09
US61/644,523 2012-05-09
US13/800,480 US9399019B2 (en) 2012-05-09 2013-03-13 Polymorph compositions, methods of making, and uses thereof
US13/800,480 2013-03-13
PCT/US2013/040265 WO2013169979A2 (en) 2012-05-09 2013-05-09 Polymorph compositions, methods of making, and uses thereof

Publications (3)

Publication Number Publication Date
JP2015522534A JP2015522534A (ja) 2015-08-06
JP2015522534A5 JP2015522534A5 (https=) 2016-04-21
JP6338573B2 true JP6338573B2 (ja) 2018-06-06

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JP2015511680A Expired - Fee Related JP6338573B2 (ja) 2012-05-09 2013-05-09 多形体組成物、その製造方法及びその使用

Country Status (15)

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US (2) US9399019B2 (https=)
EP (1) EP2846775A4 (https=)
JP (1) JP6338573B2 (https=)
KR (1) KR101784260B1 (https=)
CN (1) CN104955445A (https=)
AU (1) AU2013259476B2 (https=)
BR (1) BR112014027965A2 (https=)
CA (2) CA2872887C (https=)
GB (1) GB2517096A (https=)
HK (2) HK1202264A1 (https=)
IL (1) IL235262A0 (https=)
NZ (1) NZ629727A (https=)
RU (1) RU2014149362A (https=)
SG (1) SG11201407266PA (https=)
WO (1) WO2013169979A2 (https=)

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CN107921036A (zh) * 2015-05-29 2018-04-17 优势医疗公司 用于减少视力丧失的组合物和方法
US20190054022A1 (en) * 2016-04-07 2019-02-21 Edge Therapeutics, Inc. Formulations of site-specific, microparticulate compositions and their use to improve outcome after aneursymal subarachnoid hemorrhage
CN105944152B (zh) * 2016-06-13 2019-02-12 龙岩紫荆创新研究院 可吸收防粘医用膜的制备方法
WO2018039039A1 (en) * 2016-08-23 2018-03-01 Edge Therapeutics, Inc. Scalable microparticulate formulations containing polymorphic nimodipine form 2 prepared by a solvent evaporation process
WO2019018306A1 (en) * 2017-07-17 2019-01-24 Edge Therapeutics, Inc. ADVANCED MICROPARTICULAR FORMULATIONS CONTAINING FORM 2 OF MICRONIZED POLYMORPHIC NIMODIPINE
CN112912066B (zh) * 2018-09-08 2022-03-29 江苏九旭药业有限公司 一种尼莫地平注射液组合物及其制备方法
US12281226B2 (en) 2018-10-04 2025-04-22 Organo Plastica Polyvinyl chloride-free lipophilic polymer based aromatized plastisol
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Publication number Publication date
HK1202264A1 (en) 2015-09-25
AU2013259476A1 (en) 2014-10-30
JP2015522534A (ja) 2015-08-06
GB201418703D0 (en) 2014-12-03
US8821944B1 (en) 2014-09-02
GB2517096A (en) 2015-02-11
AU2013259476B2 (en) 2016-10-06
NZ629727A (en) 2016-06-24
IL235262A0 (en) 2014-12-31
CA2872887C (en) 2017-08-22
EP2846775A2 (en) 2015-03-18
SG11201407266PA (en) 2014-12-30
CN104955445A (zh) 2015-09-30
US9399019B2 (en) 2016-07-26
BR112014027965A2 (pt) 2017-06-27
WO2013169979A3 (en) 2015-06-18
KR101784260B1 (ko) 2017-11-06
RU2014149362A (ru) 2016-06-27
HK1207824A1 (en) 2016-02-12
CA2872887A1 (en) 2013-11-14
KR20150021517A (ko) 2015-03-02
WO2013169979A9 (en) 2015-01-08
US20130302431A1 (en) 2013-11-14
CA2961123A1 (en) 2013-11-14
WO2013169979A2 (en) 2013-11-14
EP2846775A4 (en) 2016-04-13
US20140271895A1 (en) 2014-09-18

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