PE20080116A1 - Formulaciones farmaceuticas de una forma cristalina de monohidrato de 2-(3-fluor-4-hidroxifenil)-7-vinil-1,3-benzoxazol-5-ol - Google Patents

Formulaciones farmaceuticas de una forma cristalina de monohidrato de 2-(3-fluor-4-hidroxifenil)-7-vinil-1,3-benzoxazol-5-ol

Info

Publication number
PE20080116A1
PE20080116A1 PE2007000231A PE2007000231A PE20080116A1 PE 20080116 A1 PE20080116 A1 PE 20080116A1 PE 2007000231 A PE2007000231 A PE 2007000231A PE 2007000231 A PE2007000231 A PE 2007000231A PE 20080116 A1 PE20080116 A1 PE 20080116A1
Authority
PE
Peru
Prior art keywords
formulation
weight
benzoxazole
fluor
hydroxyphenyl
Prior art date
Application number
PE2007000231A
Other languages
English (en)
Inventor
Mahesh K Krishnan
Mohamed Ghorab
Rolland W Carson
Shamin Hasan
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of PE20080116A1 publication Critical patent/PE20080116A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • 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
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A UN FORMULACION LIQUIDA O SEMISOLIDA QUE COMPRENDE: A) UN PORTADOR SELECCIONADO DE LAUROIL MACROGOL GLICERIDOS, ESTEAROIL MECROGOL GLICERIDOS, POLIETILENGLICOL, ENTRE OTROS QUE COMPRENDE DESDE 10% HASTA 99,99% EN PESO DE DICHA FORMULACION; B) UN SEGUNDO PORTADOR ADICIONAL SELECCIONADO DE CAPRILCAPROIL MACROGOLGLICERIDOS, LINOLEOIL MACROGOL GLICERIDOS, POLIALQUILEN GLICOL, POLIPROPILENGLICOL, ENTRE OTROS QUE COMPRENDE HASTA 70% EN PESO DE DICHA FORMULACION FARMACEUTICA; C) UN COMPONENTE EMULSIONANTE/SOLUBILIZANTE EN UNA CANTIDAD DE 0,01% HASTA 30% EN PESO DE DICHA FORMULACION FARMACEUTICA SELECCIONADO DE ALQUILO METALICO, COMPUESTOS DE AMONIO CUATERNARIO, SALES DE ACIDOS GRASOS, SULFOSUCCINATOS, ENTRE OTROS; D) UN COMPONENTE ANTICRISTALIZACION/SOLUBILIZACION EN UNA CANTIDAD DE 0,01% HASTA 30% SELECCIONADO DE POLIVINILPIRROLIDONA, CAPRILCAPROIL MACROGOLGLICERIDOS, ACEITE DE RICINO POLIETOXILADO, ENTRE OTROS; E) POR LO MENOS 90% EN PESO DE LA FORMA CRISTALINA DE MONOHIDRATO DE 2-(3-FLUOR-4-HIDROXIFENIL)-7-VINIL-1,3-BENZOXAZOL-5-OL. REFERIDA TAMBIEN A UN PROCESO DE PREPARACION. DICHA FORMULACION MINIMIZA LA CONVERSION POLIMORFICA SIENDO UTIL EN EL TRATAMIENTO DE ENFERMEDADES RELACIONADAS CON LA MODULACION DEL RECEPTOR SELECTIVO ESTROGENICO ERBETHA
PE2007000231A 2006-03-06 2007-03-05 Formulaciones farmaceuticas de una forma cristalina de monohidrato de 2-(3-fluor-4-hidroxifenil)-7-vinil-1,3-benzoxazol-5-ol PE20080116A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US77989206P 2006-03-06 2006-03-06

Publications (1)

Publication Number Publication Date
PE20080116A1 true PE20080116A1 (es) 2008-02-25

Family

ID=38475772

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000231A PE20080116A1 (es) 2006-03-06 2007-03-05 Formulaciones farmaceuticas de una forma cristalina de monohidrato de 2-(3-fluor-4-hidroxifenil)-7-vinil-1,3-benzoxazol-5-ol

Country Status (6)

Country Link
US (1) US20070207202A1 (es)
AR (1) AR059743A1 (es)
PA (1) PA8717801A1 (es)
PE (1) PE20080116A1 (es)
TW (1) TW200800178A (es)
WO (1) WO2007103877A2 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080176914A1 (en) * 2006-11-21 2008-07-24 Wyeth Crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080146630A1 (en) * 2006-11-21 2008-06-19 Wyeth Crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080175900A1 (en) * 2006-11-21 2008-07-24 Wyeth Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080132554A1 (en) * 2006-11-21 2008-06-05 Wyeth Crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20090239920A1 (en) * 2006-11-21 2009-09-24 Wyeth Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080241234A1 (en) * 2006-11-21 2008-10-02 Wyeth Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080175901A1 (en) * 2006-11-21 2008-07-24 Wyeth Pharmaceutical formulations of a crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080139633A1 (en) * 2006-11-21 2008-06-12 Wyeth Crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3437599A1 (de) * 1984-10-13 1986-04-17 Dolorgiet GmbH & Co KG, 5205 St Augustin Ibuprofen enthaltende weichgelatinekapseln und verfahren zu ihrer herstellung
US5468502A (en) * 1994-12-20 1995-11-21 American Home Products Corporation Ibuprofen enhancing solvent system
UA83620C2 (ru) * 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
JP2008521921A (ja) * 2004-12-02 2008-06-26 ワイス 置換ベンゾオキサゾールの製剤
US20060121110A1 (en) * 2004-12-02 2006-06-08 Wyeth Formulations of substituted benzoxazoles
WO2006060384A2 (en) * 2004-12-02 2006-06-08 Wyeth Formulations of substituted benzoxazoles
BRPI0608689A2 (pt) * 2005-03-08 2010-01-19 Wyeth Corp composto, composiÇço, processos para preparar monoidrato e a forma de cristal, e, uso de um monoidrato ou de uma forma de cristal
TW200800177A (en) * 2006-02-14 2008-01-01 Wyeth Corp Aqueous pharmaceutical formulations of ERβ selective ligands

Also Published As

Publication number Publication date
US20070207202A1 (en) 2007-09-06
TW200800178A (en) 2008-01-01
WO2007103877A2 (en) 2007-09-13
PA8717801A1 (es) 2009-04-23
AR059743A1 (es) 2008-04-23
WO2007103877A3 (en) 2007-11-22

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