WO2002049620A3 - Induced phase transition method for the production of microparticles containing hydrophobic active agents - Google Patents

Induced phase transition method for the production of microparticles containing hydrophobic active agents Download PDF

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Publication number
WO2002049620A3
WO2002049620A3 PCT/US2001/050259 US0150259W WO0249620A3 WO 2002049620 A3 WO2002049620 A3 WO 2002049620A3 US 0150259 W US0150259 W US 0150259W WO 0249620 A3 WO0249620 A3 WO 0249620A3
Authority
WO
WIPO (PCT)
Prior art keywords
production
active agents
phase transition
microparticles containing
induced phase
Prior art date
Application number
PCT/US2001/050259
Other languages
French (fr)
Other versions
WO2002049620A2 (en
Inventor
Celal Albayrak
Original Assignee
Inhale Therapeutic Syst
Celal Albayrak
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
Family has litigation
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Application filed by Inhale Therapeutic Syst, Celal Albayrak filed Critical Inhale Therapeutic Syst
Priority to EP01992358.0A priority Critical patent/EP1343480B2/en
Priority to AU2002232824A priority patent/AU2002232824A1/en
Priority to CA002432904A priority patent/CA2432904C/en
Priority to DE60128261.2T priority patent/DE60128261T3/en
Priority to JP2002550962A priority patent/JP2004516263A/en
Priority to ES01992358.0T priority patent/ES2286157T5/en
Priority to DK01992358.0T priority patent/DK1343480T4/en
Publication of WO2002049620A2 publication Critical patent/WO2002049620A2/en
Publication of WO2002049620A3 publication Critical patent/WO2002049620A3/en

Links

Classifications

    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)

Abstract

Microparticles and a method for their production is described. The process of the present invention provides a simple, quick, and efficient one-pot process for the production of microparticles containing a non-water soluble active agent. The microparticles are preferably used for pharmaceutical applications and comprise at least 80 wt% microspheres.
PCT/US2001/050259 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophobic active agents WO2002049620A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
EP01992358.0A EP1343480B2 (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophobic active agents
AU2002232824A AU2002232824A1 (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophobic active agents
CA002432904A CA2432904C (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophobic active agents
DE60128261.2T DE60128261T3 (en) 2000-12-21 2001-12-19 METHODS COMPRISING INDUCED PHASE TRANSFER TO PREPARE MICROPARTICLES CONTAINING HYDROPHOBIC ACTIVE SUBSTANCES
JP2002550962A JP2004516263A (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophobic activators
ES01992358.0T ES2286157T5 (en) 2000-12-21 2001-12-19 Induced phase transition procedure for the production of microparticles containing hydrophobic active agents
DK01992358.0T DK1343480T4 (en) 2000-12-21 2001-12-19 Induced phase transition method for the preparation of microparticles containing hydrophobic active agents.

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US25752700P 2000-12-21 2000-12-21
US60/257,527 2000-12-21
US30002101P 2001-06-21 2001-06-21
US60/300,021 2001-06-21

Publications (2)

Publication Number Publication Date
WO2002049620A2 WO2002049620A2 (en) 2002-06-27
WO2002049620A3 true WO2002049620A3 (en) 2003-05-15

Family

ID=26946029

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2001/050259 WO2002049620A2 (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophobic active agents
PCT/US2001/050105 WO2002049619A2 (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophilic active agents

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2001/050105 WO2002049619A2 (en) 2000-12-21 2001-12-19 Induced phase transition method for the production of microparticles containing hydrophilic active agents

Country Status (10)

Country Link
US (2) US7252842B2 (en)
EP (2) EP1343480B2 (en)
JP (2) JP2004516263A (en)
AT (2) ATE361057T1 (en)
AU (3) AU2002232824A1 (en)
CA (2) CA2432904C (en)
DE (2) DE60130917T2 (en)
DK (1) DK1343480T4 (en)
ES (2) ES2292634T3 (en)
WO (2) WO2002049620A2 (en)

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