WO2009047935A1 - Fine particles - Google Patents

Fine particles Download PDF

Info

Publication number
WO2009047935A1
WO2009047935A1 PCT/JP2008/061140 JP2008061140W WO2009047935A1 WO 2009047935 A1 WO2009047935 A1 WO 2009047935A1 JP 2008061140 W JP2008061140 W JP 2008061140W WO 2009047935 A1 WO2009047935 A1 WO 2009047935A1
Authority
WO
WIPO (PCT)
Prior art keywords
fine particles
salt
given
lungs
amino
Prior art date
Application number
PCT/JP2008/061140
Other languages
French (fr)
Japanese (ja)
Inventor
Hirofumi Takeuchi
Yuichi Tozuka
Yuta Miyazaki
Hikaru Sugihara
Akio Nishiura
Original Assignee
Ono Pharmaceutical Co., Ltd.
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 Ono Pharmaceutical Co., Ltd. filed Critical Ono Pharmaceutical Co., Ltd.
Publication of WO2009047935A1 publication Critical patent/WO2009047935A1/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
    • A61K31/33—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Fine particles which have a high percentage migration to the lungs and are made only of tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate or a salt thereof. Also provided are a process for producing the fine particles and a medicinal preparation comprising the particles for pulmonary inhalation. The fine particles, which have a given percentage migration to the lungs, are produced by spraying a solution of that compound or a salt thereof together with supercritical carbon dioxide in a pressure vessel having a given pressure and a given temperature to prepare a mixture solution, further spraying the mixture solution in water, and recovering the compound or salt from the resultant suspension by freeze drying, etc.
PCT/JP2008/061140 2007-10-12 2008-06-18 Fine particles WO2009047935A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-266871 2007-10-12
JP2007266871 2007-10-12

Publications (1)

Publication Number Publication Date
WO2009047935A1 true WO2009047935A1 (en) 2009-04-16

Family

ID=40549085

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/061140 WO2009047935A1 (en) 2007-10-12 2008-06-18 Fine particles

Country Status (1)

Country Link
WO (1) WO2009047935A1 (en)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01176437A (en) * 1987-12-29 1989-07-12 Ono Pharmaceut Co Ltd Method for rendering organic substance into fine particles
WO1995001221A1 (en) * 1993-07-01 1995-01-12 University Of Bradford Method and apparatus for the formation of particles
WO2000030614A1 (en) * 1998-11-23 2000-06-02 Astrazeneca Ab A process for producing particles with a converted amorphous and/or meta-stable crystalline region into crystalline state
WO2000030613A1 (en) * 1998-11-23 2000-06-02 Astrazeneca Ab New process
WO2005025506A2 (en) * 2003-09-10 2005-03-24 Map Pharmaceuticals, Inc. Aerosol formulations for delivery of dihydroergotamine to the systemic circulation via pulmonary inhalation
WO2006095788A1 (en) * 2005-03-09 2006-09-14 Ono Pharmaceutical Co., Ltd. Particle and preparation containing the particle

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01176437A (en) * 1987-12-29 1989-07-12 Ono Pharmaceut Co Ltd Method for rendering organic substance into fine particles
WO1995001221A1 (en) * 1993-07-01 1995-01-12 University Of Bradford Method and apparatus for the formation of particles
WO2000030614A1 (en) * 1998-11-23 2000-06-02 Astrazeneca Ab A process for producing particles with a converted amorphous and/or meta-stable crystalline region into crystalline state
WO2000030613A1 (en) * 1998-11-23 2000-06-02 Astrazeneca Ab New process
WO2005025506A2 (en) * 2003-09-10 2005-03-24 Map Pharmaceuticals, Inc. Aerosol formulations for delivery of dihydroergotamine to the systemic circulation via pulmonary inhalation
WO2006095788A1 (en) * 2005-03-09 2006-09-14 Ono Pharmaceutical Co., Ltd. Particle and preparation containing the particle

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