WO2003099290A1 - Produits pharmaceutiques et leurs procedes de fabrication - Google Patents

Produits pharmaceutiques et leurs procedes de fabrication Download PDF

Info

Publication number
WO2003099290A1
WO2003099290A1 PCT/US2003/015690 US0315690W WO03099290A1 WO 2003099290 A1 WO2003099290 A1 WO 2003099290A1 US 0315690 W US0315690 W US 0315690W WO 03099290 A1 WO03099290 A1 WO 03099290A1
Authority
WO
WIPO (PCT)
Prior art keywords
medicament
substance
excipient
particles
solution
Prior art date
Application number
PCT/US2003/015690
Other languages
English (en)
Inventor
Andrew Bruce Brown
Matthew Skelly FERRITER
Michiel Mary Van Oort
Original Assignee
Glaxo Group Limited
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 Glaxo Group Limited filed Critical Glaxo Group Limited
Priority to AU2003251303A priority Critical patent/AU2003251303A1/en
Publication of WO2003099290A1 publication Critical patent/WO2003099290A1/fr

Links

Classifications

    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules

Definitions

  • FIGURE 2 is a graphical illustration of the effects of spray-drying temperature and % menthol on crystallization exotherms of fluticasone propionate particles formed in accordance with the invention
  • “Pharmaceutical particles” mean particles which themselves contain at least one medicament. Pharmaceutical particles may also comprise additional components, such as as excipients or additional medicaments.
  • the inhalable particles formed in accordance with the invention are substantially crystalline.
  • the particles have an aerodynamic diameter ⁇ 10 ⁇ m and, most preferably, an aerodynamic diameter suitable for targeted delivery in the lung.
  • particles intended for treatment of local conditions are in the range of approximately 2 - 5 ⁇ m.
  • the particles intended for systemic delivery of therapeutics are preferably in the range of approximately 1 to 2 ⁇ m.
  • Salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate and physiologically acceptable salts and solvates thereof are especially preferred.
  • Most preferred medicaments are fluticasone propionate, salmeterol xinafoate, salbutamol sulphate and ipratropium bromide.
  • a further aspect of the present invention comprises pharmaceutical compositions, including particulate medicament particles formed in accordance with the present invention (i.e., neat drugs).
  • the noted compositions can similarly optionally include at least one pharmaceutically acceptable diluent or excipient.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne un procédé de production de particules pharmaceutiques comprenant une première substance cristalline, qui consiste à : disposer une première substance à proximité d'au moins un agent d'induction de cristallisation sublimable, pendant une période suffisante pour induire la cristallisation ; et à récolter les particules cristallines résultantes.
PCT/US2003/015690 2002-05-21 2003-05-20 Produits pharmaceutiques et leurs procedes de fabrication WO2003099290A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003251303A AU2003251303A1 (en) 2002-05-21 2003-05-20 Pharmaceutical products and methods of manufacture

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38223302P 2002-05-21 2002-05-21
US60/382,233 2002-05-21

Publications (1)

Publication Number Publication Date
WO2003099290A1 true WO2003099290A1 (fr) 2003-12-04

Family

ID=29584380

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/015690 WO2003099290A1 (fr) 2002-05-21 2003-05-20 Produits pharmaceutiques et leurs procedes de fabrication

Country Status (2)

Country Link
AU (1) AU2003251303A1 (fr)
WO (1) WO2003099290A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7737126B2 (en) 2004-05-24 2010-06-15 Glaxo Group Limited Purine derivative
US7985740B2 (en) 2005-07-19 2011-07-26 Glaxo Group Limited Purine derivatives as agonists of the adenosine A2A receptor
WO2016067132A1 (fr) * 2014-10-31 2016-05-06 Bend Research Inc. Procédé de formation de domaines actifs dispersés dans une matrice
US9815865B2 (en) 2013-01-07 2017-11-14 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US9822142B2 (en) 2012-05-08 2017-11-21 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US10174071B2 (en) 2012-05-08 2019-01-08 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US10675602B2 (en) 2009-03-27 2020-06-09 Bend Research, Inc. Spray-drying process

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991013646A1 (fr) * 1990-03-07 1991-09-19 Fisons Plc Dispositif d'inhalation de medicaments
US6150418A (en) * 1998-10-17 2000-11-21 Boehringer Ingelheim Pharma Kg Active substance concentrate with formoterol, suitable for storage

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991013646A1 (fr) * 1990-03-07 1991-09-19 Fisons Plc Dispositif d'inhalation de medicaments
US6150418A (en) * 1998-10-17 2000-11-21 Boehringer Ingelheim Pharma Kg Active substance concentrate with formoterol, suitable for storage

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"Physician's Desk Reference", 1997, article ARKY ET AL.: "Product Information", pages: 1089 - 1092 *
"Remington: The Science and Practice of Pharmacy", 1995, article SCIARRA J.J.: "Aerosols", pages: 1676 - 1692 *
ARKY ET AL.: "Pulmicort turbuhalere 200 mcg (AstraZeneca LP) (budesonide inhalation powder) for oral inhalation only", ELECTRONIC PHYSICIAN'S DESK REFE, 2001, XP002971649, Retrieved from the Internet <URL:pdrel.thomsonhc.com> *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7737126B2 (en) 2004-05-24 2010-06-15 Glaxo Group Limited Purine derivative
US7985740B2 (en) 2005-07-19 2011-07-26 Glaxo Group Limited Purine derivatives as agonists of the adenosine A2A receptor
US10675602B2 (en) 2009-03-27 2020-06-09 Bend Research, Inc. Spray-drying process
US9822142B2 (en) 2012-05-08 2017-11-21 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US10174071B2 (en) 2012-05-08 2019-01-08 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US10954263B2 (en) 2012-05-08 2021-03-23 Nicox Ophthalmics, Inc Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US11814408B2 (en) 2012-05-08 2023-11-14 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US9815865B2 (en) 2013-01-07 2017-11-14 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
WO2016067132A1 (fr) * 2014-10-31 2016-05-06 Bend Research Inc. Procédé de formation de domaines actifs dispersés dans une matrice
US11364203B2 (en) 2014-10-31 2022-06-21 Bend Reserch, Inc. Process for forming active domains dispersed in a matrix

Also Published As

Publication number Publication date
AU2003251303A1 (en) 2003-12-12

Similar Documents

Publication Publication Date Title
US8337816B2 (en) Dry powder medicament formulations
JP5936353B2 (ja) フルチカゾン粒子の結晶化度を改善する方法
EP2490779B1 (fr) Procédé d&#39;amélioration de la cristallinité
US20060057213A1 (en) Drug delivery particles and methods of treating particles to improve their drug delivery capabilities
WO2003028653A2 (fr) Compositions pharmaceutiques a liberation prolongee
SK5697A3 (en) Inhalation composition
JP2004500984A (ja) 結晶粒子の新規な製造および回収方法
WO2011069197A1 (fr) Formulations inhalables
US20040062719A1 (en) Particulate inhalation carrier
EP1684711A2 (fr) Composition
WO2003099290A1 (fr) Produits pharmaceutiques et leurs procedes de fabrication
CA2630772A1 (fr) Poudres respirables
EP1494644A1 (fr) Compositions sous forme de poudre seche
WO2005041922A2 (fr) Composition
Shetty Effect of Storage Humidity on Physical Stability and Aerosol Performance of Spray-Dried Dry Powder Inhaler Formulations
WO2008134817A1 (fr) Vecteurs composites pour thérapie par inhalation de poudre sèche
WO2003053406A1 (fr) Particules fluorees pour inhalation et formulation pharmaceutique

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP