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WO2012107765A3 - Particle formulation - Google Patents

Particle formulation Download PDF

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Publication number
WO2012107765A3
WO2012107765A3 PCT/GB2012/050283 GB2012050283W WO2012107765A3 WO 2012107765 A3 WO2012107765 A3 WO 2012107765A3 GB 2012050283 W GB2012050283 W GB 2012050283W WO 2012107765 A3 WO2012107765 A3 WO 2012107765A3
Authority
WO
WIPO (PCT)
Prior art keywords
pharmacologically active
active ingredients
particle
particle formulations
formulation
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/GB2012/050283
Other languages
French (fr)
Other versions
WO2012107765A2 (en
Inventor
Mark Henry SAUNDERS
Marcel De Matas
Jason Robert Jones
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LENA NANOCEUTICS Ltd
Kuecept Ltd
Original Assignee
LENA NANOCEUTICS Ltd
Kuecept 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 LENA NANOCEUTICS Ltd, Kuecept Ltd filed Critical LENA NANOCEUTICS Ltd
Publication of WO2012107765A2 publication Critical patent/WO2012107765A2/en
Publication of WO2012107765A3 publication Critical patent/WO2012107765A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • A61K9/14—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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0012—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
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • 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
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin

Landscapes

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

Abstract

The present inventions relates to combination particle formulations suitable for use in an inhaler formulation comprising a plurality of pharmacologically active ingredients characterized in that the pharmacologically active ingredients are crystalline. The present invention further comprises a particle formulation suitable for use in an inhalation formulation comprising a plurality of pharmacologically active ingredients, for example crystalline pharmacologically active ingredients characterized in that the ratio of the pharmacologically active substances has a distribution of less than ±5% of the target ratio as measured by Impactor testing. Particularly particle formulations prepared from nanoparticles, for example by spray drying of an aqueous suspension of nanoparticles. The invention further comprises methods for making said particle formulations and method of using said particle formulations in therapeutic treatments to achieve co-localisation of agents in the body, particularly when delivered as inhaled formulations to the human airways and lungs.
PCT/GB2012/050283 2011-02-09 2012-02-09 Particle formulation Ceased WO2012107765A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB1102237.3 2011-02-09
GBGB1102237.3A GB201102237D0 (en) 2011-02-09 2011-02-09 Particle formulation

Publications (2)

Publication Number Publication Date
WO2012107765A2 WO2012107765A2 (en) 2012-08-16
WO2012107765A3 true WO2012107765A3 (en) 2012-11-15

Family

ID=43836446

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2012/050283 Ceased WO2012107765A2 (en) 2011-02-09 2012-02-09 Particle formulation

Country Status (2)

Country Link
GB (1) GB201102237D0 (en)
WO (1) WO2012107765A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6285419B2 (en) 2012-05-08 2018-02-28 ニコックス アフサァルミィクス、 インコーポレイテッドＮｉｃｏｘ Ｏｐｈｔｈａｌｍｉｃｓ， Ｉｎｃ． Hydrophobic therapeutic agent preparation, manufacturing method and use thereof
US8765725B2 (en) 2012-05-08 2014-07-01 Aciex Therapeutics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
US9757395B2 (en) 2012-12-20 2017-09-12 Otitopic Inc. Dry powder inhaler and methods of use
US9757529B2 (en) 2012-12-20 2017-09-12 Otitopic Inc. Dry powder inhaler and methods of use
US9815865B2 (en) 2013-01-07 2017-11-14 Nicox Ophthalmics, Inc. Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
WO2014178891A1 (en) 2013-04-30 2014-11-06 Otitopic Inc. Dry powder formulations and methods of use
US9993488B2 (en) 2014-02-20 2018-06-12 Otitopic Inc. Dry powder formulations for inhalation
CN107072947A (en) 2014-07-31 2017-08-18 奥迪托皮克股份有限公司 dry powder formulation for inhalation
CA2962531C (en) * 2014-10-08 2023-05-23 Eratech S.R.L. Composition comprising at least one dry powder obtained by spray drying to increase the stability of the formulation
DE102016218604A1 (en) 2016-09-27 2018-03-29 Constantin Adams A particulate mixture, preferably for use in the prophylaxis and / or treatment of an airway disorder
CN115919780A (en) 2017-09-22 2023-04-07 维克图拉公司 Dry powder compositions containing magnesium stearate
US10786456B2 (en) 2017-09-22 2020-09-29 Otitopic Inc. Inhaled aspirin and magnesium to treat inflammation
WO2021216710A1 (en) * 2020-04-24 2021-10-28 The Medical College Of Wisconsin, Inc. Use of salmeterol as an anti-coronaviral agent

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080254127A1 (en) * 2000-10-06 2008-10-16 Orion Corporation Inhalation particles incorporating a combination of two or more active ingredients
US7521068B2 (en) * 1998-11-12 2009-04-21 Elan Pharma International Ltd. Dry powder aerosols of nanoparticulate drugs
EP2050437A1 (en) * 2007-10-15 2009-04-22 Laboratoires SMB Improved pharmaceutical dry powder compositions for inhalation.

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1110300C (en) 1993-10-01 2003-06-04 阿斯特拉公司 Process I
US7572430B2 (en) 2000-11-09 2009-08-11 Cyprus Amax Minerals Company Method for producing nano-particles
GB0516549D0 (en) 2005-08-12 2005-09-21 Sulaiman Brian Milling system
WO2008049954A1 (en) 2006-10-24 2008-05-02 Beneq Oy Device and method for producing nanoparticles

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7521068B2 (en) * 1998-11-12 2009-04-21 Elan Pharma International Ltd. Dry powder aerosols of nanoparticulate drugs
US20080254127A1 (en) * 2000-10-06 2008-10-16 Orion Corporation Inhalation particles incorporating a combination of two or more active ingredients
EP2050437A1 (en) * 2007-10-15 2009-04-22 Laboratoires SMB Improved pharmaceutical dry powder compositions for inhalation.

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MICHIKO KUMON ET AL: "Can low-dose combination products for inhalation be formulated in single crystalline particles?", EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 40, no. 1, 1 April 2010 (2010-04-01), pages 16 - 24, XP055036842, ISSN: 0928-0987, DOI: 10.1016/j.ejps.2010.02.004 *
REINHARD VEHRING: "Pharmaceutical Particle Engineering via Spray Drying", PHARMACEUTICAL RESEARCH, KLUWER ACADEMIC PUBLISHERS-PLENUM PUBLISHERS, NL, vol. 25, no. 5, 28 November 2007 (2007-11-28), pages 999 - 1022, XP019613056, ISSN: 1573-904X *

Also Published As

Publication number Publication date
WO2012107765A2 (en) 2012-08-16
GB201102237D0 (en) 2011-03-23

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