WO2008122425A3 - Oral compositions containing tacrolimus in amorphous form - Google Patents

Oral compositions containing tacrolimus in amorphous form Download PDF

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Publication number
WO2008122425A3
WO2008122425A3 PCT/EP2008/002716 EP2008002716W WO2008122425A3 WO 2008122425 A3 WO2008122425 A3 WO 2008122425A3 EP 2008002716 W EP2008002716 W EP 2008002716W WO 2008122425 A3 WO2008122425 A3 WO 2008122425A3
Authority
WO
WIPO (PCT)
Prior art keywords
amorphous form
active principle
compositions containing
agent
compositions
Prior art date
Application number
PCT/EP2008/002716
Other languages
French (fr)
Other versions
WO2008122425A2 (en
Inventor
Celestino Ronchi
Giancarlo Ceschel
Luca Rampoldi
Manuela Astulfoni
Original Assignee
Monteres S R L
Celestino Ronchi
Giancarlo Ceschel
Luca Rampoldi
Manuela Astulfoni
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 Monteres S R L, Celestino Ronchi, Giancarlo Ceschel, Luca Rampoldi, Manuela Astulfoni filed Critical Monteres S R L
Publication of WO2008122425A2 publication Critical patent/WO2008122425A2/en
Publication of WO2008122425A3 publication Critical patent/WO2008122425A3/en

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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
    • 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
    • A61K9/1611—Inorganic compounds
    • 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
    • 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
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds

Landscapes

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

Abstract

Fast release or modified release oral compositions containing as the active principle Tacrolimus and/or derivatives thereof in amorphous form, and: a) a 'solubilising agent' of the active principle suitable to maintain it in the amorphous form over time, b) at least one 'diluting agent' having the function to stabilize the active principle in the amorphous form, c) at least one agent being 'modulator' of the dissolution rate of the active principle from the pharmaceutical form. These compositions in form of paste, granules, powder, solution, suspension can be formulated in hard or soft gelatine capsules or can be formulated in other pharmaceutical forms for oral use. These compositions are characterized in that all the relative operations of preparation are carried out in the absence of water and/or organic solvents.
PCT/EP2008/002716 2007-04-06 2008-04-04 Oral compositions containing tacrolimus in amorphous form WO2008122425A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2007A000720 2007-04-06
ITMI20070720 ITMI20070720A1 (en) 2007-04-06 2007-04-06 ORAL COMPOSITIONS CONTAINING TACROLIMUS IN AMORPHOUS FORM

Publications (2)

Publication Number Publication Date
WO2008122425A2 WO2008122425A2 (en) 2008-10-16
WO2008122425A3 true WO2008122425A3 (en) 2009-01-08

Family

ID=39534833

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/002716 WO2008122425A2 (en) 2007-04-06 2008-04-04 Oral compositions containing tacrolimus in amorphous form

Country Status (2)

Country Link
IT (1) ITMI20070720A1 (en)
WO (1) WO2008122425A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180243224A1 (en) * 2015-08-19 2018-08-30 Vivus, Inc. Pharmaceutical formulations
CN113577032A (en) * 2021-08-27 2021-11-02 国药集团川抗制药有限公司 Preparation method of tacrolimus solid dispersion, quick-release pharmaceutical composition and application

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1064942A1 (en) * 1998-03-26 2001-01-03 Fujisawa Pharmaceutical Co., Ltd. Sustained release preparations
EP1092429A1 (en) * 1993-07-08 2001-04-18 Novartis AG Pharmaceutical preparations for drugs of low solubility
WO2005020994A1 (en) * 2003-08-29 2005-03-10 Lifecycle Pharma A/S Solid dispersions comprising tacrolimus
WO2006062334A1 (en) * 2004-12-06 2006-06-15 Hanmi Pharm. Co., Ltd. Oral micro-emulsion composition comprising tacrolimus

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1092429A1 (en) * 1993-07-08 2001-04-18 Novartis AG Pharmaceutical preparations for drugs of low solubility
EP1064942A1 (en) * 1998-03-26 2001-01-03 Fujisawa Pharmaceutical Co., Ltd. Sustained release preparations
WO2005020994A1 (en) * 2003-08-29 2005-03-10 Lifecycle Pharma A/S Solid dispersions comprising tacrolimus
WO2006062334A1 (en) * 2004-12-06 2006-06-15 Hanmi Pharm. Co., Ltd. Oral micro-emulsion composition comprising tacrolimus

Also Published As

Publication number Publication date
WO2008122425A2 (en) 2008-10-16
ITMI20070720A1 (en) 2008-10-07

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