EP2603288A1 - Granulat pharmaceutique comprenant de l'imatinib mésylate - Google Patents

Granulat pharmaceutique comprenant de l'imatinib mésylate

Info

Publication number
EP2603288A1
EP2603288A1 EP10747433.0A EP10747433A EP2603288A1 EP 2603288 A1 EP2603288 A1 EP 2603288A1 EP 10747433 A EP10747433 A EP 10747433A EP 2603288 A1 EP2603288 A1 EP 2603288A1
Authority
EP
European Patent Office
Prior art keywords
imatinib mesylate
granulate
imatinib
composition
mesylate
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.)
Withdrawn
Application number
EP10747433.0A
Other languages
German (de)
English (en)
Inventor
Dennie Johan Marijn Van Den Heuvel
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.)
Synthon BV
Original Assignee
Synthon BV
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 Synthon BV filed Critical Synthon BV
Publication of EP2603288A1 publication Critical patent/EP2603288A1/fr
Withdrawn legal-status Critical Current

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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • WO 2006/121941 discloses a melt granulation process which comprises the steps of (a) forming a mixture of imatinib mesylate with at least one release retardant, e.g., a release retarding polymer, a plasticizer or a release modifier; (b) granulating the mixture using an extruder and (c) cooling the granules.
  • a release retardant e.g., a release retarding polymer, a plasticizer or a release modifier
  • US 2007/0036850 discloses a dry granulation (by compaction) process for the preparation of imatinib Form a or ⁇ granules prior to the tabletting process.
  • the imatinib granule cores contain between 25 and 80% of imatinib together with filler-binder additives , e.g. with microcrystalline cellulose and crospovidone.
  • the population of granules has an average size of between 250-800 ⁇ , as determined by sieve analysis.
  • the invention provides a process for making a granulate comprising imatinib mesylate, which process comprises wetting imatinib mesylate with a granulation liquid, which is preferably water, ethanol and/or isopropanol and most preferably in an amount of 5 - 50 weight %, in respect to the mass of imatinib mesylate, and granulating the mixture in a suitable granulator, e.g. high shear or fluid bed granulator, followed by drying, and optionally sieving and/or milling of the produced population of granules.
  • a suitable granulator e.g. high shear or fluid bed granulator
  • the last aspect deals with the use of the pharmaceutical imatinib mesylate granulate of the present invention and/or a composition comprising it for making a medicament.
  • compositions comprising imatinib mesylate and useful for making compressed dosage forms, such as tablets, comprises the step of granulation of imatinib with filler-binders excipients to yield a "composite" granulate, i.e. a granulate comprising imatinib and at least one granulate-forming excipient.
  • the "wet granulation” as used herein is a process, which itself is well known in the art and comprises, within many technological variants, moistening a solid component or a mixture of solid components with a liquid, and vigorous mixing of the composition, whereby the wet particles of solids adhere together by cohesive forces to form larger, sometimes essentially spherical, agglomerates (a granulate).
  • the excess of the granulation liquid may be removed from the raw granulate by drying and the suitable size range of particles is obtained by sieving and/or milling the population of granules.
  • imatinib mesylate can be wet granulated without using any granulate-forming excipient, such as a filler and/or binder , to form a free flowing solid granulate material comprising ,based on a solvent-free basis, only imatinib (small amounts of used granulation liquid may be present).
  • a granulation liquid which is preferably water and/or an alcohol, e.g. ethanol or isopropanol, and processing the mixture in a suitable granulator results in a stable free flowing granulate form of imatinib mesylate with suitable characteristics for further processing.

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un granulat contenant entre 95 et 99 % d'imatinib mésylate et entre 1 et 5 % d'un liquide volatil. L'invention porte en outre sur un procédé de fabrication d'un granulat d'imatinib mésylate. Ledit procédé comprend le mouillage d'imatinib mésylate avec un liquide de granulation, et la granulation du mélange dans un granulateur, suivie du séchage, et éventuellement du tamisage et/ou du broyage de la population produite de granules, en vue d'obtenir une composition pharmaceutique pour administration orale destinée à être utilisée en médecine.
EP10747433.0A 2010-08-11 2010-08-11 Granulat pharmaceutique comprenant de l'imatinib mésylate Withdrawn EP2603288A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2010/005214 WO2012019633A1 (fr) 2010-08-11 2010-08-11 Granulat pharmaceutique comprenant de l'imatinib mésylate

Publications (1)

Publication Number Publication Date
EP2603288A1 true EP2603288A1 (fr) 2013-06-19

Family

ID=44065563

Family Applications (1)

Application Number Title Priority Date Filing Date
EP10747433.0A Withdrawn EP2603288A1 (fr) 2010-08-11 2010-08-11 Granulat pharmaceutique comprenant de l'imatinib mésylate

Country Status (5)

Country Link
EP (1) EP2603288A1 (fr)
MX (1) MX2013001653A (fr)
RU (1) RU2013110058A (fr)
WO (1) WO2012019633A1 (fr)
ZA (1) ZA201300872B (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9750700B2 (en) * 2011-06-22 2017-09-05 Natco Pharma Limited Imatinib mesylate oral pharmaceutical composition and process for preparation thereof
US20160015708A1 (en) * 2012-02-21 2016-01-21 Ranbaxy Laboratories Limited Stable dosage forms of imatinib mesylate
EP2749271A1 (fr) * 2012-12-31 2014-07-02 Deva Holding Anonim Sirketi Procédé optimisée de fabrication et formulation pharmaceutique de l'imatinib
ES2683361T3 (es) 2013-05-14 2018-09-26 Hetero Research Foundation Composiciones de Imatinib
EP3019159A4 (fr) * 2013-07-09 2017-01-18 Shilpa Medicare Limited Compositions pharmaceutiques orales comprenant du mésylate d'imatinib
EP3257499A1 (fr) 2016-06-17 2017-12-20 Vipharm S.A. Procédé pour la préparation de capsules de méthanesulfonate d'imatinib

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW225528B (fr) 1992-04-03 1994-06-21 Ciba Geigy Ag
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB0209265D0 (en) * 2002-04-23 2002-06-05 Novartis Ag Organic compounds
WO2006040779A2 (fr) 2004-10-11 2006-04-20 Natco Pharma Limited Formule à matrice flottante gastrique à libération contrôlée contenant la substance imatinib
MY148074A (en) 2005-05-10 2013-02-28 Novartis Ag Pharmaceutical compositions comprising imatinib and a release retardant
DE502006005084D1 (de) 2005-08-15 2009-11-26 Siegfried Generics Int Ag Filmtablette oder Granulat enthaltend ein Pyridylpyrimidin
PL390611A1 (pl) * 2010-03-04 2011-09-12 Tomasz Koźluk Sposób otrzymywania polimorficznej formy alfa i nowa forma polimorficzna mesylanu imatinibu
WO2011121593A1 (fr) * 2010-03-29 2011-10-06 Hetero Research Foundation Composition pharmaceutique stable d'imatinib

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
None *
See also references of WO2012019633A1 *

Also Published As

Publication number Publication date
RU2013110058A (ru) 2014-09-20
MX2013001653A (es) 2013-05-22
ZA201300872B (en) 2014-04-30
WO2012019633A1 (fr) 2012-02-16

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