WO2013139826A1 - Compositions pharmaceutiques comprenant de l'imatinib - Google Patents

Compositions pharmaceutiques comprenant de l'imatinib Download PDF

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Publication number
WO2013139826A1
WO2013139826A1 PCT/EP2013/055764 EP2013055764W WO2013139826A1 WO 2013139826 A1 WO2013139826 A1 WO 2013139826A1 EP 2013055764 W EP2013055764 W EP 2013055764W WO 2013139826 A1 WO2013139826 A1 WO 2013139826A1
Authority
WO
WIPO (PCT)
Prior art keywords
dosage form
imatinib
solid oral
weight
form according
Prior art date
Application number
PCT/EP2013/055764
Other languages
English (en)
Inventor
Charalambos PATTIHIS
Antje NORDMANN
Panagiotis PANAGOPOULOS
Konstantinos-Emmanouil PANITSAS
Original Assignee
Remedica Ltd
Pharmaceutical Oriented Services 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 Remedica Ltd, Pharmaceutical Oriented Services Ltd filed Critical Remedica Ltd
Publication of WO2013139826A1 publication Critical patent/WO2013139826A1/fr

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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Definitions

  • Imatinib is chemically designated as 4-[(4-methyl-l-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3- pyridinyl)-2-pyrimidinyl] aminoj-phenyl] benzamide, and can be represented by the chemical structure of formula (I)
  • a capsule comprising imatinib, or a pharmaceutically acceptable salt thereof, together with one or more pharmaceutically acceptable excipients, said capsule comprising said imatinib in an amount in the range of about 27.0 to 29.0% based on the weight of imatinib free base compared to the total weight of said capsule.
  • Preferred % amounts for said imatinib are as previously described.
  • a filler is included in an oral dosage form according to the present invention in an amount in the range of about 15.0 to 30.0%, based on the weight thereof compared to the total weight of the solid oral dosage form, more preferably in an amount in the range of about 15.0 to 25.0%, and even more preferably in an amount in the range of about 15.0 to 20.0%, based on the weight thereof compared to the total weight of the solid oral dosage form.
  • such disintegrants are present in an amount in the range of about 19.0 to 22.0%, based on the weight thereof compared to the total weight of the solid oral dosage form, and typically where such % weights for disintegrants are provided herein then these are based on the total amount of disintegrant present both in intra- and extra-granular phases of a solid oral dosage form according to the present invention.
  • suitable glidants include colloidal silicon dioxide, calcium silicates and talcum. Colloidal silicon dioxide is preferred and typically a glidant is present in an amount in the range of about 0.1 to 1.0%, based on the weight thereof compared to the total weight of the solid oral dosage form.
  • a glidant is present in an extra-granular phase of a solid oral dosage form according to the present invention.
  • a solid oral dosage form comprises a tablet substantially as hereinbefore described
  • the tablet comprises a film coated tablet.
  • film-coated tablet means a tablet core provided with a film coating
  • a typical film coating employs hydroxypropyl methylcellulose (hypromellose) as a key constituent together with other auxiliaries, such as plasticizers, colorants and the like.
  • compositions according to the present invention as described herein can be used in the treatment of conditions that can be alleviated by the administration of a protein tyrosine kinase inhibitor, such as imatinib or a pharmaceutically acceptable salt thereof, such as imatinib mesylate.
  • a protein tyrosine kinase inhibitor such as imatinib or a pharmaceutically acceptable salt thereof, such as imatinib mesylate.
  • compositions according to the present invention as described herein are useful in the treatment of various types of cancer and especially for the treatment of the approved indications for imatinib substantially as hereinbefore described.
  • Example 1 is provided to illustrate the invention and are not to be construed as limiting the scope of the invention in any manner.
  • Example 1
  • Hypromellose was dissolved in the granulation solvent and mixed until a clear solution was obtained.
  • Imatinib mesylate, microcrystalline cellulose and croscarmellose sodium were mixed and subsequently granulated with the granulating solution, until granules were formed. 3. The wet granules were dried and sifted.
  • Hypromellose was dissolved in the granulation solvent and mixed until a clear solution was obtained. 2. Imatinib mesylate, microcrystalline cellulose and croscarmellose sodium were mixed and subsequently granulated with the granulating solution, until granules were formed.

Landscapes

  • Health & Medical Sciences (AREA)
  • Epidemiology (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)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une forme galénique orale solide comprenant de l'imatinib, ou son sel pharmaceutiquement acceptable, conjointement avec un ou plusieurs excipients pharmaceutiquement acceptables, ladite forme galénique orale solide comprenant ledit imatinib dans une quantité comprise dans la plage d'environ 27,0 à 29,0 % sur la base du poids de la base exempte d'imatinib par rapport au poids total de ladite forme galénique orale solide.
PCT/EP2013/055764 2012-03-20 2013-03-20 Compositions pharmaceutiques comprenant de l'imatinib WO2013139826A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB1204810.4 2012-03-20
GBGB1204810.4A GB201204810D0 (en) 2012-03-20 2012-03-20 Pharmaceutical compositions

Publications (1)

Publication Number Publication Date
WO2013139826A1 true WO2013139826A1 (fr) 2013-09-26

Family

ID=46052174

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2013/055764 WO2013139826A1 (fr) 2012-03-20 2013-03-20 Compositions pharmaceutiques comprenant de l'imatinib

Country Status (2)

Country Link
GB (1) GB201204810D0 (fr)
WO (1) WO2013139826A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999003854A1 (fr) 1997-07-18 1999-01-28 Novartis Ag Modification de la forme cristalline d'un derive n-phenyl-2-pyrimidineamine, procede de preparation et d'utilisation de ce dernier
WO2003090720A1 (fr) 2002-04-23 2003-11-06 Novartis Ag Comprime a forte charge en substance medicamenteuse
US20070036850A1 (en) * 2005-08-15 2007-02-15 Siegfried Generics International Ag Film-coated tablet or granules containing as active ingredient a pyridylpyrimidine compound or a pharmaceutically acceptable salt of this compound
WO2011157450A1 (fr) * 2010-06-18 2011-12-22 Krka, D. D., Novo Mesto Nouvelle forme polymorphique d'imatinib base et préparation de ses sels

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999003854A1 (fr) 1997-07-18 1999-01-28 Novartis Ag Modification de la forme cristalline d'un derive n-phenyl-2-pyrimidineamine, procede de preparation et d'utilisation de ce dernier
WO2003090720A1 (fr) 2002-04-23 2003-11-06 Novartis Ag Comprime a forte charge en substance medicamenteuse
US20070036850A1 (en) * 2005-08-15 2007-02-15 Siegfried Generics International Ag Film-coated tablet or granules containing as active ingredient a pyridylpyrimidine compound or a pharmaceutically acceptable salt of this compound
WO2011157450A1 (fr) * 2010-06-18 2011-12-22 Krka, D. D., Novo Mesto Nouvelle forme polymorphique d'imatinib base et préparation de ses sels

Also Published As

Publication number Publication date
GB201204810D0 (en) 2012-05-02

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