WO2012087256A2 - Formulations de capsules pharmaceutiques - Google Patents

Formulations de capsules pharmaceutiques Download PDF

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Publication number
WO2012087256A2
WO2012087256A2 PCT/TR2011/000275 TR2011000275W WO2012087256A2 WO 2012087256 A2 WO2012087256 A2 WO 2012087256A2 TR 2011000275 W TR2011000275 W TR 2011000275W WO 2012087256 A2 WO2012087256 A2 WO 2012087256A2
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WO
WIPO (PCT)
Prior art keywords
formulations
glidant
pharmaceutical formulation
lubricant
formulation according
Prior art date
Application number
PCT/TR2011/000275
Other languages
English (en)
Other versions
WO2012087256A3 (fr
Inventor
Mahmut Bilgic
Original Assignee
Mahmut Bilgic
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 Mahmut Bilgic filed Critical Mahmut Bilgic
Publication of WO2012087256A2 publication Critical patent/WO2012087256A2/fr
Publication of WO2012087256A3 publication Critical patent/WO2012087256A3/fr

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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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—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
    • A61K9/20—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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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

Definitions

  • the present invention relates to pharmaceutical imatinib formulations comprising a pharmaceutically acceptable lubricant, a glidant and at least one other excipient wherein the ratio of the lubricant and the glidant to each other is minimum 5 by weight, and production methods of said formulations.
  • Imatinib mesylate which is the methane sulfonic acid addition salt of imatinib, is available on the market under the trade name Glivec by Novartis AG.
  • EP0564409 free base and pharmaceutically acceptable salts of imatinib (Formula I) have been disclosed.
  • Imatinib a tyrosine-kinase inhibitor
  • BCR-ABL enzyme a tyrosine-kinase inhibitor
  • this compound is indicated for chronic myeloid leukemia and acute lymphoblastic leukemia.
  • imatinib inhibits transmembrane receptor KIT and PDGF receptors (Merck Index, 14th edition, no: 4902, page 851).
  • Imatinib free base and its salts were first disclosed in the patent numbered EP 564409.
  • acid addition salts of imatinib and preparation methods thereof have been mentioned.
  • the active agent is available in the form of 100 and 400 mg tablet and 100 mg capsule on the market.
  • the inventor has found that homogeneous and effective mixing cannot be provided in the formulations comprising imatinib and suitable excipients; the powder mixture is agglomerated through the production line.
  • adding lubricant into the formulations is not sufficient in order to solve the problems.
  • Parameters such as adding sequence of the lubricant into the formulation, amount of the lubricant and mixing time etc. can negatively affect important factors such as solubility, physical characteristics of the end dosage form obtained.
  • the lubricant which is not used properly and in an appropriate amount causes decrease in solubility of the formulations obtained, constitution of hardly dispersible powder, failure to ensure sufficient physical characteristic (erosion, diffraction, hardness etc.) in dosage forms prepared.
  • the present invention relates to pharmaceutical imatinib formulations comprising a pharmaceutically acceptable lubricant, a glidant and at least one other excipient wherein the ratio of the lubricant and glidant to each other is minimum 5 by weight, and production methods thereof.
  • compositions of the present invention comprise imatinib minimum 80% by weight, preferably in the range of 80% to 99% by weight, more preferably in the range of 80% to 98% by weight.
  • imatinib refers to pharmaceutically acceptable salts, enantiomers, racemates, solvates, hydrates, different polymorphic forms, amorphous forms and crystalline forms of the active agent or the combinations thereof.
  • compositions of the present invention is that the active agent comprised in the formulations is imatinib mesylate salt.
  • mesylate salt of the active agent comprised in the formulations is in alpha or beta crystalline form, more preferably in alpha crystalline form.
  • One characteristic feature of the formulation comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient is that the ratio of the lubricant and the glidant to each other comprised in the formulations is minimum 5 by weight.
  • One characteristic feature of the formulation comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient is that the ratio of the lubricant and the glidant to each other comprised in the formulations is in the range of 5 to 10 by weight.
  • One characteristic feature of the formulation comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient is that the ratio of the lubricant and the glidant to each other comprised in the formulations is in the range of 6 to 8 by weight.
  • compositions of the present invention possess the features required in terms of solubility and physical characteristics.
  • the lubricants that can be used in the formulations of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient can be selected from a group comprising metallic stearates (such as magnesium stearate, calcium stearate, aluminium stearate), fatty acid esters (such as sodium stearyl fumarate), fatty acids (such as stearic acid), fatty alcohols, glyceryl behenate, mineral oil, paraffins, hydrogenated vegetable oil, leucine, polyethylene glycols (PEG), metallic lauryl sulphate (such as sodium lauryl sulphate, magnesium lauryl sulphate), sodium chloride, sodium benzoate, sodium acetate, talc, siliconized talc and/or hydrates or the combinations thereof.
  • metallic stearates such as magnesium stearate, calcium stearate, aluminium stearate
  • One characteristic feature of the formulation of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant and a glidant and at least one other excipient is that the amount of the lubricant comprised in the formulations is in the range of 1 to 3% by weight, preferably in the range of 1 to 2 % by weight.
  • the lubricant which is particularly preferred is magnesium stearate in the formulations of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient.
  • glidants that can be used in the formulations of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient can be selected from a group comprising silica, talc, colloidal silicone dioxide (Aerosil® 200, Syloid®, Cab-OSil®), magnesium trisilicate, cellulose powder, magnesium stearate and corn starch or the combinations thereof.
  • One characteristic feature of the formulation comprising imatinib as active agent and a pharmaceutically acceptable lubricant and a glidant and at least one other excipient is that the amount of the glidant comprised in the formulations is in the range of 0.1 to 1 % by weight, preferably in the range of 0.1 to 0.5 % by weight.
  • the glidant comprised in the formulations has a specific surface area in the range of 150 to 300 m 2 /g; and an average particle size is in the range of 1 to 50 nm, preferably in the range of 1 to 40 nm, more preferably in the range of 1 to 30 nm.
  • Average particle size used herein signifies volumetric average particle size and it is also shown as d 0 in short .
  • d 50 refers that one half of said substance by volume has a particle size over the value stated with d 50 , the other half of the substance has a particle size under the value stated with d 50 .
  • the average particle size in the formulations of the present invention has been measured with a device which measures particle distribution by laser diffraction (Malvern Mastersizer etc.); as for the specific surface area, it has been measured with a BET (Micromeritics ASAP 2400) device which was calibrated properly.
  • the glidant which is particularly preferred is silicone dioxide in the formulations of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient.
  • excipients which can be used in the pharmaceutical formulations of the present invention in addition to the lubricant and glidant can be selected from a group comprising disintegrant, binders, viscosity enhancing components, filling agents, drying agents, surfactants, stabilizing agents, diluents, glidants, wetting agents, coating agents designed in order to provide various release properties, pH regulators, effervescent acids, effervescent bases, gelling agents, flavouring agents, sweeteners, emulgators, antifoaming agents, protective agents, solvents or solvent combinations, colouring agents and complexing agents or the combinations thereof.
  • excipients that can be used in the pharmaceutical formulations of the present invention in addition to the lubricant and the glidant are preferably selected from a group comprising disintegrants, diluents, binders or the combinations thereof.
  • the diluents that can be used in the formulations of the present invention can be selected from a group comprising calcium carbonate, dibasic calcium phosphate, tribasic calcium phosphate, calcium sulphate, microcrystalline cellulose, dextrose, fructose, lactitol, lactose, magnesium carbonate, magnesium oxide, maltitol, maltodextrin, maltose, mannitol, simethicone, sorbitol, starch and starch derivatives (for instance corn starch), sodium chloride, sucrose, talc, xylitol or the combinations thereof.
  • the binders that can be used in the formulations of the present invention can be selected from a group comprising potato starch, wheat starch or corn starch; microcrystalline cellulose (Avicel®, Filtrak®, Heweten® or Pharmacel®), hydroxypropyl cellulose, hydroxyethyl cellulose; hydroxypropyl methyl cellulose (hydroxypropyl methyl cellulose-Type 2910 USP, hypromellose) and polyvinylpyrrolidone (for instance, Povidone® K30(BASF)), lactose, guar gum, pectin, gelatine, sodium alginate or the combinations thereof.
  • microcrystalline cellulose Avicel®, Filtrak®, Heweten® or Pharmacel®
  • hydroxypropyl cellulose hydroxyethyl cellulose
  • hydroxypropyl methyl cellulose hydroxypropyl methyl cellulose-Type 2910 USP, hypromellose
  • polyvinylpyrrolidone for instance, Povidone® K
  • the disintegrants that can be used in the formulations of the present invention can be selected from a group comprising carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, microcrystalline cellulose, methyl cellulose, chitosan, starch, sodium starch glycolate or the combinations thereof.
  • formulations of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient are powder form.
  • the powder formulations of the present invention comprising a pharmaceutically acceptable disintegrant in the range of 0.1 to 5% by weight together with imatinib as active agent can be prepared in any one of the solid forms including tablet; layered tablet (for instance bilayer tablet); capsule; enterically coated or modified release tablet; controlled release tablet; prolonged release tablet; delayed release tablet; slow or fast release tablet; fast soluble tablet; effervescent tablet; fast soluble powder mixture; water soluble powder; pellet; mini tablet; micro tablet; granule in capsule; pellet in capsule; mini tablet in capsule; micro tablet in capsule or dry powder mixture to prepare syrup; dragee; orodispersible tablet; film coated tablet or a combination thereof.
  • the powder formulations of the present invention comprising a pharmaceutically acceptable disintegrant in the range of 0.1 to 5% by weight together with imatinib as active agent is preferably in tablet or capsule dosage form.
  • the capsule that can be used can be made of a substance selected from a group comprising gelatine, chitosan, starch and/or starch derivatives, cellulose and/or cellulose derivatives or synthetic polymers.
  • the capsule is composed of telescoping body and cap parts. The body and cap parts of said capsule can be made of the same or different materials.
  • capsule material can be selected from a group comprising hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose or the combinations thereof.
  • capsule material in the case that capsule is synthetic polymer; capsule material can be selected from a group comprising polyethylene, polyester, polyethylene terephthalate, polycarbonate or polypropylene or the combinations thereof.
  • capsule material is gelatine
  • various molecular-weighted polyethylene glycol, sorbitol, glycerol, propylene glycol, titanium dioxide, polyethylene oxide- polypropylene oxide block copolymers and /or other polyalcohols and polyethers can be used as excipient.
  • the preferred capsule is preferably gelatine capsule and said capsule can be in any shape and colour.
  • said tablet dosage form can be coated with protective coating, enteric coating, film coating and/or coatings designed in order to provide various release properties (such as fast release, slow release, controlled release).
  • the film coating agents that can be used in the present invention can be selected from a group comprising cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose; polyvinyl alcohols such as iron oxides, titanium dioxide, polyethylene glycol; synthetic polymers such as polyvinyl acetal diethyl aminoacetate, aminoalkyl methacrylate copolymers and polyvinylpyrrolidone and polysaccharides such as pullulan or the combinations thereof.
  • cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose
  • polyvinyl alcohols such as iron oxides, titanium dioxide, polyethylene glycol
  • synthetic polymers such as polyvinyl acetal diethyl aminoacetate, aminoalkyl methacrylate cop
  • the enteric coating agents that can be used in the present invention can be selected from a group comprising cellulose derivatives such as hydroxypropyl methyl cellulose phthalate, hydroxypropyl methylcellulose acetate succinate, carboxymethyl ethyl cellulose, cellulose acetate phthalate; acrylic acid derivatives such as methacrylic acid copolymer L, methacrylic acid copolymer LD and methacrylic acid copolymer S; natural substances such as shellac or the combinations thereof.
  • cellulose derivatives such as hydroxypropyl methyl cellulose phthalate, hydroxypropyl methylcellulose acetate succinate, carboxymethyl ethyl cellulose, cellulose acetate phthalate
  • acrylic acid derivatives such as methacrylic acid copolymer L, methacrylic acid copolymer LD and methacrylic acid copolymer S
  • natural substances such as shellac or the combinations thereof.
  • Effective daily dose amount differs according to various factors such as patient's age, individual conditions, stage of the disease, mode of administration.
  • daily imatinib dose required for adults varies in the range of 400 mg to 800 mg.
  • amount of active agent in the oral dosage form is in the range of 50 mg to 800 mg, preferably in the range of 100 mg to 600 mg, more preferably in the range of 100 mg to 400 mg in another embodiment of the invention.
  • active agent is a pharmaceutically acceptable derivative of imatinib
  • these substances are used in the amounts corresponding to 50 mg-800 mg, preferably to 100 mg-600 mg, more preferably to 100 mg-400 mg of imatinib free base.
  • the amount of imatinib comprised in the pharmaceutical formulations of the present invention corresponds to imatinib free base in the range of 50 mg to 800 mg, preferably in the range of 100 mg to 600 mg, more preferably in the range of 100 mg and 400 mg.
  • the oral dosage form comprising an effective amount of alpha crystalline form of imatinib mesylate can be administered separately, sequentially and simultaneously with dosage forms comprising active agents belonging to groups such as rapamycin, cyclosporine, ascomycine, corticosteroid, cyclophosphamide, azathioprine, methotrexate, brequinar, leflunomide, mizoribine, mycophenolic acid and/or mycophenolate mofetil.
  • active agents belonging to groups such as rapamycin, cyclosporine, ascomycine, corticosteroid, cyclophosphamide, azathioprine, methotrexate, brequinar, leflunomide, mizoribine, mycophenolic acid and/or mycophenolate mofetil.
  • the formulation of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient is preferably produced by dry blending method.
  • Dry blending method which is used in order to produce the formulation of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient is preferably composed of the following steps:
  • the active agent, glidant and at least one other excipient are mixed dryly,
  • Final mixture is optionally compressed in tablet form or filled into capsules.
  • compositions of the present invention comprising imatinib as active agent and a pharmaceutically acceptable lubricant, a glidant and at least one other excipient are used in the treatment of acute lymphocytic leukemia, gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome, chronic myelogenous leukemia (CML), myelodysplastic syndrome and systemic mastocytosis.
  • GIST gastrointestinal stromal tumors
  • CML chronic myelogenous leukemia
  • myelodysplastic syndrome myelodysplastic syndrome and systemic mastocytosis.
  • Imatinib mesylate, the disintegrant and the glidant are mixed for production of the formulation given; the lubricant is added into the mixture and the mixture is mixed again.
  • the mixture is presented as filled into a hard gelatine capsule which is preferably made of titanium dioxide and gelatine.
  • Imatinib mesylate, the disintegrant and the glidant are mixed for production of the formulation given; the lubricant is added into the mixture and the mixture is mixed again.
  • the mixture is compressed in tablet form and coated with film coating material.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne des formulations d'imatinib pharmaceutiques contenant un lubrifiant pharmaceutiquement acceptable, un agent de glissement et au moins un autre excipient, le rapport pondéral lubrifiant/agent de glissement étant d'au minimum 5. L'invention concerne également des procédés de production associés.
PCT/TR2011/000275 2010-12-20 2011-12-19 Formulations de capsules pharmaceutiques WO2012087256A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR2010/10618 2010-12-20
TR2010/10618A TR201010618A2 (tr) 2010-12-20 2010-12-20 İmatinib içeren bir oral dozaj formu ve bu oral dozaj formunun üretimi

Publications (2)

Publication Number Publication Date
WO2012087256A2 true WO2012087256A2 (fr) 2012-06-28
WO2012087256A3 WO2012087256A3 (fr) 2012-09-27

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ID=45529174

Family Applications (3)

Application Number Title Priority Date Filing Date
PCT/TR2011/000274 WO2012087255A2 (fr) 2010-12-20 2011-12-19 Formulations pharmaceutiques
PCT/TR2011/000276 WO2012087257A2 (fr) 2010-12-20 2011-12-19 Forme galénique orale contenant de l'imatinib et production de ladite forme galénique orale
PCT/TR2011/000275 WO2012087256A2 (fr) 2010-12-20 2011-12-19 Formulations de capsules pharmaceutiques

Family Applications Before (2)

Application Number Title Priority Date Filing Date
PCT/TR2011/000274 WO2012087255A2 (fr) 2010-12-20 2011-12-19 Formulations pharmaceutiques
PCT/TR2011/000276 WO2012087257A2 (fr) 2010-12-20 2011-12-19 Forme galénique orale contenant de l'imatinib et production de ladite forme galénique orale

Country Status (2)

Country Link
TR (1) TR201010618A2 (fr)
WO (3) WO2012087255A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI608849B (zh) * 2014-06-16 2017-12-21 國邑藥品科技股份有限公司 可調控釋放度之高載藥量之醫藥組合物及其製備方法

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL394169A1 (pl) * 2011-03-09 2012-09-10 Adamed Spółka Z Ograniczoną Odpowiedzialnością Kompozycja farmaceutyczna metanosulfonianu imatinibu do napełniania jednostkowych postaci dawkowania oraz sposób jej wytwarzania
KR20140065862A (ko) * 2012-11-22 2014-05-30 에스케이케미칼주식회사 발포성 속붕해성 이매티닙 제제
GB201304699D0 (en) * 2013-03-15 2013-05-01 Remedica Ltd Pharmaceutical compositions
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
WO2019229648A1 (fr) * 2018-05-28 2019-12-05 Shivalik Rasayan Limited Compositions orales de mésylate d'imatinib

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0564409A1 (fr) * 1992-04-03 1993-10-06 Ciba-Geigy Ag Dérivés de pyrimidine et procédé pour leur préparation
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
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
US20080226731A1 (en) * 2005-05-10 2008-09-18 Madhav Vasanthavada Pharmaceutical Compositions Comprising I Matinib and a Release Retardant
US20090087489A1 (en) * 2007-09-25 2009-04-02 Bella Gerber Imatinib compositions

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITMI992711A1 (it) * 1999-12-27 2001-06-27 Novartis Ag Composti organici
GB0209265D0 (en) 2002-04-23 2002-06-05 Novartis Ag Organic compounds
GB2398565A (en) 2003-02-18 2004-08-25 Cipla Ltd Imatinib preparation and salts
ATE459341T1 (de) * 2005-06-03 2010-03-15 Elan Pharma Int Ltd Nanoteilchenförmige imatinib-mesylat- formulierungen
US20060223817A1 (en) 2006-05-15 2006-10-05 Chemagis Ltd. Crystalline imatinib base and production process therefor
CN101951889A (zh) * 2006-09-01 2011-01-19 特瓦制药工业有限公司 伊马替尼组合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0564409A1 (fr) * 1992-04-03 1993-10-06 Ciba-Geigy Ag Dérivés de pyrimidine et procédé pour leur préparation
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
US20080226731A1 (en) * 2005-05-10 2008-09-18 Madhav Vasanthavada Pharmaceutical Compositions Comprising I Matinib and a Release Retardant
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
US20090087489A1 (en) * 2007-09-25 2009-04-02 Bella Gerber Imatinib compositions

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI608849B (zh) * 2014-06-16 2017-12-21 國邑藥品科技股份有限公司 可調控釋放度之高載藥量之醫藥組合物及其製備方法

Also Published As

Publication number Publication date
WO2012087255A2 (fr) 2012-06-28
WO2012087255A3 (fr) 2012-08-16
WO2012087257A2 (fr) 2012-06-28
WO2012087257A3 (fr) 2012-09-27
WO2012087256A3 (fr) 2012-09-27
TR201010618A2 (tr) 2012-07-23

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