CO6241118A2 - Formas amorfas estabilizadas de mesilato de imatinib - Google Patents

Formas amorfas estabilizadas de mesilato de imatinib

Info

Publication number
CO6241118A2
CO6241118A2 CO09139945A CO09139945A CO6241118A2 CO 6241118 A2 CO6241118 A2 CO 6241118A2 CO 09139945 A CO09139945 A CO 09139945A CO 09139945 A CO09139945 A CO 09139945A CO 6241118 A2 CO6241118 A2 CO 6241118A2
Authority
CO
Colombia
Prior art keywords
capsule
pharmaceutical composition
lmatinib mesylate
formulation principle
composition according
Prior art date
Application number
CO09139945A
Other languages
English (en)
Inventor
Elisabete Goncalves
Oscar Kalb
Jay Parthiban Lakshman
Wolfgang Wirth
Michael Mutz
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38229765&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO6241118(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CO6241118A2 publication Critical patent/CO6241118A2/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material
    • A61K9/4825Proteins, e.g. gelatin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invención se refiere a la forma amorfa estabilizada de la sal de adición de ácido metansulfónico de 4-(4-metilpiperazin-1-ilmetil)- N-[4-metil-3-(4-(piridin-3-il)-pirimidin-2-ilamino)-fenil]-benzamida, composiciones farmacéuticas tales como cápsulas o tabletas que contienen esta forma, el uso de dicha forma en métodos de diagnóstico o, preferiblemente, para el tratamiento terapéutico de animales de sangre caliente, especialmente seres humanos, y al uso de principio de formulación estabilizando la forma amorfa de mesilato de lmatinib como un intermediario para la preparación de composiciones farmacéuticas. 1.- Una forma amorfa estabilizada de mesilato de lmatinib. 2.- Una composición farmacéutica que comprende un principio de formulación que estabiliza la forma amorfa de mesilato de lmatinib y mesilato de lmatinib amorfo, opcionalmente junto con por lo menos un vehículo farmacéuticamente aceptable. 3.- La composición farmacéutica de acuerdo con la reivindicación 2, en donde el principio de formulación se selecciona de dispersiones sólidas, complejos de ciclodextrina, y co-molienda con excipientes seleccionados. 4.- Una composición farmacéutica de acuerdo con la reivindicación 3, en donde el principio de formulación es una dispersión sólida. 5.- Una composición farmacéutica de acuerdo con la reivindicación 3, en donde el principio de formulación es un complejo de ciclodextrina. 6.- La composición farmacéutica de acuerdo con cualquiera de las reivindicaciones 2 a 5, la cual es una cápsula. 7.- La cápsula de acuerdo con la reivindicación 6, la cual contiene entre una cantidad de mesilato de lmatinib amorfo estabilizado que corresponde a 50 mg y 200 mg de mesilato de lmatinib. 8.- La cápsula de acuerdo con la reivindicación 7, en donde la cubierta contiene gelatina. 9.- La cápsula de acuerdo con la reivindicación 7, en donde la cubierta contiene dióxido de titanio. 10.- La cápsula de acuerdo con la reivindicación 7, en donde la cubierta contiene óxido de hierro rojo. 11.- La cápsula de acuerdo con la reivindicación 7, en donde la relación de peso de relleno de cápsula a cubierta de cápsula es de entre aproximadamente 100:25 y 100:50. 12.- La cápsula de acuerdo con la reivindicación 7, en donde la relación de peso de relleno de cápsula a cubierta de cápsula es de entre 100:30 y 100:40.
CO09139945A 2007-06-07 2009-12-07 Formas amorfas estabilizadas de mesilato de imatinib CO6241118A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07109816A EP2000139A1 (en) 2007-06-07 2007-06-07 Stabilized amorphous forms of imatinib mesylate
US97419707P 2007-09-21 2007-09-21

Publications (1)

Publication Number Publication Date
CO6241118A2 true CO6241118A2 (es) 2011-01-20

Family

ID=38229765

Family Applications (1)

Application Number Title Priority Date Filing Date
CO09139945A CO6241118A2 (es) 2007-06-07 2009-12-07 Formas amorfas estabilizadas de mesilato de imatinib

Country Status (27)

Country Link
US (4) US20100178336A1 (es)
EP (2) EP2305263B1 (es)
JP (2) JP5380440B2 (es)
KR (2) KR101454086B1 (es)
CN (2) CN104910134A (es)
AR (1) AR067328A1 (es)
AU (1) AU2008262059B2 (es)
BR (1) BRPI0812442A2 (es)
CA (1) CA2687741A1 (es)
CL (1) CL2008001658A1 (es)
CO (1) CO6241118A2 (es)
CY (1) CY1113178T1 (es)
DK (1) DK2305263T3 (es)
ES (1) ES2391625T3 (es)
HK (1) HK1150764A1 (es)
IL (2) IL202157A0 (es)
MX (1) MX2009013272A (es)
MY (1) MY148878A (es)
NZ (3) NZ598428A (es)
PL (1) PL2305263T3 (es)
PT (1) PT2305263E (es)
RU (1) RU2489149C2 (es)
SG (1) SG182175A1 (es)
SI (1) SI2305263T1 (es)
UY (1) UY31125A1 (es)
WO (1) WO2008154262A1 (es)
ZA (2) ZA200900796B (es)

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MX2010003200A (es) * 2007-09-25 2010-04-30 Teva Pharma Composiciones de imatibnib estables.
CZ20098A3 (cs) * 2009-01-13 2010-07-21 Zentiva, K.S. Lékové formy inhibitoru tyrosinových kináz
CZ2009570A3 (cs) 2009-08-26 2011-03-09 Zentiva, K. S. Príprava, stabilizace a využití polymorfu imatinib mesylátu pro vývoj lékových forem
WO2012080703A1 (en) * 2010-12-15 2012-06-21 Cipla Limited Pharmaceutical composition comprising imatinib
EA026665B1 (ru) 2011-11-24 2017-05-31 Имунекс Фарма Илак Санайи Ве Тикарет А.С. Твердые формы препаратов иматиниба, ресуспензируемые непосредственно перед применением
KR101386697B1 (ko) 2012-06-18 2014-04-18 아주대학교산학협력단 이매티닙 또는 이의 약학적으로 허용되는 염을 유효성분으로 포함하는 혈관 투과성 관련 질환의 치료 또는 예방용 조성물
US9439903B2 (en) 2012-10-25 2016-09-13 Cadila Healthcare Limited Process for the preparation of amorphous imatinib mesylate
CN103784411B (zh) * 2012-11-01 2016-03-23 齐鲁制药(海南)有限公司 一种盐酸厄洛替尼药用组合物及其制备方法
WO2015017728A1 (en) 2013-07-31 2015-02-05 Windward Pharma, Inc. Aerosol tyrosine kinase inhibitor compounds and uses thereof
WO2015110949A1 (en) 2014-01-22 2015-07-30 Novartis Ag Imatinib as cholesterol decreasing agent
WO2019158421A1 (en) * 2018-02-13 2019-08-22 Sandoz Ag Pharmaceutical composition of brigatinib
CN109044977A (zh) * 2018-10-26 2018-12-21 武汉工程大学 一种乐伐替尼固体分散体及其制备方法和制剂
CN114845723B (zh) * 2019-11-01 2024-09-13 正大天晴药业集团股份有限公司 包含喹唑啉衍生物或其盐的药物组合物
JP2024502990A (ja) * 2021-01-06 2024-01-24 インカーダ セラピューティクス, インコーポレイテッド 吸入可能なイマチニブ製剤

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Also Published As

Publication number Publication date
US20100178336A1 (en) 2010-07-15
CN104910134A (zh) 2015-09-16
CA2687741A1 (en) 2008-12-18
JP5380440B2 (ja) 2014-01-08
EP2305263A1 (en) 2011-04-06
ZA200900796B (en) 2010-07-28
RU2489149C2 (ru) 2013-08-10
KR20120039717A (ko) 2012-04-25
NZ581176A (en) 2012-10-26
IL237160A0 (en) 2015-03-31
SG182175A1 (en) 2012-07-30
KR101454086B1 (ko) 2014-10-27
AR067328A1 (es) 2009-10-07
US20130022672A1 (en) 2013-01-24
US20130225598A1 (en) 2013-08-29
JP2010529964A (ja) 2010-09-02
CN101678023A (zh) 2010-03-24
CL2008001658A1 (es) 2009-02-20
KR101267782B1 (ko) 2013-06-04
EP2000139A1 (en) 2008-12-10
US20140323495A1 (en) 2014-10-30
ZA200907961B (en) 2014-03-26
JP2013227324A (ja) 2013-11-07
PL2305263T3 (pl) 2012-12-31
HK1150764A1 (en) 2012-01-13
CY1113178T1 (el) 2016-04-13
DK2305263T3 (da) 2012-10-22
RU2009148985A (ru) 2011-08-20
UY31125A1 (es) 2009-01-30
ES2391625T3 (es) 2012-11-28
MX2009013272A (es) 2010-01-25
WO2008154262A1 (en) 2008-12-18
IL202157A0 (en) 2010-06-16
NZ598428A (en) 2013-06-28
NZ598427A (en) 2013-06-28
PT2305263E (pt) 2012-10-22
BRPI0812442A2 (pt) 2013-02-26
AU2008262059B2 (en) 2012-04-05
KR20100020955A (ko) 2010-02-23
SI2305263T1 (sl) 2012-10-30
EP2305263B1 (en) 2012-09-19
MY148878A (en) 2013-06-14
AU2008262059A1 (en) 2008-12-18

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