AR072062A1 - Formulaciones farmaceuticas solidas que comprenden bibw 2992 - Google Patents

Formulaciones farmaceuticas solidas que comprenden bibw 2992

Info

Publication number
AR072062A1
AR072062A1 ARP090102042A ARP090102042A AR072062A1 AR 072062 A1 AR072062 A1 AR 072062A1 AR P090102042 A ARP090102042 A AR P090102042A AR P090102042 A ARP090102042 A AR P090102042A AR 072062 A1 AR072062 A1 AR 072062A1
Authority
AR
Argentina
Prior art keywords
bibw
active substance
immediate release
dosage form
pharmaceutical dosage
Prior art date
Application number
ARP090102042A
Other languages
English (en)
Inventor
Thomas Friedl
Roman Messerschmid
Original Assignee
Boehringer Ingelheim Int
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=40941955&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR072062(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR072062A1 publication Critical patent/AR072062A1/es

Links

Classifications

    • 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
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61K9/143Intimate 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 inorganic 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
    • A61K9/14Particulate 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
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/4891Coated capsules; Multilayered drug free capsule shells
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

Una forma de dosificacion farmaceutica que contiene la sustancia activa BIBW 2992 en forma de la sal dimaleato, que proporciona un perfil de liberacion inmediata de la sustancia activa, la presente se refiere a productos intermedios compactados que comprenden sal dimaleato de BIBW 2992 (BIBW2992 MA2) en forma de un polvo preparado al utilizar una etapa de compactacion por rodillos y de tamizado combinada a partir de BIBW 2992 MA2, a mezclas intermedias preparadas a partir de dicho producto intermedio compactado, as¡ como en forma de formulaciones orales solidas que proporcionan un perfil de liberacion inmediata de la sustancia activa, hechas a partir de dicho producto intermedio compactado o a partir de dichas mezclas intermedias listas para su uso/ingesta, p. ej. formulaciones de c psula y comprimido, tales como comprimidos no revestidos o revestidos con pel¡cula preparados mediante compresion directa, y a metodos para su produccion. Reivindicacion 1: Forma de dosificacion farmaceutica de la sustancia activa BIBW 2992 MA2 (sal del API), caracterizada porque proporciona un perfil de disolucion de liberacion inmediata a lo largo del intervalo de pH fisiologicamente relevante de pH 1 - 6,8 y agua, en donde no menos de 85% (Q = 80%) se disuelve en el espacio de 60 minutos o menos in vitro under bajo las siguientes condiciones de disolucion in vitro de acuerdo con la Farmacopea Europea 6.2: aparato 2 (paletas), 900 mL de medio de disolucion de pH 1 - 6,8 o agua, y una velocidad de agitacion de 50 a 150 rpm, preferiblemente 50 o 75 rpm, a una temperatura de 37sC. Reivindicacion 4: Forma de dosificacion farmaceutica de acuerdo con cualquiera de las reivindicaciones 1 a 3, caracterizada porque proporciona un perfil de liberacion inmediata, en la que la concentracion m xima de la sustancia activa en plasma en estado estacionario (Cmax,ss) aumenta de una manera proporcional a la dosis. Reivindicacion 5: Forma de dosificacion farmaceutica de acuerdo con cualquiera de las reivindicaciones 1 a 4, caracterizada porque proporciona un perfil de liberacion inmediata, en la que el  rea bajo la curva de concentracion en plasma-tiempo del analito/sustancia activa en plasma en estado estacionario a lo largo de un intervalo de dosificacion t (AUCt,ss) aumenta de una manera proporcional en la dosis. Reivindicacion 13: Forma de dosificacion farmaceutica de acuerdo con la reivindicacion 11 o 12, para uso como una composicion farmaceutica con una actividad antiproliferativa, preferiblemente para el tratamiento de una enfermedad o estado seleccionado de enfermedades oncologicas. Reivindicacion 24: Comprimido oral solido de acuerdo con la reivindicacion 22, caracterizado por ser obtenido mediante compresion directa de una mezcla final de acuerdo con la reivindicacion 20 o 21 o mediante formacion de comprimidos de nodulos o gr nulos obtenidos mediante granulacion en humedo, en seco o en masa fundida caliente, convencional, de una mezcla intermedia de acuerdo con la reivindicacion 20 o 21. Reivindicacion 27: El comprimido de la reivindicacion 24, 25 o 26, caracterizado porque comprende 1 a 150 mg de BIBW 2992, 50 a 500 mg de soporte, aglutinante o una combinacion de los mismos, 0.1 a 5 mg de un deslizante, 1 a 15 mg de un desintegrante, y 1 a 15 mg de un lubricante.
ARP090102042A 2008-06-06 2009-06-05 Formulaciones farmaceuticas solidas que comprenden bibw 2992 AR072062A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08157800 2008-06-06
EP09160297 2009-05-14

Publications (1)

Publication Number Publication Date
AR072062A1 true AR072062A1 (es) 2010-08-04

Family

ID=40941955

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102042A AR072062A1 (es) 2008-06-06 2009-06-05 Formulaciones farmaceuticas solidas que comprenden bibw 2992

Country Status (34)

Country Link
US (1) US8545884B2 (es)
EP (1) EP2299971B1 (es)
JP (1) JP5632367B2 (es)
KR (1) KR101641517B1 (es)
CN (1) CN102056589B (es)
AR (1) AR072062A1 (es)
AU (1) AU2009254574B2 (es)
BR (1) BRPI0913379C1 (es)
CA (1) CA2726472C (es)
CL (1) CL2010001275A1 (es)
CO (1) CO6280463A2 (es)
CY (1) CY1117895T1 (es)
DK (1) DK2299971T3 (es)
EA (1) EA022168B1 (es)
EC (1) ECSP10010650A (es)
ES (1) ES2588031T3 (es)
HK (1) HK1152478A1 (es)
HR (1) HRP20161061T1 (es)
HU (1) HUE029863T2 (es)
IL (1) IL209054A (es)
MA (1) MA34030B1 (es)
ME (1) ME02478B (es)
MX (1) MX2010012939A (es)
MY (1) MY151240A (es)
NZ (1) NZ589568A (es)
PE (1) PE20100252A1 (es)
PL (1) PL2299971T3 (es)
PT (1) PT2299971T (es)
RS (1) RS54943B1 (es)
SI (1) SI2299971T1 (es)
TW (1) TWI453203B (es)
UY (1) UY31867A (es)
WO (1) WO2009147238A1 (es)
ZA (1) ZA201007805B (es)

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DE10349113A1 (de) * 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
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PL1948180T3 (pl) * 2005-11-11 2013-09-30 Boehringer Ingelheim Int Terapia skojarzona raka polegająca na podawaniu inhibitorów EGFR/HER2
CA2639936C (en) 2006-01-26 2014-06-17 Boehringer Ingelheim International Gmbh Process for preparing aminocrotonylamino-substituted quinazoline derivatives
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CN105801568B (zh) 2015-01-15 2019-07-30 杭州普晒医药科技有限公司 阿法替尼一马来酸盐晶型及其制备方法和药物组合物
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KR20180066039A (ko) * 2015-08-21 2018-06-18 프레세니어스 카비 온콜로지 리미티드 아파티닙을 포함하는 약학적 조성물
EP3156047A1 (en) 2015-10-12 2017-04-19 Sandoz Ag Afatinib-containing formulation
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK287010B6 (sk) 1999-06-21 2009-09-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyklické heterocyklické zlúčeniny, spôsob ich prípravy, farmaceutický prostriedok s ich obsahom a ich použitie
DE10063435A1 (de) 2000-12-20 2002-07-04 Boehringer Ingelheim Pharma Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
US20030225079A1 (en) 2002-05-11 2003-12-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy
DE10221018A1 (de) 2002-05-11 2003-11-27 Boehringer Ingelheim Pharma Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
DE10349113A1 (de) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
WO2007054550A1 (en) 2005-11-11 2007-05-18 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
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