ES2562279T3 - Formulaciones de apixabán - Google Patents

Formulaciones de apixabán Download PDF

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Publication number
ES2562279T3
ES2562279T3 ES11707284.3T ES11707284T ES2562279T3 ES 2562279 T3 ES2562279 T3 ES 2562279T3 ES 11707284 T ES11707284 T ES 11707284T ES 2562279 T3 ES2562279 T3 ES 2562279T3
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ES
Spain
Prior art keywords
apixaban
tablets
particles
dissolution
apixabán
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.)
Active
Application number
ES11707284.3T
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English (en)
Inventor
Jatin Patel
Charles Frost
Jingpin Jia
Chandra Vema-Varapu
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.)
Bristol Myers Squibb Co
Pfizer Inc
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Bristol Myers Squibb Co
Pfizer Inc
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Application filed by Bristol Myers Squibb Co, Pfizer Inc filed Critical Bristol Myers Squibb Co
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Publication of ES2562279T3 publication Critical patent/ES2562279T3/es
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    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • 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
    • 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
    • A61K9/4833—Encapsulating processes; Filling of capsules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring

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

Abstract

Un comprimido o una cápsula que comprenden una composición farmacéutica, en donde la composición farmacéutica comprende apixabán y un diluyente o un vehículo farmacéuticamente aceptables, en donde el apixabán está en forma de partículas y cristalina y las partículas individuales de apixabán, tanto si las partículas existen individualmente como si están aglomeradas, tienen un D90 igual a o menor de 89 μm medido por dispersión de luz láser.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
Total
100,00 mg 400 mg
Revestimiento de película
3,5 14,0
Total
103,5 mg 414 mg
La Tabla 4 muestra las composiciones de los comprimidos de apixabán preparados usando el proceso de granulación en húmedo que se ha evaluado en un estudio de BE.
Tabla 4
Ingredientes
Granulación en húmedo
5 % p/p de fármaco cargado en la granulación (% p/p)
20 mg de comprimido (mg/comprimido)
Intragranular
Apixabán
5,00 20,00
Lactosa monohidrato
70,0 280,00
Celulosa microcristalina
5,00 60,00
Croscarmelosa de sodio
2,50 10,00
Povidona
4,50 18,00
Agua purificada
17,40 69,60
Extragranular
Croscarmelosa de sodio
2,50 10,00
Estearato de magnesio
0,50 2,09
Celulosa microcristalina
10,00 10,09
Total
100,00 400,00
Revestimiento de película
3,5 14,0
Total
103,5 mg 414,0
La Tabla 5 y la Tabla 5a muestran los datos de disolución que indican que tener un proceso de granulación en seco dará como resultado una disolución más rápida comparada con la de un proceso de granulación en húmedo. Como se muestra en la Tabla 5, los comprimidos de 20 mg fabricados usando un proceso de granulación en seco tenían
10 un 79 % de apixabán disuelto en 30 minutos frente al 62 % de apixabán disuelto a los 30 minutos para los comprimidos de 20 mg fabricados usando un proceso de granulación en húmedo. El ensayo de disolución en HCl 0,1 N también indicó un comportamiento similar de disolución más rápida de los comprimidos fabricados usando el proceso de granulación en seco (58 % en 30 min), comparado con el proceso de granulación en húmedo (45 % en 30 min).
15 Tabla 5
Tiempo (minutos)
% de apixabán disuelto (USP II, 75 rpm, SLS al 0,05 % en fosfato 50 mM, pH 6,8)
Granulación en húmedo de comprimidos de 20 mg
Granulación en seco de comprimidos de 20 mg
10
38 47
20
54 70
30
62 79
45
71 86
60
76 90
Tamaño de partícula D90 (µm) del APT
83,8 83,8
Tabla 5a
Tiempo (minutos)
% de apixabán disuelto (USP II, 75 rpm, HCl 0,1 N)
Granulación en húmedo de comprimidos de 20 mg
Granulación en seco de comprimidos de 20 mg
10
30 41
7
imagen6
Las Figuras 3 y 4 ilustran los datos de disolución que muestran que mientras que el tamaño de partícula afecta a la disolución, controlar el tamaño de partícula a menos de 89 micrómetros dará como resultado una velocidad de disolución que asegurará las exposiciones in vivo consistentes. Como se ha indicado en las Figuras 3 y 4, se esperan exposiciones consistentes cuando los comprimidos de apixabán tengan más del 77 % de apixabán disuelto 5 en 30 minutos. Dado que los comprimidos con 89 micrómetros tienen > 77 % disuelto a los 30 minutos, estos comprimidos también exhibirán exposiciones que son equivalentes a las exposiciones de los comprimidos fabricados con partículas más pequeñas (tales como los comprimidos con partículas de 10 micrómetros mostrados a continuación). Mientras que la velocidad de disolución a un tamaño de partícula de apixabán de 119 micrómetros es ligeramente mayor del 77 % en 30 min para los comprimidos de 5 mg de apixabán (Figura 4), el umbral del tamaño
10 de partícula reivindicado es de menos de 89 micrómetros. Esto permite la variabilidad típica (RSD = 2 a 3 %) en los resultados de disolución, de manera que la biodisponibilidad oral de los comprimidos coincida consistentemente con la de la solución.
9

Claims (1)

  1. imagen1
    imagen2
ES11707284.3T 2010-02-25 2011-02-24 Formulaciones de apixabán Active ES2562279T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30805610P 2010-02-25 2010-02-25
US308056P 2010-02-25
PCT/US2011/025994 WO2011106478A2 (en) 2010-02-25 2011-02-24 Apixaban formulations

Publications (1)

Publication Number Publication Date
ES2562279T3 true ES2562279T3 (es) 2016-03-03

Family

ID=43901603

Family Applications (5)

Application Number Title Priority Date Filing Date
ES17178613T Active ES2757603T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán
ES11707284.3T Active ES2562279T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán
ES15190823T Active ES2714363T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán
ES17175864T Active ES2767848T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán
ES17175788T Active ES2758031T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES17178613T Active ES2757603T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán

Family Applications After (3)

Application Number Title Priority Date Filing Date
ES15190823T Active ES2714363T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán
ES17175864T Active ES2767848T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán
ES17175788T Active ES2758031T3 (es) 2010-02-25 2011-02-24 Formulaciones de apixabán

Country Status (31)

Country Link
US (5) US9326945B2 (es)
EP (7) EP3017811B1 (es)
JP (4) JP5846647B2 (es)
KR (4) KR20170126016A (es)
CN (3) CN109602716A (es)
AU (1) AU2011220775B2 (es)
BR (1) BR112012021337A8 (es)
CA (1) CA2791171C (es)
CO (1) CO6640207A2 (es)
CY (5) CY1117434T1 (es)
DK (5) DK3017811T3 (es)
ES (5) ES2757603T3 (es)
HK (2) HK1243945B (es)
HR (5) HRP20160179T1 (es)
HU (4) HUE043932T2 (es)
IL (3) IL309564A (es)
IN (1) IN2012DN06587A (es)
LT (4) LT3246021T (es)
MX (3) MX2012009244A (es)
NZ (1) NZ601738A (es)
PE (3) PE20210468A1 (es)
PL (5) PL2538925T3 (es)
PT (5) PT3251660T (es)
RS (5) RS59593B1 (es)
RU (1) RU2685724C2 (es)
SG (2) SG182750A1 (es)
SI (5) SI2538925T1 (es)
SM (5) SMT201900650T1 (es)
TR (1) TR201903195T4 (es)
WO (1) WO2011106478A2 (es)
ZA (1) ZA201205807B (es)

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