ES2531215T3 - Sistemas de administración de fármacos que comprenden un agente de bloqueo selectivo de la serotonina 5-HT3 débilmente básico y ácidos orgánicos - Google Patents

Sistemas de administración de fármacos que comprenden un agente de bloqueo selectivo de la serotonina 5-HT3 débilmente básico y ácidos orgánicos Download PDF

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Publication number
ES2531215T3
ES2531215T3 ES07717465T ES07717465T ES2531215T3 ES 2531215 T3 ES2531215 T3 ES 2531215T3 ES 07717465 T ES07717465 T ES 07717465T ES 07717465 T ES07717465 T ES 07717465T ES 2531215 T3 ES2531215 T3 ES 2531215T3
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Spain
Prior art keywords
weakly basic
coating
water
organic acid
disposed
Prior art date
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Active
Application number
ES07717465T
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English (en)
Inventor
Gopi Venkatesh
Jin-Wang Lai
Nehal Vyas
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Adare Pharmaceuticals Inc
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Aptalis Pharmatech Inc
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    • 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
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • 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
    • A61K9/2072Pills, 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
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • 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
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals

Abstract

Una forma de dosificación farmacéutica multiparticulada que comprende perlas de liberación sostenida (LS) y/o uno o más poblaciones de perlas de liberación pulsátil controlada (LPC) de: un fármaco débilmente básico, fármaco débilmente básico que comprende un agente de bloqueo selectivo de la serotonina 5-HT3 que contiene nitrógeno (N), o una sal farmacéuticamente aceptable del mismo, que tiene un pKa en el intervalo de aproximadamente 5 a 14, y una solubilidad no superior a aproximadamente 200 μg/ml a pH 6,8, y al menos un ácido orgánico farmacéuticamente aceptable como solubilizador; en la que el fármaco débilmente básico y el ácido orgánico no entran en contacto entre sí en la forma de dosificación; en la que dichas perlas de LS comprenden: un recubrimiento (barrera) de LS que comprende un polímero insoluble en agua solo o en combinación con un polímero hidrosoluble; estando dicho recubrimiento (barrera) de LS dispuesto sobre perlas de liberación inmediata (LI) que comprenden: el fármaco débilmente básico dispuesto sobre un recubrimiento de barrera interior que comprende un polímero insoluble en agua solo o en combinación con un polímero hidrosoluble o un polímero entérico; estando dicho recubrimiento de barrera interior dispuesto sobre partículas de núcleo de ácido orgánico que comprenden al menos un ácido orgánico farmacéuticamente aceptable; y en la que dichas perlas de LPC comprenden: un recubrimiento exterior de tiempo de retardo que comprende un polímero insoluble en agua en combinación con un polímero entérico, proporcionando dicho recubrimiento exterior de tiempo de retardo un tiempo de retardo de aproximadamente 2 a aproximadamente 17 horas antes del inicio de la liberación del fármaco débilmente básico; estando dicho recubrimiento exterior de tiempo de retardo dispuesto sobre perlas de liberación inmediata (LI) que comprenden: el fármaco débilmente básico dispuesto sobre un recubrimiento de barrera interior que comprende un polímero insoluble en agua solo o en combinación con un polímero hidrosoluble o un polímero entérico; estando dicho recubrimiento de barrera interior dispuesto sobre partículas de núcleo de ácido orgánico que comprenden al menos un ácido orgánico farmacéuticamente aceptable; en donde dicha forma de dosificación es adecuada para una pauta de dosificación de una vez al día en pacientes que necesitan dicha medicación.
ES07717465T 2006-01-27 2007-01-29 Sistemas de administración de fármacos que comprenden un agente de bloqueo selectivo de la serotonina 5-HT3 débilmente básico y ácidos orgánicos Active ES2531215T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US76275006P 2006-01-27 2006-01-27
PCT/US2007/061217 WO2007090082A2 (en) 2006-01-27 2007-01-29 Drug delivery systems comprising weakly basic selective serotonin 5-ht3 blocking agent and organic acids

Publications (1)

Publication Number Publication Date
ES2531215T3 true ES2531215T3 (es) 2015-03-11

Family

ID=38325269

Family Applications (2)

Application Number Title Priority Date Filing Date
ES11001973.4T Active ES2550035T3 (es) 2006-01-27 2007-01-29 Sistemas de administración de fármacos que comprenden un agente de bloqueo selectivo de la serotonina 5-HT3 débilmente básico y ácidos orgánicos
ES07717465T Active ES2531215T3 (es) 2006-01-27 2007-01-29 Sistemas de administración de fármacos que comprenden un agente de bloqueo selectivo de la serotonina 5-HT3 débilmente básico y ácidos orgánicos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES11001973.4T Active ES2550035T3 (es) 2006-01-27 2007-01-29 Sistemas de administración de fármacos que comprenden un agente de bloqueo selectivo de la serotonina 5-HT3 débilmente básico y ácidos orgánicos

Country Status (14)

Country Link
US (1) US20070190145A1 (es)
EP (2) EP2363117B1 (es)
JP (3) JP5433236B2 (es)
KR (1) KR101413613B1 (es)
CN (2) CN101410094B (es)
AU (1) AU2007211091B8 (es)
BR (1) BRPI0707324A2 (es)
CA (1) CA2640460C (es)
ES (2) ES2550035T3 (es)
IL (1) IL193020A0 (es)
NZ (1) NZ570039A (es)
RU (1) RU2490012C2 (es)
WO (1) WO2007090082A2 (es)
ZA (1) ZA200806497B (es)

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Also Published As

Publication number Publication date
WO2007090082A2 (en) 2007-08-09
JP2013249305A (ja) 2013-12-12
ES2550035T3 (es) 2015-11-04
CN101410094B (zh) 2013-04-17
JP2016014048A (ja) 2016-01-28
NZ570039A (en) 2011-07-29
EP1976491B1 (en) 2014-12-17
EP2363117A1 (en) 2011-09-07
CA2640460A1 (en) 2007-08-09
AU2007211091A8 (en) 2013-08-29
JP5918179B2 (ja) 2016-05-18
KR101413613B1 (ko) 2014-07-10
JP5433236B2 (ja) 2014-03-05
KR20080098627A (ko) 2008-11-11
RU2490012C2 (ru) 2013-08-20
US20070190145A1 (en) 2007-08-16
RU2008134912A (ru) 2010-03-10
BRPI0707324A2 (pt) 2011-05-03
ZA200806497B (en) 2009-12-30
CN103211779B (zh) 2016-03-16
JP2009524697A (ja) 2009-07-02
AU2007211091A1 (en) 2007-08-09
EP1976491A2 (en) 2008-10-08
AU2007211091B8 (en) 2013-08-29
IL193020A0 (en) 2009-09-22
WO2007090082A3 (en) 2007-12-21
CN103211779A (zh) 2013-07-24
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AU2007211091B2 (en) 2013-05-02
CA2640460C (en) 2015-05-26

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