ES2569354T3 - Forma farmacéutica multiparticular, que contiene productos activos de ácido nucleico de formulación mucoadhesiva, así como un procedimiento para la obtención de la forma farmacéutica - Google Patents

Forma farmacéutica multiparticular, que contiene productos activos de ácido nucleico de formulación mucoadhesiva, así como un procedimiento para la obtención de la forma farmacéutica Download PDF

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Publication number
ES2569354T3
ES2569354T3 ES05807707.4T ES05807707T ES2569354T3 ES 2569354 T3 ES2569354 T3 ES 2569354T3 ES 05807707 T ES05807707 T ES 05807707T ES 2569354 T3 ES2569354 T3 ES 2569354T3
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ES
Spain
Prior art keywords
mucoadhesive
polymer
range
multiparticular
pharmaceutical form
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
ES05807707.4T
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English (en)
Inventor
Rosario Lizio
Hans-Ulrich Petereit
Dave Trupti
Michael Gottschalk
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Roehm GmbH Darmstadt
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Evonik Roehm GmbH
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Publication of ES2569354T3 publication Critical patent/ES2569354T3/es
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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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5138Organic macromolecular compounds; Dendrimers 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • 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
    • A61K9/167Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5192Processes
    • 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
    • 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
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Nanotechnology (AREA)
  • Optics & Photonics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Forma farmacéutica oral multiparticular, que contiene aglomerados en bolas con un diámetro medio en el intervalo de 50 a 2500 μm, que está constituida esencialmente por a) una capa matriz interna que contiene nanopartículas que comprenden un producto activo de ácido nucleico, y están alojados una matriz constituida por un polímero con acción mucoadhesiva, pudiendo contener la matriz opcionalmente otras substancias auxiliares habituales desde el punto de vista farmacéutico, b) un revestimiento externo peliculado, constituido esencialmente por un polímero o copolímero aniónico, que puede ser formulado opcionalmente con substancias auxiliares habituales desde el punto de vista farmacéutico, en especial plastificantes, caracterizada por que la forma farmacológica multiparticular es formulada de modo que los aglomerados en bolas contenidos se liberan en el intervalo de pH del estómago, el revestimiento externo, mediante la selección de polímero o copolímero aniónico, o bien su formulación con substancias auxiliares y su grosor de capa, se ajusta de modo que se disuelve en intervalos de pH de 4,0 a 8,0 en el intestino en el intervalo de 15 a 60 min, de modo que la capa matriz que contiene producto activo, mucoadhesiva, se libera, se puede unir a la mucosa intestinal y liberar el producto activo en la misma, seleccionándose el polímero con acción mucoadhesiva de modo que, en un intervalo de +/- 0,5 unidades de pH, referido al valor de pH al que el revestimiento externo empieza a disolverse, presenta una acción mucoadhesiva de al menos ηb >=150 a 1000 mPa.s y una absorción de agua de un 10 a un 750 % en 15 minutos, y la fracción de producto activo de las nanopartículas en la capa matriz asciende como máximo a un 40 % en peso del contenido en el polímero con acción mucoadhesiva.

Description

farmacéutica
ES05807707.4T 2004-12-10 2005-11-05 Forma farmacéutica multiparticular, que contiene productos activos de ácido nucleico de formulación mucoadhesiva, así como un procedimiento para la obtención de la forma farmacéutica Active ES2569354T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102004059792 2004-12-10
DE102004059792A DE102004059792A1 (de) 2004-12-10 2004-12-10 Multipartikuläre Arzneiform, enthaltend mucoadhaesiv formulierte Nukleinsäure-Wirkstoffe, sowie ein Verfahren zur Herstellung der Arzneiform
PCT/EP2005/011864 WO2006061069A1 (de) 2004-12-10 2005-11-05 Multipartikuläre arzneiform, enthaltend mucoadhaesiv formulierte nukleinsäure-wirkstoffe, sowie ein verfahren zur herstellung der arzneiform

Publications (1)

Publication Number Publication Date
ES2569354T3 true ES2569354T3 (es) 2016-05-10

Family

ID=35709359

Family Applications (1)

Application Number Title Priority Date Filing Date
ES05807707.4T Active ES2569354T3 (es) 2004-12-10 2005-11-05 Forma farmacéutica multiparticular, que contiene productos activos de ácido nucleico de formulación mucoadhesiva, así como un procedimiento para la obtención de la forma farmacéutica

Country Status (17)

Country Link
US (1) US8568778B2 (es)
EP (1) EP1824457B1 (es)
JP (1) JP5578764B2 (es)
KR (1) KR101319773B1 (es)
CN (1) CN101060835B (es)
BR (1) BRPI0515815B8 (es)
CA (1) CA2586597C (es)
DE (1) DE102004059792A1 (es)
ES (1) ES2569354T3 (es)
HK (1) HK1110205A1 (es)
HU (1) HUE028793T2 (es)
IL (1) IL183753A (es)
MX (1) MX2007006343A (es)
PL (1) PL1824457T3 (es)
SI (1) SI1824457T1 (es)
TW (1) TW200635617A (es)
WO (1) WO2006061069A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8048413B2 (en) 2006-05-17 2011-11-01 Helene Huguet Site-specific intestinal delivery of adsorbents, alone or in combination with degrading molecules
RU2009102262A (ru) * 2006-06-26 2010-08-10 Мьючуал Фармасьютикал Компани, Инк. (Us) Композиции активного агента, способы их получения и способы применения
CN101801358A (zh) * 2007-07-16 2010-08-11 东北大学 治疗性稳定的纳米颗粒
DE102008048729A1 (de) * 2008-09-24 2010-03-25 Add Technologies Ltd Advanced Drug Delivery Multipartikuläre Tabletten und Verfahren zur deren Herstellung
EP2521570A4 (en) * 2009-12-29 2015-05-13 Impax Laboratories Inc SOLID ORAL DOSAGE FORMS WITH GASTRORETTENTION EFFECT, COMPRISING AN INFLATABLE HYDROPHILIC POLYMER
AU2010346995B2 (en) 2010-02-25 2014-12-04 Evonik Operations Gmbh Pharmaceutical or neutraceutical formulation
CN102250878B (zh) * 2011-06-03 2013-01-23 吉林大学 一种基于固相介质表面电荷的反转提取dna的方法
US9107851B2 (en) * 2012-10-15 2015-08-18 New Jersey Institute Of Technology Solventless mixing process for coating pharmaceutical ingredients
JP6912876B2 (ja) * 2016-10-06 2021-08-04 三洋化成工業株式会社 アクリル系医薬固形製剤用添加剤
CN110603057A (zh) * 2017-03-17 2019-12-20 俄亥俄州创新基金会 用于递送化学预防剂的纳米颗粒
BR112020023983A2 (pt) 2018-05-24 2021-02-23 Celanese Eva Performance Polymers Llc dispositivo implantável para liberação prolongada de um composto de fármaco macromolecular
WO2019226519A1 (en) 2018-05-24 2019-11-28 Celanese EVA Performance Polymers Corporation Implantable device for sustained release of a macromolecular drug compound
DE102020002360A1 (de) * 2020-04-18 2021-10-21 Friedrich-Schiller-Universität Jena Nanopartikel enthaltend Komplexe aus Nukleinsäuren und kationischen Copolymeren, Verfahren zu deren Herstellung und deren Verwendung zum Gentransfer in Zellen
WO2023249087A1 (ja) * 2022-06-24 2023-12-28 三生医薬株式会社 医薬組成物およびその製造方法

Family Cites Families (14)

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TW209174B (es) 1991-04-19 1993-07-11 Takeda Pharm Industry Co Ltd
ES2242198T3 (es) * 1995-10-25 2005-11-01 Octoplus B.V. Poliacrilatos y poli(alquil) acrilatos cationicos o las correspondientes acrilamidas para utilizar en sistemas de transfeccion sinteticos.
GB9700624D0 (en) * 1997-01-14 1997-03-05 Danbiosyst Uk Drug delivery composition
US6730735B2 (en) * 1997-07-03 2004-05-04 West Pharmaceutical Services Drug Delivery & Clinical Research Centre Limited Conjugate of polyethylene glycol and chitosan
EP1203590B1 (en) * 1999-08-09 2007-07-04 Dainippon Sumitomo Pharma Co., Ltd. Solid preparations containing chitosan powder and process for producing the same
US7803392B2 (en) * 2000-12-27 2010-09-28 University Of Kentucky Research Foundation pH-Sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules
WO2003007913A2 (en) * 2001-07-20 2003-01-30 Samir Mitragotri Method for oral drug delivery
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DE10332160A1 (de) 2003-07-15 2005-02-03 Röhm GmbH & Co. KG Multipartikuläre Arzneiform, enthaltend mucoadhaesiv formulierte Peptid- oder Protein-Wirkstoffe, sowie ein Verfahren zur Herstellung der Arzneiform
DE10353196A1 (de) * 2003-11-13 2005-06-16 Röhm GmbH & Co. KG Mehrschichtige Arzneiform mit einer die Abgabe einer modulatorischen Substanz beeinflussenden Matrix
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US20040224019A1 (en) * 2004-03-03 2004-11-11 Adi Shefer Oral controlled release system for targeted drug delivery into the cell and its nucleus for gene therapy, DNA vaccination, and administration of gene based drugs
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Also Published As

Publication number Publication date
DE102004059792A1 (de) 2006-06-14
BRPI0515815B8 (pt) 2021-05-25
IL183753A0 (en) 2007-09-20
CN101060835B (zh) 2013-01-02
KR20070085894A (ko) 2007-08-27
BRPI0515815A (pt) 2008-08-05
US8568778B2 (en) 2013-10-29
CA2586597C (en) 2013-09-10
JP5578764B2 (ja) 2014-08-27
IL183753A (en) 2016-12-29
PL1824457T3 (pl) 2016-07-29
MX2007006343A (es) 2007-07-04
EP1824457B1 (de) 2016-02-17
KR101319773B1 (ko) 2013-10-17
WO2006061069A1 (de) 2006-06-15
CA2586597A1 (en) 2006-06-15
BRPI0515815B1 (pt) 2019-02-05
SI1824457T1 (sl) 2016-06-30
HUE028793T2 (hu) 2017-01-30
CN101060835A (zh) 2007-10-24
US20090280183A1 (en) 2009-11-12
HK1110205A1 (en) 2008-07-11
JP2008522989A (ja) 2008-07-03
EP1824457A1 (de) 2007-08-29
TW200635617A (en) 2006-10-16

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