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
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.)
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

    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K9/50—Microcapsules 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
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5138—Organic macromolecular compounds; Dendrimers obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • 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
    • A61K9/167—Agglomerates; 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
    • A61K9/1676—Agglomerates; 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
    • 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
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/2072—Pills, 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
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered 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
    • 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
    • A61K9/50—Microcapsules 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
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5192—Processes
    • 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
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Nanotechnology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (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
DE102004059792A DE102004059792A1 (de) 2004-12-10 2004-12-10 Multipartikuläre Arzneiform, enthaltend mucoadhaesiv formulierte Nukleinsäure-Wirkstoffe, sowie ein Verfahren zur Herstellung der Arzneiform
DE102004059792 2004-12-10
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)

Families Citing this family (14)

* 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
EP2037888A2 (en) * 2006-06-26 2009-03-25 Mutual Pharmaceutical Company, Inc. Active agent formulations, methods of making, and methods of use
US20110038939A1 (en) * 2007-07-16 2011-02-17 Northeastern University Therapeutic stable nanoparticles
DE102008048729A1 (de) * 2008-09-24 2010-03-25 Add Technologies Ltd Advanced Drug Delivery Multipartikuläre Tabletten und Verfahren zur deren Herstellung
US20130064896A1 (en) * 2009-12-29 2013-03-14 Laman Lynn Alani Gastroretentive Solid Oral Dosage Forms with Swellable Hydrophilic Polymer
CA2790918C (en) 2010-02-25 2019-08-06 Evonik Roehm Gmbh Pharmaceutical or neutraceutical formulation comprising a core and a polymeric coating
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
AU2018234844B2 (en) * 2017-03-17 2024-01-25 Ohio State Innovation Foundation Nanoparticles for delivery of chemopreventive agents
EP3801378A4 (en) 2018-05-24 2022-02-23 Celanese EVA Performance Polymers LLC IMPLANTABLE DEVICE FOR THE DELAYED RELEASE OF A MACROMOLECULAR DRUG COMPOUND
JP2021524841A (ja) 2018-05-24 2021-09-16 セラニーズ・イーブイエイ・パフォーマンス・ポリマーズ・エルエルシー 高分子薬剤化合物の持続放出用の埋め込み型デバイス
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)

* Cited by examiner, † Cited by third party
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TW209174B (es) 1991-04-19 1993-07-11 Takeda Pharm Industry Co Ltd
ATE294875T1 (de) 1995-10-25 2005-05-15 Octoplus B V Kationische polyacrylate und poly(alkyl)acrylate oder die entsprechende acrylamide zur verwendung in synthetischen transfektions-systemen
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
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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
AU2002319653A1 (en) * 2001-07-20 2003-03-03 Samir Mitragotri Method for oral drug delivery
US7670627B2 (en) * 2002-12-09 2010-03-02 Salvona Ip Llc pH triggered targeted controlled release systems for the delivery of pharmaceutical active ingredients
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
DE10353186A1 (de) 2003-11-13 2005-06-16 Röhm GmbH & Co. KG Mehrschichtige Arzneiform, enthaltend eine in Bezug auf die Wirkstoffabgabe modulatorisch wirkende Substanz
DE10353196A1 (de) 2003-11-13 2005-06-16 Röhm GmbH & Co. KG Mehrschichtige Arzneiform mit einer die Abgabe einer modulatorischen Substanz beeinflussenden Matrix
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
DE102004036437A1 (de) 2004-07-27 2006-03-23 Röhm GmbH & Co. KG Multipartikuläre Arzneiform für wenig lösliche Wirkstoffe, sowie ein Verfahren zur Herstellung der Arzneiform
DE102006035549A1 (de) 2006-07-27 2008-01-31 Evonik Röhm Gmbh Arzneiform mit mindestens zweischichtiger Trennschicht

Also Published As

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

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