WO2004030649A3 - Methode zur herstellung und stabilisierung von mikro- und nanosuspensionen mit amphiphilen und polyelektrolyten - Google Patents

Methode zur herstellung und stabilisierung von mikro- und nanosuspensionen mit amphiphilen und polyelektrolyten Download PDF

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Publication number
WO2004030649A3
WO2004030649A3 PCT/EP2003/010673 EP0310673W WO2004030649A3 WO 2004030649 A3 WO2004030649 A3 WO 2004030649A3 EP 0310673 W EP0310673 W EP 0310673W WO 2004030649 A3 WO2004030649 A3 WO 2004030649A3
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WO
WIPO (PCT)
Prior art keywords
methods
polyelectrolytes
envelope
active ingredient
capsule
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PCT/EP2003/010673
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English (en)
French (fr)
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WO2004030649A2 (de
Inventor
Volker Fehring
Karsten Cremer
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Capsulution Nanoscience Ag
Volker Fehring
Karsten Cremer
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Application filed by Capsulution Nanoscience Ag, Volker Fehring, Karsten Cremer filed Critical Capsulution Nanoscience Ag
Priority to AU2003277900A priority Critical patent/AU2003277900A1/en
Publication of WO2004030649A2 publication Critical patent/WO2004030649A2/de
Publication of WO2004030649A3 publication Critical patent/WO2004030649A3/de

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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
    • A61K9/48—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
    • A61K9/5161—Polysaccharides, e.g. alginate, chitosan, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/5089—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
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
    • B01J13/02—Making microcapsules or microballoons
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
    • B01J13/02—Making microcapsules or microballoons
    • B01J13/06—Making microcapsules or microballoons by phase separation
    • B01J13/10—Complex coacervation, i.e. interaction of oppositely charged particles
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
    • B01J13/02—Making microcapsules or microballoons
    • B01J13/20—After-treatment of capsule walls, e.g. hardening
    • B01J13/22—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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth 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
    • 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
    • A61K9/10—Dispersions; Emulsions
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds 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
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • 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
    • A61K9/5073—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 having two or more different coatings optionally including drug-containing subcoatings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Dispersion Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Nanotechnology (AREA)
  • Biomedical Technology (AREA)
  • Optics & Photonics (AREA)
  • Medicinal Preparation (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • General Preparation And Processing Of Foods (AREA)

Abstract

Die vorliegende Erfindung beschreibt die Darstellung stabiler Suspensionen schwer wasserlöslicher bzw. wasserunlöslicher organischer Verbindungen, insbesondere von pharmazeutischen Wirkstoffen, diagnostischen Substanzen oder Substanzen zur Nahrungsergänzung. Die mittels bekannter Mahl-, Präzipitations- oder Kzistallisationsverfahren hergestellten Partikel mit einem mittleren Durchmesser kleiner 5 µm werden erfindungsgemäss mit einer Kapselhülle stabilisiert, die schrittweise aus bis zu 8 Schichten entgegengesetzt geladener Polyelektrolyte aufgebaut ist. Diese Hülle kann neben den Polyelektrolyten ebenfalls geladene Amphiphile beinhalten und führt durch die spezielle Abstimmung zwischen der Dicke der Hülle und ihrer Permeabilität zu keiner wesentlichen Verzögerung der Diffusion gelöster Wirkstoffmoteküle aus der Kapsel heraus. Diese Kapseln gewährleisten, dass die Freisetzung des Wirkstoffs wesentlich schneller, als die Wirkstoffauflösung ausgehend vom Zustand eines hilfsstofffreien Pulvers erfolgt. Die Kapseln bzw. ihre stabilen Suspensionen können zur Darstellung neuer pharmazeutischer Zubereitungen benutzt werden, insbesondere zur Herstellung schnellzerfallender Lyophilisate, Filme und Tabletten.
PCT/EP2003/010673 2002-09-25 2003-09-25 Methode zur herstellung und stabilisierung von mikro- und nanosuspensionen mit amphiphilen und polyelektrolyten WO2004030649A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003277900A AU2003277900A1 (en) 2002-09-25 2003-09-25 Methods for producing and stabilising microsuspensions and nanosuspensions by means of amphiphiles and polyelectrolytes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2002144503 DE10244503A1 (de) 2002-09-25 2002-09-25 Methode zur Herstellung und Stabilisierung von Mikro- und Nanosuspensionen mit Amphiphilen und Polyelektrolyten
DE10244503.6 2002-09-25

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WO2004030649A2 WO2004030649A2 (de) 2004-04-15
WO2004030649A3 true WO2004030649A3 (de) 2004-06-03

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AU (1) AU2003277900A1 (de)
DE (1) DE10244503A1 (de)
WO (1) WO2004030649A2 (de)

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* Cited by examiner, † Cited by third party
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US7101575B2 (en) 1998-03-19 2006-09-05 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. Production of nanocapsules and microcapsules by layer-wise polyelectrolyte self-assembly
US20050281886A1 (en) * 2004-05-06 2005-12-22 Ivrea Pharmaceuticals, Inc. Particles for the delivery of active agents
CN101188996B (zh) * 2005-04-27 2013-03-27 巴克斯特国际公司 表面改性的微粒及其形成和使用方法
SG144763A1 (en) * 2007-01-24 2008-08-28 Univ Singapore Reverse phase layer-by-layer encapsulation of highly water soluble materials
ES2820335T3 (es) 2007-04-16 2021-04-20 Corium Inc Matrices de microagujas coladas con disolvente que contienen agente activo
WO2009048607A1 (en) 2007-10-10 2009-04-16 Corium International, Inc. Vaccine delivery via microneedle arrays
EP2172193A1 (de) 2008-10-02 2010-04-07 Capsulution Nanoscience AG Verbesserte Nanopartikel-Zusammensetzungen schlecht löslicher Verbindungen
DE102009004368A1 (de) 2009-01-08 2010-07-15 Heraeus Kulzer Gmbh Dentalmaterialien enthaltend antimikrobielle Wirkstoffe zur Verhinderung von Plaque-Anlagerungen
EP2566501B1 (de) 2010-05-04 2019-03-13 Corium International, Inc. Verfahren und vorrichtung zur transdermalen verabreichung von parathormon mithilfe eines mikroprojektions-arrays
MX2015008157A (es) 2012-12-21 2016-02-22 Corium Int Inc Microarreglo para la entrega de agente terapeutico y metodos de uso.
CN105142711B (zh) 2013-03-12 2019-01-22 考里安国际公司 微突起施加器
EP4194028A1 (de) 2013-03-15 2023-06-14 Corium Pharma Solutions, Inc. Mehrfachaufprall-mikroprojektionsapplikatoren
ES2908339T3 (es) 2013-03-15 2022-04-28 Corium Inc Micromatriz para el suministro de un agente terapéutico y métodos de uso
JP2016514133A (ja) 2013-03-15 2016-05-19 コリウム インターナショナル， インコーポレイテッド ポリマーを含まない微細構造物を含むマイクロアレイ、製造方法および使用方法
EP3188714A1 (de) 2014-09-04 2017-07-12 Corium International, Inc. Mikrostrukturanordnung, verfahren zur herstellung und verfahren zur verwendung
US20180071261A1 (en) * 2015-03-10 2018-03-15 Lumos Pharma, Inc. Cyclocreatine microsuspension
CN104686979B (zh) * 2015-03-24 2017-06-27 浙江海洋学院 一种山核桃壳烟熏液纳米胶囊及其制备方法和用途
US10857093B2 (en) 2015-06-29 2020-12-08 Corium, Inc. Microarray for delivery of therapeutic agent, methods of use, and methods of making
CN112245409B (zh) * 2020-10-23 2022-03-15 安徽大学 一种植物蛋白-熊去氧胆酸缓释纳米粒复合微囊及其制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2135954A (en) * 1980-11-14 1984-09-12 Akad Wissenschaften Ddr Microcapsules and process for the production thereof
WO1999047252A2 (de) * 1998-03-19 1999-09-23 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Herstellung von nano- und mikrokapseln durch schichtweise polyelektrolyt-selbstassemblierung
EP1116516A1 (de) * 2000-01-13 2001-07-18 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Beschichtung von soliden Partikeln durch Mehrlegen von Polymeren
WO2001087475A1 (en) * 2000-05-19 2001-11-22 Ecole Polytechnique Federale De Lausanne Materials and methods relating to encapsulation
WO2002009864A1 (de) * 2000-08-02 2002-02-07 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Verkapselung von flüssigen templatpartikeln
DE10100689A1 (de) * 2001-01-09 2002-07-18 Henkel Kgaa Wasch- und reinigungsaktive Substanzen enthaltende Mikrokapseln

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2135954A (en) * 1980-11-14 1984-09-12 Akad Wissenschaften Ddr Microcapsules and process for the production thereof
WO1999047252A2 (de) * 1998-03-19 1999-09-23 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Herstellung von nano- und mikrokapseln durch schichtweise polyelektrolyt-selbstassemblierung
EP1116516A1 (de) * 2000-01-13 2001-07-18 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Beschichtung von soliden Partikeln durch Mehrlegen von Polymeren
WO2001087475A1 (en) * 2000-05-19 2001-11-22 Ecole Polytechnique Federale De Lausanne Materials and methods relating to encapsulation
WO2002009864A1 (de) * 2000-08-02 2002-02-07 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Verkapselung von flüssigen templatpartikeln
DE10100689A1 (de) * 2001-01-09 2002-07-18 Henkel Kgaa Wasch- und reinigungsaktive Substanzen enthaltende Mikrokapseln

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Publication number Publication date
WO2004030649A2 (de) 2004-04-15
AU2003277900A8 (en) 2004-04-23
AU2003277900A1 (en) 2004-04-23
DE10244503A1 (de) 2004-04-08

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