[go: up one dir, main page]

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

Info

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
Authority
WO
WIPO (PCT)
Prior art keywords
methods
polyelectrolytes
envelope
active ingredient
capsule
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.)
Ceased
Application number
PCT/EP2003/010673
Other languages
English (en)
French (fr)
Other versions
WO2004030649A2 (de
Inventor
Volker Fehring
Karsten Cremer
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.)
Capsulution Nanoscience AG
Original Assignee
Capsulution Nanoscience AG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Capsulution Nanoscience AG 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
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K9/48—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

Landscapes

  • 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 Ceased 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
DE10244503.6 2002-09-25
DE2002144503 DE10244503A1 (de) 2002-09-25 2002-09-25 Methode zur Herstellung und Stabilisierung von Mikro- und Nanosuspensionen mit Amphiphilen und Polyelektrolyten

Publications (2)

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

Family

ID=31984021

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/010673 Ceased WO2004030649A2 (de) 2002-09-25 2003-09-25 Methode zur herstellung und stabilisierung von mikro- und nanosuspensionen mit amphiphilen und polyelektrolyten

Country Status (3)

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

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU2005240189A1 (en) * 2004-05-06 2005-11-17 Ivrea Pharmaceuticals, Inc. Particles for the delivery of active agents
AU2006241145B2 (en) * 2005-04-27 2011-04-28 Baxter Healthcare S. A. Surface-modified microparticles and methods of forming and using the same
SG144763A1 (en) * 2007-01-24 2008-08-28 Univ Singapore Reverse phase layer-by-layer encapsulation of highly water soluble materials
US9114238B2 (en) 2007-04-16 2015-08-25 Corium International, Inc. Solvent-cast microprotrusion arrays containing active ingredient
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
US9687641B2 (en) 2010-05-04 2017-06-27 Corium International, Inc. Method and device for transdermal delivery of parathyroid hormone using a microprojection array
JP6865524B2 (ja) 2012-12-21 2021-04-28 コリウム， インコーポレイテッド 治療剤を送達するためのマイクロアレイおよび使用方法
JP6487899B2 (ja) 2013-03-12 2019-03-20 コリウム インターナショナル， インコーポレイテッド 微小突起アプリケータ
EP2968118B1 (de) 2013-03-15 2022-02-09 Corium, Inc. Mikroarray zur freisetzung therapeutischer wirkstoffe und verfahren zur verwendung
AU2014237279B2 (en) 2013-03-15 2018-11-22 Corium Pharma Solutions, Inc. Microarray with polymer-free microstructures, methods of making, and methods of use
WO2014150285A2 (en) 2013-03-15 2014-09-25 Corium International, Inc. Multiple impact microprojection applicators and methods of use
EP3188714A1 (de) 2014-09-04 2017-07-12 Corium International, Inc. Mikrostrukturanordnung, verfahren zur herstellung und verfahren zur verwendung
CN107427494A (zh) * 2015-03-10 2017-12-01 卢莫斯制药公司 环肌酸微混悬剂
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
WO2017004067A1 (en) 2015-06-29 2017-01-05 Corium International, 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

Also Published As

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

Similar Documents

Publication Publication Date Title
WO2004030649A3 (de) Methode zur herstellung und stabilisierung von mikro- und nanosuspensionen mit amphiphilen und polyelektrolyten
Kalepu et al. Insoluble drug delivery strategies: review of recent advances and business prospects
DE69105106T2 (de) Im wasser schnell suspendierbare pharmazeutische zusammensetzung.
JP4077803B2 (ja) 多孔質アパタイト粒状物を用いる安定で、味覚をマスクした製薬剤形
EP2558080B1 (de) Verbesserungen im zusammenhang mit antiviralen zusammensetzungen
CN102307573B (zh) 用于联合治疗的片剂
EP2243495A1 (de) Wirkstofffreisetzungssystem, seine herstellung und verwendung
JP2015007105A (ja) シームレスマイクロカプセルを含む固形経口剤形
JPS5914446B2 (ja) ニフエジピン含有固形製剤及びその製造方法
Rashid et al. Bioavailability enhancement of poorly soluble drugs: the holy grail in pharma industry
JP2014516080A5 (de)
Prajapati et al. Conventional and alternative pharmaceutical methods to improve oral bioavailability of lipophilic drugs
JP6103111B1 (ja) 経口医薬組成物及び該組成物からなる粒子状製剤の製造方法
WO2005025542A1 (ja) 脂溶性薬物封入微粒子、その製造法およびそれを含有する製剤
Armstrong et al. Formulation and scale-up of fast-dissolving lumefantrine nanoparticles for oral malaria therapy
Kumar et al. Design Development and Characterization of Nicardipine Solid Lipid Nano-Particulars
Kavitha et al. Effect of dissolution rate by liquisolid compact approach: an overview
KR20060021278A (ko) 고체 나노미터 의약 및 이의 제조방법
Khatri et al. Solubility enhancement techniques: an overview
CN103228279B (zh) 包含瑞伐拉赞或其盐的可注射液体组合物或可注射干粉
Karri et al. Fabrication of efavirenz freeze dried nanocrystals: formulation, physicochemical characterization, in vitro and ex vivo evaluation
Charumanee et al. Improvement of the dissolution rate of piroxicam by surface solid dispersion
Pawar et al. Development, characterization and evaluation of tinidazole nanosuspension for treatment of amoebiasis
JP2016124800A (ja) 生理活性物質含有造粒物及びその製造方法
Obeidat et al. Evaluation of enteric matrix microspheres prepared by emulsion–solvent evaporation using scanning electron microscopy

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP