WO1999049716A3 - Verfahren zur herstellung von liposomalen wirkstoffformulierungen mit hochdruckhomogemisation - Google Patents

Verfahren zur herstellung von liposomalen wirkstoffformulierungen mit hochdruckhomogemisation Download PDF

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Publication number
WO1999049716A3
WO1999049716A3 PCT/EP1999/001993 EP9901993W WO9949716A3 WO 1999049716 A3 WO1999049716 A3 WO 1999049716A3 EP 9901993 W EP9901993 W EP 9901993W WO 9949716 A3 WO9949716 A3 WO 9949716A3
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WO
WIPO (PCT)
Prior art keywords
mixture
active agent
liposomes
producing
formulation
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/EP1999/001993
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English (en)
French (fr)
Other versions
WO1999049716A2 (de
Inventor
Clemens Unger
Ulrich Massing
Regina Moog
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.)
Individual
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Individual
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 Individual filed Critical Individual
Priority to DE59914774T priority Critical patent/DE59914774D1/de
Priority to JP2000540700A priority patent/JP2002509866A/ja
Priority to EP99916882A priority patent/EP1087752B1/de
Publication of WO1999049716A2 publication Critical patent/WO1999049716A2/de
Publication of WO1999049716A3 publication Critical patent/WO1999049716A3/de
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A61K9/1277—Preparation processes; Proliposomes
    • A61K9/1278—Post-loading, e.g. by ion or pH gradient

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Die Erfindung betrifft ein Verfahren zur Herstellung von Liposomen, die als Wirkstoff mindestens eine physiologisch wirksame oder/und diagnostische Verbindung enthalten, durch Herstellen eines Gemisches von membranbildenden Amphiphilen, Dispergieren des Gemisches in Wasser und Hochdruckhomogenisation der Dispersion bis zur Bildung der Liposomen, in dem man (a) das Gemisch so einstellt, dass man eine mindestens 20 Gew.-% lipidenthaltende Liposomenzubereitung erhält; (b) dieser Liposomenzubereitung der Wirkstoff zugegeben wird; und (c) das den Wirkstoff enthaltende Gemisch solange unter mechanischer Bewegung inkubiert wird, bis mindestens 10 % der Liposomen einen Gehalt an dem Wirkstoff aufweisen, wobei die temperatur so geregelt wird, dass keine wesentliche Phospholipidhydrolyse auftritt, die Fusion aber gesteigert wird. Weiter betrifft die Erfindung die nach diesem Verfahren hergestellte Liposomenzubereitung sowie die Verwendung dieser Liposomenzubereitung als diagnostisches oder therapeutisches Mittel, das gegebenenfalls weitere Hilfs-, Trägerstoffe oder/und Stabilisatoren enthält.
PCT/EP1999/001993 1998-03-27 1999-03-24 Verfahren zur herstellung von liposomalen wirkstoffformulierungen mit hochdruckhomogemisation Ceased WO1999049716A2 (de)

Priority Applications (3)

Application Number Priority Date Filing Date Title
DE59914774T DE59914774D1 (de) 1998-03-27 1999-03-24 Verfahren zur herstellung von liposomalen wirkstoffformulierungen
JP2000540700A JP2002509866A (ja) 1998-03-27 1999-03-24 リポソーム様作用物質調剤の製造法
EP99916882A EP1087752B1 (de) 1998-03-27 1999-03-24 Verfahren zur herstellung von liposomalen wirkstoffformulierungen

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19813773A DE19813773A1 (de) 1998-03-27 1998-03-27 Verfahren zur Herstellung von liposomalen Wirkstoffformulierungen
DE19813773.7 1998-03-27

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/937,556 Continuation US20050031679A1 (en) 1998-03-27 2004-09-09 Method for producing liposomal formulations of active ingredients

Publications (2)

Publication Number Publication Date
WO1999049716A2 WO1999049716A2 (de) 1999-10-07
WO1999049716A3 true WO1999049716A3 (de) 2000-01-13

Family

ID=7862688

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1999/001993 Ceased WO1999049716A2 (de) 1998-03-27 1999-03-24 Verfahren zur herstellung von liposomalen wirkstoffformulierungen mit hochdruckhomogemisation

Country Status (5)

Country Link
EP (1) EP1087752B1 (de)
JP (1) JP2002509866A (de)
AT (1) ATE396706T1 (de)
DE (2) DE19813773A1 (de)
WO (1) WO1999049716A2 (de)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003268087A1 (en) * 2002-08-23 2004-03-11 Ian Ma Liposomal gemcitabine compositions for better drug delivery
EP1547580A1 (de) * 2003-12-23 2005-06-29 MediGene Oncology GmbH Ladung eines Camptothecin Wirkstoffes in colloidalen Nanopartikeln
EP1674081A1 (de) 2004-12-23 2006-06-28 KTB Tumorforschungsgesellschaft mbH Herstellung von lipidbasierten Nanopartikeln unter Einsatz einer dualen asymmetrischen Zentrifuge
EP1745788A1 (de) 2005-07-22 2007-01-24 KTB Tumorforschungsgesellschaft mbH Acylglycerophospholipide zur Behandlung von Krebs und Tumorkachexie
CH715456B1 (de) 2007-04-27 2020-04-30 Mibelle Ag Kosmetisches Produkt zur topischen Anwendung für den Schutz und die Erneuerung von Hautstammzellen, welches sich von dedifferenzierten Pflanzenzellen ableitet.
EP3372223B1 (de) 2015-11-02 2024-04-17 FUJIFILM Corporation Liposomzusammensetzung und verfahren zur herstellung davon

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992006676A1 (en) * 1990-10-16 1992-04-30 Micro Vesicular Systems, Inc. Method of making oil filled paucilamellar lipid vesicles
WO1992010166A1 (en) * 1990-12-11 1992-06-25 Sintetica S.A. Method for making liposomes of enhanced entrapping capacity toward foreign substances to be encapsulated
US5616341A (en) * 1987-03-05 1997-04-01 The Liposome Company, Inc. High drug:lipid formulations of liposomal antineoplastic agents
WO1997035560A1 (en) * 1996-03-28 1997-10-02 The Board Of Trustees Of The University Of Illinois Materials and methods for making improved echogenic liposome compositions

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5616341A (en) * 1987-03-05 1997-04-01 The Liposome Company, Inc. High drug:lipid formulations of liposomal antineoplastic agents
WO1992006676A1 (en) * 1990-10-16 1992-04-30 Micro Vesicular Systems, Inc. Method of making oil filled paucilamellar lipid vesicles
WO1992010166A1 (en) * 1990-12-11 1992-06-25 Sintetica S.A. Method for making liposomes of enhanced entrapping capacity toward foreign substances to be encapsulated
WO1997035560A1 (en) * 1996-03-28 1997-10-02 The Board Of Trustees Of The University Of Illinois Materials and methods for making improved echogenic liposome compositions

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BAUER, KURT H.: "A simple preparatory method for liposomes and the experimental preparation of hemoglobin- and insulin-liposomes. Review of an experimental series on the preparation of parenterally and perorally applied liposomes", PHARM. UNSERER ZEIT, 1992, 21, 71-5, XP002114668 *
PONS M ET AL: "ENROFLOXACIN LOADED LIPOSOMES OBTAINED BY HIGH SPEED DISPERSION METHOD", CHEMICAL AND PHARMACEUTICAL BULLETIN, vol. 43, no. 6, 1 June 1995 (1995-06-01), pages 983 - 987, XP000515136, ISSN: 0009-2363 *
TARDI C ET AL: "Erosion and controlled release properties of semisolid vesicular phospholipid dispersions.", J CONTROLLED RELEASE, NOV 13 1998, 55 (2-3) P261-70, NETHERLANDS, XP002114669 *

Also Published As

Publication number Publication date
WO1999049716A2 (de) 1999-10-07
DE19813773A1 (de) 1999-09-30
ATE396706T1 (de) 2008-06-15
DE59914774D1 (de) 2008-07-10
JP2002509866A (ja) 2002-04-02
EP1087752B1 (de) 2008-05-28
EP1087752A2 (de) 2001-04-04

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