EP0731689A1 - Procede permettant d'augmenter la stabilite de suspensions de liposomes contenant des principes actifs hydrophiles - Google Patents

Procede permettant d'augmenter la stabilite de suspensions de liposomes contenant des principes actifs hydrophiles

Info

Publication number
EP0731689A1
EP0731689A1 EP95903305A EP95903305A EP0731689A1 EP 0731689 A1 EP0731689 A1 EP 0731689A1 EP 95903305 A EP95903305 A EP 95903305A EP 95903305 A EP95903305 A EP 95903305A EP 0731689 A1 EP0731689 A1 EP 0731689A1
Authority
EP
European Patent Office
Prior art keywords
liposome
contain
liposome suspensions
stability
liposomes
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.)
Withdrawn
Application number
EP95903305A
Other languages
German (de)
English (en)
Inventor
Andreas Sachse
Georg Rössling
Jens Leike
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.)
Bayer Pharma AG
Original Assignee
Schering 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 Schering AG filed Critical Schering AG
Publication of EP0731689A1 publication Critical patent/EP0731689A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/18—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by a special physical form, e.g. emulsions, microcapsules, liposomes
    • A61K49/1806—Suspensions, emulsions, colloids, dispersions
    • A61K49/1812—Suspensions, emulsions, colloids, dispersions liposomes, polymersomes, e.g. immunoliposomes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/04—X-ray contrast preparations
    • A61K49/0433—X-ray contrast preparations containing an organic halogenated X-ray contrast-enhancing agent
    • A61K49/0447—Physical forms of mixtures of two different X-ray contrast-enhancing agents, containing at least one X-ray contrast-enhancing agent which is a halogenated organic compound
    • A61K49/0461—Dispersions, colloids, emulsions or suspensions
    • A61K49/0466—Liposomes, lipoprotein vesicles, e.g. HDL or LDL lipoproteins, phospholipidic or polymeric micelles
    • 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—Liposomes
    • A61K9/1277—Processes for preparing; Proliposomes

Definitions

  • the aqueous phase can contain the auxiliaries known to the person skilled in the art, such as, for example, buffer substances, isotonizing additives, cryoprotectors or water-soluble polymers such as dextran or preserving additives.
  • auxiliaries known to the person skilled in the art, such as, for example, buffer substances, isotonizing additives, cryoprotectors or water-soluble polymers such as dextran or preserving additives.
  • the liposome membrane can also contain constituents which modify the distribution of the liposomes in the blood.
  • constituents which modify the distribution of the liposomes in the blood include, for example, PEGylated derivatives of phosphatidylethanolamine (for example DSPE-PEG), lipids such as, for example, GM 1 or conjugates from sugars and hydrophobic components such as, for example, palmitic or stearic acid esters of dextran.
  • corresponding liposomes can also be provided with components that the Target distribution behavior in the body.
  • the so-called homing devices such as antibodies have to be calculated.
  • other components such as enzymes or modified drugs (eg prodrugs) can also be components of the liposome preparation.
  • the liposome formulations according to the invention with hydrophilic drugs are stable with respect to the retention of the encapsulated component when stored in the refrigerator over a period of at least 3 months, but preferably more than 6 months.
  • corresponding formulations can be achieved with appropriate formulations even at elevated temperatures (for example room temperature).
  • the liposome suspensions according to the invention can also be stored at lower temperatures ( ⁇ 0 ° C.).
  • the preparations according to the invention thus have an extremely increased storage stability compared to the previously known preparations with a simultaneously greatly reduced manufacturing outlay (there is no need to separate the non-encapsulated portion).
  • the improved shelf life of the preparations according to the invention makes commercial use of such liposome formulations appear possible for the first time.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un procédé permettant d'augmenter la stabilité de suspensions de liposomes contenant des principes actifs hydrophiles, qui se caractérise en ce que le principe actif à encapsuler dans les liposomes est dosé de manière à ce que 5 à 95 % en poids du principe actif se trouvent sous forme non encapsulée.
EP95903305A 1993-12-02 1994-11-30 Procede permettant d'augmenter la stabilite de suspensions de liposomes contenant des principes actifs hydrophiles Withdrawn EP0731689A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE4341472 1993-12-02
DE4341472A DE4341472A1 (de) 1993-12-02 1993-12-02 Verfahren zur Erhöhung der Stabilität von hydrophile Wirkstoffe enthaltenden Liposomensuspensionen
PCT/EP1994/003964 WO1995015153A1 (fr) 1993-12-02 1994-11-30 Procede permettant d'augmenter la stabilite de suspensions de liposomes contenant des principes actifs hydrophiles

Publications (1)

Publication Number Publication Date
EP0731689A1 true EP0731689A1 (fr) 1996-09-18

Family

ID=6504253

Family Applications (1)

Application Number Title Priority Date Filing Date
EP95903305A Withdrawn EP0731689A1 (fr) 1993-12-02 1994-11-30 Procede permettant d'augmenter la stabilite de suspensions de liposomes contenant des principes actifs hydrophiles

Country Status (9)

Country Link
US (1) US6475515B2 (fr)
EP (1) EP0731689A1 (fr)
JP (1) JPH09505821A (fr)
AU (1) AU1241695A (fr)
CA (1) CA2177973A1 (fr)
DE (1) DE4341472A1 (fr)
HU (1) HUT75465A (fr)
NO (1) NO962244L (fr)
WO (1) WO1995015153A1 (fr)

Families Citing this family (22)

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Publication number Priority date Publication date Assignee Title
GB9416149D0 (en) * 1994-08-10 1994-09-28 Univ Strathclyde Vesicle formulation
DE4430592A1 (de) 1994-08-20 1996-02-22 Max Delbrueck Centrum Liposomale Zubereitung, ihre Herstellung und ihre Verwendung
EP0806969A2 (fr) * 1995-02-09 1997-11-19 Schering Aktiengesellschaft Liposomes contenant des agents de contraste pour l'imagerie relative au pool sanguin intracardiaque
DE19529922A1 (de) * 1995-08-01 1997-02-06 Schering Ag Verwendung von liposomalen Zubereitungen in der indirekten MRT-Lymphographie
JP2003513030A (ja) * 1999-11-05 2003-04-08 シード・キャピタル・インヴェストメンツ−２・（エスシーアイ−２）・ベスローテン・フエンノートシャップ 低い水溶性および脂肪親和性を示す物質のカプセル化方法、およびこの方法により得られる製剤
US8357351B2 (en) * 2004-04-21 2013-01-22 Ananth Annapragada Nano-scale contrast agents and methods of use
US7713517B2 (en) * 2004-04-21 2010-05-11 Marval Biosciences, Inc. Compositions and methods for enhancing contrast in imaging
US20050255154A1 (en) 2004-05-11 2005-11-17 Lena Pereswetoff-Morath Method and composition for treating rhinitis
EP1772156A1 (fr) * 2004-07-21 2007-04-11 Konica Minolta Medical & Graphic, Inc. Colorant radio-opaque à rayons x contenant des liposomes, et processus de production
WO2006100692A2 (fr) * 2005-03-21 2006-09-28 Lifecare Innovations Pvt. Ltd. Nouvelle composition vesiculaire inter et intra multilamellaire
KR20080016621A (ko) * 2005-06-09 2008-02-21 바이올리폭스 에이비 염증성 질병 치료용 조성물 및 방법
SI1919450T1 (sl) * 2005-09-01 2014-10-30 Meda Ab Liposomski sestavek, ki vsebuje antihistaminik in kortikosteroid, in njegova uporaba za izdelavo zdravila za zdravljenje rinitisa in sorodnih motenj
CN101951835B (zh) * 2007-12-05 2015-02-11 马维尔生物科学公司 纳米级对比剂和使用方法
WO2009152445A1 (fr) * 2008-06-13 2009-12-17 Marval Biosciences, Inc. Imagerie de plaques d’athérosclérose utilisant des agents d’imagerie de liposomes
TR201818978T4 (tr) * 2011-11-04 2019-01-21 Enceladus Pharmaceuticals B V İnsanlardaki İnflamatuvar Rahatsızlıkların Tedavisine Yönelik Lipozomal Kortikosteroidler
DK2950784T3 (da) 2013-02-01 2021-07-05 Zoneone Pharma Inc Fjernladning af svagt vandopløselige lægemidler i liposomer
US20160120806A1 (en) * 2014-04-08 2016-05-05 Aradigm Corporation Nanocrystals formed in a microenvironment
US9532986B2 (en) 2014-04-08 2017-01-03 Aradigm Corporation Liposomal ciprofloxacin formulations with activity against non-tuberculous mycobacteria
WO2015156904A1 (fr) * 2014-04-08 2015-10-15 Aradigm Corporation Liposomes formant des nanocristaux de médicament suite à congélation-décongélation
WO2016022549A1 (fr) 2014-08-04 2016-02-11 Zoneone Pharma, Inc. Chargement à distance de médicaments modérément hydrosolubles dans des vésicules lipidiques
CA3034081A1 (fr) * 2016-08-18 2018-02-22 Troy Bremer Administration d'uree a des cellules de la macula et de la retine a l'aide de constructions de liposomes.
JP2023549170A (ja) * 2020-11-03 2023-11-22 ヴェセロン， インコーポレイテッド 担体を使用する治療薬の標的化送達のための組成物および方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2416008A1 (fr) * 1978-02-02 1979-08-31 Oreal Lyophilisats de liposomes
US4897355A (en) * 1985-01-07 1990-01-30 Syntex (U.S.A.) Inc. N[ω,(ω-1)-dialkyloxy]- and N-[ω,(ω-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor
US4857319A (en) * 1985-01-11 1989-08-15 The Regents Of The University Of California Method for preserving liposomes
GB8727590D0 (en) * 1987-11-25 1987-12-31 Fisons Plc Formulation
JP2792702B2 (ja) * 1988-10-05 1998-09-03 ネクスター・フアーマシユーテイカルズ・インコーポレイテツド 乾燥時に改善された安定性を示すリポソームの調製方法
IL94718A (en) * 1989-07-05 1994-10-21 Schering Ag Non-ionic carboxamide contrast agent and method of preparation
DE3934656A1 (de) * 1989-10-13 1991-04-18 Schering Ag Verfahren zur herstellung von waessrigen dispersionen
WO1993020802A1 (fr) * 1992-04-09 1993-10-28 Northwestern University Liposomes a reflexion acoustique et procedes de preparation et d'utilisation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9515153A1 *

Also Published As

Publication number Publication date
US6475515B2 (en) 2002-11-05
WO1995015153A1 (fr) 1995-06-08
HUT75465A (en) 1997-05-28
NO962244D0 (no) 1996-05-31
CA2177973A1 (fr) 1995-06-08
US20020102293A1 (en) 2002-08-01
HU9601476D0 (en) 1996-07-29
AU1241695A (en) 1995-06-19
JPH09505821A (ja) 1997-06-10
NO962244L (no) 1996-05-31
DE4341472A1 (de) 1995-06-08

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