EP1937215A2 - Composition pharmaceutique conteant un agent chelateur du fer - Google Patents

Composition pharmaceutique conteant un agent chelateur du fer

Info

Publication number
EP1937215A2
EP1937215A2 EP06793171A EP06793171A EP1937215A2 EP 1937215 A2 EP1937215 A2 EP 1937215A2 EP 06793171 A EP06793171 A EP 06793171A EP 06793171 A EP06793171 A EP 06793171A EP 1937215 A2 EP1937215 A2 EP 1937215A2
Authority
EP
European Patent Office
Prior art keywords
composition
active compound
particles
sustained release
phospholipid
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Withdrawn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
EP06793171A
Other languages
German (de)
English (en)
Inventor
Ingrid Vereyken
Okke Franssen
Carmen Masanneck
Susanne Hermanns
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.)
Neuraxo Biopharmaceuticals GmbH
Original Assignee
Neuraxo Biopharmaceuticals GmbH
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 Neuraxo Biopharmaceuticals GmbH filed Critical Neuraxo Biopharmaceuticals GmbH
Priority to EP06793171A priority Critical patent/EP1937215A2/fr
Publication of EP1937215A2 publication Critical patent/EP1937215A2/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Withdrawn legal-status Critical Current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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/225—Polycarboxylic acids
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/113—Multiple emulsions, e.g. oil-in-water-in-oil
    • 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
    • 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
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/04—Chelating agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • Desferrioxamine is used in the treatment of chronic iron overload, such as in transfusional haemosiderosis, thalassaemia major, sideroblastic anaemia, autoimmune haemolytic anaemia, and other chronic anaemias, idiopathic (primary) haemochromatosis in patients in whom concomitant disorders preclude phlebotomy, iron overload associated with porphyria cutanea tarda in patients unable to tolerate phlebotomy.
  • desferrioxamine is indicated for treating acute iron poisoning, chronic aluminium overload in patients with end-stage renal failure with aluminium-related bone disease, dialysis encephalopathy or aluminium-related anaemia.
  • microparticle compositions of desferrioxamine were made from polylactide-co-glycolide, a hydrophobic biodegradable polymer.
  • the drug load capacity of the described microparticles is too low to accomodate a dose of the active compound which would be effective over a period of at least several days.
  • polylactide-co-glycolide is known to degrade into acidic reaction products that may render the microclimate within the microparticles substantially acidic, which may lead to the degradation of the acid-labile desferrioxamine.
  • an active compound is a chemical or biological substance or mixture of substances which is useful for the diagnosis, prevention or treatment of diseases, symptoms, and other conditions of the body, or for influencing a body function.
  • the composition of the invention comprises at least one, and optionally two or more of such active compounds.
  • Other expressions which may be used as synonyms for active compounds are drugs, drug substances, active ingredients, active agents and the like.
  • sustained release form means that the respective fraction of the iron chelator is formulated and/or processed in such as way that it is released slowly after administration.
  • the sustained release characteristics may be achieved by generally known formulation methods and techniques, some of which will be described further below.
  • the iron chelator which is in sustained release form is released from the composition over a period of at least about 24 hours after administration. More preferably, the sustained release dose fraction is released over at least about 48 hours, or over at least about 72 hours. If the composition is intended for the treatment of injured nerves, and if it is intended that a single administration is used to achieve the desired therapeutic effect, it is preferred that the iron chelator is released over at least about 4 days, or at least about 5 days or even one week, depending on variable factors such as the size of the lesion and the number of injection sites per lesion. In further embodiments, the release profile is adapted to provide release over at least about 2 weeks, 3 weeks, or even 4 weeks. Without wishing to be bound by theory, it is believed that the sustained release of the iron chelator may or should be adapted to achieve a sufficient delay of scar formation that the regeneration and growth of the nervous tissue at the lesion is not inhibited.
  • the preferred duration of drug release refers to the release profile as measured in vitro by an appropriate method and at 37 0 C, using an appropriate medium such as buffer or water for injection.
  • the following method may be used to determine the in vitro release from a composition comprising sustained release particles:
  • composition is further formulated as a viscoelastic gel, which means that the viscosity is so high that the material behaves like an elastic solid if only low shear forces are exerted, and like a viscous fluid when the shear force exceeds a threshold which is defined as the yield point.
  • a gel is a semisolid system with a finite, usually rather small, yield stress.
  • the composition if designed to comprise lipid particles or liposomes as sustained release particles, is prepared by combining one or more particle-forming lipids, the iron chelator, and water, optionally in the presence of further active and/or inactive ingredients to form an aqueous dispersion.
  • the dispersion may be homogenised, using a suitable homogenising tool, such as an Ultraturrax ® or a high-pressure homogeniser.
  • the homogenisation is preferably carried out at elevated temperature, such as at a temperature which is above the phase transition temperature range, or above the melting temperature range, of the lipid(s) selected for particle formation.
  • the composition is used for the treatment of spinal cord or peripheral nerve injuries. It has been found that a single administration of the composition (per lesion) may be sufficient to provide the desired effect of scar inhibition for a period of time that is long enough to allow for nerve growth and/or regeneration. For large lesions, it may be useful to select more than one site of injection to better cover the whole lesion, which is still considered as only one administration according to the present invention. The long-lasting effectiveness of the composition is particularly beneficial in that, typically, no repeated administrations are needed.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention se rapporte à une composition pharmaceutique destinée à une administration parentérale, qui contient un chélateur du fer. Le composé actif se présente au moins partiellement sous la forme d'un composé à libération prolongée. Ladite composition, de préférence visqueuse, contient des particules à libération prolongée, telles que des particules phospholipidiques, dans lesquelles un ingrédient actif peut être incorporé. La composition selon l'invention est particulièrement utile pour traiter et régénérer des tissus nerveux, tels que des fibres nerveuses lésées, par l'intermédiaire d'une injection intraneurale ou intraspinale.
EP06793171A 2005-09-02 2006-09-04 Composition pharmaceutique conteant un agent chelateur du fer Withdrawn EP1937215A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP06793171A EP1937215A2 (fr) 2005-09-02 2006-09-04 Composition pharmaceutique conteant un agent chelateur du fer

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US71334705P 2005-09-02 2005-09-02
EP05108071 2005-09-02
PCT/EP2006/065952 WO2007026028A2 (fr) 2005-09-02 2006-09-04 Composition pharmaceutique contenant un chelateur du fer
EP06793171A EP1937215A2 (fr) 2005-09-02 2006-09-04 Composition pharmaceutique conteant un agent chelateur du fer

Publications (1)

Publication Number Publication Date
EP1937215A2 true EP1937215A2 (fr) 2008-07-02

Family

ID=36305265

Family Applications (1)

Application Number Title Priority Date Filing Date
EP06793171A Withdrawn EP1937215A2 (fr) 2005-09-02 2006-09-04 Composition pharmaceutique conteant un agent chelateur du fer

Country Status (8)

Country Link
EP (1) EP1937215A2 (fr)
JP (1) JP2009507006A (fr)
KR (1) KR20080044845A (fr)
CN (1) CN101252913A (fr)
AU (1) AU2006286445A1 (fr)
BR (1) BRPI0615349A2 (fr)
CA (1) CA2620685A1 (fr)
WO (1) WO2007026028A2 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2000134A1 (fr) * 2007-06-06 2008-12-10 Neuraxo Biopharmaceuticals GmbH Utilisation d'une substance pour l'amélioration des lésions pns
WO2014036414A2 (fr) 2012-08-30 2014-03-06 The Board Of Trustees Of The Leland Stanford Junior University Chélateurs du fer et leur utilisation pour la réduction d'échec de transplantation
EP3177269A4 (fr) 2014-08-04 2018-02-28 Zoneone Pharma, Inc. Chargement à distance de médicaments modérément hydrosolubles dans des vésicules lipidiques
WO2016025611A2 (fr) * 2014-08-13 2016-02-18 Zoneone Pharma, Inc. Formulations pharmaceutiques d'agents chélateurs utilisées en tant que système de traitement par élimination des métaux
MX2018009662A (es) * 2016-02-11 2018-09-11 Chevion Mordechai Metodo y composicion farmaceutica para tratamiento de neurodegeneracion.
EP3585385A4 (fr) * 2017-02-27 2020-12-30 The University of Adelaide Procédés et produits pour réduire les adhérences
US11479532B2 (en) 2017-06-23 2022-10-25 University Of South Florida 5-aminolevulinate synthase inhibitors and methods of use thereof
CN110464717B (zh) * 2019-09-23 2022-02-18 张建国 一种2,4-二羟基苯甲酸在制备降低血糖的药物的应用
CN114652844B (zh) * 2022-04-13 2023-10-20 南京大学 一种基于仿生学设计的纳米组装材料的制备方法及应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5023087A (en) * 1986-02-10 1991-06-11 Liposome Technology, Inc. Efficient method for preparation of prolonged release liposome-based drug delivery system
US5043166A (en) * 1987-01-09 1991-08-27 Hadasit Medical Research, Inc. Liposome/anthraquinone drug composition and method
EP0878480A1 (fr) * 1997-05-14 1998-11-18 H.W. Prof. Dr. Müller Procédé pour ameliorer la régénération nerveuse
IL130324A0 (en) * 1999-06-07 2000-06-01 Yeda Res & Dev Pharmaceutical compositions comprising iron chelators for the treatment of neurodegenerative disorders and some novel iron chelators
US8029795B2 (en) * 1999-12-30 2011-10-04 Gwathmey, Inc. Targeted iron chelator delivery system

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2007026028A2 *

Also Published As

Publication number Publication date
CN101252913A (zh) 2008-08-27
WO2007026028A2 (fr) 2007-03-08
BRPI0615349A2 (pt) 2011-05-17
AU2006286445A1 (en) 2007-03-08
CA2620685A1 (fr) 2007-03-08
WO2007026028A3 (fr) 2007-06-14
KR20080044845A (ko) 2008-05-21
JP2009507006A (ja) 2009-02-19

Similar Documents

Publication Publication Date Title
WO2007026028A2 (fr) Composition pharmaceutique contenant un chelateur du fer
RU2641605C2 (ru) Улучшенные липосомальные составы липофильных соединений
US9044381B2 (en) Method for delivering drugs to the brain
EP3142656B1 (fr) Formulations de liposomes multivésiculaires d'acide tranexamique
EP2057987B1 (fr) Composition pharmaceutique contenant une nanoparticule de statine encapsulée
EP2680820A1 (fr) Chargement liposomal actif avancé de substances médiocrement solubles dans l'eau
KR20080102303A (ko) 활성인 분자들의 투여를 위한 안정한 나노캡슐레이트 시스템
KR20070037444A (ko) 고체 미립자성 치료제의 생체외 적용방법
US8986736B2 (en) Method for delivering particulate drugs to tissues
WO2019102606A1 (fr) Formulation liposomale spécifique à un site de maladie
JP2001527040A (ja) 神経系の脳血管性疾患を治療、抑制及び防止するためのテトラサイクリン及び／又はテトラサイクリン誘導体
Rani et al. Surface-engineered liposomes for dual-drug delivery targeting strategy against methicillin-resistant Staphylococcus aureus (MRSA)
CA2279259A1 (fr) Formulation analgesique a administration parenterale encapsulee dans un liposome
US10172867B2 (en) Afobazole nanoparticles formulation for enhanced therapeutics
AU2011302885B2 (en) Non-aqueous oily injectable formulation exhibiting preservative efficacy
RU2605616C1 (ru) Липосомальное средство на основе убихинола и способ его получения
JP2006525345A (ja) 薬物耐性であると通常みなされている生物に対して抗菌薬物に効力を与える処方物
MX2008002737A (en) Pharmaceutical composition comprising an iron chelator
US7053061B2 (en) Amphotercin B structured emulsion
US6586407B1 (en) Injectable pharmaceutical formulations for partricin derivatives
AU2001280084A1 (en) Amphotericin B structured emulsion
JP7186385B2 (ja) 疾患部位特異的リポソーム製剤

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20080402

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR

17Q First examination report despatched

Effective date: 20080827

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN

18D Application deemed to be withdrawn

Effective date: 20090107