EP0831840A1 - Utilisation d'agents anti-inflammatoires non steroidiens pour ameliorer la compatibilite physiologique de preparations pharmaceutiques particulaires - Google Patents

Utilisation d'agents anti-inflammatoires non steroidiens pour ameliorer la compatibilite physiologique de preparations pharmaceutiques particulaires

Info

Publication number
EP0831840A1
EP0831840A1 EP96919720A EP96919720A EP0831840A1 EP 0831840 A1 EP0831840 A1 EP 0831840A1 EP 96919720 A EP96919720 A EP 96919720A EP 96919720 A EP96919720 A EP 96919720A EP 0831840 A1 EP0831840 A1 EP 0831840A1
Authority
EP
European Patent Office
Prior art keywords
inflammatories
steroidal anti
liposomes
pharmaceutical preparations
inn
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Withdrawn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
EP96919720A
Other languages
German (de)
English (en)
Inventor
Werner Krause
Peter Muschick
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7762219&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP0831840(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering AG filed Critical Schering AG
Publication of EP0831840A1 publication Critical patent/EP0831840A1/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Withdrawn legal-status Critical Current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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • 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
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • the invention relates to the objects characterized in the claims, that is to say the use of nonsteroidal anti-inflammatories to improve the physiological tolerance of particulate pharmaceutical preparations.
  • Particulate pharmaceutical preparations e.g. Liposomes, magnetites, cavisomes, nanoparticles, etc. have become increasingly important in both diagnostics and therapy in recent years.
  • Carrier system for the transport of diagnostically important compounds e.g.
  • Contrast agents or therapeutically usable substances, such as e.g. Gentamicin (INN).
  • INN Gentamicin
  • WO88 / 09165 describes injectable aqueous liposome preparations with iodine-containing X-ray contrast media and a method for producing corresponding formulations. Due to the sizes (0.15 - 0.3 ⁇ m) and the high contrast inclusions (iodine / lipid ratio 1.5 - 6), these formulations are particularly suitable for imaging the liver.
  • RES reticuloendothelial system
  • Waddel et al. (J. Lab. Clin. Med. 1955; 45: 697-710) describe these side effects in patients after injection of lipid emulsions as follows: reddening of the skin, sensation of heat on the face and neck, restlessness, feeling of narrowing or pressure in the chest area, cyanosis and severe back pain. The administration of antihistamines is unable to eliminate or mitigate these side effects.
  • Rabinovici et al. (Circ. Shock 1990; 31: 431-445) speculate that the undesirable effects of liposomes with encapsulated hemoglobin can be attributed to the release of PAF (platelet activating factor) and attempted - unsuccessfully - to prevent them by administration of a PAF antagonist.
  • PAF platelet activating factor
  • the initial concentration of these substances in the bloodstream which is available at the start of the application, is effective.
  • the present invention relates to the use of non-steroidal anti-inflammatories to improve the physiological tolerance of particulate pharmaceutical preparations.
  • Magnetic particles, nanoparticles, cavisomes or liposomes, in particular liposomes, which contain X-ray or NMR contrast agents can be used as particulate pharmaceutical preparations.
  • particles which serve as carriers for diagnostic or therapeutic agents are also suitable.
  • the corresponding preparation can be applied in the usual dose and contain the usual galenic additives.
  • acetylsalicylic acid indomethacin (INN), ibuprofen (INN) or ketoprofen (INN), in particular acetylsalicylic acid
  • INN indomethacin
  • ibuprofen INN
  • ketoprofen in particular acetylsalicylic acid
  • the anti-inflammatories can be contained in the usual dose, e.g. acetylsalicylic acid in a dose of 0.1-50 mg / kg body weight, preferably 5-15 mg / kg body weight, in the pharmaceutical composition.
  • the invention therefore also relates to such pharmaceutical preparations and agents.
  • the following examples are intended to illustrate the invention, without wishing to be restrictive.
  • the electrocardiogram (EKG), the heart rate (HR) and the rate of pressure increase or decrease (dP / dtmax and min) were also continuously recorded.
  • the right ventricular became after medistemal thoracotomy Stroke volume (SV) and cardiac output (CO) measured.
  • SV medistemal thoracotomy Stroke volume
  • CO cardiac output
  • the animals were then infused with liposomes loaded with an X-ray contrast medium.
  • the particle diameter was approx. 0.2 ⁇ m
  • the composition consisted of soy phosphatidylcholine / cholesterol / soy phosphatidylglycerol (6: 3: 1).
  • the dose was 10 or 250 mg iodine / kg, the injection rate 10 mg / kg / min.
  • Administration of the liposome formulation (10 mg iodine / kg) resulted in an increase in PAP and a decrease in CO in pigs.
  • acetylsalicylic acid acetylsalicylic acid (ASA, 10 mg / kg) these circulatory side effects could be completely prevented (Fig. 2 and 3).

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Dispersion Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'utilisation d'agents anti-inflammatoires non stéroïdiens comme additifs dans des préparations pharmaceutiques particulaires peut réduire les effets secondaires sur le système cardio-vasculaire lors de l'administration de telles préparations.
EP96919720A 1995-05-10 1996-05-09 Utilisation d'agents anti-inflammatoires non steroidiens pour ameliorer la compatibilite physiologique de preparations pharmaceutiques particulaires Withdrawn EP0831840A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19518221 1995-05-10
DE19518221A DE19518221A1 (de) 1995-05-10 1995-05-10 Verwendung nichtsteroidaler Entzündungshemmer zur Verbesserung der physiologischen Verträglichkeit partikulärer pharmazeutischer Zubereitungen
PCT/EP1996/001936 WO1996035429A1 (fr) 1995-05-10 1996-05-09 Utilisation d'agents anti-inflammatoires non steroidiens pour ameliorer la compatibilite physiologique de preparations pharmaceutiques particulaires

Publications (1)

Publication Number Publication Date
EP0831840A1 true EP0831840A1 (fr) 1998-04-01

Family

ID=7762219

Family Applications (1)

Application Number Title Priority Date Filing Date
EP96919720A Withdrawn EP0831840A1 (fr) 1995-05-10 1996-05-09 Utilisation d'agents anti-inflammatoires non steroidiens pour ameliorer la compatibilite physiologique de preparations pharmaceutiques particulaires

Country Status (7)

Country Link
US (1) US5874422A (fr)
EP (1) EP0831840A1 (fr)
JP (1) JPH11504930A (fr)
CA (1) CA2220052A1 (fr)
DE (1) DE19518221A1 (fr)
NO (1) NO975127L (fr)
WO (1) WO1996035429A1 (fr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020048596A1 (en) * 1994-12-30 2002-04-25 Gregor Cevc Preparation for the transport of an active substance across barriers
IL113926A (en) * 1995-05-31 2000-06-01 Korenstein Rafi Contrast medium with improved patient's tolerance thereto and its use
DE19721947C2 (de) * 1997-05-21 1999-04-22 Diagnostikforschung Inst Verwendung von pharmazeutischen Zubereitungen, die Partikel, Vesikel oder Polymere sowie nichtsteroidale Antirheumatika und/oder Thrombozytenaggregationshemmer zur Darstellung der Gefäße, Lymphknoten und des Knochenmarks enthalten
DK1031347T3 (da) 1999-01-27 2002-07-08 Idea Ag Transnasal transport/immunisering med meget tilpasselige bærere
PT1031346E (pt) 1999-01-27 2002-09-30 Idea Ag Vacinacao nao invasiva atraves da pele
WO2001001962A1 (fr) * 1999-07-05 2001-01-11 Idea Ag. Procede d'amelioration du transport a travers des barrieres semi-permeables compatibles
EP1498116A1 (fr) * 2002-03-20 2005-01-19 Hosokawa Micron Corporation Procede de fabrication de particules composites contenant un produit chimique
WO2004029068A1 (fr) * 2002-09-25 2004-04-08 Forbes Medi-Tech Inc. Derives comprenant des sterols et/ou des stanols et des classes specifiques d'agents anti-inflammatoires, et utilisation desdits derives pour le traitement ou la prevention de maladies cardiovasculaires
US20040105881A1 (en) * 2002-10-11 2004-06-03 Gregor Cevc Aggregates with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin
US20080095722A1 (en) * 2004-11-12 2008-04-24 Idea Ag Extended Surface Aggregates in the Treatment of Skin Conditions

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH672733A5 (fr) * 1987-05-22 1989-12-29 Bracco Ind Chimica Spa
US5264220A (en) * 1991-11-12 1993-11-23 Long David M Jr Method of extending the vascular dwell-time of particulate therapeutic and particulate diagnostic agents

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9635429A1 *

Also Published As

Publication number Publication date
JPH11504930A (ja) 1999-05-11
WO1996035429A1 (fr) 1996-11-14
CA2220052A1 (fr) 1996-11-14
US5874422A (en) 1999-02-23
NO975127D0 (no) 1997-11-07
NO975127L (no) 1997-12-10
DE19518221A1 (de) 1996-11-14

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