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WO1998017266A2 - Pharmaceutical preparation - Google Patents

Pharmaceutical preparation Download PDF

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Publication number
WO1998017266A2
WO1998017266A2 PCT/EP1997/005724 EP9705724W WO9817266A2 WO 1998017266 A2 WO1998017266 A2 WO 1998017266A2 EP 9705724 W EP9705724 W EP 9705724W WO 9817266 A2 WO9817266 A2 WO 9817266A2
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical preparation
preparation
preparation according
pharmaceutical
trypanosomiasis
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/EP1997/005724
Other languages
German (de)
French (fr)
Other versions
WO1998017266A3 (en
Inventor
Alain Jacques Bourdichon
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.)
Atarost Allgem Tierarzneimittelfabrik Dr Ulrich Bohmer Nachf & Co GmbH
Original Assignee
Atarost Allgem Tierarzneimittelfabrik Dr Ulrich Bohmer Nachf & Co 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 Atarost Allgem Tierarzneimittelfabrik Dr Ulrich Bohmer Nachf & Co GmbH filed Critical Atarost Allgem Tierarzneimittelfabrik Dr Ulrich Bohmer Nachf & Co GmbH
Priority to EP97912195A priority Critical patent/EP0936907A2/en
Priority to AU49482/97A priority patent/AU4948297A/en
Publication of WO1998017266A2 publication Critical patent/WO1998017266A2/en
Publication of WO1998017266A3 publication Critical patent/WO1998017266A3/en
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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles

Definitions

  • the invention relates to a pharmaceutical preparation for trypanosomiasis prophylaxis.
  • Arsenic preparations and trypan dyes were used for chemotherapy, but they have harmful side effects.
  • a preparation for trypanosomiasis prophylaxis which contains at least one active substance against protozoa from the group of the amidines, preferably diminazene di-aceturate (4,4'-diamidino-diazoaminobenzenediacetamidoacetate) and / or pentamidine ( 4,4 '- (Pentamethylenedioxy) -dibenzamidin), as well as procaine or a procaine derivative.
  • the preparation also contains phenazone, which has an antipyretic effect in the case of an existing infection.
  • the preparation is preferably used as an injection solution, so that the individual substances first in solution have to be brought.
  • a mixture of cellulose ether, in particular methyl cellulose, glycerol and water, is advantageously mixed with the solids, a clear solution being able to be prepared simply by stirring.
  • Procaine or procaine derivative e.g. hydrochloride
  • Emulsifier-water mixture glycerin
  • Water suitable for pharmaceutical purposes, e.g. physiologically balanced water
  • the preparation according to the invention enables trypanomiasis prophylaxis and advantageously the preparation is also simultaneously suitable for chemotherapy of an existing protozoan infection.
  • the preparation is particularly intended for the veterenary area. However, it is also in human medicine can be used so that, particularly advantageous for vacationers, a kind of vaccination can be carried out.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The object of the invention is to produce a pharmaceutical preparation as a treatment for the prevention of trypanosomiasis. To that end, the invention proposes a pharmaceutical preparation as a treatment for the prevention of trypanosomiasis which is characterized in that it contains at least one compound which is effective against protozoa and is selected from the group comprising amidines and procaine, or a procaine derivative.

Description

Beschreibung description

PHARMAZEUTISCHES PRÄPARAT ENTHALTEND AMIDINDERIVAT UND PROCAINPHARMACEUTICAL PREPARATION CONTAINING AMIDINE DERIVATIVE AND PROCAIN

Technisches GebietTechnical field

Die Erfindung betrifft ein pharmazeutisches Präparat zur Trypanosomiasis-Prophylaxe.The invention relates to a pharmaceutical preparation for trypanosomiasis prophylaxis.

Stand der TechnikState of the art

In Ländern mit tropischem Klima sind Infektionskrankheiten, die durch Protozoen hervorgerufen werden, weit verbreitet, wie z. B. die sogenannte Schlafkrankheit (Trypanosomiasis), die das zentrale Nervensystem schädigt und bei Nicht- behandlung zum Tod führt. Die Krankheit betrifft Mensch und Tier gleichermaßen und muß chemotherapeutisch behandelt werden.In countries with a tropical climate, infectious diseases caused by protozoa are widespread, such as: B. the so-called sleeping sickness (trypanosomiasis), which damages the central nervous system and leads to death if not treated. The disease affects humans and animals alike and must be treated with chemotherapy.

Zur Chemotherapie wurden Arsenpräparate und Trypanfarbstoffe verwendet, die jedoch gesundheitsschädliche Nebenwirkungen aufweisen.Arsenic preparations and trypan dyes were used for chemotherapy, but they have harmful side effects.

Daneben werden auch andere Präparate z. B. mit Diminazen-di- aceturat als Wirkstoff eingesetzt.In addition, other preparations such. B. with Diminazen-diacetate as an active ingredient.

Bei den bekannten Präparaten ist es jedoch nachteilig, daß keine Prophylaxe betrieben werden kann, so daß im landwirtschaftlichen Bereich Nutzvieh, das gerade eine Infektion mit Protozoen überstanden hat, sofort wieder einer möglichen Infektion ausgesetzt ist. Auch bei sofortiger neuer Therapie wird der Organismus der Tiere so stark belastet, so daß es zu Ausfällen kommen kann oder zumindest zu einer großen Schwächung des Viehs. Weiterhin können z. B. Urlauber, die nur in einer begrenzten Zeitspanne einem Infektionsrisiko ausgestzt sind, keine Vorsorge vor Urlaubsantritt treffen. Aber auch Personen, die ständig einem Infektionsrisiko ausgesetzt sind, können sich nicht vor einer Infektion schützen.In the known preparations, however, it is disadvantageous that no prophylaxis can be carried out, so that in the agricultural field, livestock that has just survived an infection with protozoa is immediately exposed to a possible infection again. Even with immediate new therapy, the organism of the animals is so heavily loaded that it can lead to failures or at least to a great weakening of the cattle. Furthermore, e.g. B. Vacationers who are exposed to an infection risk for a limited period of time do not take any precautions before the start of their vacation. But even people who are constantly at risk of infection cannot protect themselves from infection.

Darstellung der Erfindung, Aufgabe, Lösung, VorteilePresentation of the invention, task, solution, advantages

Es ist daher Aufgabe der Erfindung, ein pharmazeutisches Präparat zu schaffen, das eine Trypanosomiasis-Prophylaxe erlaubt.It is therefore an object of the invention to provide a pharmaceutical preparation which allows trypanosomiasis prophylaxis.

Diese Aufgabe wird durch die Merkmale des Anspruchs 1 gelöst.This object is solved by the features of claim 1.

Dazu ist erfindungsgemäß vorgesehen, ein Präparat zur Trypanosomiasis-Prophylaxe zu schaffen, das mindestens einen gegen Protozoen wirksamen Wirkstoff aus der Gruppe der Amidine, vorzugsweise Diminazen-di-aceturat (4,4'-Diamidino- diazoaminobenzen-diacetamidoacetat) und/oder Pentamidin (4,4'-(Pentamethylendioxy)-dibenzamidin) , sowie Procain oder ein Procain-Derivat enthält.For this purpose, it is provided according to the invention to provide a preparation for trypanosomiasis prophylaxis which contains at least one active substance against protozoa from the group of the amidines, preferably diminazene di-aceturate (4,4'-diamidino-diazoaminobenzenediacetamidoacetate) and / or pentamidine ( 4,4 '- (Pentamethylenedioxy) -dibenzamidin), as well as procaine or a procaine derivative.

Beide vorgenannten Wirkstoffe weisen ein unterschiedliches Wirkungsspektrum auf und ergänzen sich somit in ihrer Schutzwirkung.Both of the above-mentioned active substances have a different spectrum of activity and thus complement one another in their protective action.

Nach einer weiteren bevorzugten Ausführungsform ist im Präparat auch Phenazon enthalten, das im Fall einer bereits bestehenden Infektion fiebersenkend wirkt.According to a further preferred embodiment, the preparation also contains phenazone, which has an antipyretic effect in the case of an existing infection.

Vorzugsweise wird das Präparat als Injektionslösung verwendet, so daß die einzelnen Stoffe zuerst in Lösung gebracht werden müssen. Dazu wird vorteilhafterweise eine Mischung aus Celluloseether, insbesondere Methyl-Cellulose, Glycerin und Wasser mit den Feststoffen vermengt, wobei sich einfach durch Rühren eine klare Lösung herstellen läßt.The preparation is preferably used as an injection solution, so that the individual substances first in solution have to be brought. For this purpose, a mixture of cellulose ether, in particular methyl cellulose, glycerol and water, is advantageously mixed with the solids, a clear solution being able to be prepared simply by stirring.

Eine bevorzugte Ausführungsform des erfindungsgemäßen Präparats weist folgende Inhaltsstoffe auf:A preferred embodiment of the preparation according to the invention has the following ingredients:

Wirkstoffe: Diminazen-di-aceturatActive ingredients: diminazene di-aceturate

PentamidinPentamidine

Procain oder Procain-Derivat (z.B. Hydrochlorid) PhenazonProcaine or procaine derivative (e.g. hydrochloride) phenazone

Emulgator- Wasser- Gemisch: GlycerinEmulsifier-water mixture: glycerin

Methyl-CelluloseMethyl cellulose

Wasser (für pharmazeutische Zwecke geeignet, z. B. physiol. angeglichenes Wasser)Water (suitable for pharmaceutical purposes, e.g. physiologically balanced water)

Das erfindungsgemäße Präparat ermöglicht die Trypanomiasis- Prophylaxe und vorteilhafterweise ist das Präparat auch gleichzeitig für die Chemotherapie einer bestehenden Protozoen-Infektion geeignet.The preparation according to the invention enables trypanomiasis prophylaxis and advantageously the preparation is also simultaneously suitable for chemotherapy of an existing protozoan infection.

Bei der Verwendung des Präparats ergibt sich ein mindestens dreimonatiger Schutz vor einer Infektion oder auch einer Wiederholungsinfektion.When using the preparation, there is at least three months of protection against infection or a repeat infection.

Das Präparat ist insbesondere für den Veterenär-Bereich vorgesehen. Es ist jedoch auch in der Humanmedizin einsetzbar, so daß, besonders vorteilhaft für Urlauber, eine Art Schutzimpfung durchführbar ist.The preparation is particularly intended for the veterenary area. However, it is also in human medicine can be used so that, particularly advantageous for vacationers, a kind of vaccination can be carried out.

Vorteilhaft ist auch die extrem schnelle Heilung von bestehenden Infektionen innerhalb von 8 bis 12 Stunden.The extremely fast healing of existing infections within 8 to 12 hours is also advantageous.

Weitere vorteilhafte Ausgestaltungen der Erfindung sind in den Unteransprüchen gekennzeichnet. Further advantageous embodiments of the invention are characterized in the subclaims.

Claims

Ansprüche Expectations 1. Pharmazeutisches Präparat zur Trypanosomiasis-Prophylaxe, dadurch gekennzeichnet, daß das Präparat mindestens eine gegen Protozoen wirksame Verbindung aus der Gruppe der Amidine und Procain oder ein Procain-Derivat enthält.1. Pharmaceutical preparation for trypanosomiasis prophylaxis, characterized in that the preparation contains at least one compound active against protozoa from the group of amidines and procain or a procain derivative. 2. Pharmazeutisches Präparat nach Anspruch 1, dadurch gekennzeichnet,daß das Präparat Diminazen-di-acetu- rat als Wirkstoff enthält.2. Pharmaceutical preparation according to claim 1, characterized in that the preparation contains diminazene di-acetate as an active ingredient. 3. Pharmazeutisches Präparat nach Anspruch 1, dadurch gekennzeichnet, daß das Präparat Penta idin als Wirkstoff enthält.3. Pharmaceutical preparation according to claim 1, characterized in that the preparation contains Penta idin as an active ingredient. 4. Pharmazeutisches Präparat nach Anspruch 1, dadurch gekennzeichnet, daß das Präparat Diminazen-di- aceturat und Pentamidin als Wirkstoffe enthält.4. Pharmaceutical preparation according to claim 1, characterized in that the preparation contains diminazene-diacetate and pentamidine as active ingredients. 5. Pharmazeutisches Präparat nach einem der Ansprüche 1 bis5. Pharmaceutical preparation according to one of claims 1 to 4, dadurch gekennzeichnet, daß das Präparat Phenazon enthält.4, characterized in that the preparation contains phenazone. 6. Pharmazeutisches Präparat, nach einem der Ansprüche 1 bis6. Pharmaceutical preparation according to one of claims 1 to 5, dadurch gekennzeichnet, daß das Präparat in fester Form vorliegt.5, characterized in that the preparation is in solid form. 7. Pharmazeutisches Präparat nach einem der Ansprüche 1 bis 5, dadurch gekennzeichnet, daß das Präparat als wässrige Lösung vorliegt. Pharmazeutisches Präparat nach Anspruch 7 , dadurch gekennzeichnet, daß die wassrige Lösung als Lösungsvermittler einen Celluloseether und Glycerin enthält. 7. Pharmaceutical preparation according to one of claims 1 to 5, characterized in that the preparation is in the form of an aqueous solution. Pharmaceutical preparation according to claim 7, characterized in that the aqueous solution contains a cellulose ether and glycerol as solubilizers.
PCT/EP1997/005724 1996-10-18 1997-10-17 Pharmaceutical preparation Ceased WO1998017266A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP97912195A EP0936907A2 (en) 1996-10-18 1997-10-17 Pharmaceutical preparation
AU49482/97A AU4948297A (en) 1996-10-18 1997-10-17 Pharmaceutical preparation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE29618094.7 1996-10-18
DE29618094U DE29618094U1 (en) 1996-10-18 1996-10-18 Pharmaceutical preparation

Publications (2)

Publication Number Publication Date
WO1998017266A2 true WO1998017266A2 (en) 1998-04-30
WO1998017266A3 WO1998017266A3 (en) 1998-06-25

Family

ID=8030722

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1997/005724 Ceased WO1998017266A2 (en) 1996-10-18 1997-10-17 Pharmaceutical preparation

Country Status (4)

Country Link
EP (1) EP0936907A2 (en)
AU (1) AU4948297A (en)
DE (1) DE29618094U1 (en)
WO (1) WO1998017266A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000030611A3 (en) * 1998-11-24 2000-08-31 Chambord Ltd Pharmaceutical preparation

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4309415C2 (en) * 1993-03-19 1996-11-07 Alain Jaques Bourdichon Pharmaceutical preparation
EP0643964A3 (en) * 1993-08-18 1995-08-09 Medipharma Sa Use of local anesthetics for the manufacture of a medicament for the protection of plasma cell membranes.
DE19530708C2 (en) * 1995-08-21 1999-01-07 Atarost Allg Tierarzneimittelf Pharmaceutical preparation with trypanocidal properties

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000030611A3 (en) * 1998-11-24 2000-08-31 Chambord Ltd Pharmaceutical preparation

Also Published As

Publication number Publication date
DE29618094U1 (en) 1998-02-12
EP0936907A2 (en) 1999-08-25
WO1998017266A3 (en) 1998-06-25
AU4948297A (en) 1998-05-15

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