WO1997006769A2 - Composition pharmaceutique a proprietes trypanocides - Google Patents

Composition pharmaceutique a proprietes trypanocides Download PDF

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Publication number
WO1997006769A2
WO1997006769A2 PCT/EP1996/003657 EP9603657W WO9706769A2 WO 1997006769 A2 WO1997006769 A2 WO 1997006769A2 EP 9603657 W EP9603657 W EP 9603657W WO 9706769 A2 WO9706769 A2 WO 9706769A2
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical preparation
preparation according
water
weight
volume
Prior art date
Application number
PCT/EP1996/003657
Other languages
German (de)
English (en)
Other versions
WO1997006769A3 (fr
Inventor
Alain Jaques BOURDICHON
Original Assignee
Bourdichon Alain Jacques
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 Bourdichon Alain Jacques filed Critical Bourdichon Alain Jacques
Priority to APAP/P/1998/001196A priority Critical patent/AP827A/en
Priority to AU68750/96A priority patent/AU6875096A/en
Priority to EA199800218A priority patent/EA199800218A1/ru
Priority to EP96929285A priority patent/EP0845983A2/fr
Publication of WO1997006769A2 publication Critical patent/WO1997006769A2/fr
Publication of WO1997006769A3 publication Critical patent/WO1997006769A3/fr

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

Definitions

  • the invention relates to a pharmaceutical preparation with trypanozid properties for the veterinary field, in the form of an aqueous solution, the diminazenediacetate (4,4'-diamidinodiazobenzenediacetamidoacetate) and pentamidine (4,4 '- (pentamethylendioxy) ) -dibenzamidine) as trypanozide active ingredients, phenazone (1,2-dihydro-l, 5-dimethyl-2-phenyl-3H-pyrazol-3-one) as antipyretic and analgesic component as well as glycerin.
  • Arsenic preparations and trypan dyes are known as chemotherapeutic agents, but due to their arsenic
  • a preparation for the treatment of such infections in animals is a trypanozide based on diminazen powder.
  • Other commercially available trypanozides are also only available in powder form.
  • the powdered form of the medicament is extremely disadvantageous, since the powdered preparations cannot be added to the feed and they therefore have to be mixed with water in order to prepare an injection solution. It is not possible to prepare a sterile solution from the powdery preparations, since the active substances crystallize out of the solution after a short time, so that the effectiveness of the preparation is quickly lost. Such solutions are therefore not adequately storable and transportable.
  • the injection solution must therefore be prepared shortly before the injection, but this is very dangerous due to the generally available water, since it can generally contain bacteria, viruses and germs which cause additional infections in the animals, so that the animals are very heavily burdened by an additional infection.
  • a complete solution of the solids is not achieved, so that the solution for injection has a poor effectiveness.
  • the currently known powdery trypanozides thus represent a risk of additional infections or contamination, at the same time that There is a risk of underdosing of the therapeutic agent, so that the chemotherapy may have to be repeated, which naturally increases the risk potential for infections or the like.
  • aqueous solutions of diminazene diacetate which contain castor oil as a solubilizer.
  • the invention is therefore based on the object of providing a solution of a pharmaceutical preparation of the type mentioned at the outset which is stable even at high temperatures.
  • the invention provides to create a pharmaceutical preparation with trypanozid properties in the form of an aqueous solution which contains the following substances: - Diminazene di-aceturate
  • Diminazene diacetate and pentamidine are trypanoicidal active ingredients which have a different spectrum of activity and thus complement one another in their action, so that almost all types of blood parasites are detected. In addition, resistances are advantageously avoided by the combination.
  • the poor water solubility of diminazene diacetate is compensated for by the combination of the two trypanozidic active substances according to the invention, since pentamidine, which is water soluble, acts as a solubilizer.
  • the phenazone also brings about better solubility of the diminazene di-aceturate, in addition to its action as an analgesic, which advantageously alleviates pain and fever conditions in the animals which are caused by the injection or the infection.
  • Glycerin and the water-soluble cellulose ether serve as emulsifiers.
  • a stable aqueous solution can be obtained according to the combination of all of the aforementioned substances.
  • the stability of the preparation according to the invention is advantageously so great that it can also be heated to 70 ° C. over a long period of time without any signs of decomposition occurring.
  • Methyl-cellulose is preferably used as the water-soluble cellulose ether, although other cellulose ethers, such as, for. B. hydroxy-ethyl cellulose or hydroxypropyl cellulose or their mixed forms are suitable.
  • the water used is preferably water which is physiologically, ie. H. in terms of pH and osmolality.
  • the water is pH neutral and isotonic. It also has a saline content of 0.9 + 0.3%.
  • aqueous solution is obtained as a preparation which can be stored without any problems since the active ingredient cannot crystallize out. In addition, there is no risk of an additional infection since it can be produced under sterile conditions.
  • Babesiosis (Babesia bigemina, Babesia motasi, Babesia canis and other Babesia) Theileria annulata.
  • the preparation according to the invention is combined with a further antipyretic substance and / or a pain reliever.
  • a further antipyretic substance and / or a pain reliever.
  • Lidocaine, procaine or their derivatives are preferably used. If necessary, acetylsalicylic acid can also be used as a fever and pain reliever.
  • the preparation according to the invention contains isometadium hydrochloride from the group of the phenathridines as a further biocidal active ingredient.
  • Methyl cellulose physiologically adjusted water 66.5 vol.-3
  • composition in% by weight of the active ingredients is preferably:
  • Methyl cellulose 1.6% physiologically adjusted water 78.4%.
  • the preparation according to the invention has the advantage that, based on the volume, the active substance content can be doubled compared to the prior art.
  • a particular advantage is that a single injection, which is necessary for chemotherapy, also provides three-month protection against reinfections.
  • a preferred embodiment of the pharmaceutical preparation is produced by the biocidal active ingredients, the intended activity-reducing agents.
  • water Emulsifier mixture can be mixed.
  • the emulsifier / water mixture which is composed of glycerol 20% by volume, methyl cellulose 1.6% by volume and physiological water 78.4% by volume, is then added to the active substances.
  • the ready-to-use preparation can be filled sterile filtered.

Landscapes

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

Abstract

Cette composition pharmaceutique à propriétés trypanocides utile en médecine vétérinaire sous forme d'une solution aqueuse contient du diminazène-diacéturate, de la pentamidine, du phénazone, de la glycérine et un éther de cellulose soluble dans l'eau.
PCT/EP1996/003657 1995-08-21 1996-08-20 Composition pharmaceutique a proprietes trypanocides WO1997006769A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
APAP/P/1998/001196A AP827A (en) 1995-08-21 1996-08-20 Pharmaceutical preparation with trypanocidal qualities for veterinary use.
AU68750/96A AU6875096A (en) 1995-08-21 1996-08-20 Pharmaceutical composition with trypanocidal properties
EA199800218A EA199800218A1 (ru) 1995-08-21 1996-08-20 Фармацевтический препарат с трипанозидными свойствами
EP96929285A EP0845983A2 (fr) 1995-08-21 1996-08-20 Composition pharmaceutique a proprietes trypanocides

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19530708.9 1995-08-21
DE1995130708 DE19530708C2 (de) 1995-08-21 1995-08-21 Pharmazeutisches Präparat mit trypanoziden Eigenschaften

Publications (2)

Publication Number Publication Date
WO1997006769A2 true WO1997006769A2 (fr) 1997-02-27
WO1997006769A3 WO1997006769A3 (fr) 1997-05-09

Family

ID=7769997

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/003657 WO1997006769A2 (fr) 1995-08-21 1996-08-20 Composition pharmaceutique a proprietes trypanocides

Country Status (7)

Country Link
EP (1) EP0845983A2 (fr)
AP (1) AP827A (fr)
AU (1) AU6875096A (fr)
DE (1) DE19530708C2 (fr)
EA (1) EA199800218A1 (fr)
OA (1) OA10665A (fr)
WO (1) WO1997006769A2 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998017266A2 (fr) * 1996-10-18 1998-04-30 Atarost Allgem. Tierarzneimittelfabrik, Dr. Ulrich Böhmer, Nachf. Gmbh & Co. Preparation pharmaceutique contenant un derive d'amidine et de la procaine
WO2000030611A2 (fr) * 1998-11-24 2000-06-02 Chambord Ltd. Preparation pharmaceutique
WO2004105772A1 (fr) * 2003-06-03 2004-12-09 Tropmed Gmbh Preparation pharmaceutique destinee au traitement de maladies tropicales parasitaires contenant diminazene diaceturate et/ou pentamidine
CN105168121A (zh) * 2015-08-28 2015-12-23 重庆布尔动物药业有限公司 兽用复方三氮脒注射液及其制备方法
RU2638433C1 (ru) * 2016-12-15 2017-12-13 Федеральное государственное бюджетное образовательное учреждение высшего образования "Горский государственный аграрный университет" Способ повышения лечебной эффективности Диминазина-70 при пироплазмозе крупного рогатого скота
RU2638444C1 (ru) * 2016-12-15 2017-12-13 Федеральное государственное бюджетное образовательное учреждение высшего образования "Горский государственный аграрный университет" Способ повышения лечебной эффективности пироплазмоза крупного рогатого скота Неозидином-М в сочетании с лазеропунктурой

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4309415A1 (de) * 1993-03-19 1994-09-22 Alan Jacques Bourdichon Pharmazeutisches Präparat

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4309415A1 (de) * 1993-03-19 1994-09-22 Alan Jacques Bourdichon Pharmazeutisches Präparat

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ACTA TROPICA, vol. 54, no. 3-4, 1993, HOLLAND, pages 185-203, XP000651313 A.S. PEREGRINE UND M. MAMMAN: "PHARMACOLOGY OF DIMINAZENE: A REVIEW" *
FIEDLER: "LEXIKON DER HILFSSTOFFE F]R PHARMAZIE, KOSMETIK UND ANGRENZENDE GEBIETE" 1989 , EDITO CANTOR , AULENDORF XP002026875 see page 273-274 *
JAMES E.F. REYNOLDS: "MARTINDALE THE EXTRA PHARMACOPOEIA" 1993 , THE PHARMACEUTICAL PRESS , LONDON XP002026860 see page 28-29 *
TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE, vol. 80, no. 4, 1986, LONDON, pages 634-641, XP000651398 RASEROKA ET AL: "THE TRYPANOCIDAL EFFECT OF DRUGS IN DIFFERENT PARTS OF THE BRAIN" *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998017266A2 (fr) * 1996-10-18 1998-04-30 Atarost Allgem. Tierarzneimittelfabrik, Dr. Ulrich Böhmer, Nachf. Gmbh & Co. Preparation pharmaceutique contenant un derive d'amidine et de la procaine
WO1998017266A3 (fr) * 1996-10-18 1998-06-25 Alain Jacques Bourdichon Preparation pharmaceutique contenant un derive d'amidine et de la procaine
WO2000030611A2 (fr) * 1998-11-24 2000-06-02 Chambord Ltd. Preparation pharmaceutique
WO2000030611A3 (fr) * 1998-11-24 2000-08-31 Chambord Ltd Preparation pharmaceutique
WO2004105772A1 (fr) * 2003-06-03 2004-12-09 Tropmed Gmbh Preparation pharmaceutique destinee au traitement de maladies tropicales parasitaires contenant diminazene diaceturate et/ou pentamidine
CN105168121A (zh) * 2015-08-28 2015-12-23 重庆布尔动物药业有限公司 兽用复方三氮脒注射液及其制备方法
RU2638433C1 (ru) * 2016-12-15 2017-12-13 Федеральное государственное бюджетное образовательное учреждение высшего образования "Горский государственный аграрный университет" Способ повышения лечебной эффективности Диминазина-70 при пироплазмозе крупного рогатого скота
RU2638444C1 (ru) * 2016-12-15 2017-12-13 Федеральное государственное бюджетное образовательное учреждение высшего образования "Горский государственный аграрный университет" Способ повышения лечебной эффективности пироплазмоза крупного рогатого скота Неозидином-М в сочетании с лазеропунктурой

Also Published As

Publication number Publication date
DE19530708C2 (de) 1999-01-07
EP0845983A2 (fr) 1998-06-10
AP827A (en) 2000-04-28
OA10665A (en) 2002-09-25
AP9801196A0 (en) 1998-03-31
DE19530708A1 (de) 1997-02-27
AU6875096A (en) 1997-03-12
EA199800218A1 (ru) 1998-12-24
WO1997006769A3 (fr) 1997-05-09

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