WO1995005181A2 - Agent anti-parasitaire destine aux animaux - Google Patents

Agent anti-parasitaire destine aux animaux Download PDF

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Publication number
WO1995005181A2
WO1995005181A2 PCT/BG1994/000007 BG9400007W WO9505181A2 WO 1995005181 A2 WO1995005181 A2 WO 1995005181A2 BG 9400007 W BG9400007 W BG 9400007W WO 9505181 A2 WO9505181 A2 WO 9505181A2
Authority
WO
WIPO (PCT)
Prior art keywords
drug
avermectins
animals
avm
praziquantel
Prior art date
Application number
PCT/BG1994/000007
Other languages
English (en)
Other versions
WO1995005181A3 (fr
Inventor
Marin Dragov Drumev
Drago Marinov Drumev
Bojidar Spasov Petkov
Boris Grigorov Georgiev
Boevska Iana Dimitrova Mizinska
Katia Stoianova Radeva
Diana Tencheva Dancheva
Maria Veselinova Todorova
Georgi Shterev Jgumov
Mariana Ivanova Karanikolova
Todorka Vassileva Karpacheva
Georgi Vassilev Petrov
Todorka Dimitrova Jgumova
Ilia Ivanov Iliev
Original Assignee
Biovet-Joint Stock Company
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 Biovet-Joint Stock Company filed Critical Biovet-Joint Stock Company
Publication of WO1995005181A2 publication Critical patent/WO1995005181A2/fr
Publication of WO1995005181A3 publication Critical patent/WO1995005181A3/fr

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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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof

Definitions

  • This invention concerns antiparasitic drug for farm and domestic animals in the cases of cestodes, trematodoses, nematodoses, as well as in the cases of pests (insect and acar) invasions.
  • the compound 2-(cyclohexylcarbonyl)-1 ,2,3,6,7-11b-hexahydro-4H-pyrazino[2,1- a] isoquinolin-4-one [MERCK INDEX, Eleventh edition, Merck & Co., Inc., Rahway, N.J., USA, 1989] has a INN (International Nonproprietary Name) praziquantel (PQ). It is applied in the veterinary practice as an antiparasitic drug with anticestodal and antitrematodal action. This substance however is known as not efficient against nematodes and external parasites (pests), [ROBERSON, E.L.
  • Avermectins as known, represent antibiotics with wide-spectrum antiparasitic activity, produced by Streptomycetes, [MERCK INDEX, 11th Edition, Merck & Co., Inc., Rahway, N.J., USA, 1989].
  • the highest antiparasitic effectiveness of them reveal the antibiotic fraction B- (B-
  • the avermectins are endectocides, i.e. they act both against internal and external parasites: as antheiminthics with antinematodal effect and as antiectoparasitics acting as insecticides and acaricides against mange mites and pasture ticks, and against blood-sucking insects.
  • the ivermectins (22,23-dihydroavermectins) are hydroginated analogues of the avermectins and have also an analogous biological activity, [CAMPBELL, W.C., Ivermectin and Abamectin, Springer-Verlag, New York, 1989].
  • the name 'avermectins' in this description from here will be used for the natural avermectins, for the semisynthetic ivermectins and for the technical products containing avermectins and ivermectins as well.
  • the disadvantage of avermectins is that they do not manifest any anticestodal and antitrematodal effects.
  • the mode of action of the anthelminthics boils down to the following:
  • the drug ought to get and to cross the contact areas of the parasites (for the nematodes - the cuticle and through their alimentary canal - the intestinal epithelium, but for the cestodes - tegument) and to penetrate into their inside.
  • the purpose of the present invention is the developing of a highly effective drug for parasitic control of wide spectrum of internal and external parasites of animals.
  • the present invention represents a drug for parasitic control of animals, containing 2-(cyclohexylcarbonyl)1 , 2,3,6,7-11b-hexahydro-4H-pyrazino[2,1- a]isoquinolin-4-one and avermectins (equalized in terms of biological activity to B-JA fraction) in quantitative proportions from 10:1 to 50:1.
  • the combination of the active components such as praziquantel and avermectins (or their technical products containing avermectins) is suitable for the production of pharmaceuticals.
  • the dosage form may contain the active substances mixed with the usual constituents, as indicated in the examples given.
  • the drug formulation, according to the invention, may be applied orally and in some cases parenterally.
  • Electron-microscopic photos of Toxocara canis after single application of PQ and of AVM
  • Electron-microscopic photos of Toxocara canis after a combined application of PQ + AVM
  • composition of a solid dosage form in % Composition of a solid dosage form in %:
  • the granulation should be performed in a whirlpool drier.
  • the granules formed may be applied as a premix, or after a suitable processing with slipping, lubricating and disintegrating constituents, it may be tabletted or capsulated.
  • Example 3 The technological processing is as per Example 1.
  • Example 3 The technological processing is as per Example 1.
  • composition of a solid dosage form in % Composition of a solid dosage form in %:
  • PQ is not active as an antinematodal remedy, [ROBERSON, E.L. - Anticestodal and Antinematodal Drugs, in: Veterinary Pharmacology and Therapeutics, 6th Ed., by N.A. Booth and L.E. McDonald, Iowa State University Press, Ames, Iowa, 50010, USA, 1988,928-949], in fact is not completely indifferent with respect to the nematodes examined. It affects, applied single, the integrity of their cuticle and of the intestinal wall, (Tables 1 , Tabulated diagram 1 , Fig. 1 and 3), although it does not give rise to death of the parasites.
  • the AVM in the cases of single application lead to serious damages in the structure of the cuticle and the intestinal epithelium of both nematodes (Table 1 , Fig. 1 and 3).
  • the injuries caused to both pattern parasites by the combination PQ+AVM are the heaviest - in the cuticle (unsticking, pocket-formation, tearing), in the intestinal epithelium (vesical structures formation among the microvilli, formation of myelinic structures, vacuolization and necroses), in the cases of Toxocara canis - with damages also in the hypoderma and the basal membrane; in the cases of Ascaris suum - with more necrotic alterations (Table 1, Tabulated diagram 1 , Fig. 2 and 4).
  • the stronger injuries in the structures of the nematodes examined by the combination of PQ + AVM could be explained by the influence of the PQ which creates an invasion atrium for the easier penetration of the AVM into the organisms of the parasites and its stronger effect respectively.
  • Electron-microscopic photos of Toxocara canis after single application of
  • Electron-microscopic photos of Toxocara canis after a combined application of PQ + AVM

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un agent anti-parasitaire, destiné aux animaux de compagnie et d'élevage, permettant de traiter les infestations à cestodes, trématodes et nématodes et les invasions de nuisibles (tiques, mites et insectes. Elle permet de mettre au point un agent très efficace pour la lutte anti-parasitaire chez les animaux en s'attaquant à un large spectre de parasites internes et externes. Cet agent réalise une combinaison entre le praziquantel et les avermectines, d'où une influence anthelmintique renforcée par le praziquantel sur les nématodes, et par les avermectines sur les cestodes, un élargissement du spectre anti-parasitaire qui englobe les infestations à helminthes, dues aux cestodes, nématodes et trématodes, et les invasions d'arachnidés (de nuisibles) dues aux tiques, mites et autres insectes. On observe une bonne tolérance chez l'animal même en cas de dose thérapeutique décuplée.
PCT/BG1994/000007 1993-08-12 1994-07-21 Agent anti-parasitaire destine aux animaux WO1995005181A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
BG98037A BG61064B1 (bg) 1993-08-12 1993-08-12 Лекарствено средство за обезпаразитяване на животни
BG98037 1993-08-12

Publications (2)

Publication Number Publication Date
WO1995005181A2 true WO1995005181A2 (fr) 1995-02-23
WO1995005181A3 WO1995005181A3 (fr) 1995-03-30

Family

ID=3925385

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/BG1994/000007 WO1995005181A2 (fr) 1993-08-12 1994-07-21 Agent anti-parasitaire destine aux animaux

Country Status (2)

Country Link
BG (1) BG61064B1 (fr)
WO (1) WO1995005181A2 (fr)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0717993A3 (fr) * 1994-11-28 1996-11-13 Virbac Sa Compositions antihelmintiques pour équidés
WO1996038165A2 (fr) * 1995-06-02 1996-12-05 Bayer Aktiengesellschaft Agents endoparasiticides
US6207179B1 (en) 2000-05-18 2001-03-27 Phoenix Scientific, Inc. Parasiticidal formulation for animals and a method of making this formulation
WO2002094288A1 (fr) * 2001-04-04 2002-11-28 Pfizer Limited Compositions veterinaires comprenant des derives d'oxime avermectine et du praziquantel
JP2006522154A (ja) * 2003-04-04 2006-09-28 メリアル リミテッド 動物用駆虫局所製剤
WO2010107791A2 (fr) 2009-03-17 2010-09-23 Concert Pharmaceuticals, Inc. Composés de pyrazinoisoquinoline
CN107961277A (zh) * 2016-10-20 2018-04-27 王腊俊 一种治疗猪绦虫病的复方药物
CN115813872A (zh) * 2022-12-27 2023-03-21 佛山市南海东方澳龙制药有限公司 动物用复方伊维菌素驱虫片及其制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2252730A (en) * 1991-02-12 1992-08-19 Ancare Distributors Anthelmintic formulations containing praziquantel

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA842571B (en) * 1983-04-07 1985-11-27 Merck & Co Inc Novel synergistic antiparasitic combinations

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2252730A (en) * 1991-02-12 1992-08-19 Ancare Distributors Anthelmintic formulations containing praziquantel

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Section Ch, Week 8609, Derwent Publications Ltd., London, GB; Class B02, AN 86'061936 & ZA,A,8 402 571 (MERCK & CO. INC.) 7 October 1985 *

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0717993A3 (fr) * 1994-11-28 1996-11-13 Virbac Sa Compositions antihelmintiques pour équidés
US5824653A (en) * 1994-11-28 1998-10-20 Virbac S.A. Anthelmintic compositions for equidae
WO1996038165A2 (fr) * 1995-06-02 1996-12-05 Bayer Aktiengesellschaft Agents endoparasiticides
WO1996038165A3 (fr) * 1995-06-02 1997-01-09 Bayer Ag Agents endoparasiticides
AU703048B2 (en) * 1995-06-02 1999-03-11 Bayer Intellectual Property Gmbh Endoparasiticidal compositions
US6159932A (en) * 1995-06-02 2000-12-12 Bayer Aktiengesellschaft Endoparasiticidal compositions
US6207179B1 (en) 2000-05-18 2001-03-27 Phoenix Scientific, Inc. Parasiticidal formulation for animals and a method of making this formulation
US6858601B2 (en) 2000-05-18 2005-02-22 Phoenix Scientific, Inc. Parasiticidal formulation for animals
WO2002094288A1 (fr) * 2001-04-04 2002-11-28 Pfizer Limited Compositions veterinaires comprenant des derives d'oxime avermectine et du praziquantel
JP2006522154A (ja) * 2003-04-04 2006-09-28 メリアル リミテッド 動物用駆虫局所製剤
WO2010107791A2 (fr) 2009-03-17 2010-09-23 Concert Pharmaceuticals, Inc. Composés de pyrazinoisoquinoline
CN107961277A (zh) * 2016-10-20 2018-04-27 王腊俊 一种治疗猪绦虫病的复方药物
CN115813872A (zh) * 2022-12-27 2023-03-21 佛山市南海东方澳龙制药有限公司 动物用复方伊维菌素驱虫片及其制备方法

Also Published As

Publication number Publication date
WO1995005181A3 (fr) 1995-03-30
BG61064B1 (bg) 1996-10-31
BG98037A (en) 1995-02-28

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