RU2708089C1 - Method for protection of dogs against flea infestations - Google Patents

Abstract

FIELD: veterinary medicine.

SUBSTANCE: invention relates to veterinary medicine and is a method for protecting dogs from flea infestations involving external treatment of animal body parts with an insectoacaricide agent, characterized by that in order to increase the effectiveness of the method, the insectoacaricide agent used is a composition containing active substances abamectin and fipronil, ethyl cellosolve and polyethylene glycol as dissolvent, hexamidine diisetionate as auxiliary substances – 0.05 g, eucalyptus essential oil – 3 % and additionally as an agent promoting penetration of drugs under the skin, dimethylsulphoxide at the following ratio of components, wt%: abamectin – 0.1, fipronyl – 0.5, hexamidine diisetionate – 0.05, essential oil of eucalyptus – 3, dimethylsulphoxide –- 10, ethyl cellosolve – 30–40, polyethylene glycol-1500 – 16, isopropyl alcohol – balance up to 100, wherein composition is applied by method of local application on areas of body – area withers, dewlap, shoulders, hips and abdomen – in dose 0.03 ml/kg per animal.

EFFECT: method provides higher effectiveness of dogs protection against flea invasions.

1 cl, 1 tbl, 3 ex

Description

The present invention relates to the field of veterinary medicine, namely to measures to combat parasitic diseases (flea infestations) of animals, in particular kenocephalidosis of dogs and can be used in the field of veterinary medicine.

Ctenocephalidosis of dogs is an invasive warm-blooded disease caused by blood-sucking insects of the fleas Ctenocephalides canis, which are temporary ectoparasites (they are divided into woolly and nesting by their lifestyle). Currently, fleas of this species are distributed around the world and are able to parasitize more than 50 animal species, including dogs, cats, rodents and humans [1, 2].

In a systematic sense, canine flea belongs to the type of arthropods (Arthopoda), the class of insects (Insecta), the order of fleas (Siphonaptera), the suborder (Pulicomorpha), the superfamily (Pulicoidea), the genus Ctenocephalides, and the species Ctenocephalides canis [2].

In most animals with ktenocephalidosis, infection occurs in the external environment outside the house, in direct contact with sick animals, through objects of care or clothing, as well as harmful rodents that transmit parasitic arthropods. [3]. Fleas feed on blood, and therefore a massive defeat by flea infestations causes enormous damage to the health of animals: fatness and immunity are reduced, allergic reactions are observed. After the incubation period, as a rule, there is an active development of invasion with inflammatory reactions from the secondary microflora [1]. In most cases, flea dermatitis is difficult to cure, and there is also a high risk of reinfestation if a strict course of treatment is not followed and inadequate prevention [3]. Most of the flea development cycle occurs outside the host. Adults suck blood for several minutes, then move to another part of the body or migrate to another animal or land. In the external environment, adults can survive up to six months without nutrition if necessary. Therefore, today the problem of the spread and parasitization of fleas is global and requires a comprehensive approach to its solution.

The known "Method of controlling animal pests" (RF patent 2508102, 2014). To protect a mammal from fleas, an oral or parenteral administration to a mammal of a compound of formula 1, its N-oxide or salt, is carried out in a pesticidally effective amount that acts against fleas for 48 hours after oral or parenteral administration to a mammal.

There are "Topical formulations comprising the 1-N-arylpyrazole derivative and formamidine" (RF patent 2361401, 2009), the invention provides new topical formulations containing at least one 1-N-arylpyrazole derivative and formamidine, such as amitraz, and methods for treating, controlling, or preventing parasite infestation in mammals or birds. The compositions of the invention also include an ectoparasicidal, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethriod insecticide and / or anthelmintics, such as benzimidazoles or imidazothiazoles. Ectoparasites that can be controlled, treated or prevented with the present invention include ticks, fleas, ticks, scabies, lice, mosquitoes, flies and vermiform cattle larvae.

"The drug against demodicosis and ectoparasites" (RF patent 94030861, 1997), which consists of the following components, wt. %: permethrin 1-50, TEAC 0.05-0.2, castor oil 0.5-5, DMSO 20-40, levomecithin 985 μg / mg 0.5-5, ethyl alcohol the rest. The drug will find application in demodicosis, notothedrosis, scabies, as well as against fleas in dogs and other carnivores (cats, foxes, arctic foxes, etc.).

There is an “Insecticidal drug" cypam "" (RF patent 2113789, 1998), the drug is recommended for the treatment of animals from ectoparasites, in particular from ticks, fleas, lice-eaters, it includes: cypermethrin 0.1-1.0; amitraz 0.1-1.0; dimethyl sulfoxide 0.001-20.0; polyethylene oxide rest.

There is an “Insect-acaricidal substance for combating the ectoparasites of dogs and cats” (RF patent 2312100, 2007), which is a phenylpyrazole derivative in which the cyano group, trifluoromethylsulfenyl group and amino group are attached to the pyrazole structure in the third, fourth and fifth positions, respectively, and to phenyl the cycle attached in the second and sixth positions on the chlorine atom, characterized in that in the fourth position to the phenyl cycle attached to the trichlorosilyl group.

Known "An improved method for the systemic administration of insecticides such as 2,4-dienoic acid to terrestrial mammals" (RF patent 2225113, 2004), which is the introduction to a mammal of an insecticide from the class of 2,4-dienoic acid, its salt or ester in an amount that is fatal to fleas and / or for their eggs.

There is an “Insecticidal preparation” (RF patent 2163439, 2001), which contains phenytrotion (0.1-3.0 wt.%), Permethrin (0.05-1.0 wt.%), Neopinamine-forte (0.05 -0.75 wt.%), Piperonyl butoxide as a synergist (0.1-2.0 wt.%), Solvent (the rest) and propellant (10-60 wt.%). The preparation additionally contains triethylene glycol (0.2-2.0 wt.%) And perfume attracting action (0.05-1.0 wt.%).

"Insecticide and acaricidal drug for combating animal ectoparasites" morinilin "" (RF patent 2112379, 1998), is an insect-acaricidal composition based on deltamethrin and amitraz. Additionally, dimethyl sulfoxide is introduced into the drug. As a hydrophobic base, the preparation contains polyethylene oxide. The drug is active against the causative agent of demodicosis of dogs, sarcoptoid ticks, lice, fleas, and lice eaters.

There is an “Antiparasitic drug for treating dogs and cats” (RF patent 2356562, 2009), with endo - and ectoparasites, which contains as an active substance it contains avermectins complex, in which at least 75 wt. % are avermectin A2 and avermectin B2.

On the basis of fipronil, Dana insecticide and acaricidal drugs are known (patent of the Russian Federation 2181243, 2002)., Insectal-plus (patent of the Russian Federation 2340181, 2007), insecticide and acaricidal composition and concentrate (patent of the Russian Federation 2384065, 2007), a medicine for of treating and preventing arachnoentomoses of mammalian animals (RF patent 2348398, 2007), a method for treating and preventing arachno-entomoses of mammalian animals and a medicament for treating and preventing arachno-entomoses of mammalian animals (RF patent 232797, 2007; RF patent 2329796, 2007 ), compositions for n For external use, by topical application, containing fipronil (RF patent 2480197, 2008).

There is a “Method for the treatment of dog demodicosis” (RF patent No. 2634265, 2016), an insect-acaricidal composition, characterized in that in order to increase the effectiveness of the method, a composition containing the active substances abamectin and fipronil is used as a solvent, ethyl cellosolve and polyethylene glycol as a solvent, and additionally as an agent that promotes the penetration of drugs under the skin.

In the above means and methods, we did not find a composition containing fipronil and abamectin to protect dogs from flea infestations.

The aim of the invention was the creation of an effective way to protect dogs from flea infestations, by using a composition having high insecticidal effectiveness and the ability to protect animals from attack and suction of fleas for a long time.

This goal is achieved by using a composition containing the active substances abamectin and fipronil, as excipients, hexamidine diethionate, essential oil of eucalyptus, as a solvent ethyl cellosolve, isopropyl alcohol and polyethylene glycol and, in addition, dimethyl sulfoxide as an agent that promotes the penetration of medicinal substances under the skin, in the following ratios of components, wt. %:

Abamectin - 0.1

Fipronil - 0.5

Hexamidine diisetionate - 0.05

Eucalyptus Essential Oil - 3

Dimethyl sulfoxide - 10

Ethyl cellosolve - 30-40

Polyethylene glycol-1500 - 16

Isopropyl alcohol - the rest is up to 100

Abamectin is a substance from the group of macrocyclic lactones with antiparasitic action.

Fipronil - a substance from the group of phenylpyrazoles, has an antiparasitic effect. Fipronil has a mechanism of action similar to ivermectin (blocking of GABA-dependent receptors), but has a lower average effective exposure time and slow metabolism. Recently, as a result of the widespread use of drugs containing macrocyclic lactones, various parasites have developed resistance to such drugs. The introduction of insecticides from another chemical group, in particular the phenylpyrazole group, and having a similar mechanism of action, helps to solve this problem.

Hexamidine diisethionate - a cationic antiseptic from the dibenzamidine group, has a bacteriostatic effect against most gram-positive and gram-negative microorganisms, is able to maintain its activity in the presence of biological substances of the body (pus, blood, serous fluid).

Eucalyptus essential oil is a clear liquid, it contains cineole, tannins, organic acids, flavanoids and various aldehydes, which helps to destroy odors that attract arthropods.

Dimethyl sulfoxide is an organic solvent that promotes the penetration of various medicinal substances under the skin.

Polyethylene glycol-1500 is a low molecular weight ethylene oxide polymer used as a thickener.

Isopropyl alcohol is the simplest secondary monohydric alcohol, an organic solvent.

Ethyl cellosolve - an organic solvent from the group of alcohols, is absorbed through the skin.

The finished composition is a transparent homogeneous liquid from white to light yellow in color, with a specific odor. Get the composition by mechanical mixing of the components included in its composition, at a temperature of 40-50 ° C. According to the proposed invention, the composition is applied once by local application to localization sites (the withers, underbodys, shoulder, thigh and abdomen) at a dose of 0.05 ml / kg per animal for dogs. The product is applied to a dry, contaminated skin and hair integument.

The invention is illustrated by the following examples:

Example 1. The study of the optimal ratio of abamectin and fipronil in experiments to protect dogs from flea infestations.

In 2015, in order to determine the optimal ratio of the two active substances fipronil and abamectin, we laid the experience on the basis of a veterinary clinic. In the experiment, 50 animals invaded by fleas of Ctenocephalides canis were used, which were divided into 10 groups of 5 animals each. The first group was treated by local application to the area of the withers, breast, shoulder, thigh and abdomen in a dose of 0.45 ml per animal with the following composition:

Abamectin - 0.1%

Hexamidine diisetionate - 0.05 g

Eucalyptus essential oil - 3%

Dimethyl sulfoxide - 10%

Polyethylene glycol-1500 - 16%

Ethyl cellosolve - 30-40%

Isopropyl alcohol - the rest is up to 100

The second group was treated with the same composition, but with the addition of fipronil - 0.05%.

Abamectin - 0.1%

Fipronil - 0.05%

Hexamidine diisetionate - 0.05 g

Eucalyptus essential oil - 3%

Dimethyl sulfoxide - 10%

Polyethylene glycol-1500 - 16%

Ethyl cellosolve - 30-40%

Isopropyl alcohol - the rest is up to 100

Subsequent groups (3 to 10) were treated with the same composition, increasing the content of fipronil by 0.05% in each group. The research results showed that in the range of 0.45-0.55 wt. % fipronil there is an increased activity of the compositions, which indicates the optimal ratio of fipronil and abamectin, which is in the middle of the range 5: 1 and in this composition corresponds to the content of fipronil 0.5 wt. %

Example 2. Preparation of the composition

At a temperature of 50-60 ° C, 0.1 g of abamectin was dissolved in 30 g of ethyl cellosolve. Then, at the same temperature, 0.5 g of fipronil was dissolved in the resulting solution, hexamidine diisethionate - 0.05 g, eucalyptus essential oil - 3%, 10 g of dimethyl sulfoxide, 16 g of polyethylene glycol were added and thoroughly mixed until completely dissolved. The mass of the resulting solution was adjusted to 100 g by adding the required amount of isopropyl alcohol.

Example 3. The study of the effectiveness of the method of protecting dogs from flea infestations.

In 2015-2017 We have tested the claimed method of protecting dogs from flea infestations. For this purpose, 4 experimental and 1 control groups of 10 animals each were formed. Experimental animals were treated with the composition according to example 2. In order to protect dogs from flea infestations, the composition was applied by local application to the localization sites of fleas (the withers, chest, shoulder, thigh and abdomen) at doses of 0.005, 0.01, 0.03 and 0 , 05 ml / kg per animal, twice with an interval of 5 days. Control animals were treated with distilled water. The research results are presented in table 1.

As a result of the experiments, it was found that when protecting dogs from flea infestations, the extensivity (EE) of the composition at doses of 0.005 ml / kg was 10% after 72 hours; after 48 hours in doses of 0.01, 0.03 and 0.05 ml / kg 30%, 50%, 80%, and, accordingly, after 72 hours 0.01 ml / kg - 70%, 0.03 and 0.05 ml / kg - 100%. With Intensity Efficiency (IE) after 24 hours, 4.6%, 10.9%, 16.5%, 22.9% after 48 hours, 6.3%, 36.3%, 66.2%, 81.7% and 72 hours 14.4%, 60.6%, 100%

Thus, the technical solution of the claimed invention improves the efficiency of the method of protecting dogs from flea infestations. Abamectin in combination with Fipronil in low doses allows to obtain 100% therapeutic efficacy

Sources of information taken into account:

1. Lyutikova I.A. Ktenocephalidosis of dogs and cats in the Moscow metropolis: distribution, pathogenesis, therapy. Abstract. diss. Cand. veterinarian, sciences. - Moscow. - 2008 .-- 23 p.

2. Medvedev S.G. The experience of system analysis of the evolution of the flea order (siphonaptera) // Readings in memory of N.A. Kholodkovsky. 2005. No. 57-2. S. 1-170.

3. Roslavtseva S.A. The epidemiological significance of fleas and disinsecticides in the fight against them // Epidemiology and Sanitation. - 2001. - No. 1. - S. 56-61.

4. RF patent 2480197, 2013.

5. RF patent 2508102, 2014.

6. RF patent 2361401, 2009.

7. RF patent 94030861, 1997.

8. RF patent 2113789, 1998.

9. RF patent 2312100, 2007.

10. RF patent 2225113, 2004.

11. RF patent 2163439, 2001.

12. RF patent 2112379, 1998.

13. RF patent 2356562, 2009.

14. RF patent 2181243, 2002.

15. RF patent 2340181, 2007

16. RF patent 2384065, 2007.

17. RF patent 2348398, 2007.

18. RF patent 232797, 2007

19. RF patent 2329796, 2007.

20. RF patent 2480197, 2008.

21. RF patent No. 2634265, 2016.

Claims (10)

A method of protecting dogs from flea infestations, including external processing of body parts on animals with an insecticide and acaricidal agent, characterized in that in order to increase the effectiveness of the method, a composition containing the active substances abamectin and fipronil is used as a solvent, ethyl cellosolve and polyethylene glycol as auxiliary of hexamidine diisionionate - 0.05 g, eucalyptus essential oil - 3% and additionally as an agent that promotes drug penetration substances under the skin, dimethyl sulfoxide in the following ratios of components, wt. %: Abamectin - 0.1 Fipronil - 0.5 Hexamidine diisetionate - 0.05 Eucalyptus Essential Oil - 3 Dimethyl sulfoxide - 10 Ethyl cellosolve - 30-40 Polyethylene glycol-1500 - 16 Isopropyl alcohol - the rest is up to 100, moreover, the composition is applied by local application to areas of the body - the area of the withers, chest, shoulder, thigh and abdomen - at a dose of 0.03 ml / kg per animal.