RU2384065C2 - Insect-acaricide agent - Google Patents

Abstract

FIELD: agriculture.

SUBSTANCE: insect-acaricide agent is described, which contains composition of fipronyl and alphacipermetrine as active substances with their following concentration, wt %, in the overall composition of the agent: Fipronyl 0.01-10.0, Alphacipermetrine 0.01-10.0, with the ratio of weight parts of 1 part of fipronyl to 0.1-20 parts of alphacipermetrine. Invention may be used to fight carriers of various transmissible and skin infections, to eliminate insets in areas of pets keeping, elimination of domestic dust mites, which increase allergic exposure of human and animals bodies.

EFFECT: agent may be applied in the form of lotion, solution, spray, drops for topical application, hair conditioner, etc.

8 cl, 1 tbl, 6 ex

Description

The invention relates to the field of veterinary medicine and can be used to protect animals (and birds) from insects - flying and non-flying (Flea detachment (Siphonaptera), Lice detachment (Anorlura), Fly and Mosquito detachment (Diptera), Puhoyed detachment (Mallophaga) ) and arachnids (parasitiform ticks of the squads Ixodidae and Argasidae), for controlling vectors of various vector-borne and skin infections, for killing insects in places where pets are kept, killing house dust mites that increase the allergenic load on animals and humans.

Prevention of natural focal infections of viral, bacterial, protozoal and rickettsial etiology, the causative agents of which are transmitted by ixodid ticks (tick-borne encephalitis (TBE), borreliosis (IKB)), is a public health problem. Representatives of the families Ixodidae Argasidae, Sarcopnidae and Demodicidae have the greatest epidemiological spread in the spread of animal diseases (pyroplasmosis, borreliosis, otodectosis, demodecosis, sarcoptoidosis, notoedrosis, and pricking itching). Modern prevention of tick-borne infections is based on the nonspecific protection of humans and animals from the attack of ticks, carriers of infections, since there are no vaccines against most of these infections. This problem is solved by using acaricidal agents for personal protection.

In addition, urban areas are largely inhabited by other synanthropic arthropods (mosquitoes, fleas, crickets, flies, ants, etc.), potential carriers of pathogens of a number of infections. In veterinary practice, protection of domestic animals (cats, dogs, horses, etc.) and farm animals from insects such as lice, fleas, lice, skin parasites, mosquitoes, gadflies, and flies is of great importance.

Therefore, the urgent task of modern veterinary medicine is the development of insect-repellent agents that would possess the properties of quick, reliable protection against a wide range of insects and ticks, would have low toxicity and a fairly long-lasting effect.

Compounds related to pyrethroids, organophosphorus preparations, carbamates and heterocyclic derivatives are mainly used to control insects. Formulations containing one compound as the active substance usually have a relatively narrow spectrum of insecticidal activity, a short protective action time and lead to the rapid development of resistance to the active substance in insect populations.

Existing combined insecticides along with quite high efficiency also have a number of significant disadvantages, because often do not take into account the combination of properties of compounds related to the mechanism of action, spectrum of action, onset of effect, duration of effect, ways of circulation and excretion from the body, toxicity, stability when used - on the skin on the surface of various materials (photostability, enzymatic lability), etc. .

A known composition for the treatment of arachnoentomiasis containing fipronil and esfenvalerate as active substances (RF patent 2181243, 2002). The disadvantages of the composition are a limited range of purposes - for the treatment of arachnoentomiasis in animals and the inactivity of esfenvalerate against taiga ticks. The effect of a temporary increase in tick aggression due to esfenvalerate is possible, which increases the risk of bites and accelerates the absorption of ticks at the initial moment of contact with the skin of an animal or human.

Known insect-acaricidal composition for a mammal containing fipronil and benzyl benzoate as active substances (RF patent 2283590, 2006). However, benzyl benzoate and fipronil do not have a quick contact effect, they are acceptable only for products with long-term application and with the possibility of long-term contact with an insect for manifestation sufficient insectoacaricidal activity.

Known acaricidal agent containing, as the active substance, a mixture of alpha-pericamethrin and didecyldimethylammonium bromide. Alfacipermetrin is used in an amount of 0.01-0.15% (RF patent 2242967, 2004). The disadvantage of this tool is the use in the composition of this composition of a quaternary ammonium compound (QAS) - didecyldimethylammonium bromide, which acts as an antimicrobial and disinfectant, but does not have a significant effect on prolonging the effect or expanding the spectrum of acaricidal activity of the agent. This combination allows you to expand the indications for the use of funds by combining the insecticidal and disinfecting properties of the components, but does not change the insecticidal characteristics of the tool.

Also known acaricidal agent, including imiprotrin and alfacipermethrin (RF patent 2280983, 2006). The disadvantages of this tool is that both components are characterized by a quick knock-off effect, but they do not have a sufficient duration of the insecticidal action associated with the specifics of penetration and distribution in the animal’s body. Therefore, this combination will be effective for surface treatment to protect predominantly from cockroaches, ants, etc. due to the rapid contact action, but it will not be effective enough to provide a prolonged insectoacaricidal action when applied directly to the skin and / or coat of the animal.

The proposed insecticaricidal agent is devoid of the disadvantages inherent in the known combined means, due to the fact that it contains as active substances a composition of fipronil and alfacipermethrin at their concentration in wt.% In the total composition of the agent:

Fipronil 0.01-10.0 Alfacipermethrin 0.01-10.0

Moreover, the ratio of the mass fractions of fipronil and alfacipermethrin, depending on the form of the preparation, can vary from 1 to 0.1 to 1 to 20, respectively.

Pyrethroid alphacipermethrin is a mixture of two enantiomers (1R) - cis - S and (1S) - cis - R in a 1: 1 ratio. It has high acaricidal activity, a quick onset of action, sharply limits the movement of ticks on the surface, does not accelerate the absorption of ticks to the animal.

The disadvantages of alfacipermethrin are: destruction under the influence of the sun's UV (photolability), relatively high toxicity to animals, irritating effect, deep penetration through the skin, moderate persistence and excretion from the body not only through the skin and hair, i.e. a relatively rapid decrease in concentrations in external tissues and a decrease in contact exposure.

Fipronil is an insecticide from the group of arylpyrazoles (phenylpyrazoles) of contact, intestinal and partially systemic action with a long protective effect. It effectively inhibits the development of ticks and flying insects - from orders of winged and orthopterans, etc. Fipronil affects the central nervous system of ectoparasites, without affecting the central nervous system of animals.

When applied to the skin, fipronil is localized in the sebaceous glands, without entering the animal’s blood. Thus, the effect of the "reservoir" is created, which provides a long-term effect and preservation of efficiency when bathing the animal with shampoo. With sebum, fipronil spreads over the surface of the skin and coat. Prolonged exposure to sunlight on a preparation applied to walls, materials, or animals does not reduce the effectiveness of the preparation.

The disadvantage of fipronil for topical (drip, local) use is the delayed action against ectoparasites (after approximately 24 hours of gradual distribution over the entire surface of the animal’s body).

The invention used a composition of substances with a quick (immediate) and slower (delayed) acaricidal and insecticidal lethal effect.

The use of fipronil, which is superior in duration to the effect of alphacipermethrin and is characterized as a less toxic (less irritating) compound for humans and animals, reduces the general toxicity of the composition of fipronil and alphacipermethrin while maintaining activity and effectiveness. Fipronil and alfacipermethrin complement each other in other indicators that are important for practical use in protecting various species of animals, when used in different seasons, they provide a synergistic effect and increase the versatility of insecticaricidal activity of the composition.

Table 1 presents the results of a study of the properties of solutions of individual substances of fipronil and alphacipermethrin in comparison with their composition in relation to adult forms of ixodid ticks (Ixodes persulcatus and Ixodes ricinus).

Developed ready-made forms of an insect-acaricidal agent based on the use of a combination of fipronil and alfacipermethrin provide more reliable protection of animals and people from tick attacks than mono-agents of these substances, repellent agents and comparable known analogues.

One of the finished forms of insecticide and acaricide is drops for topical use (drip application on the skin, for example, on the withers of an animal), intended for long-term protection of animals from ticks and insects (from 2 weeks or more). The droplets contain fipronil in a concentration of wt.% Not less than 0.5% (preferably 7%) and alfacipermethrin in a concentration of wt.% Not less than 0.25% (preferably 1.0%).

The finished form in the form of a lotion, solution, spray for application to wool, skin, and feathers of birds has an insect-repellent effect with a repellent effect for at least 3 hours and with an insect-acaricidal effect for at least 1 week and contains fipronil in a concentration of wt.% Not more than 1% (preferably 0.1%) and alphacipermethrin in a concentration of wt.% Not more than 1% (preferably 0.1%). Additionally, repellents, for example acrep and / or DETA, with a total mass fraction of repellents of at least 5%, are included in the composition of this form.

This form of the product is used by aerosol propellant or non-propellant type of spraying or direct application with a napkin, mitt, etc., to provide an insect repellent effect in order to protect animals from attacks of insects and ticks in the spring and autumn when walking in the forest, etc. n., for targeted local application for the direct destruction of sucked (ticks) or insects. It can also be used for external treatment of dressings to protect wounds from flies.

The liquid form (solution, lotion, emulsion) for use as a spray for treating animals with a duration of effect of at least 1 week (10-14 days) contains fipronil in a concentration of wt.% Not more than 1% (preferably 0.1%) and alphacipermetrin in a concentration of wt.% not more than 1% (preferably 0.3%).

This form of the product is used to process curtains, mosquito nets, walls, bedding, etc. in the conditions of tourism, fishing, hunting and labor, on vacation, on farms, in stables, in aviaries, in other household and residential premises, in competitions with a high number and activity of blood-sucking insects and ticks; to protect against insects spreading through rodents.

Each of the listed forms may additionally contain as active ingredient benzyl benzoate in a working concentration of wt.% At least 0.1% (preferably 1%) and / or an extract of melia (Mélia azedárach L.) in a concentration of wt.% At least 0.1 % (preferably 0.5%). Fir and / or vanillin essential oil additives are also possible to aromatize, deodorize and enhance the repellent effect.

Each of these forms (preferably a composition for topical use) can be used to include in the collar obtained from polymeric, natural or combined materials. When wearing a collar, the animals provide a protective insecticide and acaricidal effect.

The finished form in the form of a conditioner for wool in the form of a balm or spray combines a short acaricidal effect (2-3 days) with cosmetic and hygienic properties: it provides effective dry cleaning of the coat (improving combing, reducing hair tangling, combing and mechanical removal of insects), antifungal effect reducing the formation of dandruff. The balm contains fipronil in a concentration of wt.% Not more than 0.1% (preferably 0.02%) and alfacipermetrin in a concentration of wt.% Not more than 0.1% (preferably 0.02%) and additionally contains the active ingredients - benzyl benzoate in a concentration wt.% not more than 1% and an extract of melia (Melia azedárach L.) in a concentration of wt.% not more than 1%. As additional auxiliary components providing easy combing of wool and other cosmetic and hygienic effects, conditioning additives, such as cellulose derivatives and silicones, are used.

The product can be produced in the form of a concentrate in liquid form, which is diluted to recommended working concentrations before use. The content of fipronil in the concentrate is up to 5% (preferably 1%), alpha-pericamethrin up to 10% (preferably 5%). The content of benzyl benzoate in the concentrate can be up to 10%, and the extract of melia up to 3%.

Before use, the concentrate is diluted 20-30 times in water and is applied by aerosol or other method of application to the treated surfaces.

Examples

Acaricidal drops (composition for topical use)

Recipe

Fipronil 7 g Alfacipermethrin 1 g

Auxiliary components up to 100 ml: PEG 400, ethanol, isopropyl alcohol, antioxidant, PEG 40 hydrogenated castor oil, lavender essential oil.

Appointment and method of application

Used for the prevention and control of ectoparasites (fleas and ticks) of dogs and cats. The drug in the form of drops is applied to the skin at the withers (between the shoulder blades). Spread the coat and slowly apply the required amount of the product onto the skin slowly, evenly distribute more than 1 ml of the product evenly over the entire length of the spine. Dosage: for cats, 0.1 ml (5 drops) per 1 kg of weight, for dogs, 0.8-1 ml (50 drops) per 10 kg of weight. If possible, apply the drug in a place inaccessible to licking or use a muzzle at the time of application and absorption of drops.

The result

The drug provided insect-acaricidal protection against tick attacks for at least 40 days, and for fleas for at least 60 days.

Insectorepellent spray

Recipe

Acrep 15 g IR 3535 10 Fipronil 0.1 g Alfacipermethrin 0.1 g

Auxiliary components up to 100 ml: PEG 400, ethyl alcohol, isopropyl alcohol, antioxidant, povidone, PEG 40 hydrogenated castor oil, lavender essential oil.

Appointment and method of application

The product was used in a non-propellant-based packaging with a spray nozzle for applying the drug in the form of a spray. The bottle is held vertically, directing the spraying of the spray from a distance of 10-25 cm against the growth of the coat (lifting the long coat), if necessary, process the ammunition and clothing of the animal (blanket, etc.). Processing is carried out before walking in places with a high risk of insect attacks (especially ticks) based on: for cats and dogs - 2-3 ml per kg of weight, for horses 60-120 ml for full treatment. When processing took into account that one press of the spray device spray corresponds to 0.7 ml of the drug. Avoid contact with eyes, mucous membranes, open wounds, therefore, in these places, the product should be distributed with great accuracy, for example, using a napkin or sponge.

The result

The repellent effect was formed immediately and remained on the wool for up to 8 hours, on the tissues for up to 5 days. The tool provided acaricidal protection for at least 10 days.

When applying the product to a wound dressing (aerosol until the bandage is lightly wetted), the preparation provided protection from flies for at least 6 hours.

Insect-acaricidal solution for processing animal welfare facilities

Recipe

Benzyl benzoate 1.0 g Melia Extract 0.5 Alfacipermethrin 0.3 g Fipronil 0.1 g

Auxiliary components up to 100 ml: PEG 400, ethanol, isopropyl alcohol, antioxidant, povidone, PEG 40 hydrogenated castor oil, lavender essential oil, methylated spirits (bitrex).

Appointment and method of application

The product was used in a non-propellant-based packaging with a spray nozzle for applying the drug in the form of a spray. The bottle is held vertically, directing the spray from a distance of 20-30 cm to the treated surfaces (floor, walls, bedding, stall, aviary, kennel, etc.).

The result

The drug provided protection against the spread and attacks of various insects and ticks in places where animals were kept for at least 2 weeks.

Insectoacaricidal concentrate for the preparation of a solution for processing animal welfare facilities

Recipe

Benzyl benzoate 10.0 g Alfacipermethrin 5.0 g Fipronil 1.0 g Melia Extract 1,0

Auxiliary components up to 100 ml: PEG 400, ethyl alcohol, isopropyl alcohol, antioxidant, PEG 40 hydrogenated castor oil, lavender essential oil, denatured alcohol (bitrex).

Appointment and Method of Application

The drug is used to treat places of animal welfare in order to protect against flying and flightless insects (mosquitoes, midges, midges, flies, gadflies) and ticks.

They are used for processing curtains, mosquito nets, walls, ceilings, awnings, bedding, ammunition, etc. on farms, in stables, in aviaries, in competitions, in conditions of tourism, fishing, hunting and during exertion, on vacation, with a high number and activity of insects and ticks. Destroys arthropods, prevents their reproduction and distribution through carriers - rats, etc.

Before use, the concentrate is diluted 20-30 times with water (0.5 l of concentrate per 1-1.5 buckets of water). The degree of dilution (20-30) depends on the activity of insects and ticks. Mixing is carried out in a clean container by introducing the concentrate into water with constant stirring. Storage in diluted form until use no more than 10 hours, intensively mix before application.

Contains bitterness (bitrex) to protect treated surfaces from licking and cracking by animals.

The diluted product is applied in an aerosol way (using any device for aerosolizing liquids) on the treated surface or applied using napkins.

Processing is carried out at the rate of 10-20 ml of diluted funds per 1 m ² .

Consumption: 1 bottle of 0.5 liter is bred into 1-1.5 buckets, which is enough for processing from 500 m ² to 1.5 thousand m ² .

The result

The duration of the insecticaricidal effect is at least 10 days.

Wool conditioner with insecticide effect

Recipe

Alfacipermethrin 0.02 g Fipronil 0.02 g Benzyl benzoate 0.2 g Melia Extract 0.2

Auxiliary components up to 100 ml: ethyl alcohol, isopropyl alcohol, PEG 400, water, polyquartenium-10, DC 5330, antioxidant, PEG 40 hydrogenated castor oil, lavender essential oil.

Appointment and method of application

The tool combines insecticaricidal properties with cosmetic and hygienic characteristics. They are used for dry cleaning of hair - combing will improve, hair tangles will be reduced, combing and mechanical removal of insects is facilitated. The product was used in a package on an unpropellent basis with a spray nozzle for applying the drug in the form of a spray. The bottle is held vertically directing the spraying of the spray from a distance of 10-25 cm against the growth of the coat, lifting the long coat. Processing is performed before walking the animal at the rate of: for cats and dogs - 2-3 ml per kg of weight.

The result

The drug provided insecticide protection against tick attacks for at least 3 days. The drug facilitates combing hair and mechanical removal of ticks after walking. In addition, when using the drug, a decrease in the formation of dandruff was noted.

Collar with insecticidal effect

Recipe

It is a polyvinyl chloride tape impregnated with an insect-acaricidal composition corresponding to the composition for topical application, at the rate of 0.7-0.8 g of active substance per 10 g of tape. The collar is packaged in a hermetically sealed bag, enclosed in individual consumer packaging.

Appointment and method of application

Used for long-term protection against fleas, ticks.

Put a collar on the neck of the animal (dog, cat) at least one day before going to places where there is a potential attack of ticks. Before walking in places of a large accumulation of ticks, additionally treat the limbs of the animal with a spray. The use of a collar to increase the effectiveness of protection against ticks is best combined with other forms of the drug for a similar purpose in the form of drops or spray.

The result

The active components that make up the collar, gradually standing out from the surface of the tape, are transferred to the hairline of the animal and have an insecticide effect on insects and ticks. As a result, the collar provided protection against fleas for 3 months, from ticks for 1.5 months,

All the funds from the above examples, subject to the recommendations for use, do not have a local irritant, skin-resorptive and sensitizing effect.

In all these cases, the proposed combination of insecticide and acaricidal components provides:

- a synergistic effect, manifested in increasing the effectiveness of insecticide and acaricidal action in comparison with monocomponent agents,

- expansion of indications for appointment,

- acceleration of the onset and prolongation of insecticaricidal action in comparison with single drugs.

Adding repellents to the composition of the finished form of the drug increases their acaricidal effectiveness and determines the presence of a protective effect against blood-sucking flying insects.

Table 1. Comparable properties and characteristics Fipronil Solution 200 μg / ml Alphacipermethrin Solution 200 μg / ml The composition of fipronil and alfacipermethrin at 200 μg / ml The onset of acaricidal effect in vivo with topical application, hour 20 ± 4 2.0 ± 0.5 1.0 ± 0.2 Duration of in vivo effect for topical use, days 5 ± 0.5 1.5 ± 0.5 9 ± 1,5 The effectiveness of acaricidal action in contact with ticks treated tissue LD 50 mcg / g 0.29 ± 0.06 0.23 ± 0.05 0.19 ± 0.04 Mortality in an hour,% 10 ± 1.2 42 ± 2.6 63 ± 3.1 Mortality in a day,% 90 ± 4,2 94 ± 4.3 one hundred The effect of reducing tick activity by suction time, min (with a placebo control of 5 min) 10 ± 1 18 ± 2 32 ± 2 Ways of distribution and excretion from the body with external use Through the skin and bloodstream. Cumulation and secretion through the sebaceous glands Excretion through the skin, feces, urine Excretion mainly through the skin, sebaceous glands. Photostability, spectrophotometrically on the dynamics of a decrease in the peak area in the UV region after exposure to the sun high low high Enzyme sensitivity low high moderate Toxicity - refers to hazard class IV according to GOST 12.1.007-76 - MPC in the air of the working area - 0.01 mg / m ³ - refers to hazard class IV according to GOST 12.1.007-76 - MPC in the air of the working area - 0.5
mg / m ³ - refers to hazard class IV according to GOST 12.1.007-76 - MPC in the air of the working area - 0.5 mg / m ³ Skin-irritating and sensitizing effect (drip method, exposure time 24 hours) - lack
- lack - moderate
- lack - weak
- lack

Claims (8)

1. Insecticide and acaricidal agent containing, as active substances, a composition of fipronil and alfacipermetrin at their concentration in wt.% In the total composition of the agent:
fipronil 0.01-10.0 alfacipermethrin 0.01-10.0
with a ratio of mass fractions of 1 part of fipronil to 0.1-20 parts of alphacipermethrin. 2. The tool according to claim 1, characterized in that it is in the form of drops in the form of drops for topical use and contains fipronil in a concentration of 2.5-10 wt.% And alpha-pericamethrin in a concentration of 0.25-2.5 wt.%. 3. The tool according to claim 1, characterized in that it is a ready-made form in the form of a lotion, solution or spray for application to the hair, skin, plumage of birds and contains fipronil in a concentration of 0.05-1.0 wt.% And alphacipermetrin in concentration of 0.01-1.0 wt.% and additionally contains repellents in a concentration of 5 wt.% or more. 4. The tool according to claim 1, characterized in that it is a ready-made form in the form of a solution, lotion or emulsion for processing places of keeping animals and contains 0.05-1.0 wt.% Fipronil and 0.05-1.0 wt. .%. alfacipermethrin. 5. The tool according to any one of claims 2 to 4, characterized in that it further comprises benzyl benzoate in a concentration of 0.1-1.0 wt.% And / or an extract of melia (Melia azedarach L.) in a concentration of 0.1-1, 0 wt.%. 6. The tool according to claim 1, which is a ready-made conditioner for wool in the form of a balm or spray, characterized in that it contains fipronil in a concentration of 0.01-0.1 wt.%, Alfacipermetrin in a concentration of 0.01-0.1 wt.% and additionally may contain benzyl benzoate in a concentration of not more than 1 wt.% and extract of melia (Melia azedarach L.) in a concentration of not more than 1 wt.%. 7. The tool according to claim 1, characterized in that it is a concentrate in liquid form, which contains, wt.%:
fipronil 0.5-5.0 alfacipermethrin 5.0-10.0 benzyl benzoate to 10 melia extract until 3 Excipients rest 8. The tool according to claim 1, characterized in that it is used as part of a collar made of polymer, natural or combined materials.