Composition of synergistic action for controlling parasitic acarids on animals

FIELD: animal science.

SUBSTANCE: the innovation deals with applying high-activity composition of synergistic action for controlling parasitic acarids on animals that contains the combination of pyrethroid and nicotinyl compounds and, also, the method for treating animals infected with parasitic acarids in the course of which it is necessary to treat animals with the above-mentioned composition.

EFFECT: higher efficiency of control.

6 cl, 9 ex, 4 tbl

 

The present invention relates to compositions for combating parasitic acaridae on animals, and more particularly to compositions synergistic action to combat parasitic acaridae on animals.

It is known that pyrethroids are applied against acarid. For example, in U.S. patent 5,236,954 described liquid-phase composition of PYRETHROID concentration, most 50 wt.%, you can use as the basis for other containing pyrethroids compositions in physical phases other than liquid, and describes methods of using this composition as a means to destroy parasites. It is also known that nicotinamine connection, in particular chloronicotinyl, effective against fleas. In PCT application WO 93/24 002 describes that certain derivatives of 1-[N-(halo-3-pyridylmethyl)]-N-methylamino-1 alkylamino-nitroethylene suitable for systemic use against fleas from Pets. In U.S. patent 6,001,858 described dermal application chloronicotinyl compounds, which are particularly suitable for control of parasitic insects, such as fleas, lice and flies on animals.

Object of the invention is the development of highly active compositions for combating parasitic acaridae on animals, allowing to expand the Arsenal of tools to combat parasitic acaridae.

Set for the ache is solved by the proposed composition of the synergistic action to combat parasitic acaridae on animals containing a combination of a PYRETHROID and nicotinamidase connections.

PYRETHROID insecticides are more stable synthetic analogues of naturally occurring pyrethrins. Pyrethroids bind to membrane receptors along the nerve axon, causing prolonged opening of sodium channels, resulting in prolonged depolarization, the re-excitation of nerve and synapse violations, leading to symptoms of hyperphosphatemia. Nicotinamide compounds have a specific mode of action and biological properties that are anatomically and physiologically different from the properties of pyrethroids. They are associated with nicotinergic receptors in the postsynaptic region of the nerve that keeps the chemical acetylcholine transmitter signals between nerves from binding and signaling. According to reports, chloronicotinyls connection is more specific than the pyrethroids, for binding sites on the nerves of insects compared with the nerves of acarid and vertebrates.

Without being bound to any particular theory of the invention, it is assumed that nicotinamine connection is not associated with the number of receptor sites on the postsynaptic areas nerves of acarid sufficient to ensure activity. Thus, chloronicotinyls connection ineffective or only in the scarlet degree active against ticks and ixodid ticks.

However, the combination of a PYRETHROID and chloronicotinyl insecticide provides enhanced activity against mites and ticks. The increased activity is particularly noticeable if you use two connections for rapid destruction of acarid, then apply one PYRETHROID, and then again two connections at the end of the effective processing, when the effect of some pyrethroids begins to decline.

Illustrative, but not limiting examples of the PYRETHROID is permethrin, fentin, cypermethrin, cigalotrin, lambda cigalotrin, cyfluthrin, cyphenothrin, tralomethrin, telocity, deltamethrin, kabalikat, fluvalinate, flumethrin and fenvalerate. It is preferable permethrin [(3-phenoxy-phenyl)methyl-3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate], flumethrin [α-cyano(4-fluoro-3-phenoxy)-benzyl-3-[2-chloro-2-(4-chlorophenyl)-vinyl]-2,2-dimethylcyclopropanecarboxylate] and cyfluthrin [α-cyano(3-phenoxyphenyl)-methyl-3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate].

Chloronicotinyl compounds are known, for example, EP-A№№580553, 464830, 428941, 425978, 386565, 383091, 375907, 364844, 315826, 259738, 254859, 235725, 212600, 192060, 163855, 154178, 136636, 303570, 302833, 306696, 189972, 455000, 135956, 471372, 302389; DE-A No. 3639877, 3712307; JP-A№№03220176, 02207083, 63307857, 63287764, 03246283, 049371, 03279359, 03255072; U.S. patent 5,034,524, 4,948,798, 4,918,086, 5,039,686 and 5,034,404; PCT application no WO 91/17659, 91/4965; FR-A No. 2611114.

These compounds can in order to be represented by the General formula (I)

where

R means hydrogen, optionally substituted radicals from the series: acyl, alkyl, aryl, aralkyl, heteroaryl or heteroaromatic;

And means monofunctional group from the series of: hydrogen, acyl, alkyl, aryl, or means of bifunctional group associated with the radical Z;

E. means of electron-terminating radical;

X means the radical-CH= or =N-, and it is possible that the radical-CH= instead of atom N is linked to the radical Z;

Z means a cross-functional team from a number of: alkyl, -O-R, -S,-R,

or means of bifunctional group associated with radical or the radical X.

Especially preferred compounds of formula (I) are those in which the radicals have the following meaning:

R means hydrogen and optionally substituted radicals from the series: acyl, alkyl, aryl, aralkyl, heteroaryl, heteroaromatic.

Acyl radicals which may be mentioned are formyl, alkylsulphonyl, arylcarbamoyl, alkylsulfonyl, arylsulfonyl, (alkyl)-(aryl)-phosphoryl, which, in turn, can be overridden.

As the alkyl may be referred to C1-10-alkyl, especially With1-4-alkyl, specifically methyl, ethyl, isopropyl, sec - or tert-butyl, which, in turn, can be overridden.

As the aryl may be mentioned is phenyl or naphthyl, especially phenyl.

As aralkyl can be mentioned phenylmethyl or phenethyl.

As heteroaryl can be mentioned heteroaryl containing up to 10 ring atoms and N, O or S, especially N as the heteroatoms. I can specifically be mentioned thienyl, furyl, thiazolyl, imidazolyl, pyridyl and benzothiazolyl.

As heteroallyl can be mentioned heteroaromatic or heteroaromatic containing up to 6 ring atoms and N, O or S, especially N as the heteroatoms.

As an exemplary and preferred substituents can be specified as follows:

alkyl, preferably containing from 1 to 4, especially 1 or 2 carbon atoms, such as methyl, ethyl, n - and ISO-propyl and n-, ISO - and tert-butyl; alkoxy group, preferably containing from 1 to 4, in particular 1 or 2 carbon atoms, such as methoxy, ethoxy-, n - and ISO-propyloxy - and n-, ISO - and tert-butiki group; alkylthio group, preferably containing from 1 to 4, in particular 1 or 2 carbon atoms, such as methylthio, ethylthio-, n - and ISO-propylthio - and n-, ISO - and tert-butylthio group; halogenated, preferably containing from 1 to 4, in particular 1 or 2 carbon atoms and preferably from 1 to 5, in particular 1 to 3 halogen atoms, and halogen atoms may be identical or different, preferably it is fluorine atoms, chlorine or brough is a, especially fluorine, such halogenation may be trifluoromethyl; hydroxyl; halogen, preferably fluorine, chlorine, bromine and iodine, especially fluorine, chlorine or bromine; piano-, nitro-, amino-group; monoalkyl and dialkylamino group, preferably containing from 1 to 4, in particular 1 or 2 carbon atoms in the alkyl group, such as methylamino-, methyl-ethyl-amino, n - and ISO-propylamino - methyl-n-butylamino group; carboxyl; carbalkoxy-group containing preferably 2 to 4, in particular 2 or 3 carbon atoms, such as carbomethoxy and carboethoxy group; sulfo (SO3H); alkylsulfonyl, preferably containing from 1 to 4, in particular 1 or 2 carbon atoms, such as methylsulphonyl and ethylsulfonyl; arylsulfonyl containing preferably from 6 to 10 aryl carbon atoms, such as phenylsulfonyl and heteroarenes and heteroarylboronic group, such as chloropyridine and chloronitrotoluenes-group.

And most preferably means hydrogen and optionally substituted radicals from the series: acyl, alkyl or aryl, which preferably have the meanings specified for R. And Additionally means of a bifunctional group. It may be mentioned optionally substituted alkylene containing 1-4, especially 1-2 carbon atoms, possible substituents correspond to the substituents mentioned above, and Alki ENOVIA group may be interrupted by heteroatoms from the series N, Oh and S.

A and Z together with the atoms to which they are joined, can form a saturated or unsaturated heterocyclic ring. Heterocyclic ring may contain 1 or 2 identical or different heteroatoms and/or heterogroup. Preferred heteroatoms are oxygen atoms, sulfur or nitrogen, and the preferred heterographs - N-alkyl, where alkyl in N-alkyl group preferably contains from 1 to 4, especially 1 or 2 carbon atoms. As the alkyl may be mentioned methyl, ethyl, n - and ISO-propyl and n-, ISO - and tert-butyl. Heterocyclic ring contains from 5 to 7, preferably 5 or 6 ring atoms.

As examples of heterocyclic rings may be mentioned imidazolidin, pyrrolidine, piperidine, piperazine, hexamethyleneimine, hexahydro-1,3,5-triazine, hexahydroazepin and morpholine, each of which may be optionally substituted, preferably the stands.

E. means of electron-giver radical, especially can be referred to NO2CN and halogenoalkanes, such as 1,5-halogen-C1-4-carbonyl, especially COCF3.

X is-CH= or-N=.

Z signifies optionally substituted radicals: alkyl, -OR, -SR or-NRR, where R and the substituents preferably correspond to the above-mentioned values.

Z may indicate, separately from the above-mentioned ring, and together the atom, with which it is associated, and with radical = - for X, saturated or unsaturated heterocyclic ring. Heterocyclic ring may contain 1 or 2 identical or different heteroatoms and/or groups. Preferred heteroatoms are oxygen atoms, sulfur or nitrogen, and the preferred heterographs - N-alkyl, where alkyl in N-alkyl group preferably contains from 1 to 4, in particular 1 or 2 carbon atoms. As the alkyl may be mentioned methyl, ethyl, n - and ISO-propyl and n-, ISO - and tert-butyl.

Heterocyclic ring contains from 5 to 7, preferably 5 or 6 ring atoms.

As examples of heterocyclic rings may be mentioned pyrrolidine, piperidine, piperazine, hexamethyleneimine, morpholine and N-methylpiperazine.

Most preferred are compounds of General formula (II) and (III):

where

n denotes 1 or 2,

The mandated. means one of the above substituents, in particular halogen, in particular chlorine,

A, Z, X and E have the above values,

Specifically, you can specify the following connection:

In the method of obtaining the composition according to the present invention the active ingredients can be combined in any convenient way, for example in the form of an aqueous solution, suspension or emulsion or in the form of a solid matrix, such as labels for the ears or collars. Preferably, both of the active ingredient were dissolved in one or more solvents used in the composition. The active ingredients can be combined by mixing with fillers, such as liquid solvents, liquefied gases under pressure and/or solid carriers, possibly with the use of surface-active substances.

The concentration of the active ingredients in the proposed composition should be effective to combat parasitic insects is whether acaridae. Usually PYRETHROID may be present in concentrations of from 0.1 to 60 wt.%, preferably from 40 to 60 wt.% Nicotinamide compounds may be present in concentrations of from 0.001 to 60 wt.%, preferably from 0.1 to 25 wt.%. Most preferably the composition contains at least 40 wt.% PYRETHROID, in particular permethrin, and 8-10 wt.% nicotineamide compounds, in particular Imidacloprid. Drugs that should be diluted before use contain the active substance in concentrations from 0.1 to 90 wt.%. For dermal use in animals, the composition preferably contains the active substance in concentrations of from 0.1 to 25 wt.%, more preferably from 5 to 20 wt.%. Given these guidelines, specialist in the art will be able to choose the type and concentration of pyrethroids, which are not toxic to mammals, especially cats.

Used solvents are selected from the group including, for example, water, oils, pyrrolidone, alcohols and cyclic carbonates; possible co-solvents of similar groups. Preferred oils include light mineral oil and vegetable oil. The preferred pyrrolidone is N-organic. Preferred alcohols include, for example, aromatic or aliphatic alcohols, such as glycol, benzyl alcohol, isopropanol, ethanol, diethyl who glycol, propylene glycol, 2-octyl-1-dodecanol and tetrahydrofurfuryl alcohol. They are present in a concentration of from at least 0.01 to 95 wt.%, preferably from 1 to 30 wt.%, particularly preferably from 1 to 20 wt.%. Preferred cyclic carbonates include ethylene carbonate resulting and propylene carbonate. Particularly preferred is propylene carbonate, which may be present in a concentration of from 2.5 to 99,9999%by weight, preferably from 7.5 to 90 wt.%, most preferably from 10 to 90 wt.%.

Other suitable auxiliary components are: preservatives, such as benzyl alcohol (not required if already present as a solvent), trichloroethanol, p-hydroxybenzoic esters, n-butanol, piperonyl piperonyl and water as the amplifier solubility. They are present in a concentration of from 0 to 15 wt.%, preferably from 2.5 to 12.5 wt.%, particularly preferably from 2.5 to 10.0 wt.%. The total number of active ingredients, solvents and additives is 100 wt.%.

Thickeners can be, for example, inorganic thickeners such as bentonites, colloidal silicic acid, aluminum monostearate, organic thickeners such as cellulose derivatives, polyvinyl alcohols, polyvinylpyrrolidone and their copolymers, acrylates and methacrylates.

Used dyes are dyes which do, approved for use in drugs, these dyes can be dissolved or suspended.

Lubricating agents include, without limitation oils such as di-2-ethylhexyl adipate, isopropyl myristate, dipropyleneglycol pelargonate, cyclic and acyclic silicone oils such as Dimethicone, as well as their copolymers and ternary copolymers with ethylene oxide, propylene oxide and formaldehyde, fatty acid esters, triglycerides and fatty alcohols.

Antioxidants may be, for example, sulfites or metabisulfite, such as potassium metabisulfite, ascorbic acid, bottled hydroxytoluene, butilirovannyj hydroxyanisole, tocopherol. Light stabilizers are, for example, substances of class of benzophenone or acid Novantisol (vinylbenzenesulfonic acid). Binding agents are, for example, polymeric thickeners such as cellulose derivatives, starch derivatives, polyacrylates, naturally occurring polymers, such as alginates and gelatin.

Additives are emulsifiers, such as nonionic surfactants, for example polyoxyethylene castor oil, polyoxyethylene the sorbitol monooleate, sorbitol monostearate, glycerol monostearate, polyoxyethyl stearate, alkylphenol polyglycolether esters; impolitically surfactant is substance, such as N-lauryl-β-iminodipropylamine disodium or lecithin; anionic surfactants such as sodium lauryl sulfate, sulfates of fatty esters of alcohols, salt of monoethanolamine, mono/dialkyl-polyglycolide ester, phosphoric ester; and cationic surfactants such as cetyltrimethylammonium chloride.

Being low toxicity for warm-blooded species, the composition according to the present invention are suitable for combating parasitic acaridae on animals, including dogs, cats, horses, cattle, pigs, sheep and humans. Composition active against all or individual stages of development of the pests and against resistant and normal sensitive species of parasites.

In practice, the composition can be applied in any convenient way. When dermal application, for example, the composition can be applied to the animal drops in a small but effective amount, Synergistic results are obtained regardless of whether applied active substances together in the form of individual compounds or, which is preferred, in the form of common stock.

The combination is particularly effective against Acarina (ticks and mites). The combination is particularly effective against species Demacentor variabilis and Rhipicephalus sangumeus ticks on dogs. These results are unexpected, as agonists or antagonists and eticholeve receptors insects, such as Imidacloprid, do not have significant activity against acarid, such as mites and ticks; however, their combination with permethrin leads to a significant increase activity against these parasites.

The composition according to the present invention may optionally contain other active ingredients, such as insect growth regulators (pyriproxifen, methoprene that do not interact with the drug and does not reduce the effectiveness of the combination).

It is preferable nicotinoyl compounds that can be used for the purposes of the invention include Imidacloprid, thiacloprid, clothianidin, AKD 1022 and Ti 435.

Further, the invention is illustrated by examples in which all parts and percentages are mass, unless otherwise specified.

EXAMPLES

Example 1

The objective of this study is to determine the impact of combination on fleas and ticks for 30 days at the dermal application in dogs. The effect of the combination compared with the influence of one of permethrin, Imidacloprid, fipronil and selamectin. The last two compounds are present in the products that are currently used to control fleas and ticks.

Thirty-six dogs are divided into six groups of 6 dogs each. Every dog used to be applied on the skin the preparation of the investigating number: "Kiltix", the drug corporations Voeg containing 45 wt.% permethrin, Advantage®product Corporation Voeg containing 9.1 wt.% Imidacloprid, a combination of drugs Kiltix and Advantage, containing 45 wt.% permethrin and 9.1 wt.% Imidacloprid, Top Spot®drug production Merial, containing 9.7% fipronil or Revolution®, a product of Pfizer Inc., containing 12% (weight/volume) of selamectin. Drugs used in appropriate doses, according to the instructions on the various use of drugs. Control dogs do not handle. All products presented in the dosing tubes for drawing.

For the period from 7 to 14 days before treatment dogs wash with mild shampoo without drugs and carefully comb to remove existing fleas and ticks. Day -3 dogs infect 100 hungry adult ixodid ticks (50 Dermacentor variabilis and 50 Rhipiciphalus sanguineus) and 100 hungry adult fleas. Live fleas and ticks count at day-1. Dogs spread over the total number of live ticks until it is processed from a larger number to a smaller one. To study selected 36 dogs with the highest number. Each group of 6 dogs is one unit. The treatment is carried out in a random way within one block of the dogs.

Each dog visually check for the presence of fleas and ticks at 1, 7 14, 21 and 28 days after treatment. For counting fleas and ticks hair pushing his fingers. At icyhot the number of live mites. 2, 8, 15, 22 and 29 day visually count the number of live mites. 3, 9, 16, 23 and 30 day dog comb. Calculate the remaining live fleas and ticks and remove them.

Doses of different compounds are given in table 1.

td align="center"> Apply the contents of the tube onto the skin in one spot between the shoulder blades
Table 1

The dose of the compounds used dermal dogs
GroupProcessingDoseApplication
145% Permethrin<33 pounds =1.5 ml

>33 pounds =2×1.5 ml
<33 pounds: 1.5 ml of the solution on the back between the shoulder blades

>33 pounds: 1.5 ml between the shoulder blades +1.5 ml of the sacrum at the base of the tail
2of 9.1% Imidacloprid< £ 10 =0.4 ml

11-20 lbs =1.0 ml

21-55 lbs =2.5 ml

>55 pounds =4,0 ml
On his back at one point, between the shoulder blades

Evenly apply 3-4 points on the back between the shoulder blades to base of tail
345% Permethrin

+9,1% Imidacloprid
Same as above for both productsApply according to the instructions above, but do not apply both products in one spot
49.7% Fipronil<22 pounds =0,67 ml

23-44 lb =1.3 ml

45-48 pounds =2,68 ml
512% Selamectin

(120 mg/ml)
the 10.1-20 lbs =0.5 ml

of 20.1-40 lbs =1.0 ml

40,1 -85 pounds =2.0 ml
Apply the contents of the tube onto the skin in one spot between the shoulder blades
6ControlNo processing
The results of this study are shown in Tables 2, 3 and 4.

/tr>
Table 2

COMPARATIVE EFFECTIVENESS

D. VARIABILIS

The PERCENTAGE of CONTROL
Study dayImidaclopridPermethrinImidacloprid + PermethrinFipronilSelamectin
1-12,036,264,2*92,926,2
216,953,981,9*10046,7
330,975,396,410070,8
732,5for 95.297,010023,1
835,396,198,410061,2
939,4to 97.198,610083,2
1450,391,597,498,716,6
1566,492,999,210032,7
1668,496,899,210046,1
2150,290,887,7of 92.72,7
2240,185,194,598,7and-0.6
2350,289,397,710024,7
2838,879,3**91,869,70,1
* Application of Fipronil significantly different from the combined application of Imidacloprid and Permethrin

** Joint application of Imidacloprid and Permethrin differs significantly from the use of Fipronil

Table 3

COMPARATIVE EFFECTIVENESS

R. SANGUINEUS

The PERCENTAGE of CONTROL
Study dayImidaclopridPermethrin/td> Imidacloprid + PermethrinFipronilSelamectin
115,572,7of 76.896,3-13,1
242,475,085,910048,5
335,985,091,810087,4
767,299,4the 98.910083,9
872,010010010083,6
966,699,010010095,6
1453.5for 95.2for 95.299,4a 21.5
1558,2the 98.9of 98.210046,0
1654,099,498,499,470,9
2141,589,4of 87.086,0-7,0
2218,991,791,8100-2,2
23-5,391,599,01008,2
2839,168,684,665,3-16,0

Table 4

COMPARATIVE EFFECTIVENESS

FLEAS (Siphoneptera)

The PERCENTAGE of CONTROL
DayImidaclopridPermethrinImidacloprid + PermethrinFipronilSelamectin
-11,5of 5.427,722,415,1
189,8100100100of 87.3
393,9100100100100
779,4100100100100
9of 87.8100100100100
1471,910010010099,7
1665,1100100100100
2152,910099,810099,8
2341,999,6100100
2843,998,698,410086
307,799,498,710098

From this study we can draw the following important conclusions.

1. The combination of permethrin and Imidacloprid provides a more rapid death of both species of ticks (D. variabilis and R. sanguineus)than permethrin or Imidacloprid separately. The combination has ensured the death of mites on 82-86% on day 2 after applying and about 100% mortality of both species of ticks on day 3 after application. When using one of permethrin required 7 days to achieve 100% destruction of ticks. When applying selamectin required 9 days to reach only 83% of the deaths of D. variabilis, and then the connection was lost activity. Selamectin provided earlier death of R. sanguineus (87% on day 3), however, the efficacy of the death of mites from selamectin has declined rapidly and was insignificant to 16 days after application. Fipronil provided early death similar to death from the combination of permethrin and Imidacloprid.

2. The time period in which considerable control of ticks, when using a combination of permethrin and Imidacloprid was significantly longer than when using odnogoporyadka, one of Imidacloprid, selamectin or fipronil. The data indicate that the use of the combination of permethrin and Imidacloprid provides control of ticks of both species at 85-92% to 28 days after application.

3. The presence in the composition of permethrin did not affect the mortality of fleas on dogs. Table 4 shows that one permethrin provided some effect of the death of fleas from 1 to 21 days, while Imidacloprid killed all the fleas from 1 to 30 day. The combination of permethrin and Imidacloprid provided equally effective death fleas from 1 to 30 day. Selamectin was not as effective as Imidacloprid or as a combination of Imidacloprid and permethrin. When applying the last of the preparation needed 3 days for a significant loss of fleas, and then this effect decreased to 28 days after application. When applying fipronil watched the level of the death of fleas equal to the level of destruction in the application of Imidacloprid or a combination of Imidacloprid and permethrin.

4. Rapid onset of death as fleas and ticks when using a combination of permethrin and Imidacloprid indicates the effective dissemination of both active ingredients.

5. The duration of the period in which the combination remained active against ticks of both species and fleas, indicates adequate distribution of the active ingredients in the skin of animals. This is closely in line is Chislennoe indicates, the combination of a PYRETHROID and nicotinergic compounds results in a synergistic effect of the death of mites and remains effective against the death of fleas. Effect of death of ticks when using a combination began earlier and lasted longer than when using one of permethrin or Imidacloprid.

Example 2

This study is to assess the safety of different compounds. It is determined by examination of the skin in the location (s) of application and behavior of dogs after application. None of the compounds did not cause irritation at the application site, and no dog expressed concerns after application. Thus determined that the combination of permethrin and Imidacloprid safe, non-irritating and effective against ticks and fleas. It is expected that it will be effective against other species of ticks, as they react similar to ixodid ticks.

Example 3

Repeat example 2 with the difference that to fight ixodid ticks apply tailored and permethrin (experience), as well as clothianidin and permethrin (experiment b).

In the case of combating parasitic acaridae D. Varriabilis 3 days after treatment, the degree of mortification is to 97.1% (experiment a) and 97,3% (experiment b), whereas in case of separate application of both active substances, the degree of killing is in the experience and only 24.5% and 75.3% of the cuts in estwenno, as in experiment b), only 23.9 percent and 75.3%, respectively. In the case of combating parasitic acaridae R. Sanguineus 3 days after treatment, the degree of killing is 93,6% (experiment a) and 94,1% (experiment b), whereas in case of separate application of both active substances, the degree of killing is in the experience and only 33.8% and 85%, respectively, in experiment b) -only 32,4% and 85%, respectively.

Synergism is also apparent when the use of a composition containing a combination of above-mentioned pyrethroids and nicotinic compounds.

The following examples illustrate the proposed composition in the form of ready-to-use homogeneous solution.

Example 4

The homogeneous solution, applied with a stain consisting of

45 g of permethrin

10 g of Imidacloprid

with 44.8 g of N-methylpyrrolidone

0.1 g of citric acid

0.1 g of butylhydroxytoluene as antioxidant.

Example 5

The homogeneous solution, applied with a stain consisting of

45 g of permethrin

10 g thiacloprid

of 40.8 g of N-methylpyrrolidone

4.0 g of water

0.1 g of citric acid

0.1 g of butylhydroxytoluene.

Example 6

The homogeneous solution, applied with a stain consisting of

45 g of permethrin

10 g To clothianidin

with 44.8 g of N-methylpyrrolidone

0.1 g of citric acid

0.1 g of butylhydroxytoluene.

Example 7

The homogeneous solution, applied with a stain consisting of

45 is permethrin

7.5 g AKD-1022

43,3 g of N-methylpyrrolidone

4.0 g of water

0.1 g of citric acid

0.1 g of butylhydroxytoluene.

Example 8

The homogeneous solution, applied with a stain consisting of

and 47.5 g of flumethrin

10 g of Imidacloprid

to 38.3 g of N-methylpyrrolidone

4.0 g of water

0.1 g of citric acid

0.1 g of butylhydroxytoluene.

Example 9

The homogeneous solution, applied with a stain consisting of

47,5 g spraying with cyfluthrin

10 g of Imidacloprid

of 42.3 g of N-methylpyrrolidone

0.1 g of citric acid

0.1 g of butylhydroxytoluene.

1. The composition is a synergistic action to combat parasitic acaridae on animals containing a combination of a PYRETHROID and nicotinamidase connections.

2. The composition according to claim 1, characterized in that the concentration of PYRETHROID compounds is from 0.1 to 60 wt.%, and the concentration nicotinell compound is from 0.001 to 25 wt.%, in relation to the total weight of the composition.

3. The composition according to claim 1, characterized in that as a PYRETHROID compounds it contains permethrin.

4. The composition according to claim 1, characterized in that as nicotinell compounds it contains Imidacloprid.

5. The composition according to claim 1, characterized in that as a PYRETHROID compounds it contains permethrin, and as nicotinell compound is Imidacloprid.

6. The method of processing animal is, infected parasitic acaridae, in which the treatment is carried out with a composition according to claim 1.



 

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10 cl, 10 dwg, 9 tbl, 14 ex

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2 ex

FIELD: veterinary, in particular formulation for controlling of mammalian skin pests.

SUBSTANCE: claimed formulation contains (mass %): fipronil 0.3-5; methopren up to 1 %; benzylbenzoate 5-40 and balance: alcohol solvent. Formulation of present invention is useful in agriculture and treatment of domestic and wild animals, as well as treatment of apartments.

EFFECT: effective formulation for controlling of mammalian skin pests with prolonged storage time.

4 cl, 5 ex

FIELD: organic chemistry, pesticides.

SUBSTANCE: claimed composition represents mixture of carvacrol and thymol compounds with salt of transition metal, namely zinc, wherein carvacrol and thymol compound/zinc ratio is from 60:40 to 65:35. Also described is pesticide composition containing mixture of carvacrol and thymol compounds with salt of transition metal, namely zinc, and at least one carrier, wherein weight ratio of carvacrol to thymol is 10:1. Claimed method for parasite controlling includes step of composition blending with carrier and application thereof onto target area.

EFFECT: composition for pest controlling and prevention of contamination with pests such as insect, mite, fungi or parasites.

FIELD: veterinary science.

SUBSTANCE: the suggested preparation contains Trichlorfon and 30%-ethanol at the following ratio of components, weight%: Trichlorfon 3.5-3.7 and 30%-ethanol or 3%-boric acid solution in 30%-ethanol - up to 100. Application of this innovation enables to shorten therapy terms and improves therapeutic effect.

EFFECT: higher efficiency of therapy.

4 ex

FIELD: medicine.

SUBSTANCE: method involves administering antihistamine preparations and antibiotics, applying external treatment of injured skin areas with Hypchlophos, intramuscularly introducing anatoxin vaccine against animal staphylococcosis and immunostimulating agent like Immunoparasitan. Reinfusion session is applied at the treatment beginning after ultrasonic proper blood irradiation having been applied at a dose of 1-3 cm3/kg of body mass. Vitamin B12 is additionally intramuscularly introduced at a dose of 3-7 mcg/kg of body mass at the treatment course end. Hypchlophos is applied as oil emulsion in 1:1 proportion. Reinfusion combined with ultrasonic proper blood irradiation is administered together with anatoxin vaccine introduction at the same day continuing the treatment within 2-3 days.

EFFECT: enhanced effectiveness in normalizing metabolism processes and in increasing immunostimulation; reduced toxic adverse side effects.

4 cl, 1 tbl

FIELD: organic chemistry, veterinary science.

SUBSTANCE: invention relates to a method for control over exto- and endoparasites taken among group including acariform mites, parasitoformous mites and nematodes parasitizing in animals, productive cattle and domestic animals. Method involves applying veterinary preparation comprising 1-[4-chloro-3-(3-chloro-5-trifluoromethyl-2-pyridyloxy)phenyl]-3-(2,6-difluoro)urea and compound of the formula (i):

wherein R1 means one of radicals:

or ; R2 means -CH(CH3)-CH3, -CH(CH3)-C2H5, -C(CH3)=CH-CH(CH3)2 or cyclohexyl; R3 means hydrogen atom or hydroxy-group if a bond between atoms 22 and 23 represents a double bond, or it means hydrogen atom or group =N-O-CH3 if an ordinary bond presents between atoms 22 and 23; R4 means HO-, and the preparation can be in free form or in physiologically acceptable form. Invention provides preparing preparations with good tolerance and rapid effect and persistence with respect to different helminth-associated diseases, parasitiformous and acariformous mites being without adverse effect on normal behavior of animals.

EFFECT: valuable properties of compounds.

7 cl, 3 tbl, 8 ex

FIELD: veterinary science.

SUBSTANCE: the present innovation deals with overall treatment of velvet antlers with chemical preparation due to spraying in case of loose movement of animals through their pen as a corridor open from both sides, as preparation one should apply "Butox" at deltametrin concentration being 0.002-0.003% and dosage being 250-350 ml/animal.

EFFECT: higher efficiency.

3 ex, 2 tbl

FIELD: organic chemistry, chemical technology, insecticides.

SUBSTANCE: invention describes new compounds of the formula (X): wherein R1 means -CH2-Het; R means unsubstituted (C1-C20)-alkyl or (C1-C20)-alkyl that is substituted with one or some phenyls, or it means unsubstituted phenyl or phenyl substituted with (C1-C6)-alkyl, or it means (C1-C6)-alkyl that is substituted with cyclohexyl or means unsubstituted (C3-C7)- cyclohexyl or substituted with one or some substitutes taken among the group including halogen atom and (C1-C6)-alkyl, or it means biphenyl, or phenoxyphenyl; T and U each means independently from one another (C1-C6)-alkyl; R2, R'2 mean hydrogen atom; Het means pyridyl that is substituted with halogen atom. Also, invention describes a method for preparing compound of the formula (X) by interaction of compound of the formula (XX) with acid R-COOH and isolation of the end product from reaction mixture wherein substitutes R, R1, R2, R'2, T and U have values indicated for the formula (X); Hal means halogen atom. Also, invention describes a parasiticidal composition for control of blood-sucking insects. Invention provides preparing compounds eliciting parasiticidal activity with expressed prolonged effect.

EFFECT: improved preparing method, valuable properties of compounds and composition.

11 cl, 8 tbl, 8 ex

FIELD: medicine, parasitology.

SUBSTANCE: the present innovation deals with preparations to be applied for parasites control. The suggested parasiticidal composition for local application for an animal contains pyrethroid or pyrethrin and a carrier. As a carrier it contains an alkylglycol ether with terpene or terpene's derivative. The method for fighting with infecting by ectoparasites in animals deals with local application of the suggested parasiticidal composition. The innovation enables to decrease crystallization of the active substance.

EFFECT: higher efficiency.

18 cl, 5 ex, 11 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel ester compounds represented by the formula (1): wherein values for R1, R2, A, X, R3, R4, Alk1, Alk2, l, m, D, R8 and R9 are determined in the invention claim. Also, invention relates to inhibitor of matrix metalloproteinase (MTP), a pharmaceutical composition able to inhibit activity of MTP selectively, agents used in treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery diseases, obesity, diabetes mellitus or hypertension wherein the pharmaceutical composition is prepared in capsulated formulation, and to a biphenyl compound of the formula (100) given in the invention description.

EFFECT: valuable medicinal properties of compounds.

53 cl, 78 tbl, 17 ex

FIELD: pharmaceutical industry, in particular cyprofloxacine solution.

SUBSTANCE: claimed solution contains cyprofloxacine hydrochloride, sodium salt of ethylenediamine-N,N,N1,N1-tetraacetic acid, α-hydroxypropionic acid, sodium chloride, water for injections.

EFFECT: drug of increased biological availability without side effects.

3 tbl

FIELD: organic chemistry, medicine, endocrinology, pharmacy.

SUBSTANCE: invention relates to new derivatives of acylphenylurea of the formula (I) and to their physiologically acceptable salts possessing property of glycogen phosphorylase inhibitors. In compound of the formula (I) A means phenyl and phenyl residue can be substituted three times with fluorine (F), chlorine (Cl), bromine (Br) atoms, -CF3, -NO2, -O-(C1-C6)-alkyl, -SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, -COOH; R1 means hydrogen atom (H), (C1-C6)-alkyl; R2 means H, (C1-C6(-alkyl, -CO-(C1-C6)-alkyl; 3, R4, R5 and R6 mean independently of one another H, F, Cl, Br, -O(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C7)-cycloalkyl, -COOH, -COO-(C1-C6)-alkyl; X means oxygen (O), sulfur (S) atom; R7 means (C1-C10)-alkylene-COOH, (C1-C10)-alkylene-COO-(C1-C6)-alkyl, (C1-C10)-alkylene-NH2, (C1-C10)-alkylene-NH-(C1-C6)-alkyl, (C1-C10)-alkylene-N-[(C1-C6)-alkyl]2, (C1-C10)-alkylene-B wherein B means piperidinyl or furyl. Also, invention relates to a pharmaceutical composition and a method for preparing the pharmaceutical composition. Proposed compounds can be used for preparing pharmaceutical composition useful for declining level of blood glucose and for treatment of diabetes mellitus type II.

EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.

7 cl, 2 sch, 2 tbl, 1 ex

FIELD: medicine, pharmacology, pharmacy.

SUBSTANCE: invention relates to composition possessing an anti-inflammatory effect and useful for oral administration in form of emulsion preliminary concentrate. Composition comprises NO-releasing nonsteroid anti-inflammatory drug, surface-active substance, oil or semisolid fat and forms in situ emulsion of type oil-in-water after contact with aqueous medium, such as gastroenteric fluid. Also, invention relates to a medicinal formulation based on thereof, oral emulsion, set based on thereof and a method for treatment of inflammation and pain. Proposed compositions possess the improved availability.

EFFECT: improved and valuable properties of composition.

40 cl, 1 tbl, 20 ex

The invention relates to medicine, in particular, neurology, and for the treatment of symptoms of spasticity and spasms, which are avoided by a centrally mediated decrease in muscle tone

The invention relates to medicines, in particular to a mixture of isomers (9)-tetradecanoate

The invention relates to novim retinoid compounds of General formula I, II, III, IV with retinoid negative hormone biological activity and/or activity of antagonist retinoids, compositions based on them, a method of determining the retinoid antagonists hormones,the method of treating a pathological state in a mammal, vospriimchivosti to treatment with retinoid antagonist or negative hormone by injection of compound I or II

The invention relates to new compounds of General formula I

< / BR>
in which R1selected from the group consisting of hydrogen, unsubstituted or optionally substituted aralkyl, unsubstituted or optionally substituted orelkinoservisa, unsubstituted or optionally substituted allyloxycarbonyl, unsubstituted or optionally substituted alkyl and hydroxyamino group; R2selected from the group consisting of hydrogen, unsubstituted or optionally substituted orelkinoservisa, unsubstituted or optionally substituted allyloxycarbonyl, aminosidine group; R3selected from the group consisting of hydrogen, unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R4selected from the group consisting of unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R5and R6that may be the same or different, each independently selected from the group consisting of hydrogen, unsubstituted or optionally substituted alkyl, unsubstituted or optionally substituted cycle>and R6taken together with the nitrogen atom to which they are attached, form an unsubstituted or optionally substituted heterocyclic group; R7selected from the group consisting of hydrogen, hydroxy, unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R8selected from the group consisting of hydrogen, hydroxy, unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl, and R9selected from the group consisting of hydrogen, hydroxy, amino and a group of the formula-X-Y, in which X is selected from the group consisting of unsubstituted or optionally substituted (C1-C6)-alkylene and unsubstituted or optionally substituted phenylene, and Y denotes a group of formula-a-b or a-B, where a is selected from the group consisting of unsubstituted or optionally substituted (C1-C6)-alkylene, imino and unsubstituted or optionally substituted (C1-C6)-alkylamino, and selected from the group consisting of hydrogen, amino, amidino, acylmethyl, unprotected or optionally protected bis (phosphono)methyl, provided that R7, R8and R are not simultaneously represent

The invention relates to chemical-pharmaceutical industry, concerns the solution of isotretinoin (13-CIS-retinoic acid) and treatment of skin diseases

FIELD: organic chemistry, in particular agent for controlling of sanguivorous insects.

SUBSTANCE: claimed agent contains (mass %): liquid insecticide soap 0.5-1.0; Atremia sp. hydrolysate 0.5-1.0, and balance: water. Method fro production of said agent also is disclosed.

EFFECT: working emulsion with increased moistening activity and effectiveness; improved agent for aphis controlling.

2 cl, 4 tbl, 4 ex

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