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Insectoacaricidal agent

IPC classes for russian patent Insectoacaricidal agent (RU 2243761):
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Insecticide cover for seeds Insecticide cover for seeds / 2243657
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Insecticide cover for seeds Insecticide cover for seeds / 2243657
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Insectoacaricidal agent / 2243761
Invention relates to medical desinsection, household chemistry, and plant protection agents, in particular to contact- and intestinal-type insecticidal and acaricidal preparation, which can be used in medical desinsection area, agriculture, personal support farms, and urban domestic life for controlling pest insects and ticks. Insectoacaricidal agent of invention containing an active principle, preferably of pyrethroid series (e.g. cypermetrin), and solvent additionally contains effective amounts of dodecyldimethylammonium bromide molten together with active principle. Amounts of dodecyldimethylammonium bromide and cypermetrin may vary each between 10 and 500 g/L. Solvent can be deodorized kerosene.
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Insectoacaricidal agent / 2243761
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FIELD: biologically active substances.

SUBSTANCE: invention relates to medical desinsection, household chemistry, and plant protection agents, in particular to contact- and intestinal-type insecticidal and acaricidal preparation, which can be used in medical desinsection area, agriculture, personal support farms, and urban domestic life for controlling pest insects and ticks. Insectoacaricidal agent of invention containing an active principle, preferably of pyrethroid series (e.g. cypermetrin), and solvent additionally contains effective amounts of dodecyldimethylammonium bromide molten together with active principle. Amounts of dodecyldimethylammonium bromide and cypermetrin may vary each between 10 and 500 g/L. Solvent can be deodorized kerosene.

EFFECT: achieved stability, efficiency, low price, and toxic safety of claimed agent.

5 cl, 2 tbl, 2 ex

 

The invention relates to medical pest control, household chemicals and herbicides, in particular insecticidal and acaricidal drugs contact and stomach action, which may find application in medical practice pest control, agriculture, private farms and household for the destruction of harmful insects and mites.

Known insecticidal and acaricidal preparations for agriculture based on synergistic combinations of Supratidal (organophosphorus insecticide) or Sadana (ORGANOTIN acaricide) with benzalkonium salts and dioktyldimethylammonium containing anions of polymeric acids, such as anions of polymethylenepolyphenylisocyanate, polystyrenesulfonate, polyacrylic acid, copolymer of methacrylic and styrelseledamot, copolymer of acrylic and maleic acids [1]. The disadvantages of these HOUR - weak synergistic effect, the difficulty of obtaining and the associated high cost, which makes their use uneconomical (cheaper to just increase the consumption of conventional insecticide or acaricide). Industrial production of these HOURS is missing.

Known drugs contact and stomach action for the destruction of a wide range of harmful insects (beetles, bugs, plant-eating and blood-sucking ticks, flies, woodlice and other), sod is readie HOUR formula [RR 1R2R3N]+X-(where R-R3is alkyl, halogenated alkyl, alkenyl or the halogenated alkenyl and X is halogen), which have chemosterilant activity [2]. Amongst those listed in this patent a specific HOUR is dominated by iodides with allyl, 2-chlorallyl or 2-chlorobutadiene radical, which are the most active chemosterilants. Examples of their application are food bait in a sugar syrup with the addition of 1% allyltrimethylsilane [CH2=CHCH2N(CH3)3]+I-or 0.5% 2-globalitemsneeded [CH2=CClCH2N(CH3)3]+I, effective against screwworm Cochliomya hominovorax. The shortcomings of such an HOUR unavailability on an industrial scale, chemical instability in the compositions and high toxicity for warm-blooded.

Known means of contact action to kill cockroaches and other household insects based on a synergistic combination of a PYRETHROID insecticide with lipophilic salts, benzalkonium and didecyldimethylammonium type [C12H25N(CH3)2CH2C6H5]+X-and [(C10H21)2N(CH3)2]+X-(where X is the residue of stearic, saaristomeri, lauric or dodecylbenzensulfonate) [3]. The experimental data, a CR is entered in this patent, show that the claimed HOURS equivalent as synergists to the corresponding chlorides. Their disadvantages are weak synergistic effect (tested on cockroaches working emulsion contained 0.5% of tetramethrin in combination with a huge number of HOUR - 20%), the difficulty of obtaining and lack of industrial production.

Described insecticidal preparations for destroying termites and soil-inhabiting pests, containing combinations of didecyldimethylammoniumchloride, dioctyldimethylammonium or octylacrylamide with organophosphorus insecticides - fenitrothion or predatation [4]. These drugs are alcohol solution with a very high content of active ingredients (for example, 64% of didecyldimethylammoniumchloride, 5% fenitrothion and 31% of methanol), resulting in low efficiency and greater toxicity to warm-blooded.

Known means of contact steps to eliminate house dust mites, which contain the usual insectoacaracide (PYRETHROID, organophosphorus or other) in combination with an antiseptic that can kill bacteria and fungi that serve as food for the ticks [5]. In the example of the solution of 0.75% of cyhalothrin (a PYRETHROID of insectoacaracide) and 8% of benzylaniline with the addition of isothiazolinones in diethylene glycol. PR is the application of this drug (without dilution) on the filter surface conditioning destruction dwell in them house dust mites was 94,66% after 1 hour and 100% in 2 hours. About synergy HOUR in this patent is not mentioned. The disadvantages of the above means, a narrow scope and a very high content of active ingredients, which accounts for its low cost and relatively greater toxicity to humans and domestic animals. In addition, diethylene glycol possesses narcotic properties, due to which it is used in the composition respecively drug is not desirable. Thus, from among the above HOURS only benzylaniline and didecyldimethylammoniumchloride with less favorable price ratio:efficiency than traditional insecticides. In addition, benzylaniline always contains a mixture of chloride benzyl - substance tear smell, which makes it impossible to use in insecticidal food baits.

Closest to the present invention is insecticide and acaricide composition containing the active ingredient predominantly class of pyrethroids and the solvent (RF Patent 2102060,1998) [6]. This composition is used mainly in the form of powders, tablets, crayons, suspensions. To achieve the effective result of the application of emulsion concentrates require a sharp increase in consumption norms. On this basis, these emulsion concentrates rarely recommended to use the program to kill household insects.

The technical result of the invention - creation stuff means of contact and stomach action for the destruction of harmful insects and mites, which contain available on an industrial scale H in combination with conventional insecticides and acaricides, high efficiency, stability, superior known tools for efficiency and Toxicological safety.

The technical result is achieved in that stuff means, containing the active ingredient predominantly class of pyrethroids and the solvent according to the invention, contains additional didecyldimethylammonium effective amount, fused with the active substance. It is reasonable as the active substance to use cypermethrin. Preferably, the tool may contain didecyldimethylammonium in the amount of 10-500 g/l and cypermethrin in the amount of 10-500 g/l as a solvent it may contain deodorized kerosene.

Didecyldimethylammonium [(C10H21)2N(CH3)2]+Br-(DDAB) - known as H (RF patent 2155186, 27.08.00), can be applied in the form of the free compounds (chemically pure substance or product) or in the form of clathrates with urea DDAB, and clathrates have no smell.

Due to the extremely high and varied antimicrobial activity DDAB offer us the means to destroy not only harmful insects and mites, but carried them pathogenic bacteria, fungi and viruses. This eliminates the need for special additional processing, which further increases the economic benefits from the use of the inventive preparations.

Content DAB in the proposed medication is 0.01-50%, if these drugs include traditional insecticides and acaricides.

To date DDAB was known mainly as a component of such disinfectants as "Veltolen" (patent of the Russian Federation 2095086, 11.10.97), "Veltodez" (patent of the Russian Federation 2189834, 27.09.02), "Veltolen-extra" (patent of the Russian Federation 2158142, 27.10.00).

Table 1 presents the Toxicological characteristics DAB and its clathrates in comparison with didecyldimethylammoniumchloride, benzalkonium and some conventional insecticides. As can be seen from this table, the toxicity DAB is approximately at the same level that didecyldimethylammoniumchloride and benzylaniline, and all these HOURS and, especially, the clathrates DDAB less toxic to warm-blooded than traditional insecticides.

Contact insecticidal activity of combinations DAB with cypermethrin towards the red cockroach confirmed by laboratory research, are presented below.

EXAMPLE 1. In our experiments we used laboratory culture of the German cockroach, available in NII of Disinfectology (NIID) of the Minis is ersta of health of the Russian Federation. Cockroaches were selected as the test object because they are more resistant to insecticides than other insects. The tests were carried out on glass plates by certified methodology [7, method 3.11].

The experiments were conducted using alcohol solutions technical DDAB and technical cypermethrin. The results are shown in table 2.

As can be seen from this table, the combination of 0.12% DAB+0,06% cypermethrin has the same activity as 0.1% cypermethrin. However, it is cheaper and less toxic to warm-blooded. It contains additive DDAB not only increases the activity of cypermethrin, but also imparts new properties - the ability to overcome resistance to insects and mites that are resistant to cypermethrin, and destroy their portable pathogens.

EXAMPLE 2. Prepare stuff emulsion concentrate. This was mixed with 150 g of technical DDAB (considering 80%) with 32 g of cypermethrin technical (considering 95%) and elevated temperature 45°received by fusing a synergistic complex of the active substance. Diluted 110 g of emulsifier was added in deodorized kerosene to 1 L. Received the following structure:

Technical DDAB (considering 80%) 150 g

Technical cypermethrin (considering 95%) 32 g

The emulsifier 100 g

Dezod risovanny kerosene to 1 l

Cypermethrin is a PYRETHROID insecticide that is commonly used in emulsion concentrates for the destruction of harmful insects and mites in medical practice pest control, agriculture, and private farms.

Technical cypermethrin and technical DDAB - viscous semi-liquid mass, slowly soluble in organic solvents. The fusion between them allows to get the active synergetic complex, the dilution of which the emulsifier provides almost instant dissolving it in kerosene at the third stage of the process. To obtain the final product in the form of stable microemulsions recommended third stage with vigorous stirring, gradually adding a solution of the active complex in a thin stream or spraying it through a nozzle. In case of separate addition of cypermethrin, DDAB and emulsifier to kerosene reaction is the formation of an active complex flows in time and does not reach the end.

As the emulsifier may be used any known combination of nonionic surfactants with dodecylbenzenesulfonate calcium (European patent 736252, 09.10.96; U.S. patent 4353897, 12.10.82; U.S. patent 4388297, 14.06.83).

When testing this drug on the cockroaches analogously to example 1 at a dilution of 1:100 (1 ml 99 ml of water, which is matching the 0,12% DAB and 0.03% cypermethrin) observed 100%mortality of insects in the control after 24 hours. The cost of such a working solution 2-4 times less than the working solutions prepared from commercial 25-percentage of emulsion concentrates cypermethrin used in medical disinsection ("Sipes", "Sipas-super", "Cybertron", "Cidor", "Nimbus", "Zyvox" and others).

When the test emulsion concentrate against the Colorado potato beetle on potato against aphids and leafrollers in Apple, raspberry, and currant and against ticks for raspberries and cucumbers at a dilution of 1:2000 (5 ml per 10 l of water) and the flow rate of the working solution of 5 liters per 100 m2landings or 2-5 liters per tree was almost 100%mortality of the pest.

Due to the wide range of activity cypermethrin we offer the drug can also be used against the house and garden ants, fleas, bed bugs, beetles and larvae of flies and mosquitoes. The presence in its composition of two active substances with different mechanisms of action allows you to destroy resistant cypermethrin populations of harmful insects and mites, and the presence of deodorized kerosene as solvent provides no odor and reduces the fire risk of the proposed drug compared with its conventional counterparts on the basis of xylene.

LIST of USED MATERIALS

1. U.S. patent 5164179, 17.11.92.

2. U.S. patent 3397275, 13.08.68.

3. The Japan Patent 09059109, 04.03.97.

4. The Japan patent 61-57506, 24.03.86.

5. Patent UK 2359023, 15.08.01.

6. RF patent 2102060, 20.01.98.

7. Methods of testing disinfectants for evaluation of their safety and efficacy. Decl. The health Ministry of the Russian Federation No. 01-12/75-97. - M., 1998, part 3.

Table 1
Name of toxicant The value of LD50mg/kg
  oral (rat) skin (rabbit)
The chlorpyrifos 135-163 1000-2000
Alpha-cypermethrin 79-400 1600
Cypermethrin 187-326 >2000
Permethrin 430-500 >2000
Didecyldimethylammoniumchloride 788 3600
Benzylaniline 700-750 >2500
DCAB 730-800 >2500
Velton 1350-1500 >2500
Table 2
Abbreviations: par. - paralysis, N. - knockdown, N.N. - irreversible knockdown, died. - death. Statutory performance indicator for PYRETHROID and organophosphorus insecticides contact action - not less than 100% died. after 24 hours.
DV and their contents in the working solution Insecticidal efficiency (%) controlled through
  15 min 24 hours 48 hours
Cypermethrin 0,0075% 70 pairs. 80 N.+20 pairs. 20 N.N.+80 pairs.
0,015% 100 pairs. 50 N.+50 pairs. 20 were killed. + 30 N.N.+50 pairs.
0,03% 100 pairs. 10 were killed.+20 N.N.+70 pairs. 40 were killed. + 60 pairs.
0,06% 20 N.+80 pairs. 40 were killed. + 60 N.N. 60 killed.+40 pairs.
0,1% 100 N. 100 were killed. -
DAB 0.03% of the Chicks who metrin 0,0075% 60 N.+40 pairs. 100 N.N. 100 N.N.
DAB 0,06% Cypermethrin 0,03% 100 N. 60 killed.+40 N.N. 100 were killed.
DAB 0,12% Cypermethrin 0,06% 100 N. 100 killed.. -
DAB 0,24% Cypermethrin 0,06% 100 N. 100 were killed. -

1. Insecticide and acaricide remedy containing the active substance, mainly class of pyrethroids and a solvent, characterized in that it additionally contains didecylammonium bromide and/or clathrate didecyldimethylammonium with urea effective amount, fused with the active substance.

2. Insecticide and acaricide tool according to claim 1, characterized in that the active substance contains cypermethrin.

3. Insecticide and acaricide tool according to claim 1 or 2, characterized in that it contains didecylammonium bromide and/or clathrate didecylammonium bromide with urea in an amount of 10-500 g/l

4. Insecticide and acaricide tool according to claim 2 or 3, characterized in that it contains cypermethrin in the amount of 10-500 g/l

5. Insecticide and acaricide product PP 4, characterized in that dissolve the El contains deodorized kerosene.

 

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