CN113951268A - Sanitary insecticidal composition containing trifluoro-benzene pyrimidine and application thereof - Google Patents
Sanitary insecticidal composition containing trifluoro-benzene pyrimidine and application thereof Download PDFInfo
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
- A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
- A01N43/22—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom rings with more than six members
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Abstract
The invention relates to a sanitary insecticidal composition containing trifluoro-benzene pyrimidine, which consists of an active component A and an active component B, wherein the weight ratio of the active component A to the active component B is 80: 1-1: 80; the active component A is trifluorobenzene pyrimidine, and the active component B is any one of spinosad and spinetoram. The composition has good activity effect on mosquitoes (larvae) and flies (larvae), and has obvious synergistic effect compared with a single agent.
Description
Technical Field
The invention relates to a sanitary insecticidal composition, the active component of which contains trifluoro-fluoropyrimidine and is used for preventing and controlling mosquitoes (larvae) and flies (larvae).
Technical Field
Trifluzopyrimidine (triflumzopyrim), a mesoionic insecticide developed by DuPont. Has good control effect on various pests such as lepidoptera, homoptera and the like. The action mechanism of the trifluoro-benzene pyrimidine is unique, and the trifluoro-benzene pyrimidine is a compound which can inhibit but not activate a nicotinic acetylcholine receptor and has no cross resistance with other pesticides. The trifluoropyrimidine has low toxicity, is environment-friendly, and has low acute toxicity to fish and aquatic organisms.
Spinosad (Spinosad) and Spinetoram (Spinetoram), which are macrolide compounds, are secondary metabolites produced by aerobic fermentation of the actinomycetes, Saccharopolyspora spinosa. Spinetoram is derived from naturally occurring spinosyns, and is optimized. Spinosad is used abroad in livestock and poultry raising places for controlling winged insects such as stable flies, houseflies, western horn flies and the like, and can also be used as a grain storage protective agent for controlling lepidoptera pests and beetles. The spinetoram has a wider insecticidal spectrum than spinosad, is effective in preventing and controlling pests of spinosad and has a special effect on pests difficult to prevent and control such as codling moth and the like.
Mosquitoes and flies are important vector biological pests, not only can disturb the daily life of people, but also can transmit various pathogens through biology and mechanics, and threaten the health of human beings. The breeding ground treatment is one of the important means in the control of mosquitoes and flies. The types of the current commonly used agents for treating mosquitoes and flies are pyrethroid insecticides, organophosphorus insecticides and carbamate insecticides, and the high-frequency use makes the problem of drug resistance of the insecticides increasingly prominent. 2017-2018, the research on the drug resistance of aedes albopictus to common insecticides in different areas in China indicates that the aedes albopictus larvae generate different degrees of drug resistance to pyrethroid insecticides, organophosphorus insecticides and carbamate insecticides: 85% of monitoring points generate medium and high resistance to deltamethrin, 75% of monitoring points generate medium and high resistance to permethrin, 78.57% of monitoring points generate medium and high resistance to beta-cypermethrin, 27.78% of monitoring points generate medium and high resistance to propoxur, and 36.84% of monitoring points generate medium and high resistance to disulfur. The sanitary insecticide needs to be supplemented by a novel insecticidal component with a novel action mechanism.
The applicant finds that the triflumopyrimidine has an excellent killing effect on sanitary insect pests, namely mosquitoes (larvae) and flies (larvae), and has a better effect after being compounded with spinosad insecticides (spinosad and spinetoram). Trifluoropyrimidine is currently the only compound that inhibits acetylcholine receptors, is not cross-resistant to other insecticides, and has not been used in the field of hygiene to control mosquitoes (larvae) and flies (larvae). The compound composition has the characteristics of high efficiency and low toxicity, and provides a novel agent for treating breeding of mosquitoes (larvae) and flies (larvae). Is favorable for the resistance control of mosquitoes and flies.
Disclosure of Invention
The present invention provides a new sanitary insecticidal effective component-trifluoro-benzene pyrimidine for preventing and controlling mosquito (larva) and fly (larva).
The invention provides a sanitary insecticidal composition containing trifluorophenylpyrimidine, which is used for preventing and controlling mosquitoes (larvae) and flies (larvae).
The above object of the present invention is achieved by the following technical solutions:
the sanitary insecticidal composition is characterized in that: the composition comprises an active component A and an active component B, wherein the active component A is trifluorobenzene pyrimidine, and the active component B is one of spinosad and spinetoram.
The sanitary insecticidal composition is characterized in that the weight ratio of the active component A to the active component B is 80: 1-1: 80.
The sanitary insecticidal composition is characterized in that the weight ratio of the active component A to the active component B is 20: 1-1: 10.
The sanitary insecticidal composition is characterized in that the weight ratio of the active component A to the active component B is 10: 1-1: 5.
The sanitary insecticidal composition is characterized in that the preparation is various formulations prepared by a conventional method, including but not limited to emulsion in water, microemulsion, missible oil, suspending agent, granules, wettable powder, water dispersible granules and the like. The reasonable dosage form is selected according to actual conditions.
The invention is suitable for preventing and controlling mosquitoes (larvae) and flies (larvae). When in use, the proper use method (spraying, retention spraying, hot fogging, spraying, powder spraying, broadcasting and the like) is selected according to the actual situation for treatment.
Compared with the prior art, the invention has the innovation points that:
(1) the two active components provided by the invention have large difference of action mechanisms, and the compounded insecticidal activity has obvious synergy.
(2) Compared with the traditional sanitary insecticidal components, the components in the sanitary insecticidal composition provided by the invention have different action mechanisms, and are beneficial to the resistance control of sanitary pests.
(3) The novel compound composition is added to the field of domestic sanitary pesticides, has obvious pesticide effect and can be widely popularized and applied.
Detailed Description
The invention is further illustrated by the following specific examples.
The present invention is not limited to the following specific examples. It will be appreciated by those skilled in the art that the present invention encompasses all alternatives, modifications and equivalents as may be included within the scope of the claims.
Application example 1: indoor efficacy test of culex pipiens pallens larvae
Test subjects: culex pipiens pallens, larvae of 3 years old, indoor sensitive strain. Selecting test insects which are bred indoors, healthy and active and have consistent age and incubation days.
Test agents: trifluorobenzene pyrimidine (technical, 96%); spinosad (technical, 92%); spinetoram (technical, 81.2%); acetone and pure reagent; and (4) distilled water. The preparation method comprises the steps of weighing a proper amount of raw medicines of trifluorobenzene pyrimidine, spinosad and spinetoram respectively, adding a proper amount of acetone for dissolving, and preparing the required concentration of the standby liquid medicine by using distilled water according to the table 1.
TABLE 1 ratio and concentration of the series of medicinal liquids
The test method comprises the following steps: reference pesticide registration sanitary insecticide indoor efficacy test and evaluation part 5: the mosquito larva control agent NY/T1151.5-2014. Adding 500mL of test liquid medicine (diluted with distilled water into 7-11 series concentrations) and control solution (blank control and solvent control) into 1L beaker, placing 30 heads of 3-year-old larvae of healthy and viable culex pipiens pallens, and observing and recording death and pupation conditions of the larvae at 24h, 48h and 72h respectively. The tip of the forceps is used to touch the larva gently, and if the larva has slow reaction and can not float to the water surface or is in a paralysis spasm or dying state, the larva is considered to be dead. And after 72h, standard feeding is resumed and the eclosion condition is observed, wherein the normal eclosion is recorded as the number of live insects, and the non-eclosion is recorded as the number of dead insects. Each treatment of test agent, solvent control and blank control was set to 3 replicates respectively.
The killing rate was calculated as a percentage (%).
M-kill rate, in percent (%);
Nm-number of dead insects in bars;
n-total number of test insects, in bars.
And (3) test results: the results of the indoor efficacy test of the triflumfluoropyrimidine, spinosad and spinetoram in different compounding ratios on culex pipiens pallens larvae are shown in tables 2 and 3.
TABLE 2 Compound ratio of Trifluoropyrimidine (A) and spinosad (B) against culex pipiens pallens larvae
As can be seen from Table 2, the different compounding ratios of trifluorobenzene pyrimidine and spinosad have good killing effect on culex pipiens larvae with light color, and the best killing effect is achieved when the compounding ratio is 5: 1-1: 10.
TABLE 3 killing effect of compound ratio of trifluoro-benzene pyrimidine (A) and spinetoram (B) on culex pipiens pallens larvae
As can be seen from Table 3, the different compounding ratios of trifluorobenzene pyrimidine and spinetoram have good killing effect on culex pipiens pallens larvae, and the best killing effect is achieved when the compounding ratio is 5: 1-1: 20.
The combined toxicity evaluation of the compound ratio of the triflumopyrimidine, the spinosad and the spinetoram on culex pipiens larvae is as follows:
the evaluation method comprises the following steps: and evaluating the combined toxicity of the compounds by a co-toxicity coefficient method. Co-toxicity coefficient method, also known as SuThe n method is a quantitative calculation method. First, the LC of each single dose is determined for 72h50Calculating the single-dose toxicity index according to a formula; then compounding single dosage to obtain LC of compounded agent50And finally, calculating the co-toxicity coefficient according to a formula.
The judgment basis is as follows: if the co-toxicity coefficient CTC is more than or equal to 120, the synergistic effect is shown after the two single agents are compounded; if the co-toxicity coefficient CTC is less than or equal to 80, the antagonism is indicated after the two single agents are compounded; if the co-toxicity coefficient is 80< CTC <120, the additive effect is shown after the two single agents are compounded. The calculation formula is as follows:
measured virulence index of compounded (A + B)
The virulence index of the compound (A + B) theoretical virulence index TTI (A agent) is multiplied by the mass percentage of the A agent in the mixed preparation and multiplied by the mass percentage of the B agent in the mixed preparation
The results of the combined toxicity of the triflumfluoropyrimidine, the spinosad and the spinetoram on culex pipiens larvae are shown in tables 4 and 5 by adopting a co-toxicity coefficient method.
TABLE 4 Combined virulence effects of trifluoropyrimidine and (A) and spinosad (B) on Culex pipiens pallens larvae
| Test liquid medicine | LC50(mg/L) | TI | ATI | TTI | CTC |
| Trifluorophenylpyrimidines | 0.151 | 100 | - | - | - |
| Spinosad | 0.089 | 169.7 | - | - | - |
| A:B＝80:1 | 0.090 | - | 167.7 | 100.8 | 166.3 |
| A:B＝40:1 | 0.096 | - | 157.3 | 101.7 | 154.6 |
| A:B＝20:1 | 0.075 | - | 201.3 | 103.3 | 194.8 |
| A:B＝10:1 | 0.068 | - | 222.0 | 106.3 | 208.8 |
| A:B＝5:1 | 0.059 | - | 255.9 | 111.6 | 229.3 |
| A:B＝1:1 | 0.060 | - | 251.6 | 134.8 | 186.6 |
| A:B＝1:5 | 0.062 | - | 243.5 | 158.1 | 154.0 |
| A:B＝1:10 | 0.065 | - | 232.3 | 163.3 | 142.2 |
| A:B＝1:20 | 0.066 | - | 228.7 | 166.3 | 137.5 |
| A:B＝1:40 | 0.067 | - | 225.3 | 168.0 | 134.1 |
| A:B＝1:80 | 0.072 | - | 209.7 | 168.8 | 124.2 |
The results of the combined toxicity effect of the triflumfluoropyrimidine and the spinosad in different compounding ratios on culex pipiens larvae show in table 4 that when the triflumfluoropyrimidine and the spinosad are compounded and the compounding ratio of the triflumfluoropyrimidine and the spinosad is 5:1, LC (liquid chromatography) is adopted50The value is minimal. According to a co-toxicity coefficient method, the combined toxicity of the triflorouracil and the spinosad in each compounding ratio is evaluated to culex pipiens pallens larvae, the compounding ratio of the triflorouracil to the spinosad is 80: 1-1: 80, the co-toxicity coefficients are all larger than 120, and the synergy is shown; when the compounding ratio of the trifluoro-benzene pyrimidine to the spinosad is 5:1, the co-toxicity coefficient is the largest, and the synergistic effect is the most obvious.
TABLE 5 Combined virulence effects of Trifluoropyrimidine, A and spinetoram B on Culex pipiens pallens larvae
In Table 5, the results of the combined toxicity of the different compounding ratios of the trifluoropyrimidine and the spinetoram on culex pipiens pallens show that when the compounding ratio of the trifluoropyrimidine and the spinetoram is 5:1, LC (liquid chromatography) is adopted50The value is minimal. According to a co-toxicity coefficient method, evaluating the combined toxicity of the compound proportion of trifluorobenzene pyrimidine and spinetoram on culex pipiens pallens larvae, finding that the compound proportion of trifluorobenzene pyrimidine and spinetoram is between 80: 1-1: 80, the co-toxicity coefficients are all more than 120, and showing synergistic effect; when the compounding ratio of the trifluoro-benzene pyrimidine to the spinetoram is 5:1, the co-toxicity coefficient is the largest, and the synergistic effect is the most obvious.
Application example 2: indoor efficacy test of housefly larvae
Test subjects: housefly, 1-3 instar larva, indoor sensitive strain. Selecting test insects which are bred indoors, healthy and active and have consistent age and incubation days.
Test agents: trifluorobenzene pyrimidine (technical, 96%); spinosad (technical, 92%); spinetoram (technical, 81.2%); acetone and pure reagent; and (4) distilled water. The preparation of the liquid medicine to be used is shown in Table 1.
The test method comprises the following steps: adding not less than 50mL of test liquid medicine (diluted with distilled water into 7-11 series concentrations of test liquid medicine) into 100mL beaker, and simultaneously setting blank control and solvent control. Soaking the test insect in the medicinal liquid, taking out for 5-10 s, sucking off the excessive medicinal liquid with filter paper, restoring standard feeding, and observing eclosion condition. Each treatment was repeated 4 times, with 15 replicates. And investigating the death condition of the test insects at 24h, 48h and 72h after treatment. The death standard of the test insects is judged to be that the insects shrink obviously or the needles can not climb normally, the normal eclosion is recorded as the number of live insects, and the non-eclosion is recorded as the number of dead insects. The total number of test insects and the number of dead insects were recorded.
The mortality rate is calculated as a percentage (%) according to the following formula:
in the formula:
p-mortality in percent (%);
k-represents the number of dead insects, in head;
n-represents the total number of insects treated, in heads.
And (3) test results: the results of the indoor efficacy test of the triflumfluoropyrimidine, spinosad and spinetoram in different compounding ratios on housefly larvae are shown in tables 6 and 7.
TABLE 6 indoor pharmacodynamic activity of each compounding ratio of trifluorfluoropyrimidine (A) and spinosad (B) on housefly larvae
The compounding ratio of the trifluoropyrimidine to the spinosad has good indoor drug effect activity on housefly larvae, and the activity effect is best when the compounding ratio is 20: 1-1: 10.
TABLE 7 indoor pharmacodynamic activity of each compounding ratio of trifluorophenylpyrimidine (A) and spinetoram (B) on housefly larvae
The compounding ratio of the trifluoro-benzene pyrimidine and the spinetoram is good in indoor drug effect activity of housefly larvae, and the activity effect is best when the compounding ratio is 5: 1-1: 10.
The combined toxicity effect evaluation of the compound ratios of the triflumfluoropyrimidine, the spinosad and the spinetoram on housefly larvae is as follows: .
The evaluation method comprises the following steps: and evaluating the combined toxicity of the compounds by a co-toxicity coefficient method.
The judgment basis is as follows: if the co-toxicity coefficient CTC is more than or equal to 120, the synergistic effect is shown after the two single agents are compounded; if the co-toxicity coefficient CTC is less than or equal to 80, the antagonism is indicated after the two single agents are compounded; if the co-toxicity coefficient is 80< CTC <120, the additive effect is shown after the two single agents are compounded. The calculation formula is as follows:
measured virulence index of compounded (A + B)
The virulence index of the compound (A + B) theoretical virulence index TTI (A agent) is multiplied by the mass percentage of the A agent in the mixed preparation and multiplied by the mass percentage of the B agent in the mixed preparation
The results of the combined toxicity of triflumfluoropyrimidine, spinosad and spinetoram on housefly larvae are shown in tables 8 and 9 by adopting a co-toxicity coefficient method.
TABLE 8 Combined virulence effects of trifluoropyrimidine and (A) and spinosad (B) on Musca domestica larvae
| Test liquid medicine | LC50(mg/L) | TI | ATI | TTI | CTC |
| Trifluorophenylpyrimidines | 2.27 | 100 | - | - | - |
| Spinosad | 1.32 | 171.9 | - | - | - |
| A:B＝80:1 | 1.61 | - | 140.9 | 100.8 | 139.6 |
| A:B＝40:1 | 1.56 | - | 145.5 | 101.7 | 143.0 |
| A:B＝20:1 | 1.10 | - | 206.3 | 103.4 | 199.5 |
| A:B＝10:1 | 0.98 | - | 231.6 | 106.5 | 217.4 |
| A:B＝5:1 | 0.89 | - | 255.0 | 111.9 | 227.9 |
| A:B＝1:1 | 0.90 | - | 252.2 | 135.9 | 185.6 |
| A:B＝1:5 | 0.91 | - | 249.4 | 159.9 | 156.0 |
| A:B＝1:10 | 0.97 | - | 234.0 | 165.5 | 141.4 |
| A:B＝1:20 | 0.98 | - | 231.6 | 168.4 | 137.5 |
| A:B＝1:40 | 0.99 | - | 229.3 | 170.1 | 134.8 |
| A:B＝1:80 | 1.10 | - | 206.4 | 171.0 | 120.7 |
The results of the combined toxicity of triflumfluoropyrimidine and spinosad on housefly larvae show in table 8 that when triflumfluoropyrimidine and spinosad are compounded and the compounding ratio of triflumfluoropyrimidine to spinosad is 5:1, LC (liquid chromatography) is adopted50The value is minimal. According to a co-toxicity coefficient method, the combined toxicity of the triflorouracil and the spinosad on housefly larvae is evaluated, the compounding ratio of the triflorouracil to the spinosad is 80: 1-1: 80, the co-toxicity coefficients are all larger than 120, and the synergy is shown; when the compounding ratio of the trifluoro-benzene pyrimidine to the spinosad is 5:1, the co-toxicity coefficient is the largest, and the synergistic effect is the most obvious.
TABLE 9 Combined virulence effects of trifluorfluoropyrimidine, A and spinetoram (B) on Musca domestica larvae
The results of the combined toxicity of triflumfluoropyrimidine and spinetoram on housefly larvae show in Table 9 that when triflumfluoropyrimidine and spinetoram are combined and the ratio of the combination ratio of the triflumfluoropyrimidine to the spinetoram is 5:1, LC (liquid chromatography) is adopted50The value is minimal. According to a co-toxicity coefficient method, the combined toxicity of the compound proportion of trifluorobenzene pyrimidine and spinetoram on housefly larvae is evaluated, the compound proportion of trifluorobenzene pyrimidine and spinetoram is between 80: 1-1: 80, the co-toxicity coefficients are all more than 100, and a synergistic effect is shown; when the compounding ratio of the trifluoro-benzene pyrimidine to the spinetoram is 5:1, the co-toxicity coefficient is the largest, and the synergistic effect is the most obvious.
The invention relates to a pesticide composition containing trifluoro-benzene pyrimidine and the application thereof, which has been described by specific examples, and the relative other objects can be realized by the persons skilled in the art through appropriate changes of raw materials, process conditions and the like without departing from the content of the invention, and all similar substitutions and changes are obvious to the persons skilled in the art and are considered to be included in the scope of the invention.
Claims (6)
1. A sanitary insecticidal composition containing trifluorobenzene pyrimidine is characterized in that the composition comprises an active component A and an active component B, wherein the active component A is trifluorobenzene pyrimidine, the active component B is spinosad or spinetoram, and the weight ratio of the active component A to the active component B is 80: 1-1: 80.
2. A sanitary insecticidal composition according to claim 1, characterized in that: the weight ratio of the active component A to the active component B is 80: 1-1: 80.
3. A sanitary insecticidal composition according to claim 1, characterized in that: the weight ratio of the active component A to the active component B is 20: 1-1: 10.
4. A sanitary insecticidal composition according to claim 1, characterized in that: the weight ratio of the active component A to the active component B is 10: 1-1: 5.
5. The sanitary insecticidal composition according to claims 1 to 4, wherein the preparation is prepared into various dosage forms by conventional methods, including but not limited to emulsion in water, microemulsion, suspending agent, emulsifiable concentrate, granule, wettable powder, water dispersible granule, etc.
6. Use of a pesticidal hygiene composition according to any of claims 1 to 5 for controlling a pesticidal hygiene, characterized in that: the sanitary insect is mosquito (larva) and fly (larva).
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| DE102023000590A1 (en) | 2023-02-21 | 2024-08-22 | Discovery Purchaser Corporation | Triflumezopyrim for mosquito control |
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| DE102023000590A1 (en) | 2023-02-21 | 2024-08-22 | Discovery Purchaser Corporation | Triflumezopyrim for mosquito control |
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