CN104542652A - Antibacterial composition containing polyoxin and thifluzamide - Google Patents
Antibacterial composition containing polyoxin and thifluzamide Download PDFInfo
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- CN104542652A CN104542652A CN201410831626.7A CN201410831626A CN104542652A CN 104542652 A CN104542652 A CN 104542652A CN 201410831626 A CN201410831626 A CN 201410831626A CN 104542652 A CN104542652 A CN 104542652A
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- thifluzamide
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Abstract
The invention relates to an antibacterial composition containing polyoxin and thifluzamide. The antibacterial composition comprises effective components of polyoxin and thifluzamide in binary combination. The mass ratio of polyoxin to thifluzamide is (1-25):(25-1). The preparation comprises the following components in percentage by mass: 1-80% of polyoxin and thifluzamide as effective components, and the balance of auxiliary components which are allowable and acceptable in pesticides. The dosage forms of the antibacterial composition provided by the invention refer to missible oil, suspending agents, wettable powder, aqueous solutions, water dispersible granules, emulsion in water, micro-emulsion, granules and micro capsules. The antibacterial composition can be mainly used for preventing and treating diseases such as sheath blight of rice and wheat.
Description
Technical field
The present invention relates to technical field of pesticide combination, particularly relate to a kind of bactericidal composition containing polyoxin and thifluzamide.
Background technology
Polyoxin (polyoxin, No. CAS: 19396-03-3) is the metabolite that streptomyces aureus produces, and belongs to broad-spectrum antibiotics series bactericidal agent.There is good Uptake and translocation effect.Its mechanism of action is the chitinous biosynthesis of interference germ cell wall, makes somatic cells wall can not carry out biosynthesis and causes germ dead.Germ tube contacts after medicament with mycelia, local bulkiness, breaks, overflows cell inclusion, and can not normal development, causes death.Therefore also there is the effect suppressing germ to produce spore and scab expansion.To cucumber downy mildew, powdery mildew, black fleck disease of ginseng, apple, pears graywall, and rice sheath blight disease has good preventive effect.
Thifluzamide (thifluzamide, No. CAS: 130000-40-7, thiophene fluorine bacterium amine) belongs to thiazole amide bactericide, has strong Uptake and translocation and long lasting effect.Thifluzamide all has activity to pathomycetes such as Rhizoctonia, Puccinia, Ustilago, Tilletia, corticium, nuclear cavity Pseudomonas, thifluzamide all has good control efficiency to many kinds of fungal diseases, can be widely used in the various crop such as water paddy and wheat class, peanut, cotton, beet, coffee, potato, lawn.Production is mainly used in the banded sclerotial blight of preventing and treating paddy rice and wheat class.
Use the most effective means that chemical agent is controlling plant diseases.But long-term use single chemical bactericide continuously high dose, easily cause the problems such as the remaining of medicament, environmental pollution and resistance to pesticide resistance fungi development.Composite or the mixture of rational chemical bactericide has expansion fungicidal spectrum, improve control efficiency, extend the optimum period for applying fertilizer, reduce dosage, reduce poisoning, minimizing remains, delay Antifungal resistance and the actively feature such as drug-fast generation and development, bactericide compounded is one of the effective method the most solved the problem.Develop new product bactericide price constantly rises, and by contrast, exploitation is efficient with research, low toxicity, low-residual composite and mixture has small investment, the lead time is short and be subject to domestic and international attention, numerous and confused increasing develops dynamics.We are on the basis of lab screening and field trial, filter out polyoxin and thifluzamide carries out composite, have obvious synergistic effect.And about polyoxin and thifluzamide composite bactericidal composition and apply and there is no people at present and reported.
Summary of the invention
Based on above situation, the object of the invention is to provide a kind of new and effective pesticide sterilizing composite.Be mainly used in the diseases such as the banded sclerotial blight of control paddy rice and wheat class.
Technical scheme of the present invention is realized by following measures:
Contain a bactericidal composition for polyoxin and thifluzamide, active ingredient polyoxin and the thifluzamide two yuan of this bactericidal composition are composite, and all the other are auxiliary element.In wherein said bactericidal composition, the mass ratio of active ingredient polyoxin and thifluzamide is 1 ~ 25: 25 ~ 1, described bactericidal composition of the present invention is through toxicity test experimental verification, when the mass ratio of polyoxin and thifluzamide is 1 ~ 10: 10 ~ 1, synergistic effect is better.
The formulations of pesticide that described bactericidal composition of the present invention can be prepared are missible oil, suspending agent, wetting powder, aqua, water dispersible granules, aqueous emulsion, microemulsion, granule, microcapsule formulations.Wherein active ingredient polyoxin and thifluzamide gross mass in the formulation accounts for 1% ~ 80% of the whole quality of the pharmaceutical preparations, and when wherein accounting for 10% ~ 60%, toxicity reaches good balance with residual, and cost is also lower.
The specific embodiments of the formulations of pesticide that bactericidal composition of the present invention is mixed with is as follows:
Described bactericidal composition is cream preparation, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Conventional emulsifier 10 ~ 30 parts; Conventional solvents 20 ~ 50 parts; Conventional synergist 1 ~ 5 part.The concrete production stage of this cream preparation be first active ingredient polyoxin and thifluzamide are added dissolve completely in solvent after add emulsifier again, synergist becomes transparent and homogeneous oily liquids after stirring, filling, namely can be made into the cream preparation of the present composition.
Described bactericidal composition is suspending agent, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Dispersant 5 ~ 20 parts; Antifreezing agent 1 ~ 5 part; Thickener 0.1 ~ 2 part; Defoamer 0.1 ~ 0.8 part; Penetrating agent 0 ~ 10 part; PH value regulator 0.1 ~ 5 part; Water, surplus.The concrete production stage of this suspending agent is for first to mix other auxiliary agents, mix through high speed shear, add active ingredient polyoxin and thifluzamide, abrading-ball 2 ~ 3 hours in ball crusher, make a diameter all at below 5mm, namely can be made into the aqueous suspension formulations of the present composition.
Described bactericidal composition is wetting powder, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Dispersant 3 ~ 10 parts; Wetting agent 1 ~ 5 part; Filler, surplus.The concrete production stage of this wetting powder is: mixed with thifluzamide and dispersant, wetting agent and filler by active ingredient polyoxin by above-mentioned formula, uniform stirring in stirred tank, mixing after airslide disintegrating mill, namely can be made into the wetting powder of the present composition.
Described bactericidal composition is water dispersible granules, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Dispersant 3 ~ 10 parts; Wetting agent 1 ~ 10 part; Disintegrant 1 ~ 5 part; Filler, surplus.The concrete production stage of this water dispersible granules is: mixed with thifluzamide and dispersant, wetting agent, disintegrant and filler by active ingredient polyoxin by above-mentioned formula, pulverize with micro jet, through mediating, then add in fluidized-bed granulation dryer and to carry out after granulation, drying, screening, through sample analysis, namely can be made into the water dispersible granules of the present composition.
Described bactericidal composition is aqueous emulsion, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Emulsifier 3 ~ 30 parts; Solvent 5 ~ 15 parts; Stabilizing agent 2 ~ 15 parts; Antifreezing agent 1 ~ 5 part; Defoamer 0.1 ~ 8 part; Thickener 0.2 ~ 2 part; Water, surplus.The concrete production stage of this aqueous emulsion is: first polyoxin and thifluzamide, solvent and emulsifier, cosolvent are added together, and makes to be dissolved into uniform oil phase; By part water, antifreeze, other the insecticides adjuvant such as antimicrobial mixes uniformly aqueous phase; While high-speed stirred, oil phase is added aqueous phase in a kettle., slowly add water until reach phase inversion point, open clipper and carry out high speed shear, and add remaining water, shear about half an hour, form the aqueous emulsion of oil-in-water type, namely can be made into the aqueous emulsion of the present composition.
Described bactericidal composition is microemulsion, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Emulsifier 10 ~ 30 parts, antifreezing agent 1 ~ 8 part, stabilizing agent 0.5 ~ 10 part, Conventional solvents cosolvent 20 ~ 50 parts.Polyoxin and thifluzamide cosolvent are dissolved completely, then add other compositions such as emulsifier, antifreezing agent stabilizing agent, Homogeneous phase mixing, finally adds water, can be made into microemulsion after fully stirring.
Described bactericidal composition is granule, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Wetting dispersing agent 1 ~ 10 part; Thickener 0.1 ~ 5 part; Defoamer 0.1 ~ 5 part; Castor oil, surplus is supplied.Each components such as active ingredient polyoxin and thifluzamide, dispersant, stabilizing agent, defoamer and solvent are mixed in the ratio of filling a prescription, after putting into the grinding of sand milling still, sends into mixing in mixer for well-distribution and get product.
Described bactericidal composition is aqua, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; Wetting dispersing agent 0.1 ~ 30 part; Antifreezing agent 2 ~ 8 parts; Defoamer 0.1 ~ 1 part; Thickener 0.1 ~ 3 part; Spreader-sticker 5 ~ 15 parts; Water, surplus is supplied.By active ingredient polyoxin and thifluzamide, dissolve completely with cosolvent, then add other compositions such as dispersant, antifreezing agent, defoamer, Homogeneous phase mixing, finally adds water, after fully stirring, finished product.
Described bactericidal composition is microcapsule formulations, and the mass fraction of component is: polyoxin 1 ~ 25 part; Thifluzamide 1 ~ 25 part; 5 ~ 20 parts, urea; 5 ~ 20 parts, formaldehyde; Emulsifying dispersant 5 ~ 20 parts; Antifreezing agent 1 ~ 5 part; Thickener 0.1 ~ 2 part; Defoamer 0.1 ~ 0.8 part; Water, surplus.Urea and formaldehyde (amount of substance ratio is about l:1.5 ~ 2.0) is added in the there-necked flask that agitating device is housed, regulate the pH value of solution to about 8 ~ 9 with sodium hydroxide solution, then be warming up to 70 ~ 80 DEG C, be obtained by reacting stable urea resin prepolymer.Get a certain amount of polyoxin and thifluzamide is dissolved in cyclohexane, and add emulsifying dispersant in the solution, with vigorous stirring, the O/W type stable emulsion that to be made into the aqueous solution containing emulsifying dispersant be aqueous phase.Above-mentioned urea resin prepolymer is added in emulsion, adjust ph, polymerization reaction take place under acid catalysed conditions, oil phase substance is wrapped, form microcapsule granule.Slow intensification, solidification, temperature controls at 40 ~ 50 DEG C, hardening time 1h.Select to add appropriate auxiliary agent, stable microcapsules.
Wherein above-described emulsifier is selected from calcium dodecyl benzene sulfonate and aliphatic acid polyethenoxy ether, alkylphenol polyoxyethylene sulfosuccinate, styrylphenol polyoxyethylene ether, polyoxyethylene nonylphenol ether, castor oil polyoxyethylene ether, aliphatic acid polyethenoxy base ester, any one in polyoxyethylene aliphatic alcohol ether or more than one any mixtures than composition.
Described solvent is dimethylbenzene or biodiesel, toluene, diesel oil, methyl alcohol, ethanol, n-butanol, isopropyl alcohol, turpentine-based vegetable oil code name is ND-45, solvent naphtha, dimethyl formamide, dimethyl sulfoxide (DMSO), one or more in water equal solvent are arbitrarily than the mixture of composition.
It is LG-3, GY-D1252, GY-D1256, SNWGF-01 that described dispersant is selected from polycarboxylate code name, lignosulfonates code name is 201107,201108, alkylphenol polyoxyethylene methyl ether condensate sulfate, alkylsulfonate calcium salt, naphthalene sulfonic acid-formaldehyde condensation product sodium salt, alkylphenol polyoxyethylene, polyoxyethylene carboxylate, aliphatic amine polyoxyethylene ether, one or more in fatty acid glyceride APEO.
Described wetting agent is selected from lauryl sodium sulfate, calcium dodecyl benzene sulfonate, Nekal BX, moistening bleeding agent F, alkylbenzenesulfonate polyoxyethylene triphen phosphenylic acid salt dimly, spaonin powder, silkworm excrement, one or more in soapberry powder.
Described disintegrant is selected from bentonite, urea, ammonium sulfate, aluminium chloride, citric acid, succinic acid, one or more in sodium bicarbonate.
Described thickener is selected from xanthans, carboxymethyl cellulose, carboxyethyl cellulose, methylcellulose, Magnesiumaluminumsilicate, in polyvinyl alcohol one or more.
Described stabilizing agent is selected from sodium citrate, the one in resorcinol.
Described antifreezing agent is selected from ethylene glycol, propane diols, one or more in glycerine.
Described defoamer is selected from silicone oil, silicone compound, C
10-20saturated fat acid compounds, C
8-10one or more of fatty alcohol.
Described filler is selected from kaolin, diatomite, bentonite, attapulgite, white carbon, starch, one or more in precipitated calcium carbonate.
The composite bactericide that the present invention is active ingredient with polyoxin and thifluzamide has obvious synergistic effect, delays the drug-fast generation in key, and reduces into product cost and use cost, is mainly used in the diseases such as the banded sclerotial blight of control paddy rice and wheat class.
Embodiment
For making technical scheme of the present invention, object and advantage are clearly understood, the following specific embodiment of the present invention is described, but the present invention is not limited to these examples.The mode that effect experimental of the present invention adopts indoor biometrics and field trial to combine, if no special instructions, the ratio below mentioned is all ratio of quality and the number of copies.
Embodiment: polyoxin and thifluzamide different ratio co-toxicity are tested.
1.1 reagent agent
The former medicine of 95% thifluzamide, the former medicine of 90% polyoxin, above-mentioned former medicine provides by research and development department of extra large rel medicine company limited company.
1.1.2 for examination pathogen
Rhizoctonia solani Kuhn germ, separation and purification gained from the incidence of leaf in rice in Hunan field, PDA inclined-plane is cultivated in 4 DEG C of refrigerators and preserves.
1.1.3 for examination medium
PDA medium: potato 200g, glucose 20g, agar 20g, water 1000ml
AEA medium: dusty yeast 5 g/L, glycerine 20mL/L, M g SO4 0.2 5 g/L, Na NO3 6 g/L, KCL0.5g/L, KH 2 P O4 1.5g/L, agar powder 20 g/L, deionized water 1 L
1.2 test method and Tests of Synergistic Actions
1.2.1 two kinds of single doses are to the toxicity test of sheath blight fungus
Polyoxin and thifluzamide proper amount of acetone are dissolved, and are made into the mother liquor of 10000 μ g/ml, Cord blood at 4 DEG C, stand-by, test front sterile water and are diluted to a series of concentration.
The bacterium dish of diameter 5 mm after preculture, is inoculated in respectively on the AEA flat board containing variable concentrations gradient, cultivates under 25 DEG C of dark conditions by Rhizoctonia solani Kuhn on AEA medium.Often process repetition 3 times.When control strain colony diameter grows to 6.5 more than c m, " right-angled intersection method " is adopted to measure.According to the linear regression analysis between the probit value of inhibiting rate and the logarithm value of medicine series concentration, obtain the EC that two kinds of single doses suppress mycelial growths
50value, correlation coefficient and virulence regression equation.
1.2.3 mixture toxicity test
Carry out the toxicity test of mixture according to mixed ratio by single dose toxicity test method.
According to the EC of the abundant method of Sun Yun by each process of mensuration
50value is converted into actual mixed toxicity index (ATI); According to the proportioning of mixture, obtain theoretical mixed toxicity index (TTI), by the co-toxicity coefficient (CTC) of following formulae discovery mixture.
Single dose toxicity index=(standard agent EC
50/ reagent agent EC
50) * 100;
ATI=(standard agent EC
50/ reagent agent (using with) EC
50) * 100;
The content (%) of toxicity index X B in using with of content (the %)+B of toxicity index X A in using with of TI I=A;
CTC =（ATI / TTI ）*100；
If co-toxicity coefficient large 120, shows there is synergistic effect; If be starkly lower than 100 (less than 80), be indicated as antagonism; Between 100 ~ 120, be indicated as summation action.
2.1 toxicity test results
Table 1 thifluzamide and polyoxin are to the toxicity test of gray mold of cucumber
As can be seen from the table, the result of the test of different proportion proportioning shows, dilute respectively in active ingredient ratio and all show stronger synergistic effect, wherein with polyoxin and thifluzamide for the good suggestion of synergistic effect when 1:10 ~ 10:1 carries out further field control effectiveness test to suitable proportion about 1:10 ~ 10:1 mixture preparation, to evaluate its field practical application effect.
field trial measures rice sheath blight disease controlling effect
3.1.1 application method
Test dispenser twice altogether, check plot spray equivalent clear water.When making up a prescription, after first medicament fully being dissolved with a small amount of water, then add suitable quantity of water carry out complete stool spraying process, even spraying.All adopt power driven sprayer during spray medicine, operating pressure is 2.0 ~ 2.3 kg/cm
2, shower nozzle aperture 1.2 mm.Community spouting liquid is used by 675 liters/hectare, and liquid is sprayed application to crop complete stool uniformly.
investigation method
Experimental field be located at Hunan, the rice field selecting occurring degree medium is that experimental field soil fertility is medium, and irrigation and drainage are convenient.Adopt bilinear sampling method, 5 points are got in every community, look into 5 caves at often, and during investigation, 2 blades in the fixing middle part of every strain carry out fixed point inspection.
Carry out classification according to rice sheath blight disease grade scale, record total strain number, diseased plant number, severity, calculate diseased plant rate, disease index and preventive effect.
Rice sheath blight disease grade scale is
0 grade: complete stool is anosis;
1 grade: 4th blade and following leaf sheath thereof, blade morbidity (be 1st slice leaf with sword-like leave);
3 grades: 3rd blade and following leaf sheath thereof, blade morbidity;
5 grades: 2nd blade and following leaf sheath thereof, blade morbidity;
7 grades: sword-like leave blade and following leaf sheath thereof, blade morbidity;
9 grades: complete stool falls ill, withered ahead of time.
control time and number of times
Test is investigated 4 times altogether, i.e. disease index investigation before medicine, preventive effect investigation in 10 days after the 1st medicine, 10 days and preventive effect investigation in 20 days after 2 medicines.
drug effect computational methods
Sick leaf rate (%)=sick number of sheets/investigate the total number of sheets × 100;
Disease index=∑ (the sick number of sheets × relative level numerical value at different levels)/(investigating the total number of sheets × 9) × 100;
Control efficiency (%)=(before 1-(blank district medicine after disease index × treatment region medicine disease index)/(after blank district medicine before disease index × treatment region medicine disease index)) × 100.
poisoning investigation method
Whether after dispenser, continuous 7d estimates medicament has poisoning to crop.
result of the test and analysis
The effect of each process water prevention rice sheath blight is in table 2
Table 2 respectively processes the effect of the water prevention rice sheath blight
interpretation of result:
In sum, the present invention contains the bactericidal composition of polyoxin and thifluzamide, has good control efficiency to rice sheath blight disease, and it is to Target crops safety.Complex preparation not only increases preventive effect, and expands fungicidal spectrum, widens the scope of application, reduces costs, and plays the double effect controlled of a medicine, alleviate manpower and materials to multiple diseases, improves productivity effect.So the invention of this complex preparation is of great significance social tool with popularization.
Claims (4)
1. one kind contains the bactericidal composition of polyoxin and thifluzamide, it is characterized in that: the active ingredient of this bactericidal composition is polyoxin and thifluzamide binary built, all the other are auxiliary element, and wherein the mass ratio of active ingredient polyoxin and thifluzamide is 1 ~ 25: 25 ~ 1.
2. bactericidal composition according to claim 1, is characterized in that: polyoxin and thifluzamide gross weight in the formulation accounts for 1% ~ 80% of the whole quality of the pharmaceutical preparations.
3. bactericidal composition according to claim 2, is characterized in that: polyoxin and thifluzamide gross weight in the formulation accounts for 5% ~ 60% of the whole quality of the pharmaceutical preparations.
4. the bactericidal composition according to claim 1 or 2 or 3, is characterized in that: the formulation of this bactericidal composition is missible oil, suspending agent, aqua, wetting powder, water dispersible granules, aqueous emulsion, microemulsion, granule, microcapsule formulations
.
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| CN201410831626.7A CN104542652A (en) | 2014-12-29 | 2014-12-29 | Antibacterial composition containing polyoxin and thifluzamide |
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| CN201410831626.7A CN104542652A (en) | 2014-12-29 | 2014-12-29 | Antibacterial composition containing polyoxin and thifluzamide |
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