Pesticidal compositions comprising macrolide active ingredients

Abstract

There is provided a suspension composition comprising: a) at least one macrolide active substance; b) at least one aromatic sulphonate condensed with formaldehyde; and c) ammonium sulfate. The invention also provides application of the suspending agent composition in controlling pest infestation. Also provided is a method of improving the stability of a macrolide active compound in a suspension formulation, the method comprising using a combination of a formaldehyde condensed aromatic sulphonate and ammonium sulfate in the formulation.

Description

[0001] The present invention relates to an insecticidal composition comprising a macrolide active substance, and more particularly to an insecticidal suspension concentrate. The present invention also relates to the preparation and use of the suspension concentrate.

[0002] Insecticidal active substances based on macrolides are well known in the field of agricultural chemicals. Examples of members of this type of insecticidal active substances include avermectin, emamectin, pleocidin, ethyl pleocidin, ivermectin, abamectin and methylamino avermectin. These macrolide compounds have relatively large molecular weight, complex spatial structure, a large amount of oxygen atoms and / or hydroxyl groups, and all contain lactone rings. Therefore, due to the effect of hydrogen bonds, macrolide insecticidal compounds are easily reunited when combined with compounds with polyhydroxyl and / or polyoxygen structures.

[0003] A common form of agricultural chemical formulations used on a commercial scale is a suspension. Suspension concentrates include a suspension of solid particles of the agricultural chemical active ingredient in a suitable liquid medium (usually water). Suspension concentrate products tend to precipitate. The sedimentation rate conforms to Stokes' sedimentation law:

[0004] w=[2g(ρs-ρ)gr 2 ] / 9μ

[0005] Among them, ρs is the particle density, ρ is the liquid density, μ is the liquid viscosity, r is the particle radius, and g is the gravitational acceleration.

[0006] To combat the tendency to settle, it is known to add thickeners to suspension products to adjust the fluid viscosity of the system and slow down the rate of settling. This in turn reduces water separation and stratification during storage of the product and improves the physical stability of the product.

[0007] The most commonly used thickeners in suspension products are high molecular weight compounds, such as xanthan gum, guar gum, cellulose, hydroxymethyl cellulose, starch, polyvinyl alcohol, polyvinyl pyrrolidone and its derivatives. These thickeners all contain relatively more hydroxyl groups and / or oxygen atoms. Therefore, as mentioned above, due to hydrogen bonding, macrolide insecticide active substance molecules tend to aggregate with these thickener molecules. Therefore, these high molecular weight organic thickeners are not suitable for suspensions containing macrolide active ingredients. This will lead to reduced physical stability of the suspension preparation, thereby reducing the efficacy of the product.

[0008] Therefore, there is a need for a technology to improve the stability and efficacy of macrolide insecticide compounds when formulated as suspension concentrates.

[0009] The present invention provides a suspension composition, which comprises:

[0010] a) at least one macrolide active substance;

[0011] b) at least one aromatic sulfonate condensed with formaldehyde; and

[0012] c) Ammonium sulfate.

[0013] It has been unexpectedly discovered that the combination of formaldehyde-condensed aromatic hydrocarbon sulfonates and ammonium sulfate can significantly improve the storage stability of suspension concentrates containing active macrolide compounds.

[0014] Specifically, it has been found that in the suspension of the present invention, the combination of the aromatic sulfonate of formaldehyde condensation and ammonium sulfate slows down the particle sinking rate of the suspension. Therefore, the storage stability of the suspension of the present invention is significantly improved without adding an additional thickener, particularly a polymer organic thickener, to the suspension. The combination of the aromatic sulfonate of formaldehyde condensation and ammonium sulfate in the suspension can prevent undesirable phenomena, such as macrolide particles sinking to the bottom, water separation, flocculation, stratification, etc. during storage, thereby improving the physical stability of the suspension. This in turn also improves the efficacy of the suspension, particularly maintaining the activity level of the macrolide component.

[0015] The combination of the formaldehyde-condensed aromatic sulfonate and ammonium sulfate according to the present invention allows the use of a low-viscosity macrolide-containing suspension agent without the occurrence of macrolide sedimentation, water separation, flocculation, stratification and the like during storage, thereby significantly improving the storage stability of the macrolide-containing suspension agent. Specifically, the present invention allows the viscosity of the suspension agent to be less than 800 mPa.s, preferably less than 600 mPa.s, more preferably less than 400 mPa.s, and especially less than 300 mPa.s, which is technically beneficial to the preparation, handling and use of the suspension agent.

[0016] Suspension formulations comprise solid particles of the macrolide active ingredient suspended in a liquid medium. The liquid medium may comprise any suitable liquid component or a mixture of two or more thereof. Suitable liquid components are those components that can not dissolve the macrolide active substance. Suitable liquid components may be any one or at least two combinations of soybean oil, corn oil, rapeseed oil, epoxidized soybean oil, methyl oleate, ethyl laurate, methyl linolenate, palmitic acid, linseed oil, mineral oil and water. For many embodiments, water is a preferred liquid medium.

[0017] The suspension composition of the present invention comprises a macrolide as an active ingredient, in particular an insecticidal macrolide. Such macrolides are known in the art. The macrolide is preferably selected from avermectin, emamectin benzoate, spinosad, spinetoram, ivermectin, abamectin. Preferred macrolides are spinosad, spinetoram, emamectin and emamectin benzoate. Spinosad is a particularly preferred macrolide.

[0018] The macrolide active substance may be present in the suspension of the present invention in any suitable amount. Preferably, the macrolide active substance is present in an amount of at least 1 g / L, more preferably at least 2 g / L, even more preferably at least 5 g / L, still more preferably at least 7.5 g / L, particularly at least 10 g / L. Preferably, the macrolide active substance is present in an amount of at most 600 g / L, more preferably at most 575 g / L, even more preferably at most 550 g / L, still more preferably at most 525 g / L, particularly at most 500 g / L. Preferably, the macrolide active substance is present in an amount of 1 to 600 g / L, more preferably 5 to 550 g / L, even more preferably 10 to 500 g / L.

[0019] The suspension composition of the present invention also contains formaldehyde condensed aromatic sulfonates. The term "aromatic" is understood to include any aromatic moiety, including but not limited to naphthalene, phenyl, phenol and cresol. Naphthalene is a particularly preferred aromatic. The aromatic moiety may also be optionally substituted with at least one alkyl group to form an alkyl aromatic hydrocarbon. The aromatic moiety may be monosubstituted, disubstituted or polysubstituted with a substituent. Herein, the term "alkyl" includes primary alkyl, secondary alkyl and tertiary alkyl. In a preferred embodiment, the alkyl substituent is C 1 -C 30 Alkyl groups, examples of which include methyl, ethyl, propyl, butyl, isopropyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, and dodecyl groups.

[0020] In a particularly preferred embodiment of the present invention, the alkyl sulfonate is a naphthalene sulfonate or a salt thereof condensed with formaldehyde, as shown in Formula I:

[0021]

[0022] in:

[0023] R 1 each independently selected from hydrogen, alkali metal, alkaline earth metal, ammonium, mono-, di-, or tri-C 1 -C 4 Alkylamine, or mono-, di- or tri-C 1 -C 4 a hydroxyalkylamine moiety; and

[0024] R2 are each independently selected from hydrogen, C 1 -C 30 a straight chain or branched alkyl or alkenyl group; and

[0025] n is an integer from 1 to 25.

[0026] Preferably, R 1 Selected from alkali metals, alkaline earth metals, ammonium, mono-, di-, or tri-C 1 To C 4 Alkylamine, or mono-, di- or tri-C 1 -C 4 a hydroxyalkylamine moiety; and

[0027] Preferably, R 2 C 1 -C 20 Alkyl, more preferably C 1 -C 15 Alkyl, more preferably C 1 -C 1 2 alkyl groups, especially C 1 -C 6 Alkyl. Examples of suitable alkyl groups include methyl, ethyl, isopropyl, n-butyl and sec-butyl.

[0028] Each naphthalene moiety may contain one or more R 2 Substituent. Each R 2 It may be present at any single position or combination of positions on the naphthalene moiety.

[0029] As mentioned above, the aromatic hydrocarbon sulfonate condensed with formaldehyde can be provided in the composition in the form of a salt. Examples of suitable salts include: alkali metal salts, i.e., R 1 is an alkali metal, such as sodium and potassium; and an alkaline earth metal, that is, R 1 is an alkaline earth metal, such as magnesium and calcium; an amine salt, that is, R in Formula I 1 is an amine group, such as monomethylamine, dimethylamine and triethylamine. Particularly preferred are alkali metal salts, especially sodium salts.

[0030] As noted above, naphthalene is the preferred aromatic moiety. Examples of commercially available sodium salts of formaldehyde-condensed naphthalene sulfonates include: Tersperse TM 2001, Tersperse TM 2100, Tersperse TM 2105 and Tersperse TM 2158; and Tamol available from BASF TM NH and NN series.

[0031] In the composition of the present invention, particularly preferred are alkylnaphthalene sulfonates condensed with formaldehyde, namely R 2 The compound of formula I is an alkyl group. More particularly preferred is the sodium salt of an alkyl naphthalene sulfonate condensed with formaldehyde. The average molecular weight of the sodium salt may be 300-2000, preferably 400-1000, and most preferably 500-750. Examples of commercially available sodium salts of alkyl-substituted naphthalene sulfonates condensed with formaldehyde include: Morwet Nafion, available from Akzo Nobel; TM D-425, MorwetT TM D-450 and Morwed TM D-809; available from Huntsman Corporation as Tersperse TM 2425 and Tersperse TM 2020; and Supragil available from Rhodia Inc TM MNS-90 and MNS-425.

[0032] Other aromatic sulfonates condensed with formaldehyde include: salts of phenol condensed with formaldehyde, such as the commercial product Tamol TM PP and DN; and sodium salts of cresols condensed with formaldehyde, such as the commercial product Dispersogen from Clariant TM 1494 and Rapidaminreserve TM CL.

[0033] In the suspension of the present invention, the content of the aromatic hydrocarbon sulfonate condensed with formaldehyde can be any suitable amount to provide the required stability of the macrolide active component. Preferably, the aromatic hydrocarbon sulfonate condensed with formaldehyde is present in an amount of at least 1g / L, more preferably at least 2g / L, even more preferably at least 5g / L, still more preferably at least 7.5g / L, and particularly at least 10g / L. Preferably, the aromatic hydrocarbon sulfonate condensed with formaldehyde is present in an amount of at most 200g / L, more preferably at most 175g / L, even more preferably at most 150g / L, still more preferably at most 125g / L, particularly at most 100g / L, more particularly at most 80g / L, and also particularly at most 60g / L. Preferably, the aromatic hydrocarbon sulfonate condensed with formaldehyde is present in an amount of 1 to 200g / L, more preferably 5 to 150g / L, even more preferably 10 to 100g / L, and particularly 10 to 60g / L.

[0034] Suspension agent of the present invention also comprises ammonium sulfate.Ammonium sulfate can be present in any suitable amount to provide the required stability of macrolide active component.Preferably, the amount of ammonium sulfate is at least 0.1g / L, more preferably at least 1g / L, even more preferably at least 5g / L, more preferably at least 7.5g / L, particularly at least 10g / L.Preferably, the amount of ammonium sulfate is at most 100g / L, more preferably at most 80g / L, even more preferably at most 50g / L, also preferably at most 40g / L, particularly at most 30g / L, more particularly at most 25g / L, also particularly at most 20g / L.Preferably, the amount of ammonium sulfate is 0.1 to 100g / L, more preferably 1 to 80g / L, more preferably 5 to 50g / L, especially 10 to 30g / L, more particularly 10 to 20g / L.

[0035] The weight ratio of the macrolide active component and the aromatic hydrocarbon sulfonate condensed with formaldehyde can be any suitable range. Preferably, the macrolide active component is present in excess of weight compared to the aromatic hydrocarbon sulfonate condensed with formaldehyde. Preferably, the weight ratio of the macrolide active component and the aromatic hydrocarbon sulfonate condensed with formaldehyde in the suspension is at least 2:1, more preferably at least 2.5:1, even more preferably at least 3:1, more preferably at least 3.5:1. Preferably, the weight ratio of the macrolide active component and the aromatic hydrocarbon sulfonate condensed with formaldehyde in the suspension is at most 18:1, more preferably at most 15:1, even more preferably at most 14:1, also preferably at most 13:1, particularly at most 12:1. Preferably, the weight ratio of the macrolide active component to the aromatic hydrocarbon sulfonate condensed with formaldehyde in the suspension concentrate is 2:1 to 18:1, more preferably 2.5:1 to 15:1, still more preferably 3:1 to 14:1, still more preferably 3.5:1 to 12:1, and particularly 4:1 to 12:1.

[0036] The weight ratio of the macrolide active component and ammonium sulfate can be in any suitable range. Preferably, the weight of the macrolide active component is in excess compared to ammonium sulfate. Preferably, the weight ratio of the macrolide active component and ammonium sulfate in the suspension is at least 6:1, more preferably at least 8:1, even more preferably at least 10:1, and more preferably at least 12:1. Preferably, the weight ratio of the macrolide active component and ammonium sulfate in the suspension is at most 35:1, more preferably at most 30:1, even more preferably at most 28:1, even more preferably at most 26:1, and particularly at most 24:1. Preferably, the weight ratio of the macrolide active component and ammonium sulfate in the suspension is 6:1 to 35:1, more preferably 8:1 to 30:1, more preferably 10:1 to 28:1, more preferably 12:1 to 26:1, and particularly 12:1 to 24:1.

[0037] The weight ratio of the aromatic hydrocarbon sulfonate condensed with formaldehyde to the ammonium sulfate may be in any suitable range. Preferably, the weight of the aromatic hydrocarbon sulfonate condensed with formaldehyde is in excess compared to the ammonium sulfate. Preferably, the weight ratio of the aromatic hydrocarbon sulfonate condensed with formaldehyde to the ammonium sulfate in the suspension agent is at least 1:1, more preferably at least 1.1:1, even more preferably at least 1.2:1, even more preferably at least 1.3:1. Preferably, the weight ratio of the aromatic hydrocarbon sulfonate condensed with formaldehyde to the ammonium sulfate in the suspension agent is at most 5:1, more preferably at most 4.5:1, even more preferably at most 4:1, even more preferably at most 3.5:1, especially at most 3:1. Preferably, the weight ratio of the aromatic hydrocarbon sulfonate condensed with formaldehyde to ammonium sulfate in the suspending agent is 1:1 to 5:1, more preferably 1.1:1 to 4.5:1, more preferably 1.2:1 to 4:1, more preferably 1.3:1 to 3.5:1, especially 1.3:1 to 3:1.

[0038] An advantage of the suspension of the present invention is that there is no need to use a thickener, particularly an organic polymer thickener. As a result, a suspension with a low system viscosity can be formed. The viscosity of the suspension depends on factors such as the concentration of the active macrolide component in the composition. The viscosity is preferably less than 800 mPa.s, more preferably less than 600 mPa.s, more preferably less than 400 mPa.s, particularly less than 300 mPa.s, and more particularly less than 200 mPa.s. The viscosity mentioned herein refers to the viscosity of the suspension measured using the following viscometer: Brookfield DV-II+Pro, Spindle #2.

[0039] Even at low viscosity, the suspension concentrate of the present invention can remain stable during long-term storage, because the combined effect of the alkylnaphthalene sulfonate and ammonium sulfate stabilizes the suspended particles of the macrolide active substance, for example, slows down the sedimentation rate of the macrolide particles.

[0040] The suspension of the present invention can be any form of preparation in which solid particles of the macrolide active ingredient are suspended in a liquid medium. Examples of such preparations include suspension concentrates (SC), suspoemulsions (SE) and microcapsule suspension-suspension concentrates.

[0041] The components of the suspension concentrate composition and the techniques for their use are known in the art. The suspension concentrate of the present invention may further comprise one or more agrochemically acceptable adjuvants. Suitable adjuvants include one or more dispersants, wetting agents, emulsifiers, preservatives, defoamers, colorants, pH adjusters, inert carriers and solvents.

[0042] The suspension formulation may include one or more solvents. Suitable solvents are those that cannot dissolve the macrolide active substance. Suitable solvents may be any one or a combination of at least two of soybean oil, corn oil, rapeseed oil, epoxidized soybean oil, methyl oleate, ethyl laurate, methyl linolenate, palmitic acid, linseed oil, mineral oil and water. For many embodiments, water is a preferred solvent.

[0043] The suspension formulation may include one or more dispersants. Suitable dispersants are any substances used for this purpose in agricultural chemical formulations. Dispersants may be one or more nonionic, amphoteric, cationic and anionic (polymer) surfactants. Preferred dispersants include sulfonic acids, sulfosuccinates / salts, fatty acid methyl taurates / salts, tristyrylphenol ethoxylates and alkoxylates, tri-sec-butylphenol ethoxylates, sulfated cresol-formaldehyde condensates, sulfated condensates of naphthalene and alkylnaphthalene, lignin sulfonates, phosphates of ethoxylated fatty alcohols, tristyrylphenol and tri-sec-butylphenol, and copolymers of ethoxylated fatty alcohols, polyacrylic acid, polymethacrylic acid and acrylates, ether sulfates of tristyrylphenol and tri-sec-butylphenol, and polymeric dispersants.

[0044] Suitable wetting agents that may be included in the suspension formulation are any substances used for this purpose in agricultural chemical formulations. Suitable wetting agents include anionic wetting agents, such as alkali metal salts, alkaline earth metal salts or ammonium salts of anionic wetting agents. Preferred wetting agents include naphthalene sulfonates, such as disodium salts of methylene dinaphthalene sulfonate, sodium naphthalene sulfonate-formaldehyde condensates and ammonium naphthalene sulfonate-formaldehyde condensates; alkylnaphthalene sulfonates, such as sodium alkylnaphthalene sulfonates; benzene sulfonates; alkylbenzene sulfonates, such as sodium cumene sulfonate, potassium cumene sulfonate, sodium xylene sulfonate and sodium toluene sulfonate; alkane sulfonates, such as sodium tetradecane sulfonate; alpha-olefin sulfonates, such as sodium alpha-olefin sulfonate; sulfosuccinates, such as sodium dioctyl sulfosuccinate; alkyl phosphates / esters, such as lauryl myristyl phosphate / ester; and alkyl sulfates, such as sodium lauryl sulfate, sodium hexadecyl stearyl sulfate, sodium hexadecyl sulfate, sodium myristyl sulfate and sodium hexadecyl stearyl sulfate.

[0045] Suitable emulsifiers for inclusion in the suspension concentrate are any substances used for the purposes of the present invention in agrochemical formulations, including reaction products of alkylphenols with ethylene oxide and / or propylene oxide, ethoxylated nonylphenol, castor oil ethoxylates, mixtures of polyalkoxylated alcohols (Atlox 4894), alkyl calcium salts, alkylbenzenesulfonic acid calcium salts, sorbitol derivatives or polyethylene oxide-sorbitol fatty acid esters.

[0046] Suitable preservatives are any substances employed for such purposes in agrochemical formulations, for example alkylisothiazolinones and benzisothiazolinones.

[0047] Suitable defoamers are any substances used for this purpose in agrochemical formulations, for example salts of silicones, long-chain alcohols and fatty acids.

[0048] Suitable colorants are any substances used for this purpose in agrochemical formulations, for example titanium dioxide, zinc oxide, blue pigments or Pigment Red BBN (Fast Red BBN).

[0049] Suitable pH adjusters are any of the substances used for this purpose in agrochemical formulations, including phosphoric acid, acetic acid, citric acid, sodium carbonate, sodium bicarbonate, potassium phosphate, potassium hydrogen phosphate and potassium dihydrogen phosphate.

[0050] In one embodiment of the present invention, the suspending agent comprises:

[0051] 1) 1 to 600 g / L of at least one macrolide active substance,

[0052] 2) 1 to 200 g / L of at least one aromatic sulfonate condensed with formaldehyde, and

[0053] 3) 0.1 to 100 g / L of ammonium sulfate.

[0054] In a preferred embodiment of the present invention, the suspending agent comprises:

[0055] 1) 1 to 600 g / L of at least one macrolide active substance,

[0056] 2) 1 to 200 g / L of at least one aromatic sulfonate condensed with formaldehyde,

[0057] 3) 0.1 to 100 g / L of ammonium sulfate,

[0058] 4) 0 to 100 g / L of an agrochemically acceptable surfactant, and

[0059] 5) Fill up to 1L with water.

[0060] In one embodiment of the present invention, the suspending agent comprises:

[0061] 1) 1 to 600 g / L of spinosad,

[0062] 2) 1 to 200 g / L of at least one aromatic sulfonate condensed with formaldehyde, and

[0063] 3) 0.1 to 100 g / L of ammonium sulfate.

[0064] In another preferred embodiment of the present invention, the suspending agent comprises:

[0065] 1) 50 to 500 g / L of spinosad,

[0066] 2) 1 to 200 g / L of at least one sodium alkylnaphthalene sulfonate condensed with formaldehyde, and

[0067] 3) 0.1 to 100 g / L of ammonium sulfate.

[0068] In another preferred embodiment of the present invention, the suspending agent comprises:

[0069] 1) 50 to 500 g / L of spinosad,

[0070] 2) 10 to 50 g / L of at least one sodium alkylnaphthalene sulfonate condensed with formaldehyde,

[0071] 3) 10 to 30 g / L of ammonium sulfate,

[0072] 4) 0 to 80 g / L of an agrochemically acceptable surfactant, and

[0073] 5) Fill up to 1L with water.

[0074] The average particle size of the macrolide particles in the suspension of the present invention may be at least 0.1 μm, preferably at least 0.3 μm, more preferably at least 0.5 μm, and even more preferably at least 1 μm. The average particle size of the macrolide particles in the suspension of the present invention may be at most 15 μm, preferably at most 10 μm, more preferably at most 8 μm, and even more preferably at most 5 μm. The average particle size of the macrolide particles in the suspension of the present invention may be about 0.1 to about 10 μm, preferably about 0.5 to 8 μm, and more preferably about 1 to 5 μm.

[0075] Techniques for forming suspension formulations of the present invention are known in the art.

[0076] In another aspect, the present invention provides a method for controlling pests in a locus, the method comprising applying to the locus a suspension formulation as described above.

[0077] Typically, the suspension is diluted with a solvent, most suitably water, before applying it to the site. Techniques for applying the suspension or its dilutions to the site are known in the art and include spraying.

[0078] Suspensions can be applied to control insect pests of plants. Suspensions can be applied directly to plants, plant parts or the site where plants are growing or will grow.

[0079] In another aspect, the present invention provides use of the suspension as described above for controlling insects.

[0080] The amount of suspension used will depend on many factors, such as the habits of the pest to be controlled, the time of application, the number of applications and environmental conditions. Generally, the amount of macrolide active ingredient required for pest control is 5 to 100 g / ha.

[0081] As used herein, the term "locus" refers to any place where pests may grow, including plant stems, leaves, roots, seeds, or soil.

[0082] The suspension concentrate of the present invention can be used to control pests in various plants, especially valuable crops such as wheat, rice, soybean, corn, cotton, cucumber, tomato and cabbage.

[0083] As described above, the present invention resides in the discovery that the combination of formaldehyde-condensed aromatic hydrocarbon sulfonates and ammonium sulfate can significantly improve the stability of macrolide active compounds in suspension concentrates.

[0084] Thus, in another aspect, the present invention provides the use of a combination of formaldehyde condensed arene sulfonate and ammonium sulfate for improving the stability of a macrolide active compound in a suspension formulation.

[0085] In addition, the present invention provides a method for improving the stability of a macrolide active compound in a suspension formulation, the method comprising using a combination of a formaldehyde-condensed aromatic hydrocarbon sulfonate and ammonium sulfate in the formulation.

[0086] Embodiments of the present invention will now be discussed by way of the following examples. Example

[0087] Example 1-240g / L spinosad suspension

[0088] The suspension is prepared from the following ingredients:

[0089]

[0090] The suspension was prepared by the following method:

[0091] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0092] Example 2-480g / L spinosad suspension

[0093] The suspension is prepared from the following ingredients:

[0094]

[0095]

[0096] The suspension was prepared by the following method:

[0097] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0098] Example 3-60g / L ethyl spinetoram suspension

[0099] The suspension is prepared from the following ingredients:

[0100]

[0101] The suspension was prepared by the following method:

[0102] The above components are combined and stirred and mixed at room temperature until a uniform suspension is obtained. The resulting suspension is ground in a sand mill at a temperature not exceeding 40° C. to obtain a final aqueous spinetoram suspension. The average particle size of the spinetoram particles is 4 μm or less.

[0103] Example 4-50 g / L Emamectin Benzoate Suspension

[0104] The suspension is prepared from the following ingredients:

[0105]

[0106] The suspension was prepared by the following method:

[0107] The above components are combined and stirred and mixed at room temperature until a uniform suspension is obtained. The resulting suspension is ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous emamectin suspension. The average particle size of the emamectin particles is 5 μm or less.

[0108] Comparative Example 1-240 g / L spinosad suspension

[0109] The suspension is prepared from the following ingredients:

[0110]

[0111] The suspension was prepared by the following method:

[0112] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0113] Comparative Example 2-240g / L Spinosad Suspension

[0114] The suspension is prepared from the following ingredients:

[0115]

[0116] The suspension was prepared by the following method:

[0117] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0118] Comparative Example 3-240g / L Spinosad Suspension

[0119] The suspension is prepared from the following ingredients:

[0120]

[0121] The suspension was prepared by the following method:

[0122] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0123] Comparative Example 4-480g / L Spinosad Suspension

[0124] The suspension is prepared from the following ingredients:

[0125]

[0126] The suspension was prepared by the following method:

[0127] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0128] Comparative Example 5-480g / L Spinosad Suspension

[0129] The suspension is prepared from the following ingredients:

[0130]

[0131] The suspension was prepared by the following method:

[0132] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0133] Comparative Example 6-480g / L Spinosad Suspension

[0134] The suspension is prepared from the following ingredients:

[0135]

[0136] The suspension was prepared by the following method:

[0137] The above components were combined and stirred and mixed at room temperature until a uniform suspension was obtained. The resulting suspension was ground in a sand mill at a temperature not exceeding 40° C. to obtain the final aqueous spinosyn suspension. The average particle size of the spinosyn particles was 4 μm or less.

[0138] Comparative Example 7-60 g / L of Spinetoram Suspension Concentrate

[0139] The suspension is prepared from the following ingredients:

[0140]

[0141]

[0142] The suspension was prepared by the following method:

[0143] The above components are combined and stirred and mixed at room temperature until a uniform suspension is obtained. The resulting suspension is ground in a sand mill at a temperature not exceeding 40°C to obtain a final aqueous spinetoram suspension. The average particle size of the spinetoram particles is 5 μm or less.

[0144] Comparative Example 8-50 g / L Emamectin Benzoate Suspension

[0145] The suspension is prepared from the following ingredients:

[0146]

[0147] The suspension was prepared by the following method:

[0148] The above components are combined and stirred and mixed at room temperature until a uniform suspension is obtained. The resulting suspension is ground in a sand mill at a temperature not exceeding 40° C. to obtain a final aqueous emamectin benzoate suspension. The average particle size of emamectin benzoate particles is 2 μm or less.

[0149] Performance Testing

[0150] 1. Viscosity test

[0151] The viscosity of each liquid suspension prepared in the above examples and comparative examples was tested according to the procedure of CIPAC MT 192. The viscosity was measured using a Brookfield DV-II+ Pro viscometer, with spindle #2 selected, at 30 rpm.

[0152] The results are shown in Table 1 below.

[0153] 2. Stability test

[0154] A sample of each suspension prepared in the above Examples and Comparative Examples was placed in a 100 ml graduated cylinder and placed in a constant temperature oven and stored for 14 days at 54° C. Then, the cylinder was taken out and placed at room temperature to observe the properties of each sample.

[0155] The results are shown in Table 1 below.

[0156] Table 1

[0157]

[0158] The results in Table 1 show that in the suspension of the present invention, after high temperature storage, the separation degree of water and product is low, there is no aggregation and flocculation phenomenon, and there is no precipitation. This is especially true when the viscosity of the sample does not exceed 600mPa.s. Due to the low viscosity, the suspension exhibits good fluidity and excellent pourability.

[0159] In contrast, the suspension concentrate of the comparative example exhibited severe water separation and precipitation during hot storage. Attempts to reduce these phenomena by adding thickeners to increase the viscosity of the system were unsuccessful and still resulted in aggregation and severe flocculation.

Claims

1. A suspension composition, comprising: a) at least one macrolide active substance; b) at least one aromatic hydrocarbon sulfonate condensed with formaldehyde; and c) Ammonium sulfate.

2. The suspending agent according to claim 1, in, The composition is an aqueous suspension.

3. The suspending agent according to claim 1 or 2, in, The macrolide active substance is selected from avermectin, emamectin, emamectin benzoate, spinosad, spinetoram, ivermectin and a mixture of two or more thereof.

4. The suspension according to claim 3, in, The macrolide active substance is spinosad.

5. The suspension according to claim 1, in, The aromatic hydrocarbon sulfonate is an alkylnaphthalene sulfonate.

6. A suspension concentrate as claimed in any one of the preceding claims, in, The aromatic hydrocarbon sulfonate is a salt of aromatic hydrocarbon sulfonate.

7. The suspension according to claim 6, in, The salts are alkali metal salts.

8. A suspension concentrate as claimed in any one of the preceding claims, in, The aromatic hydrocarbon sulfonate condensed with formaldehyde is present in an amount of 1 to 200 g / L.

9. A suspension concentrate as claimed in any one of the preceding claims, in, The ammonium sulfate is present in an amount of 0.1 to 100 g / L.

10. A suspension concentrate as claimed in any one of the preceding claims, in, The weight ratio of the macrolide active substance to the aromatic hydrocarbon sulfonate condensed with formaldehyde in the suspension is 2:1 to 18:

1.

11. A suspension concentrate as claimed in any one of the preceding claims, in, The weight ratio of the macrolide active substance to the ammonium sulfate in the suspension is 6:1 to 35:

1.

12. A suspension concentrate as claimed in any one of the preceding claims, in, The weight ratio of the aromatic hydrocarbon sulfonate condensed with formaldehyde to the ammonium sulfate in the suspending agent is 1:1 to 5:

1.

13. A suspension concentrate as claimed in any one of the preceding claims, in, The macrolide active substance is suspended in a liquid medium, and the liquid medium includes soybean oil, corn oil, rapeseed oil, epoxidized soybean oil, methyl oleate, ethyl laurate, methyl linoleate, palmitic acid, linseed oil, mineral oil, water or a mixture thereof.

14. A suspension concentrate as claimed in any one of the preceding claims, in, The suspending concentrate does not contain a polymeric organic thickener.

15. The suspension according to claim 14, in, The suspending agent does not contain xanthan gum, guar gum, cellulose, hydroxymethyl cellulose, starch, polyvinyl alcohol, polyvinyl pyrrolidone and derivatives thereof.

16. A suspension concentrate as claimed in any one of the preceding claims, in, The suspending agent comprises: 1) 1 to 600 g / L of at least one macrolide active substance, 2) 1 to 200 g / L of at least one aromatic sulfonate condensed with formaldehyde, and 3) 0.1 to 100 g / L of ammonium sulfate.

17. The suspension according to claim 16, in, The suspending agent comprises: 1) 1 to 600 g / L of at least one macrolide active substance, 2) 1 to 200 g / L of at least one aromatic sulfonate condensed with formaldehyde, 3) 0.1 to 100 g / L of ammonium sulfate. 4) 0 to 100 g / L of an agrochemically acceptable surfactant, and 5) Fill up to 1L with water.

18. A suspension concentrate as claimed in any one of the preceding claims, in, The suspending agent comprises: 1) 50 to 500 g / L of spinosad, 2) 1 to 200 g / L of at least one sodium alkylnaphthalene sulfonate condensed with formaldehyde, and 3) 0.1 to 100 g / L of ammonium sulfate.

19. A method of controlling pests in a locus, the method comprising applying to the locus a suspension concentrate as claimed in any one of the preceding claims, optionally wherein the suspension concentrate composition is diluted with water.

20. Use of a suspension concentrate composition as claimed in any one of claims 1 to 18 for controlling insects.

21. Use of a combination of formaldehyde condensed aromatic hydrocarbon sulfonates and ammonium sulfate for improving the stability of macrolide active compounds in suspension formulations.

22. A method of improving the stability of a macrolide active compound in a suspension formulation comprising using a combination of a formaldehyde condensed aromatic hydrocarbon sulfonate and ammonium sulfate in the formulation.

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