WO2022042639A1 - Spinosad tablet, and preparation method therefor and use thereof - Google Patents

Abstract

The present invention relates to the technical field of mosquito prevention and control, and specifically relates to a spinosad tablet, and a preparation method therefor and the use thereof. The spinosad tablet is composed of a slow-release layer and a quick-release layer. The quick-release layer can be quickly disintegrated after being put into water, and spinosad is then released and effectively diffuses into the water to act to kill mosquitoes; and the slow-release layer can protect the activity and stability of spinosad in water, slowly release spinosad for a long time, and prevent and control mosquitoes in water in a long-acting mode, thereby greatly reducing the use amount and the number of times of delivery of medicine needed for preventing and controlling mosquitoes in water, and reducing the influence thereof on the environment.

Description

A kind of spinosad tablet and its preparation method and application

cross reference

This application claims the priority of Chinese Patent Application No. 2020108807955 filed on August 27, 2020 with the patent title of "Spinosamycin tablet and its preparation method and application", the entire disclosure of which is incorporated by reference in its entirety This article.

technical field

The invention relates to the technical field of mosquito prevention and control, in particular to a spinosad tablet for preventing and controlling mosquitoes in water bodies and a preparation method and application thereof.

Background technique

Mosquitoes are hygienic pests that are more harmful to humans. After mating with blood-sucking mosquitoes, females need to find a host to suck blood, and then spread various diseases including malaria and dengue fever. After sucking blood, the female will lay eggs in the water or at the edge of the water. Mosquito eggs can only hatch in water. Mosquito larvae live in the water and breathe air on the water surface through the stomata.

The use of traditional chemical pesticides to control mosquitoes has disadvantages such as high pollution and easy generation of resistance. Therefore, mosquito control needs to develop in the direction of high efficiency, low toxicity, no pollution, and no damage to the ecological environment.

Spinosad is a new type of macrolide bio-insecticide, which is a secondary metabolite of Saccharopolyspora spinosa. Its active ingredient is a mixture of spinosad A and spinosad D. It has efficient control activity against Lepidoptera pests, some Diptera (mosquitoes, flies, etc.), Coleoptera, Hymenoptera, and Thysanoptera pests.

Spinosad has a unique mechanism of insecticidal action, making it difficult to develop cross-resistance with other insecticides. Its main target is the nicotinic acetylcholine receptor (nAChR) of insects, but studies have shown that it is the same as the same There is little cross-resistance to the neonicotinoid insecticides acting on the nAChR. Spinosad has high environmental safety, its leaching and volatility in water is very weak, it will not pollute groundwater and the atmosphere, and its photodegradation half-life in water is less than 1 day. Spinosad has low toxicity to non-target organisms, does not kill natural enemies, has extremely low toxicity to birds, is safe to humans and mammals, and has no teratogenic, mutagenic, and carcinogenic effects, and has only slight toxicity to aquatic animals ( The 96-hour LD ₅₀ of bound fish was 30 mg/L, bluegill was 5.9 mg/L, and carp was 5 mg/L). The safety of spinosad is that other insecticides do not have or rarely have. The result of evaluating the safety of spinosad by vertebrate selectivity ratio (VSR) shows that its safety is 300% of that of abamectin. -400 times, 5 times that of methylamino abamectin, and 3000 times that of chlorpyrifostrobin.

At present, the main dosage forms of spinosad include suspending agent, water emulsion, water dispersible granule, microemulsion and so on. However, these formulations are mostly used for spraying plants and are not suitable for controlling insects in water. When spinosad is used in water environment, spinosad has the problems of easy photolysis, poor stability, short half-life (photolysis half-life in water is less than 1 day), and poor water solubility, making it difficult to apply Long-term control of mosquitoes in water; moreover, the difficulty of rapid and effective release and diffusion in water also limits the efficacy of spinosad.

SUMMARY OF THE INVENTION

In order to solve the technical problems existing in the prior art, the purpose of the present invention is to provide a spinosad tablet, which has the functions of disintegrating immediate release and slow release long-acting at the same time, and can be used for long-acting prevention and treatment of water mosquito.

In order to achieve the above purpose, the present invention has developed a new dosage form of spinosad, which is a tablet containing an immediate-release layer and a sustained-release layer. Fast-acting and long-lasting effects, among which, the immediate-release layer can quickly release spinosad when encountering water, so that spinosad can enter the water body evenly and quickly, and kill the existing mosquitoes in the water in a short time; while the slow-release layer It can slowly release spinosad, and effectively control mosquitoes in the water body.

Specifically, the technical scheme of the present invention is as follows:

The present invention provides a spinosad tablet, comprising a slow-release layer and an immediate-release layer; the slow-release layer comprises spinosad and a slow-release carrier; the slow-release carrier comprises 10% by mass of the slow-release layer -87% calcium compounds.

Preferably, the sustained-release carrier comprises a calcium-containing compound in an amount of 10%-30% by mass of the sustained-release layer.

Preferably, the sustained-release carrier comprises a calcium-containing compound and PEG in a mass ratio of (1-20):1.

According to the physicochemical properties of spinosad and the environmental characteristics and long-acting requirements of spinosad tablets used in water, the screening of slow-release carriers is carried out in the present invention. It is found in the present invention that the compounded use of calcium-containing compound and PEG as a sustained-release carrier shows excellent sustained-release effect and effectively improves the stability of spinosad in water. By controlling the ratio of calcium-containing compound and PEG, spinosad can be released at a suitable and stable rate, which can ensure the long-term effect and insecticidal effect of the tablet in water.

The calcium-containing compound described above is one or more selected from calcium sulfate, calcium carbonate, and calcium hydroxide.

The molecular weight of the above-mentioned PEG is 4000-7000.

Preferably, the calcium-containing compound is calcium sulfate. The sustained-release carrier is preferably calcium sulfate and PEG in a mass ratio of (2-5):1.

In the above-mentioned sustained-release layer, the mass ratio of spinosad and sustained-release carrier is preferably 1:(3-50). By controlling the ratio of spinosad to slow-release carrier within the above-mentioned range, better slow-release long-acting and suitable spinosad release rate can be obtained.

Preferably, in the sustained-release layer, the mass ratio of spinosad and sustained-release carrier is preferably 1:(3-5).

The immediate release layer in the spinosad tablet of the present invention is used to rapidly release spinosad in water, and the immediate release layer comprises spinosad, an immediate release carrier, an acid source disintegrant and an alkali source disintegrant wherein, the immediate-release carrier is one or more selected from PEG, mannitol, and citric acid.

The immediate release carrier described above is preferably PEG. The present invention finds that among the above-mentioned immediate-release carriers, using an appropriate amount of PEG as an immediate-release carrier can improve the stability of spinosad in water, and the combination of disintegrants can make the spinosad tablet rapidly in contact with water. Disintegrates, spreads effectively.

The molecular weight range of the PEG suitable for the present invention is preferably 4,000 to 7,000, and more preferably 6,000.

In the above-mentioned immediate-release layer, the mass ratio of spinosad to immediate-release carrier is preferably 1:(2-40). More preferably, it is 1:(2-20).

In the above-mentioned immediate-release layer, the mass percentage content of the acid source disintegrant and the alkali source disintegrant is 10-20%. Controlling the acid source disintegrant and the alkali source disintegrant in the above content range can better control the release and diffusion rate of spinosad in the immediate-release layer, improve the uniformity of the distribution of spinosad in water, and make the immediate release Spinosad in the layer can quickly and effectively exert the effect of killing mosquitoes.

Wherein, the acid source disintegrating agent is one or more selected from malic acid, citric acid, oxalic acid, adipic acid and tartaric acid; the alkali source disintegrating agent is selected from sodium carbonate, sodium bicarbonate, sodium hydroxide, One or more of potassium carbonate and potassium bicarbonate.

Preferably, the acid source disintegrant is citric acid, and the alkali source disintegrant is sodium bicarbonate.

In the spinosad tablet of the present invention, the mass ratio of the spinosad in the immediate-release layer and the slow-release layer is 1:(1-30). Preferably it is 1:(1-20).

Preferably, in the spinosad tablet, the mass percentage of spinosad is 0.2-30%.

In addition to the above-mentioned ingredients, the spinosad tablet of the present invention also contains a tablet adjuvant permitted in the pharmaceutical field. The adjuvants include dispersants, wetting agents, binders, lubricants and fillers.

Specifically, the spinosad tablet of the present invention includes the following components:

The immediate release layer includes: spinosad 0.2-7.5 parts, PEG 3-10 parts, alkali source disintegrant 2-9 parts, acid source disintegrating agent 2-9 parts, dispersant 1-2 parts, wetting agent 1-2 parts, 0.5-1 part of binder, 1-3 parts of lubricant, 50-80 parts of filler;

The sustained release layer includes: spinosad 0.2-34 parts, calcium sulfate 10-87 parts, PEG 3-20 parts, dispersing agent 1-2 parts, wetting agent 1-2 parts, adhesive 0.5-1 part, 1-3 parts of lubricant, 10-70 parts of filler.

Wherein, the dispersing agent is one or more selected from naphthalene sulfonate, lauryl alcohol polyoxyethylene ether, and sodium polyphosphate. The wetting agent is one or more selected from sodium dodecylbenzenesulfonate, lignosulfonate, and succinic acid. The binder is one or more selected from polyvinylpyrrolidone and sodium carboxymethylcellulose. The lubricant is one or more selected from white carbon black and sodium carboxymethyl starch. The filler is one or more selected from kaolin, magnesium stearate, lactose, and bentonite.

The invention provides a preferred spinosad tablet formulation, the immediate release layer of the tablet has excellent rapid disintegration and diffusion properties, the sustained release layer has excellent sustained release long-term effect, and can effectively kill mosquitoes in water And has better stability. Specifically, the tablet includes the following components:

Immediate release layer: spinosad 0.5-7.5 parts, PEG 3-10 parts, sodium bicarbonate 2-9 parts, citric acid 2-9 parts, sodium polyphosphate 1-2 parts, lignosulfonate 1-2 parts parts, 0.5-1 part of polyvinylpyrrolidone, 1-3 parts of sodium carboxymethyl starch, and lactose supplemented to 100 parts;

Slow-release layer: 1-20 parts spinosad, 10-87 parts calcium sulfate, 3-10 parts PEG, 1-2 parts naphthalene sulfonate, 1-2 parts lignosulfonate, 0.5-polyvinylpyrrolidone 1 part, white carbon black 1-3 parts, magnesium stearate supplemented to 100 parts.

The above-mentioned reagents used in the present invention are all conventional reagents in the art, and belong to commercially available products, which are not limited in detail in the present invention.

The present invention also provides a preparation method of the spinosad tablet, comprising: putting each component of the slow-release layer and each component of the immediate-release layer into a double-cone mixing and drying machine respectively, and after mixing evenly, pouring into spray boiling granulation The granulated material is sieved, and the sieved slow-release layer and immediate-release layer materials are sent to the tablet press according to the ratio of the two layers for tableting and molding.

The present invention also provides the application of the spinosad tablet in preventing and controlling mosquitoes in water bodies.

The beneficial effects of the present invention are as follows: the present invention provides a spinosad tablet suitable for use in an aqueous environment, which comprises an immediate-release layer and a sustained-release layer, wherein the immediate-release layer can be used after being put into water. It disintegrates quickly, releases spinosad and spreads efficiently in water to exert insecticidal effect; while the slow-release layer can protect the activity and stability of spinosad in water, and release spinosad slowly and for a long time.

The spinosad tablet of the invention overcomes the problems that spinosad is unstable in water and is easy to be photolyzed, releases active ingredients only when it encounters water, and can prolong the duration of efficacy of spinosad in water From 9 to 12 weeks, it can effectively prevent and control mosquito larvae in the water area; at the same time, it maintains the fast, effective, safe and pollution-free characteristics of spinosad, and the auxiliary materials used have little impact on the environment. Using the spinosad tablets provided by the invention can greatly reduce the amount of drug use and the number of injections required for mosquito control during the mosquito breeding season, save control costs, improve control efficiency, and reduce the impact on the environment. It is used in moist and easy-to-retain areas (such as cisterns, swamp wetlands, ditches, etc.) where mosquitoes breed and breed.

The spinosad tablet of the invention has the characteristics of good insecticidal effect, low cost, convenient use, excellent stability during storage (the quality guarantee period can reach 2 years), environmental safety, no phytotoxicity and the like. It has high application value in mosquito control practice.

Description of drawings

FIG. 1 is a graph showing the relationship between the release amount of spinosad from spinosad tablets and time in Experimental Example 1 of the present invention.

detailed description

The preferred embodiments of the present invention will be described in detail below with reference to the examples. It should be understood that the following examples are given for illustrative purposes only, and are not intended to limit the scope of the present invention. Those skilled in the art can make various modifications and substitutions to the present invention without departing from the spirit and spirit of the present invention.

The experimental methods used in the following examples are conventional methods unless otherwise specified.

The materials, reagents, etc. used in the following examples can be obtained from commercial sources unless otherwise specified. The PEG used in the following examples is PEG6000.

Example 1

This embodiment provides a spinosad tablet, which is composed of an immediate-release layer and a slow-release layer, wherein the total content of the immediate-release layer and the slow-release layer spinosad is 7.5%, and the tablet weight is 1.33 g. The immediate release layer is 0.2g, and the sustained release layer is 1.13g. The formula for the immediate and extended release layers per 100 servings is as follows:

Immediate release layer (100 parts): 5 parts spinosad, 10 parts PEG, 7 parts sodium bicarbonate, 7 parts citric acid, 1 part sodium polyphosphate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts of sodium carboxymethyl starch, supplemented to 100 parts of lactose;

Slow release layer (100 parts): 8 parts spinosad, 24 parts calcium sulfate, 7 parts PEG, 1 part naphthalene sulfonate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts white carbon black , magnesium stearate supplement to 100 servings.

The preparation method of the above spinosad tablets: accurately weigh each material according to the formula, put the slow-release layer and the immediate-release layer materials into their respective double-cone mixing dryers at the same time, and after mixing evenly, put them into a spray boiling granulator , carry out granulation, the granulated material is sieved, and the sieved slow-release layer and immediate-release layer materials are sent to the tablet press according to the double-layer ratio, and put into the tablet press in order to be compressed. Finished product after testing.

The spinosad tablets in the following examples were all prepared by the above method, and are not listed separately.

Example 2

This embodiment provides a spinosad tablet, which is composed of an immediate-release layer and a slow-release layer. The immediate release layer is 0.2g, and the sustained release layer is 1.13g. The formula for the immediate and extended release layers per 100 servings is as follows:

Immediate release layer (100 parts): 2 parts spinosad, 10 parts PEG, 7 parts sodium bicarbonate, 7 parts citric acid, 1 part sodium polyphosphate, 1 part lignosulfonate, 0.7 part polyvinylpyrrolidone, 2 parts of sodium carboxymethyl starch, supplemented to 100 parts of lactose;

Slow release layer (100 parts): 7 parts spinosad, 14 parts calcium sulfate, 7 parts PEG, 1 part naphthalene sulfonate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts white carbon black , magnesium stearate supplement to 100 servings.

Comparative Example 1

This comparative example provides a spinosad tablet, which is different from Example 1 only in that PEG is replaced with stearic acid.

Comparative Example 2

This comparative example provides a spinosad tablet, which differs from Example 1 only in that PEG is removed, and only calcium sulfate is used as a slow-release carrier, and the amount of calcium sulfate is 31 parts.

Comparative Example 3

This comparative example provides a spinosad tablet, which is composed of an immediate-release layer and a slow-release layer, the total content of spinosad in the immediate-release layer and the slow-release layer is 7.5%, the tablet weight is 1.33 g, The immediate release layer is 0.2g, and the sustained release layer is 1.13g. The formulations of the immediate-release and extended-release layers per 100 servings are as follows: .

Immediate release layer (100 parts): 5 parts spinosad, 10 parts PEG, 12 parts sodium bicarbonate, 12 parts citric acid, 1 part sodium polyphosphate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts of sodium carboxymethyl starch, supplemented to 100 parts of lactose;

Slow release layer (100 parts): 8 parts spinosad, 8 parts calcium sulfate, 5 parts PEG, 1 part naphthalene sulfonate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts white carbon black , magnesium stearate supplement to 100 servings.

Comparative Example 4

This comparative example provides a spinosad tablet, which is composed of an immediate-release layer and a slow-release layer, the total content of spinosad in the immediate-release layer and the slow-release layer is 7.5%, the tablet weight is 1.33 g, The immediate release layer is 0.2g, and the sustained release layer is 1.13g. The formulations of the immediate-release and extended-release layers per 100 servings are as follows: .

Immediate release layer (100 parts): 5 parts spinosad, 10 parts PEG, 1 part sodium bicarbonate, 1 part citric acid, 1 part sodium polyphosphate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts of sodium carboxymethyl starch, supplemented to 100 parts of lactose;

Slow release layer (100 parts): 8 parts spinosad, 24 parts calcium sulfate, 1 part PEG, 1 part naphthalene sulfonate, 1 part lignosulfonate, 0.8 part polyvinylpyrrolidone, 2 parts white carbon black , magnesium stearate supplement to 100 servings.

Experimental Example 1 Release analysis of spinosad tablets

The spinosad tablets of Examples 1 to 2 and Comparative Examples 1 to 4 were placed in water, and HPLC was used to detect the content of spinosad at different times, and to analyze the release degree of spinosad tablets over time. As shown in Table 1 and Figure 1.

Table 1 Release of spinosad tablets

The results showed that the slow-release effect of spinosad tablets was significantly reduced by using the slow-release carriers of comparative examples 1 and 2. Among them, only calcium sulfate was used as the slow-release carrier, the initial spinosad was released faster, and the spinosad was The element is released into the water too early, the content in the water is very low in the later stage, and the insecticidal effect is reduced; the calcium sulfate is combined with stearic acid, the release speed is slow, and spinosad is partially decomposed in the water, and the insecticidal effect is reduced.

The slow release effect of calcium sulfate and PEG as the slow release carrier is obviously improved, and a higher insecticidal effect can be achieved in about 60 days, and the problem of spinosad starting to decompose during release is slowed down, ensuring that more water is available. The content of fungicidal to achieve a higher insecticidal effect.

If the content of acid source and alkali source in the immediate-release layer is too low or too high, the release rate of spinosad will be affected. If the release rate of the immediate-release layer is too fast, spinosad will be rapidly dissolved in water, resulting in local The content of active ingredients increases rapidly, and the distribution of active ingredients is uneven, which affects the insecticidal effect. The ratio of calcium sulfate and PEG in the slow-release layer also affects the release rate of spinosad. If the release rate of the slow-release layer is too slow, the concentration of active ingredients will be low, which will reduce the insecticidal effect, and the water-soluble decomposition amount of spinosad will increase; if the slow-release layer is dissolved too quickly, the lasting effect of the product will be affected.

Experimental Example 2 Analysis of the control effect of spinosad tablets

Taking the third-instar Aedes mosquito larvae as the research object, the killing effects of spinosad tablets of Examples 1-2 and Comparative Examples 1-4 on mosquitoes were analyzed.

Test site: Miyun District, Beijing.

Test object: third instar Aedes larvae.

The test method is as follows:

1. A transparent plastic pool (80cm×50cm×50cm), placed in a cool place with a ceiling, covered with a dust-proof net to prevent foreign mosquitoes from laying eggs in the pool. Take pond water from a branch canal of a river in Beijing, and pour 150L of pond water into each pond.

2. Put 1 spinosad sustained-release tablet (placed in the net tank) in the pool, set up a blank control pool without adding spinosad, and set 4 repetitions for each group.

3. Make up the pond water to 150L every day according to the evaporation loss.

4. In the first week, 125 3rd instar Aedes larvae were put into the test pool. 125 3rd instar Aedes mosquito larvae were added to the test tank every week.

5. Transfer the pupae to a small plastic cup with pond water every week, put them in the adult cage, and wait for emergence.

6. According to the ratio of the number of eclosion adults to the number of larvae put in, calculate the efficacy, or the eclosion inhibition rate.

7. According to the lethality rate of larvae and the emergence rate of pupae, observe the decline rate of drug effect every week.

The calculation formulas of eclosion inhibition rate and larval mortality are as follows:

eclosion inhibition rate (%)=(treatment mortality-control mortality)*100%/(1-control mortality);

Larval mortality (%) = 100% - pupation rate.

Table 2 and Table 3 show the mosquito killing effect of spinosad tablets in water field experiments.

Table 2 The water body on-site control effect of the spinosad tablet of Example 1

weeks after application	Larval Mortality %	Pupation rate %	Pupa emergence rate %	Feather suppression rate %
1	100	0	0	100
2	100	0	0	100
3	100	0	0	100
4	100	0	0	100
5	100	0	0	100
6	98	2	0	100
7	95	5	0	100
8	91	9	0	100
9	86	14	4	94.8
10	62	38	13	85.2
11	38	62	twenty four	74.3
12	25	75	48	46.5

Table 3 On-site mosquito killing effect of spinosad tablets in water bodies

The above results show that the insecticidal effect of the spinosad tablets of Examples 1 and 2 is significantly higher than that of Comparative Examples 1 to 4, and among them, the spinosad tablet of Example 1 has the best effect. For the spinosad tablet of Example 1, the eclosion inhibition rate was 100% and the efficacy decrease rate was 0% in 1-8 weeks after application; the eclosion inhibition rate in the 9th week was 94.8%, and the efficacy decrease rate was 5.2%, the eclosion inhibition rate can be controlled at 90-100%, therefore, the spinosad tablet has a drug effect time of 9 weeks, and can be administered again every 9 weeks.

Although, the present invention has been described in detail in the above general description, specific embodiments and tests, but on the basis of the present invention, some modifications and improvements can be made to it, which is very important to those skilled in the art. Obvious. Therefore, any modifications or improvements made without departing from the present invention fall within the scope of the claimed protection of the present invention.

Industrial Applicability

The invention provides a spinosad tablet and a preparation method and application thereof. The spinosad tablet consists of a sustained-release layer and an immediate-release layer. The immediate-release layer can quickly disintegrate after being put into water, release spinosad and effectively diffuse in water to kill mosquitoes; while the slow-release layer can protect the activity and stability of spinosad in water, releasing slowly and for a long time Spinosad can effectively prevent and control mosquitoes in water bodies, greatly reduce the amount of drugs used and the number of injections required for mosquito control in water, and reduce the impact on the environment. It has good economic value and application prospects.

Claims (10)

1. A spinosad tablet, characterized in that it comprises a sustained-release layer and an immediate-release layer;

   The sustained-release layer comprises spinosad and a sustained-release carrier;

   The sustained-release carrier comprises a calcium-containing compound in a mass fraction of 10%-87% of the sustained-release layer.
2. The spinosad tablet according to claim 1, wherein the sustained-release carrier comprises a calcium-containing compound and PEG in a mass ratio of (1-20):1.
3. The spinosad tablet according to claim 1 or 2, wherein the calcium-containing compound is one or more selected from calcium sulfate, calcium carbonate, and calcium hydroxide; and/or, the The molecular weight of the PEG is 4000-7000;

   Preferably, the calcium-containing compound is calcium sulfate; in the sustained-release layer, the mass ratio of the spinosad to the sustained-release carrier is 1:(3-50).
4. The spinosad tablet according to any one of claims 1-3, wherein the immediate release layer comprises spinosad, an immediate release carrier, an acid source disintegrant and an alkali source disintegrant; Described immediate-release carrier is one or more selected from PEG, mannitol, citric acid;

   Preferably, in the immediate-release layer, the mass ratio of the spinosad to the immediate-release carrier is 1:(2-40).
5. The spinosad tablet according to any one of claims 1 to 4, characterized in that, in the immediate-release layer, the mass percentage content of the acid source disintegrant and the alkali source disintegrant is 10-20 %; the acid source disintegrating agent is one or more selected from malic acid, citric acid, oxalic acid, adipic acid and tartaric acid; the alkali source disintegrating agent is selected from sodium carbonate, sodium bicarbonate, One or more of sodium hydroxide, potassium carbonate, potassium bicarbonate;

   Preferably, the acid source disintegrant is citric acid, and the alkali source disintegrant is sodium bicarbonate.
6. The spinosad tablet according to any one of claims 1 to 5, wherein

   The mass ratio of spinosad in the immediate-release layer and the slow-release layer is 1: (1-30);

   Preferably, in the spinosad tablet, the mass percentage of spinosad is 0.2-30%.
7. The spinosad tablet according to any one of claims 1 to 6, wherein the immediate release layer comprises: 0.2-7.5 parts of spinosad, 3-10 parts of PEG, an alkali source disintegrant 2-9 parts, acid source disintegrating agent 2-9 parts, dispersing agent 1-3 parts, wetting agent 1-2 parts, adhesive 0.5-1 part, lubricant 1-3 parts, filler 50-80 parts ;

   The slow-release layer comprises: spinosad 0.2-34 parts, calcium sulfate 10-87 parts, PEG 3-20 parts, dispersing agent 1-2 parts, wetting agent 1-2 parts, adhesive 0.5-1 part parts, 1-3 parts of lubricant, 10-70 parts of filler;

   Preferably, the dispersing agent is one or more selected from naphthalene sulfonate, laureth, and sodium polyphosphate;

   The wetting agent is one or more selected from sodium dodecylbenzenesulfonate, lignosulfonate, and succinic acid;

   The binder is one or more selected from polyvinylpyrrolidone and sodium carboxymethylcellulose;

   Described lubricant is one or more selected from white carbon black, sodium carboxymethyl starch;

   The filler is one or more selected from kaolin, magnesium stearate, lactose, and bentonite.
8. The spinosad tablet according to any one of claims 1 to 7, characterized in that it comprises the following components:

   Immediate release layer: spinosad 0.5-7.5 parts, PEG 3-10 parts, sodium bicarbonate 2-9 parts, citric acid 2-9 parts, sodium polyphosphate 1-2 parts, lignosulfonate 1-2 parts parts, 0.5-1 part of polyvinylpyrrolidone, 1-3 parts of sodium carboxymethyl starch, and lactose supplemented to 100 parts;

   Sustained release layer: 1-20 parts spinosad, 10-87 parts calcium sulfate, 3-20 parts PEG, 1-2 parts naphthalene sulfonate, 1-2 parts lignosulfonate, 0.5-polyvinylpyrrolidone 1 part, white carbon black 1-3 parts, magnesium stearate supplemented to 100 parts.
9. The method for preparing spinosad tablets according to any one of claims 1 to 8, characterized by comprising: putting each component of the slow-release layer and each component of the immediate-release layer into a double-cone mixing and drying machine, respectively, and mixing After uniform, it is put into a spray boiling granulator for granulation. The granulated material is sieved, and the sieved slow-release layer and immediate-release layer materials are sent to the tablet press according to the ratio of the two layers. forming.
10. Application of the spinosad tablet according to any one of claims 1 to 8 in preventing and controlling mosquitoes in water bodies.

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