CN106942247A - Emamectin-benzoate effervescent tablet and preparation method thereof - Google Patents

Abstract

The invention discloses a kind of preparation method of emamectin-benzoate effervescent tablet.Emamectin-benzoate effervescent tablet, the composition that it is formulated is as follows, by percentage to the quality：Methylaminoemamectin benzoate 1 5%, acid source 10 20%, alkali source 10 20%, dispersant 2 6%, wetting agent 2 4%, adhesive 2 6%, disintegrant 3 20%, filler 19 70%.Preparation method：（1）Well mixed be added in pulverizer of raw material is crushed, and obtains pulvis；（2）Pulvis is added to compressing tablet in tablet press machine.Emamectin-benzoate effervescent tablet produced by the present invention has processing simple, and metering is accurate, and performance is stable, storage, transport, it is easy to use, the features such as security is good, while the problem of solving emamectin-benzoate easy photodissociation, extends the storage period of preparation.

Description

Emamectin benzoate effervescent tablet and preparation method thereof

technical field

The invention relates to the preparation technology of emamectin benzoate effervescent tablet.

Background technique

Emamectin benzoate has stomach poisoning and contact killing effects, has a high activity on lepidopteran insect larvae, and has a good control effect on vegetable root-knot nematodes. As a biopesticide, emamectin benzoate has the characteristics of ultra-high efficiency, low toxicity, and low residue. It is an important species for pest control on vegetables, fruit trees, cotton, rice and other crops.

Emamectin benzoate has a wide insecticidal spectrum, high biological activity, low toxicity, environmental protection, and is difficult to produce drug resistance. However, the existing processing formulations of emamectin benzoate are mainly emulsifiable concentrates, microemulsions, water emulsions and suspension concentrates, wherein a large amount of organic solvents and emulsifiers are used in the processing of emulsifiable concentrates and microemulsions, and the production cost is high. And it is easy to pollute the environment; the content of active ingredients in aqueous emulsions and suspensions is low, and physical stability problems such as stratification, precipitation and emulsion are prone to occur during storage and use, and the production, storage and transportation of liquid preparations are inconvenient. Emamectin benzoate can also be processed into water-dispersible granules, but the formation of granules requires the addition of a larger proportion of binders, resulting in slow disintegration of the granules.

Effervescent tablet is a tablet dosage form that uses acid source and alkali source to generate CO ₂ when they meet with water, so that the tablet can be quickly disintegrated to form a uniform suspension. Compared with liquid preparations, effervescent tablets have the advantages of accurate measurement, simple processing, low production cost, convenient storage, transportation and use. Compared with other solid preparations (such as water-dispersible granules), effervescent tablets have the characteristics of disintegration, fast dispersion, high hardness, and more convenient transportation and use. However, at present, effervescent tablets mainly use wet granulation, the process is cumbersome, and some wet granulation wastes a lot of organic solvents. For example, the authorized publication numbers are CN102823589A, CN101874491A, CN101658165A, CN102177906A and other effervescent tablet patents, all of which require water or organic solvents in the preparation process, and the preparation methods all include a drying process, and the acid and alkali need to be divided into two parts for preparation.

Contents of the invention

The purpose of this invention is to provide a kind of emamectin benzoate effervescent tablet and preparation method thereof, the present invention uses the emamectin benzoate effervescent tablet of dry method preparation to have operation Simple, accurate measurement, fast disintegration, safe and convenient in the process of production, transportation, storage and use, it can be sprayed with water or directly thrown into the paddy field. It is a safe, environmentally friendly and labor-saving dosage form.

The object of the present invention is achieved by the following technical solutions, a kind of emamectin benzoate effervescent tablet, according to mass percent, is made up of following raw materials:

The acid source is one of tartaric acid, citric acid, fumaric acid, adipic acid and malic acid, and the alkali source is one of sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate and calcium carbonate. , the dispersant is one to several kinds of lignosulfonate, modified lignosulfonate and naphthalenesulfonate formaldehyde condensate, the wetting agent is alkylnaphthalenesulfonate, alkylsulfuric acid One or several kinds of salt, sulfonate, fatty acid or fatty acid ester sulfate, phosphate ester, the binder is polyvinylpyrrolidone, polyvinyl alcohol, polyethylene glycol, hydroxymethyl cellulose, xanthan gum and polyacrylic acid One of sodium, the disintegrant is one of soluble starch, white carbon black, diatomaceous earth, urea, ammonium sulfate, and the filler is one of kaolin, diatomaceous earth, light calcium carbonate, attapulgite and clay A sort of.

A kind of emamectin benzoate effervescent tablet preparation method, comprises the steps:

(1) Mix all the components in proportion and evenly add them into a pulverizer to pulverize to more than 200 mesh to prepare a uniform powder.

(2) Take the powder obtained in the step (1) of required quality, join in tablet press machine and compress, obtain emamectin benzoate effervescent tablet.

Preferably, the tablet has a mass of 2-10 g.

Compared with the prior art, the present invention has the following beneficial effects:

First, the present invention uses the powder direct compression method to make emamectin benzoate into effervescent tablets, which avoids the disadvantages of production, storage and transportation of liquid preparations, and solves the problem of water dispersible granules at the same time. Compared with wet granulation, it is simpler and more environmentally friendly, and it is also in line with the development direction of labor-saving, safe and environmentally friendly pesticide formulation processing.

Second, the effervescent tablet manufactured by the present invention has the advantages of stable performance, safety and convenience during production, transportation, storage and use.

Third, the emamectin benzoate effervescent tablet manufactured by the present invention has the characteristics of simple processing, accurate measurement, stable performance, convenient storage, transportation, and good safety, and solves the problem of emamectin benzoate at the same time. The problem that the vermectin benzoate is easy to photolyze prolongs the storage period of the preparation.

Description of drawings

Fig. 1 emamectin benzoate effervescent tablet makes flowchart;

Fig. 2 appearance diagram of emamectin benzoate effervescent tablet;

Fig. 3 disintegration diagram in water of emamectin benzoate effervescent tablet;

Fig. 4 emamectin benzoate effervescent tablet suspension diagram.

detailed description

In order to make the object, technical solution and advantages of the present invention clearer, the present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments. It should be understood that the specific implementation examples described here are only used to explain the present invention, and are not intended to limit the present invention.

Example 1

1) Get 1g emamectin benzoate former drug, 4g tartaric acid, 4g sodium bicarbonate, 0.8g alkylnaphthyl acid sodium salt, 0.8g sodium lignosulfonate, 1.2g polyvinylpyrrolidone, Add 2g of diatomite and 6.2g of kaolin into a pulverizer and pulverize to a size above 200 mesh to prepare 20g of powder.

2) Get the powder in the 8.5g step (1) and join in the tablet press machine, promptly make the 8.5g emamectin benzoate effervescent tablet. The production process is shown in Figure 1, and the product appearance is shown in Figure 2.

Example 2

1) Get 1g emamectin benzoate former drug, 4g tartaric acid, 4g sodium bicarbonate, 0.8g alkylnaphthyl flow acid sodium salt, 0.8g 2-naphthalenesulfonic acid formaldehyde polymer sodium salt, 1.2 Add 2 g of polyvinylpyrrolidone, 2 g of diatomaceous earth, and 6.2 g of kaolin into a pulverizer and pulverize to 200 mesh to prepare 20 g of powder.

2) Get the powder in the 8.5g step (1) and join in the tablet press machine, promptly make the 8.5g emamectin benzoate effervescent tablet. The production process is shown in Figure 1, and the product appearance is shown in Figure 2.

Example 3

1) Get 1g emamectin benzoate former drug, 4g tartaric acid, 4g sodium bicarbonate, 0.8g alkylnaphthyl flow acid sodium salt, 0.8g modified lignosulfonate, 1.2g polyethylene Pyrrolidone, 2g of diatomaceous earth, and 6.2g of kaolin were added into a pulverizer and pulverized to 200 mesh to prepare 20g of powder.

2) Get the powder in the 8.5g step (1) and join in the tablet press machine, promptly make the 8.5g emamectin benzoate effervescent tablet. The production process is shown in Figure 1, and the product appearance is shown in Figure 2.

Example 4

1) Get 1g emamectin benzoate former drug, 4g tartaric acid, 4g sodium bicarbonate, 0.8g alkylnaphthyl acid sodium salt, 0.8g sodium lignosulfonate, 1.2g polyvinylpyrrolidone, Add 2g of starch and 6.2g of kaolin into a pulverizer and pulverize to 200 mesh to prepare 20g of powder.

2) Get the powder in the 8.5g step (1) and join in the tablet press machine, promptly make the 8.5g emamectin benzoate effervescent tablet. The production process is shown in Figure 1, and the product appearance is shown in Figure 2.

Example 5

1) Take 1g emamectin benzoate technical substance, 4g tartaric acid, 4g sodium bicarbonate, 0.8g alkylnaphthyl flow acid sodium salt, 0.8g 2-naphthalenesulfonic acid formaldehyde polymer sodium salt, 1.2g Add polyvinylpyrrolidone, 2g starch, and 6.2g kaolin into a pulverizer and pulverize to 200 mesh to prepare 20g powder.

2) Get the powder in the 8.5g step (1) and join in the tablet press machine, promptly make the 8.5g emamectin benzoate effervescent tablet. The production process is shown in Figure 1, and the product appearance is shown in Figure 2.

Example 6

1) Get 1g emamectin benzoate former drug, 4g tartaric acid, 4g sodium bicarbonate, 0.8g alkylnaphthyl flow acid sodium salt, 0.8g modified lignosulfonate, 1.2g polyethylene Add pyrrolidone, 2g starch, and 6.2g kaolin into a pulverizer and pulverize to 200 mesh to prepare 20g powder.

2) Get the powder in the 8.5g step (1) and join in the tablet press machine, promptly make the 8.5g emamectin benzoate effervescent tablet. The production process is shown in Figure 1, and the product appearance is shown in Figure 2.

The product that above-mentioned 6 embodiments obtain is carried out quality and stability test, and the results are shown in Table 1:

The quality control index test result of table 1 emamectin benzoate effervescent tablet

The disintegration results are shown in Figure 3. The suspension rate test results are shown in Figure 4.

Note: The test method is as follows:

①Disintegration time

Different qualities of effervescent tablets have different disintegration time requirements. Put the sample into a glass beaker (500 mL in volume) filled with 400 mL of standard hard water, and it is qualified if it is less than 7 minutes.

②Suspension rate

Take 1g of the sample and make it into a suspension for 30 minutes, and the active ingredient exceeds 60% to be qualified.

③Hardness

Tested with a hardness tester, if the hardness reaches 5 or above, it is qualified.

④Heat storage stability

Seal the sample and place it in a constant temperature drying oven at (54±2)°C, store it for 14 days and take it out, and the active ingredient is ≥ 95% compared with the heat storage, which is qualified.

It can be seen that the effervescent tablet has the characteristics of rapid disintegration, high suspension rate, qualified hardness and stability.

The above descriptions are only preferred embodiments of the present invention, and are not intended to limit the present invention. Any modifications, equivalent replacements and improvements made within the spirit and principles of the present invention should be included in the protection of the present invention. within range.

Claims (9)

1. emamectin-benzoate effervescent tablet, it is characterized in that, the composition of the effervescent tablet formula is as follows, with matter Measure percentages：Methylaminoemamectin benzoate 1-5%, acid source 10-20%, alkali source 10-20%, dispersant 2-6%, profit Humectant 2-4%, adhesive 2-6%, disintegrant 3-20%, filler 19-70%.

2. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that the acid source is Any one in tartaric acid, citric acid, fumaric acid, hexanedioic acid and malic acid or two or more any mixture.

3. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that the alkali source is Any one in sodium carbonate, sodium acid carbonate and saleratus, potassium carbonate, calcium carbonate or two or more any mixed Compound.

4. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that the dispersant For any one in lignin sulfonate, modified lignin mahogany sulfonate class and naphthalenesulfonate formaldehyde condensation compound class or appoint Two kinds of mixtures of meaning or any three kinds of mixtures.

5. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that the wetting agent For alkylnaphthalene sulfonate, alkyl sulfate, sulfonate, aliphatic acid, fatty acid ester sulfate and phosphate any one or appoint Anticipate two or more mixture.

6. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that described adhesive To be any one in polyvinylpyrrolidone, polyvinyl alcohol, polyethylene glycol, hydroxymethyl cellulose, xanthans and Sodium Polyacrylate Kind.

7. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that the disintegrant For any one in soluble starch, white carbon, diatomite, urea, ammonium sulfate.

8. emamectin-benzoate effervescent tablet according to claim 1, it is characterised in that the filler is Any one in kaolin, diatomite, precipitated calcium carbonate, attapulgite and clay.

9. the preparation method of the emamectin-benzoate effervescent tablet according to claim any one of 1-8, its It is characterised by, comprises the following steps：

（1）It is added in pulverizer and is crushed after all components are mixed in proportion, prepares uniform pulvis；It is described to crush Fineness is more than 200 mesh；

（2）Weigh step（1）In obtained pulvis, be added to compressing tablet in tablet press machine, that is, obtain emamectin benzoate benzoic acid Salt effervescent tablet agent, tablet quality is in 2-10 g.