CN115251049A - Pesticide solubilizing carrier and preparation method and application thereof - Google Patents
Pesticide solubilizing carrier and preparation method and application thereof Download PDFInfo
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- CN115251049A CN115251049A CN202210947762.7A CN202210947762A CN115251049A CN 115251049 A CN115251049 A CN 115251049A CN 202210947762 A CN202210947762 A CN 202210947762A CN 115251049 A CN115251049 A CN 115251049A
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- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
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- A01N25/04—Dispersions, emulsions, suspoemulsions, suspension concentrates or gels
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- A01N37/44—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
- A01N37/50—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids the nitrogen atom being doubly bound to the carbon skeleton
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
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- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
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- A01N47/10—Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof
- A01N47/24—Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof containing the groups, or; Thio analogues thereof
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- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
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- A01N47/28—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
- A01N47/34—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N< containing the groups, e.g. biuret; Thio analogues thereof; Urea-aldehyde condensation products
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- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
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- A01N47/28—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
- A01N47/38—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N< containing the group >N—CO—N< where at least one nitrogen atom is part of a heterocyclic ring; Thio analogues thereof
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- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
- A01N47/40—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides
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- A01N51/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds having the sequences of atoms O—N—S, X—O—S, N—N—S, O—N—N or O-halogen, regardless of the number of bonds each atom has and with no atom of these sequences forming part of a heterocyclic ring
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- A01N57/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds
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- A01N57/32—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-nitrogen bonds containing heterocyclic radicals
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- A01P—BIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
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- A01P7/00—Arthropodicides
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Abstract
The invention discloses a pesticide solubilizing carrier and a preparation method and application thereof, wherein the pesticide solubilizing composite carrier is formed by compounding dimer acid and a water-soluble polymer, and the water-soluble polymer is one of ethylene oxide/propylene oxide copolymer (EO/PO) and polyvinylpyrrolidone (PVP). The invention uses dimer acid and water-soluble polymer to compound to form a solubilizing carrier of insoluble pesticide, and improves the solubility of the insoluble drug in water. The composite carrier converts the insoluble drug crystal into amorphous form, and the dimer acid and the water-soluble polymer can form a stable drug-carrying system through hydrogen bond combination, so that the stability of the pesticide preparation is improved.
Description
Technical Field
The invention belongs to the field of agriculture, relates to a pesticide solubilizing carrier, a preparation method and application thereof, and particularly relates to a drug solubilizing carrier taking dimer acid and water-soluble polymer as raw materials.
Background
In China, in recent decades, the constituent organic chemical pesticides used for crop maintenance and pest control have been rapidly developed. In order to meet the demand of diversifying the active ingredients of the pesticide, various preparation products are produced at the same time. Good pesticide species, the success of formulation processing is half of its success. In these years, with the concern on the safety of people, livestock, fish and the environment and the continuous development of agriculture, new dosage forms which are safer, more efficient and more economical to process by occupation are needed to treat various defects of the processed dosage forms of the traditional Chinese medicine.
The preparation method of the water-soluble medicine in agriculture is simple, and the cost is relatively low. However, most of pesticides are poorly water-soluble drugs, and the formulation of the drugs is always the focus of the research on the pesticide formulation. At present, most pesticide formulations in the market are missible oil, wettable powder, suspending agent, granules and powder. The processing of the missible oil needs a lot of organic solvents, so that the pesticide damage is easy to occur, and the safety in the processes of production, storage and transportation is poor; when the granules are directly applied, the pesticide injury is easy to occur; micron-sized dust is generated in the preparation process of the wettable powder, so that the preparation is extremely harmful to human bodies, cross contamination of workshops is easy to occur, and the wettable powder is gradually eliminated from China due to the fact that the country stops registering the dosage form because of environmental protection requirements; the suspending agent belongs to a crude dispersion system formed by suspending pesticide particles which are insoluble in water, and is generally unstable in storage, and phenomena such as layering, bottom caking and the like are easy to occur; the powder is easy to drift off when powder is sprayed, pollutes the environment, is not easy to attach to the surface of the plant, and has low recovery rate, short lasting period and much loss.
Dimer acid CAS No.61788-89-4 with molecular formula C 36 H 64 O 4 Molecular weight 560.91. The raw materials for preparing dimer acid in industry are mostly octadecanoic unsaturated fatty acids, such as tall oil fatty acid, cotton oleic acid, soybean oleic acid, sunflower oil fatty acid, canola oil fatty acid, and the like. Because of wide raw material source, active chemical reactivity and good performance stability, and the characteristic of the structure of the dimer acid, the dimer acid becomes a very useful chemical intermediate. It is a mixture of various isomers, the major components of which are dimers, small amounts of trimers or multimers, and traces of unreacted monomers. The application of dimer acid in agriculture is rarely reported, particularly in the aspect of pesticide preparations, the dimer acid structure contains a large number of amphoteric groups, namely hydrophilic groups and hydrophobic groups, and the combination of the dimer acid and a flexible water-soluble polymer can improve the solubility and dispersity of insoluble drugs in water, further improve the stability of the pesticide preparations and the bioavailability of the drugs, so that the dimer acid has a wide application prospect in the aspect of pesticide preparations.
The hydrophilic/lipophilic property of the Ethylene Oxide (EO) and Propylene Oxide (PO) copolymer (EO/PO) can be realized by adjusting the EO/PO ratio in the molecule, and the EO/PO copolymer has good thermal oxidation resistance, chemical stability, surface activity, biodegradability, relatively low viscosity and excellent wetting property, thereby becoming an important nonionic surfactant and having wide application.
Disclosure of Invention
The invention aims to provide a pesticide solubilizing carrier, a preparation method and application thereof aiming at the defects of the pesticide preparation, and solves the problems that the pesticide is difficult to dissolve in water, the dispersed water solution of the pesticide is unstable, the preparation process is not environment-friendly and the like.
Therefore, the technical scheme of the invention is as follows:
a drug solubilizing carrier characterized by: the drug solubilizing carrier is formed by compounding dimer acid and water-soluble polymer, the mass ratio of the dimer acid to the water-soluble polymer is 1: 4-9, and the water-soluble polymer is one of ethylene oxide-propylene oxide copolymer (EO/PO) and polyvinylpyrrolidone.
The above-mentioned solubilizing carrier for drugs is characterized in that the physical state of the solubilizing carrier for agricultural chemicals may be a liquid state or a solid state.
According to the method for solubilizing the insoluble pesticide, the insoluble pesticide is selected from cyazofamid, thiamethoxam, difenoconazole, trifloxystrobin, imidacloprid, abamectin, fipronil, thiodicarb, chlorbenzuron, fosthiazate, pyridaben, imazaquin, furosemide, indoxacarb and acetamiprid; the water-soluble formulation comprising the poorly soluble drug and the drug solubilizing carrier according to claim 1, wherein the poorly soluble drug accounts for 25 to 55% by mass of the total composite solubilizing carrier.
Preferably, the drug carrier is prepared by a hot-melt method: the dimer acid and the water-soluble polymer are stirred for 1 to 2.5 hours by magnetic force under the oil bath of 55 to 80 ℃ by a hot melting method to obtain a uniform and stable hot melt; adding the insoluble drug, continuing to stir for 30-90 min by magnetic force to obtain a uniform system, and cooling to obtain the pesticide preparation of the composite carrier.
The pesticide preparation is characterized in that: the pesticide preparation prepared by the composite carrier releases water, the mass ratio of the pesticide preparation to the water is 90-200, the particle size of the pesticide preparation after being dispersed in the water reaches the nanometer level, and the average hydrated particle size is 150-250 nm.
The invention uses the dimer acid and the water-soluble polymer to compound to form the pesticide solubilizing carrier, thereby improving the solubility of the insoluble pesticide in water. The composite carrier converts the insoluble drug crystal into amorphous form, and the dimer acid and the water-soluble polymer can form a stable drug-carrying system through hydrogen bond combination, so that the stability of the pesticide preparation is improved, the preparation process is environment-friendly, and the organic solvent is polluted.
Detailed Description
The invention is further illustrated by the following examples, which are not meant to be limiting.
In the present invention, all percentages are by weight unless otherwise specified, and all equipment and materials, etc. are commercially available or commonly used in the industry.
Example 1
Selecting polyether F68 (CAS No.9003-11-6, average molecular weight 8350) with weight of 6.0g, magnetically stirring dimer acid and polyether F68 at 70 deg.C in oil bath for 1.5h by hot melting method to obtain uniform and stable hot melt, adding crude drug with total solubilizing carrier mass of 40%, magnetically stirring for 40min to obtain uniform system, and cooling to obtain pesticide preparation with composite carrier. The experimental components are shown in table 1 below.
Table 1:
2.0g of the obtained pesticide preparation is put into a beaker, 250ml of distilled water is added, and the mixture is stirred on a magnetic stirrer of 100r/min at the temperature of 25 ℃. Record the complete disintegration time of the drug solids in the beaker. Diluting the completely disintegrated medicinal liquid by 100 times, standing, collecting supernatant, introducing sample through 0.45 μm microporous membrane, measuring its peak area by High Performance Liquid Chromatography (HPLC), and calculating the amount of the medicine dissolved in water according to standard curve.
Example 2
Selecting polyether F38 (CAS No.9003-11-6, average molecular weight 5000) with weight of 6.0g, magnetically stirring 1.2g of dimer acid and polyether F38 at 70 ℃ in an oil bath by a hot melting method for 1.5h to obtain a uniform and stable hot melt, adding cyazofamid with the mass of 40% of the total solubilizing carrier, continuously magnetically stirring for 40min to obtain a uniform system, and cooling to obtain the pesticide preparation of the composite carrier.
2.0g of the solid preparation obtained was placed in a beaker, 250ml of distilled water was added thereto, and the mixture was stirred at 25 ℃ on a magnetic stirrer at 100 r/min. Record the complete disintegration time of the drug solids in the beaker. Diluting the completely disintegrated medicinal liquid by 100 times, standing, collecting supernatant, introducing sample through 0.45 μm microporous filter membrane, measuring its peak area by HPLC, and calculating the dissolved amount of the medicine in water according to standard curve.
Example 3
Selecting 6.0g of polyvinylpyrrolidone-k 60 (CAS No.9003-39-8, average molecular weight 160,000), magnetically stirring 1.2g of dimer acid and PVP-k60 in an oil bath at 80 ℃ for 2 hours by a hot melting method to obtain a uniform and stable hot melt, adding cyazofamid accounting for 40% of the total solubilizing carrier by mass, continuing to magnetically stir for 50 minutes to obtain a uniform system, and cooling to obtain the pesticide preparation with the composite carrier.
2.0g of the solid preparation obtained was placed in a beaker, 250ml of distilled water was added thereto, and the mixture was stirred at 25 ℃ on a magnetic stirrer at 100 r/min. Record the complete disintegration time of the drug solids in the beaker. Diluting the completely disintegrated medicinal liquid by 100 times, standing, collecting supernatant, introducing sample through 0.45 μm microporous filter membrane, measuring its peak area by HPLC, and calculating the dissolved amount of the medicine in water according to standard curve.
Example 4
Selecting 6.0g of polyvinylpyrrolidone-k 30 (CAS No.9003-39-8, average molecular weight 40,000), magnetically stirring 1.2g of dimer acid and PVP-k30 at 60 ℃ in an oil bath by a hot melting method for 1.5h to obtain a uniform and stable hot melt, adding cyazofamid accounting for 40% of the total solubilizing carrier by mass, continuously magnetically stirring for 30min to obtain a uniform system, and cooling to obtain the pesticide preparation with the composite carrier.
2.0g of the solid preparation obtained was placed in a beaker, 250ml of distilled water was added thereto, and the mixture was stirred at 25 ℃ on a magnetic stirrer at 100 r/min. Record the complete disintegration time of the drug solids in the beaker. Diluting the completely disintegrated medicinal liquid by 100 times, standing, collecting supernatant, introducing sample through 0.45 μm microporous filter membrane, measuring its peak area by HPLC, and calculating the dissolved amount of the medicine in water according to standard curve.
The results obtained for the above examples are shown in table 2:
TABLE 2 drug dissolution profiles of different drug substance solubilizing carriers
The results of examples 2 to 4 are shown in Table 3.
Table 3 drug dissolution of different polymer solid formulations.
Group of | Disintegration time(s) | Particle size (nm) | Cumulative dissolution Rate (%) | Saturated solubility (mg/ml) |
Example 2 | 89 | 215 | 97.1 | 4.7 |
Example 3 | 213 | 195 | 95.8 | 6.1 |
Example 4 | 165 | 231 | 96.7 | 3.9 |
The method for measuring the cumulative dissolution rate in examples 1 to 4 is a method for measuring the dissolution rate of a pesticide prepared from a composite carrier (dimer acid and EO/PO) by referring to the "slurry method" of 0931, a general guideline of chinese pharmacopoeia on 2015 edition. Accurately weighing a proper amount of novel pesticide prepared by the composite carrier, ultrasonically degassing 1000mL of distilled water for 6min, taking the degassed distilled water as a dissolution medium, setting the temperature of an RCZ-6C3 intelligent dissolution instrument to be 37 +/-0.5 ℃, the paddle rotation speed to be 100r/min, taking 5m1 dissolution liquid by using a disposable 5m1 injector when the dissolution time is 5min,10min,20min,40min and 60min, supplementing isothermal 5mL of ultrasonically degassed distilled water into a dissolution cup, filtering the 5mL dissolution liquid by a 0.45 mu m microporous filter membrane, carrying out HPLC (high performance liquid chromatography) detection, and calculating the dissolution rates of the composite carrier rutin solid dispersion at different times. And the cumulative dissolution rate thereof was calculated according to the following formula.
Y n ′=Y n +(Y 1 +Y 2 +Y 3 +Y n-1 )V 1 /V 2
In the formula:
y' n is the cumulative dissolution rate (%) calculated at the nth time;
yn is the dissolution rate (%) calculated at the nth time;
V 1 volume of dissolution medium (mL) for each supplement;
V 2 the total volume (mL) of the dissolution medium in the dissolution cup.
The particle size test method in examples 1 to 4 was to take a proper amount of the pesticide preparation prepared from the composite carrier in a proper amount of distilled water, dilute the completely disintegrated suspension, place the diluted suspension in a particle size cup, place the cup in a nanometer particle size analyzer, and measure the particle size of the suspension of the pesticide preparation prepared from the composite carrier.
The result shows that the slightly soluble drug preparation prepared by taking the dimer acid-water-soluble high polymer as the drug carrier has high disintegration speed, excellent accumulative dissolution rate and saturated solubility, environment-friendly and free of dust and organic solvent pollution in the preparation process, and the solubility of the slightly soluble drug can be increased by 100-2000 times.
Claims (6)
1. A pesticide solubilizing carrier and a preparation method and application thereof are characterized in that: the carrier is formed by compounding dimer acid and water-soluble polymer, and the mass ratio of the dimer acid to the water-soluble polymer is 1: 4-9.
2. The pesticide-solubilizing complex carrier of claim 1, wherein: the water-soluble polymer is one of ethylene oxide/propylene oxide copolymer (EO/PO) and polyvinylpyrrolidone (PVP).
3. The pharmaceutical solubilizing complex carrier of claim 1, wherein the physical state of said pesticidal solubilizing carrier can be either liquid or solid.
4. The pesticide solubilizing carrier, the preparation method and the application thereof as claimed in claim 1, wherein the pesticide is selected from the group consisting of: cyazofamid, thiamethoxam, difenoconazole, trifloxystrobin, imidacloprid, abamectin, fipronil, thiodicarb, chlorbenzuron, fosthiazate, pyridaben, imazaquin, furosemide, indoxacarb and acetamiprid; the insoluble drug and the drug solubilizing carrier are compounded to form the pesticide preparation, and the insoluble drug accounts for 25-55% of the total solubilizing carrier.
5. The poorly soluble pesticidal formulation according to claim 4, characterized in that it is prepared by a method comprising the steps of: the dimer acid and the water-soluble carrier are stirred magnetically for 0.5 to 2.0 hours in an oil bath at the temperature of between 55 and 80 ℃ by a hot melting method to obtain a uniform and stable hot melt; adding the insoluble drug, continuing to stir for 30-90 min by magnetic force to obtain a uniform system, and cooling to obtain the pesticide preparation.
6. The pesticide formulation according to claim 5, characterized in that its method of use is: the pesticide preparation prepared by the carrier releases water, the mass ratio of the pesticide preparation to the water is 90-200, the pesticide preparation and the water are mixed and stirred uniformly, the particle size reaches the nanometer level after the pesticide is dispersed in the water, and the average hydrated particle size is 150-250 nm.
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