CN115251049A - Pesticide solubilizing carrier and preparation method and application thereof - Google Patents

Pesticide solubilizing carrier and preparation method and application thereof Download PDF

Info

Publication number
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
Authority
CN
China
Prior art keywords
pesticide
water
carrier
preparation
solubilizing
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202210947762.7A
Other languages
Chinese (zh)
Inventor
潘荣
覃慧
季东鑫
金志敏
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Zhejiang University of Technology ZJUT
Original Assignee
Zhejiang University of Technology ZJUT
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Zhejiang University of Technology ZJUT filed Critical Zhejiang University of Technology ZJUT
Priority to CN202210947762.7A priority Critical patent/CN115251049A/en
Publication of CN115251049A publication Critical patent/CN115251049A/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, 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
    • A01N25/02Biocides, 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 containing liquids as carriers, diluents or solvents
    • A01N25/04Dispersions, emulsions, suspoemulsions, suspension concentrates or gels
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, 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
    • A01N37/02Saturated carboxylic acids or thio analogues thereof; Derivatives thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, 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
    • A01N37/44Biocides, 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
    • A01N37/50Biocides, 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
    • A01N43/04Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
    • A01N43/06Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings
    • A01N43/08Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings with oxygen as the ring hetero atom
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/501,3-Diazoles; Hydrogenated 1,3-diazoles
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/581,2-Diazines; Hydrogenated 1,2-diazines
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/64Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
    • A01N43/647Triazoles; Hydrogenated triazoles
    • A01N43/6531,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90Biocides, 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, 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
    • A01N47/02Biocides, 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 no bond to a nitrogen atom
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, 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
    • A01N47/08Biocides, 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 one or more single bonds to nitrogen atoms
    • A01N47/10Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof
    • A01N47/24Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof containing the groups, or; Thio analogues thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, 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
    • A01N47/08Biocides, 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 one or more single bonds to nitrogen atoms
    • A01N47/28Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
    • A01N47/34Ureas 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, 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
    • A01N47/08Biocides, 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 one or more single bonds to nitrogen atoms
    • A01N47/28Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
    • A01N47/38Ureas 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, 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
    • A01N47/40Biocides, 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N51/00Biocides, 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
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N57/00Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds
    • A01N57/26Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-nitrogen bonds
    • A01N57/32Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-nitrogen bonds containing heterocyclic radicals
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01PBIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P1/00Disinfectants; Antimicrobial compounds or mixtures thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01PBIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P3/00Fungicides
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01PBIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P7/00Arthropodicides
    • A01P7/02Acaricides
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01PBIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P7/00Arthropodicides
    • A01P7/04Insecticides

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

Pesticide solubilizing carrier and preparation method and application thereof
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:
Figure BSA0000280663890000031
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
Figure BSA0000280663890000051
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.
CN202210947762.7A 2022-07-29 2022-07-29 Pesticide solubilizing carrier and preparation method and application thereof Pending CN115251049A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210947762.7A CN115251049A (en) 2022-07-29 2022-07-29 Pesticide solubilizing carrier and preparation method and application thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN202210947762.7A CN115251049A (en) 2022-07-29 2022-07-29 Pesticide solubilizing carrier and preparation method and application thereof

Publications (1)

Publication Number Publication Date
CN115251049A true CN115251049A (en) 2022-11-01

Family

ID=83748216

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202210947762.7A Pending CN115251049A (en) 2022-07-29 2022-07-29 Pesticide solubilizing carrier and preparation method and application thereof

Country Status (1)

Country Link
CN (1) CN115251049A (en)

Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995034200A1 (en) * 1994-06-10 1995-12-21 Fernz Corporation Limited Biodegradable sustained release composition
JPH1121540A (en) * 1997-07-02 1999-01-26 Ishihara Chem Co Ltd Anhydrous transparent gel containing functional component
WO2002010244A2 (en) * 2000-07-27 2002-02-07 3M Innovative Properties Company Biocidal polyurethane compositions and method of use
CN1341012A (en) * 1999-01-25 2002-03-20 宝洁公司 Cleaning compositions
US20050158271A1 (en) * 2000-10-11 2005-07-21 Lee Sang C. Pharmaceutical applications of hydrotropic polymer micelles
KR20080020165A (en) * 2006-08-31 2008-03-05 조선대학교산학협력단 Locally solubilized controlled release matrix tablet of poorly soluble drugs
CN102427722A (en) * 2009-05-08 2012-04-25 禾大公司 Surfactants in agrochemical formulations
CN105052902A (en) * 2015-08-04 2015-11-18 清华大学 Sustained and controlled release pesticide nanometer emulsion and preparation method thereof
CN107125249A (en) * 2017-05-05 2017-09-05 奎克化学(中国)有限公司 A kind of compound disinfectant and metalworking fluid containing it and preparation method thereof
US20170280711A1 (en) * 2012-11-01 2017-10-05 Huntsman Petrochemical Llc Polyamide and Polyimide Sticker Adjuvants
CN111165474A (en) * 2019-12-31 2020-05-19 苏州丰倍生物科技有限公司 Pesticide dissolution promoter, application thereof and high-content preparation
CN113287608A (en) * 2021-05-11 2021-08-24 浙江工业大学 Drug solubilization system and application thereof in pesticide preparation
CN113426366A (en) * 2021-05-12 2021-09-24 浙江工业大学 Soluble chitosan-PVP compound emulsifier and preparation method and application thereof
CN114748633A (en) * 2022-04-13 2022-07-15 浙江工业大学 Preparation method of composite carrier applied to drug solubilization

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995034200A1 (en) * 1994-06-10 1995-12-21 Fernz Corporation Limited Biodegradable sustained release composition
JPH1121540A (en) * 1997-07-02 1999-01-26 Ishihara Chem Co Ltd Anhydrous transparent gel containing functional component
CN1341012A (en) * 1999-01-25 2002-03-20 宝洁公司 Cleaning compositions
WO2002010244A2 (en) * 2000-07-27 2002-02-07 3M Innovative Properties Company Biocidal polyurethane compositions and method of use
US20050158271A1 (en) * 2000-10-11 2005-07-21 Lee Sang C. Pharmaceutical applications of hydrotropic polymer micelles
KR20080020165A (en) * 2006-08-31 2008-03-05 조선대학교산학협력단 Locally solubilized controlled release matrix tablet of poorly soluble drugs
CN102427722A (en) * 2009-05-08 2012-04-25 禾大公司 Surfactants in agrochemical formulations
US20170280711A1 (en) * 2012-11-01 2017-10-05 Huntsman Petrochemical Llc Polyamide and Polyimide Sticker Adjuvants
CN105052902A (en) * 2015-08-04 2015-11-18 清华大学 Sustained and controlled release pesticide nanometer emulsion and preparation method thereof
CN107125249A (en) * 2017-05-05 2017-09-05 奎克化学(中国)有限公司 A kind of compound disinfectant and metalworking fluid containing it and preparation method thereof
CN111165474A (en) * 2019-12-31 2020-05-19 苏州丰倍生物科技有限公司 Pesticide dissolution promoter, application thereof and high-content preparation
CN113287608A (en) * 2021-05-11 2021-08-24 浙江工业大学 Drug solubilization system and application thereof in pesticide preparation
CN113426366A (en) * 2021-05-12 2021-09-24 浙江工业大学 Soluble chitosan-PVP compound emulsifier and preparation method and application thereof
CN114748633A (en) * 2022-04-13 2022-07-15 浙江工业大学 Preparation method of composite carrier applied to drug solubilization

Similar Documents

Publication Publication Date Title
EP0173964B1 (en) A biocidal fine powder, its manufacturing method and a suspension for agricultural use containing the above powder
CN108902158B (en) Suspending agent containing pyraclostrobin composition and application thereof
Zhu et al. Avermectin loaded carboxymethyl cellulose nanoparticles with stimuli-responsive and controlled release properties
CN110946133B (en) Nano photolysis-resistant controlled-release pesticide with lignin as coating matrix and preparation method thereof
CN109479876A (en) Suspending agent and preparation method thereof
CN103651381B (en) A kind of mite-killing preparation and application thereof
CN110973152A (en) High-efficiency cypermethrin nano water aqua and preparation method and application thereof
CN110999902A (en) Nanometer water agent containing prochloraz and processing method thereof
EP2059124B1 (en) Polymeric surfactant useful for the preparation of pesticidal agrochemical compositions
CN109258631A (en) Suspending agent and preparation method thereof
CN103299994B (en) Solid microemulsion and preparation method thereof
TW200406149A (en) Agricultural chemical composition in granular form
CN1063914C (en) Plant protection pesticide containing avermectin
CN110622965A (en) Preparation method of leaf surface affinity type pesticide nano microcapsule based on tannic acid modification
WO2017133868A1 (en) Powdery formulations with surface active substances on solid, water-soluble carriers, method for the production and use thereof
JP2770400B2 (en) Pesticide solid formulation
CN115251049A (en) Pesticide solubilizing carrier and preparation method and application thereof
EP0259982B1 (en) Solid iodophor composition
CN113287608B (en) Drug solubilization system and application thereof in pesticide preparation
CN106135236B (en) A kind of AVM and Envidor compounding aqueous suspension agent and preparation method thereof
CN101623255B (en) Artesunate nanoemulsion drug composition and preparation method thereof
CN1098250A (en) Composition pesticide
CN1663378A (en) Pesticide formulation of nimbin and emamectin benzoate and preparing method thereof
CN1290412C (en) Medicine composition for killing schistosome, and its prepn. method
CN1291646C (en) Peparation of water dispersed soft particle of pesticide

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination