CN106665645B - A kind of refining dipterex composition and the preparation method and application thereof - Google Patents
A kind of refining dipterex composition and the preparation method and application thereof Download PDFInfo
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- CN106665645B CN106665645B CN201611199419.XA CN201611199419A CN106665645B CN 106665645 B CN106665645 B CN 106665645B CN 201611199419 A CN201611199419 A CN 201611199419A CN 106665645 B CN106665645 B CN 106665645B
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- refining dipterex
- dipterex
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION 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
- A01N57/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds
- A01N57/18—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds
- A01N57/20—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing acyclic or cycloaliphatic radicals
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION 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
- A01N25/00—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
- A01N25/34—Shaped forms, e.g. sheets, not provided for in any other sub-group of this main group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
Abstract
The invention belongs to technical field of pesticide preparations, and in particular to a kind of refining dipterex composition, and preparation method and application are further disclosed.Refining dipterex composition of the present invention, refining dipterex raw medicine, complex enzyme agent and the functional additive for being 100:0.5-3:2-5 including mass ratio.Refining dipterex composition of the present invention, using refining dipterex raw medicine as effective component, in the booster action of addition complex enzyme agent and functional additive, further enhance the anthelminthic effect of trichlorfon technical, either for the infection of faecal egg, or the desinsection of the infection conditions of internal organ helminth, refining dipterex tablet of the present invention can effectively be driven away；Importantly, metrifonate tablet of the present invention can obtain higher anthelminthic effect under the addition of lower effective dose, effective purge ratio is close to 100%.
Description
Technical field
The invention belongs to technical field of pesticide preparations, and in particular to a kind of refining dipterex composition, and further disclose
Preparation method and application.
Background technique
Metrifonate, scientific name O, O- dimethyl-(2,2,2- tri- chloro- 1- hydroxyethyl) phosphonate ester, Chinese nickname include enemy hundred
Worm soluble powder, metrifonate is for animals, trichlorphon original powder, dimethyl-(the chloro- 1- hydroxyethyl of 2,2,2- tri-) phosphate, purification
Metrifonate etc..Metrifonate is a kind of organophosphorus insecticide, and industrial products are white solid, molecular weight 257.43, sterling fusing point
83-84 DEG C, density 1.73 (20 DEG C), 10% aqueous solution index of refraction is 1.3439,7.8 μ Pa of vapour pressure (20 DEG C).Metrifonate tool
There is aromatic odor, water and organic solvent can be dissolved in, 100 milliliters 15.4 grams of water dissolvable at 25 DEG C, and as temperature increases, enemy
The solubility of hundred worms in water increases.Metrifonate property is more stable, but meets alkali and be then hydrolyzed into DDVP, and acute toxicity LD50 value is
Big white mouse is orally 560~630mg/kg.
Metrifonate belongs to organophosphorus pesticide-phosphate type one kind, and hydroxyl replaces shape by organic group in phosphoric acid molecules
Becoming phosphoric acid at the compound of phosphorus carbon key, phosphoric acid is esterified as phosphate, and acceptable daily intake is 0.01mg/ (kg.d),
For the toxicity of metrifonate based on acute poisoning, slow poisoning is smaller.Metrifonate is more stable in acid and neutral solution, in alkalinity
Under the conditions of easily decompose and lose toxicity, but metrifonate decompose under alkaline condition after can obtain product DDVP, make its toxicity increase
It is 10 times big.
The main function of metrifonate is used as insecticide, is a kind of organophosphorus insecticide, is had efficient, less toxic, low
The characteristics of residual is a kind of broad spectrum insecticide.Metrifonate is had concurrently action of contace poison, is also there is osmotically active based on stomach poison function,
Suitable for the pests with chewing mouthparts and domestic animal parasitism on the crops such as rice, wheat, vegetables, tea tree, fruit tree, mulberry tree, cotton
The prevention and treatment of worm, sanitary insect pest.Metrifonate is also very wide in agriculturally application range, can be used for preventing and treating cabbage caterpillar, Amrasca biguttula (Ishida), Sang Ye
The prevention and treatment of the various pests such as silkworm, Phellinus, weevil, fruit tree sawfly, drosophila；It can also be used for treatment snail fever, be in herding
A kind of good multiple-effect pest repellant.
Trichlorphon original powder can be processed into the various dosage forms such as pulvis, wettable powder, soluble powder and emulsion and use, can also
Poison bait is made in direct obtained aqueous solution, for preventing and treating agriculture, the woods, gardening pest insect of biting mouthparts and sucking mouth parts, underground
Pest etc.；After raw medicine can also being refined purification processes, for preventing and treating pig, ox, horse, epizoa in mule livestock body, to family and
Public health insect is effective.
Summary of the invention
For this purpose, technical problem to be solved by the present invention lies in a kind of refining dipterex composition is provided, further to mention
The desinsection drug effect of high refining dipterex.
In order to solve the above technical problems, refining dipterex composition of the present invention, including mass ratio are 100:0.5-
Refining dipterex raw medicine, complex enzyme agent and the functional additive of 3:2-5.
Preferably, the mass ratio of the refining dipterex raw medicine, complex enzyme agent and functional additive is 100:1.5:3.
The complex enzyme agent is selected from the mixture of one or more of phytase, beta-lactamase or lysozyme, and excellent
Select three's mixed in equal amounts.
The functional additive is selected from the mixture of one or more of hyaluronic acid, polyglutamic acid or trehalose, and
It is preferred that three's mixed in equal amounts.
The invention also discloses a kind of methods for preparing the refining dipterex composition, including take a selected amount of described
Refining dipterex raw medicine, complex enzyme agent and functional additive, and the step of being mixed.
The invention also discloses add customary adjuvant, according to made from common process as the refining dipterex composition
Metrifonate preparation.
The invention also discloses a kind of refining dipterex tablets, conventional auxiliary by the refining dipterex composition addition
Expect, according to tablet made from common process.
Preferably, the raw material for preparing of the tablet includes:
More preferably, the raw material for preparing of the tablet includes:
The invention also discloses a kind of methods for preparing the refining dipterex tablet, include the following steps:
(1) it stocks up: a selected amount of starch being taken to add water that starch slurry is made, it is spare；
(2) softwood: taking a selected amount of refining dipterex raw medicine and calcium monohydrogen phosphate, sequentially adds trough-type mixture machine stirring, and
Starch slurry is added to stir and evenly mix, softwood is made；
(3) it pelletizes: gained softwood being pelletized according to common process, is dried and whole grain processing, and by after whole grain
Grain is added a selected amount of hard magnesium and mixes；
(4) tabletting: by above-mentioned particle carry out tabletting to get.
The invention also discloses the purposes that the refining dipterex composition is used to prepare metrifonate insecticidal preparation.
The insecticide is helminth insecticide for animals, including endoparasite and vermin, specifically, described
Insecticide is for driving away domestic animal gastrointestinal nematode parasites, pig fasciolopsis, bot, warble, sheep nose fly maggot and tick, mite, flea, lice
Equal helminths.
The insecticidal preparation be it is for oral administration, a secondary amounts be every 1Kg weight, horse 30-50mg, ox 20-40mg, sheep 80-
100mg, goat 50-70mg, pig 80-100mg.
Refining dipterex composition of the present invention, using refining dipterex raw medicine as effective component, expelling parasite principle and enemy
Hundred worms are approximate, in conjunction with the cholinesterase of polypide, inhibit the activity of cholinesterase, accumulate acetylcholine largely, interfere worm
The nervimuscular neuromuscular juinction of body, causes sensitive helminth to be benumbed and dead.And in addition complex enzyme agent and functional additive
Booster action, the anthelminthic effect of trichlorfon technical is further enhanced, either for the infection of faecal egg or internal organ
The desinsection of the infection conditions of helminth, refining dipterex tablet of the present invention can effectively be driven away；Importantly, this
Higher anthelminthic effect can be obtained, effective purge ratio connects under the addition of lower effective dose by inventing the metrifonate tablet
Nearly 100%.
Specific embodiment
Refining dipterex raw medicine of the present invention is the refining dipterex raw medicine powder that the prior art can purchase, can also be according to existing
There is purification technique known to technology to carry out refinement treatment to trichlorfon technical and obtain, such as Chinese patent CN 102234292B public
A kind of metrifonate purifying technique is opened.Refining dipterex raw medicine involved in following embodiments is to implement according to above patent document
Method is made in example 2.
1 refining dipterex tablet of embodiment
Refining dipterex composition described in the present embodiment includes the refining dipterex raw medicine that mass ratio is 100:1.5:3, answers
Synthase agent and functional additive.
The complex enzyme agent is that phytase, beta-lactamase and lysozyme are mixed with the mass ratio of 1:1:1.
The functional additive is that hyaluronic acid, polyglutamic acid and trehalose are mixed with the mass ratio of 1:1:1.
Refining dipterex tablet described in the present embodiment has the following raw material preparation:
The method of the present embodiment preparation refining dipterex tablet, includes the following steps:
(1) it stocks up: the starch slurry for taking a selected amount of starch to add water that about 14wt% is made, it is spare；
(2) softwood: taking a selected amount of refining dipterex raw medicine and calcium monohydrogen phosphate, sequentially adds trough-type mixture machine and stirs 15 points
Clock, and starch slurry (being cooled to 40 DEG C or less) is added and stirs and evenly mixs 10 minutes, softwood is made；
(3) it pelletizes: using oscillating granulator, cross the granulation of 12 meshes, the particle prepared is placed in basin, control
Wet grain thickness is no more than 1.5cm, in 40 DEG C of aeration-dryings；Period, up to 30 minutes stirrings for the first time of temperature, rear every 20 minutes stirrings are once simultaneously
Record；Particle after drying is crossed into 14 mesh sieves, control powder and particle fraction are about 3:7, and V-type is added in whole good particle and is mixed
A selected amount of hard magnesium is added in conjunction machine, is mixed 10 minutes；
(4) tabletting: tablet press machine hopper is added in appropriate above-mentioned particle and carries out tabletting, and checks slice weight, hardness, thickness, collapse
Xie Du, friability and appearance to get.
2 refining dipterex tablet of embodiment
Refining dipterex composition described in the present embodiment includes the refining dipterex raw medicine, compound that mass ratio is 100:3:2
Enzyme agent and functional additive.
The complex enzyme agent is that phytase, beta-lactamase and lysozyme are mixed with the mass ratio of 1:1:1.
The functional additive is that hyaluronic acid, polyglutamic acid and trehalose are mixed with the mass ratio of 1:1:1.
Refining dipterex tablet described in the present embodiment has the following raw material preparation:
The method of the present embodiment preparation refining dipterex tablet is same as Example 1.
3 refining dipterex tablet of embodiment
Refining dipterex composition described in the present embodiment includes the refining dipterex raw medicine that mass ratio is 100:0.5:2, answers
Synthase agent and functional additive.
The complex enzyme agent is that phytase, beta-lactamase and lysozyme are mixed with the mass ratio of 1:1:1.
The functional additive is that hyaluronic acid, polyglutamic acid and trehalose are mixed with the mass ratio of 1:1:1.
Refining dipterex tablet described in the present embodiment has the following raw material preparation:
The method of the present embodiment preparation refining dipterex tablet is same as Example 1.
4 refining dipterex tablet of embodiment
Refining dipterex tablet described in the present embodiment prepare raw material and ratio is same as Example 1, difference be only that,
The refining dipterex composition includes refining dipterex raw medicine, phytase and the polyglutamic acid that mass ratio is 100:1.5:3.
5 refining dipterex tablet of embodiment
Refining dipterex tablet described in the present embodiment prepare raw material and ratio is same as Example 1, difference be only that,
The refining dipterex composition includes that mass ratio is the refining dipterex raw medicine of 100:1.5:3, beta-lactamase and transparent
Matter acid.
6 refining dipterex tablet of embodiment
Refining dipterex tablet described in the present embodiment prepare raw material and ratio is same as Example 1, difference be only that,
The refining dipterex composition includes refining dipterex raw medicine, lysozyme and the trehalose that mass ratio is 100:1.5:3.
Comparative example 1
Refining dipterex tablet described in this comparative example prepare raw material and ratio is same as Example 1, difference be only that,
The refining dipterex composition includes the refining dipterex raw medicine and complex enzyme agent that mass ratio is 100:4.5.
The complex enzyme agent is that phytase, beta-lactamase and lysozyme are mixed with the mass ratio of 1:1:1.
Comparative example 2
Refining dipterex tablet described in this comparative example prepare raw material and ratio is same as Example 1, difference be only that,
The refining dipterex composition includes the refining dipterex raw medicine and functional additive that mass ratio is 100:4.5.
The functional additive is that hyaluronic acid, polyglutamic acid and trehalose are mixed with the mass ratio of 1:1:1.
Experimental example
1.1 material
Obtained refining dipterex tablet in embodiment 1-6 and comparative example 1-2, and be pair with existing refining dipterex raw medicine
As usual.
Experimental animal: to the bi-crossbreeding of 300 5 months ages in days of certain pig farm raising, pig parasitic ovum excrement is carried out
It checks, and does detailed record, selection infects 100 more serious pigs and is randomly divided into 10 groups, every group 10, marks, and carries out
Test.
1.2 methods and result
Test pig Investigation On Parasitic Infections: taking one group of 10 test pig to butcher before test, carries out Fasciola hepatica, silk ribbon
The inspection of worm, gastrointestinal nematode and other parasitic infection amounts.Determine this area's pig main parasitic worm Mean abund ance.
Other 9 groups of experiments are applied into refining dipterex tablet in embodiment 1-6, comparative example 1-2 with pig respectively, and with purification
Trichlorfon technical is control, calculates according to every kg weight administration 100mg preparation of pig, twice daily, takes orally.
The faecal egg inspection of each group test pig, observation infection worm are carried out with McMaster method after administration 7,14,21 days
Ovum reduces situation, and Redution of eggs is calculated by following equation, and experimental result is shown in the following table 1:
1 faecal egg infective dose alimentary canal worm's ovum amount of table reduces situation
Each experimental animal Mean abund ance variation in test front and back: total Test pig send slaughterhouse to be slaughtered after the test
It kills, and collects the inspection that internal organ do Fasciola hepatica, tapeworm, gastrointestinal nematode and other parasitic infection amounts.Before determining test
The situation of change of each group Mean abund ance, deworming rates are calculated by following equation afterwards, and each helminth expelling parasite situation is recorded in
The following table 2:
Each helminth of table 2 tests forward backward averaging infection intensity situation of change (deworming rates %)
| Number | Fasciola hepatica deworming rates/% | Tapeworm deworming rates/% | Gastrointestinal nematode parasites deworming rates/% |
| Embodiment 1 | 99.2% | 99% | 99.5% |
| Embodiment 2 | 99% | 99.1% | 99.2% |
| Embodiment 3 | 99.3% | 99% | 99.1% |
| Embodiment 4 | 97.9% | 98.2% | 98.1% |
| Embodiment 5 | 98.1% | 98.2% | 98.0% |
| Embodiment 6 | 97.9% | 98.1% | 97.9% |
| Comparative example 1 | 71.2% | 70.8% | 70.1% |
| Comparative example 2 | 70.9% | 71.1% | 70.8% |
| Reference examples | 70.3% | 71.3% | 71.2% |
It can be seen that the infection conditions either for the infection of faecal egg or internal organ helminth from upper table data
Desinsection, refining dipterex tablet of the present invention can effectively drive away, and effective purge ratio is close to 100%.In addition, from upper
Table data are it can also be seen that individually the preparation of addition complex enzyme agent or functional additive, anthelminthic effect and exclusive use oppose hundred
The effect of worm raw medicine is suitable, it is contemplated that above-mentioned experiment is the purification enemy hundred of the present invention in the case where identical medicament applied amount
Worm tablet is even more further to improve anthelminthic effect in the case where lower effective dose.
Obviously, the above embodiments are merely examples for clarifying the description, and does not limit the embodiments.It is right
For those of ordinary skill in the art, can also make on the basis of the above description it is other it is various forms of variation or
It changes.There is no necessity and possibility to exhaust all the enbodiments.And it is extended from this it is obvious variation or
It changes still within the protection scope of the invention.
Claims (8)
1. a kind of refining dipterex composition, which is characterized in that by the refining dipterex original that mass ratio is 100:0.5-3:2-5
Medicine, complex enzyme agent and functional additive composition；
The complex enzyme agent is selected from the mixture of one or more of phytase, beta-lactamase or lysozyme；
The functional additive is selected from the mixture of one or more of hyaluronic acid, polyglutamic acid or trehalose.
2. a kind of method for preparing refining dipterex composition described in claim 1, which is characterized in that a selected amount of including taking
The refining dipterex raw medicine, complex enzyme agent and functional additive, and the step of being mixed.
3. as refining dipterex composition described in claim 1 addition customary adjuvant, according to metrifonate made from common process
Preparation.
4. a kind of refining dipterex tablet, which is characterized in that added by refining dipterex composition described in claim 1 conventional
Auxiliary material, according to tablet made from common process.
5. refining dipterex tablet according to claim 4, which is characterized in that the raw material for preparing of the tablet includes:
6. a kind of method for preparing refining dipterex tablet described in claim 5, which comprises the steps of:
(1) it stocks up: a selected amount of starch being taken to add water that starch slurry is made, it is spare；
(2) softwood: taking a selected amount of refining dipterex raw medicine and calcium monohydrogen phosphate, sequentially adds trough-type mixture machine stirring, and be added
Starch slurry stirs and evenly mixs, and softwood is made；
(3) it pelletizes: gained softwood being pelletized according to common process, is dried and whole grain processing, and the particle after whole grain is added
Enter a selected amount of hard magnesium to mix；
(4) tabletting: by above-mentioned particle carry out tabletting to get.
7. the purposes that refining dipterex composition described in claim 1 is used to prepare metrifonate insecticidal preparation or pesticide.
8. purposes according to claim 7, which is characterized in that the insecticide is helminth insecticide for animals.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1220874A (en) * | 1997-10-27 | 1999-06-30 | Ss制药株式会社 | Drug composition with controlled drug release rate |
| CN101934070A (en) * | 2009-07-02 | 2011-01-05 | 天津瑞普生物技术股份有限公司 | Veterinary antibacterial drug composition containing lysozyme and oligosaccharide and application thereof |
| CN104337822A (en) * | 2013-07-25 | 2015-02-11 | 青岛康地恩动物药业有限公司 | Compound tablets containing mebendazole and dipterex and used for deworming on pets, and preparation method thereof |
-
2016
- 2016-12-22 CN CN201611199419.XA patent/CN106665645B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1220874A (en) * | 1997-10-27 | 1999-06-30 | Ss制药株式会社 | Drug composition with controlled drug release rate |
| CN101934070A (en) * | 2009-07-02 | 2011-01-05 | 天津瑞普生物技术股份有限公司 | Veterinary antibacterial drug composition containing lysozyme and oligosaccharide and application thereof |
| CN104337822A (en) * | 2013-07-25 | 2015-02-11 | 青岛康地恩动物药业有限公司 | Compound tablets containing mebendazole and dipterex and used for deworming on pets, and preparation method thereof |
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Address after: 253100 Eastern District, Pingyuan County Economic Development Zone, Dezhou City, Shandong Province Applicant after: Dezhou Jingxin Pharmaceutical Co., Ltd. Address before: 253100 Eastern District, Pingyuan County Economic Development Zone, Dezhou City, Shandong Province Applicant before: Dezhou Jingxin Pharmaceutical Co., Ltd. |
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Denomination of invention: The invention relates to a refined trichlorfon composition and a preparation method and application thereof Effective date of registration: 20210914 Granted publication date: 20190827 Pledgee: Pingyuan County sub branch of Postal Savings Bank of China Ltd. Pledgor: Dezhou Jingxin Pharmaceutical Co.,Ltd. Registration number: Y2021980009326 |