CN117547530A - A kind of flairana insecticidal and odor repellent spray and its preparation method and application - Google Patents
A kind of flairana insecticidal and odor repellent spray and its preparation method and application Download PDFInfo
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- CN117547530A CN117547530A CN202311565322.6A CN202311565322A CN117547530A CN 117547530 A CN117547530 A CN 117547530A CN 202311565322 A CN202311565322 A CN 202311565322A CN 117547530 A CN117547530 A CN 117547530A
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Abstract
本发明提供了一种氟雷拉纳杀虫驱味喷雾剂及其制备方法和应用，所述氟雷拉纳喷雾剂包括氟雷拉纳、有机溶剂、抗氧化剂、透皮剂和驱味剂；所述抗氧化剂包括BHT、BHA和没食子酸丙酯中的一种或多种；所述透皮剂包括碳酸丙烯酯、二乙二醇单乙醚和肉豆蔻酸异丙酯中的一种或多种；所述驱味剂包括芬多精精油、柠檬精油和檀香精油中的一种或多种；有机溶剂较好溶解氟雷拉纳，与抗氧化剂形成良好的溶液稳定性，增加产品保质期；合适的透皮剂能够促进提高药物快速吸收，减少使用量；本发明成分简单安全，促进广泛使用，对环境污染危害大大降低，添加天然提取精油，能够驱赶宠物异味。The invention provides a Freilana insecticidal and odor-repelling spray and its preparation method and application. The Freilana spray includes Freilana, an organic solvent, an antioxidant, a transdermal agent and an odor-repelling agent. ; The antioxidant includes one or more of BHT, BHA and propyl gallate; the transdermal agent includes one or more of propylene carbonate, diethylene glycol monoethyl ether and isopropyl myristate or A variety of; the odor repellent includes one or more of phytoncide essential oil, lemon essential oil and sandalwood essential oil; organic solvents can better dissolve flrellana, form good solution stability with antioxidants, and increase product Shelf life; suitable transdermal agents can promote rapid absorption of drugs and reduce usage; the composition of the invention is simple and safe, promotes widespread use, greatly reduces environmental pollution hazards, and adds naturally extracted essential oils to drive away pet odors.
Description
Technical Field
The invention relates to the technical field of pesticide preparation, in particular to a flularna insecticidal odor-expelling spray and a preparation method and application thereof.
Background
Fluorine Lei Lana (Fluralaner) belongs to isoxazoline pesticides, is applied to agricultural pesticides at the earliest, and is focused and developed into a novel long-acting agent for expelling ectoparasites of pets by researchers at home and abroad in recent years. Has activity on gamma-aminobutyric acid (GABA-) and glutamic acid-gated chlorine channels, has good insect resistance to parasites such as ticks, fleas and mites, and has no obvious toxic influence on mammals. Has the drug generation characteristics of high lipophilicity, easy absorption, medium to high distribution, low clearance rate and long half-life period, has a certain long-acting property, and can absorb, distribute, metabolize and eliminate the difference between species in animal bodies.
Patent application number: CN202210137143.1, name: the invention relates to a fluorine Lei Lana soft chewing composition, a soft chewing tablet, a preparation method and application thereof, which are used for oral external insect expelling of dogs, and the components comprise fluorine Lei Lana, corn starch, soybean protein powder, chicken liver powder, hydroxypropyl cellulose, polyethylene glycol 3350, polyethylene glycol 15 hydroxystearate, glycerol and soybean oil. The fluorine Lei Lana soft chewing composition, in particular to soft chewing tablets, has stable property and wide clinical application, but can not meet the palatability of all dogs, has complex ingredients and higher cost, and can also cause adverse reactions such as vomiting, appetite reduction, flatulence and the like.
Patent application number: cn202310791213.X, name: the invention discloses a fluororanafine composition, which can realize that fluororanafine is prepared into injection, and can supplement iron and improve immunity when being administered, and the composition comprises a glucoheptic anhydride iron solution and fluorine Lei Lana, so that the injection is inconvenient and is unfavorable to use.
Patent application number: 202111631718.7, name of invention: the invention relates to a fluororalston insecticide and a preparation method and application thereof, wherein the fluororalston insecticide comprises fluorine Lei Lana, a cosolvent, a compound diluent and an organic solvent, has good stability and water solubility, is suitable for mass production, but has large use amount of solution, and generates waste liquid after use, thereby causing great environmental pollution.
Patent application number: 202010850355.5, name of invention: the compound fluorine Lei Lana suspension and the preparation and application thereof, wherein each 100ml of the compound fluorine Lei Lana suspension contains 0.5-5g of fluorine Lei Lana, 0.05-2g of praziquantel, 5-30g of tween 80, 2-15ml of ethanol, 10-50g of dimethyl sulfoxide and the balance of water, so that the stability of fluorine Lei Lana after being dissolved in water is effectively solved, the insect repellent spectrum of fluorine Lei Lana is enlarged, but the compound preparation is not applicable to all clients and has the same environmental pollution problem as a solution formulation.
The currently marketed and approved fluororalston products are available from Intel International Inc., and the dosage forms include chewable tablets, drops, and solutions. The products on the market have the series of problems of high selling price, large dosage and the like. Few domestic enterprises master the product preparation technology and are limited to the dosage forms of raw material factories.
Disclosure of Invention
The invention provides a flularna insecticidal odor-expelling spray and a preparation method and application thereof, and aims to solve the problems of the background technology.
The invention is realized in such a way that the fludaruna insecticidal odor-expelling spray comprises fluorine Lei Lana, an organic solvent, an antioxidant, a transdermal agent and an odor-expelling agent; the antioxidant comprises one or more of BHT, BHA and propyl gallate; the transdermal agent comprises one or more of propylene carbonate, diethylene glycol monoethyl ether and isopropyl myristate; the odor-expelling agent comprises one or more of Fendol essential oil, lemon essential oil and sandalwood essential oil.
Preferably, the volume of the fluorine Lei Lana spray is 1L, the fluorine Lei Lana g/L to 25g/L and the antioxidant is 0.1 g/L to 0.5g/L; 25-125g/L of transdermal agent and 50-100g/L of odor-expelling agent, wherein the organic solvent is supplemented to 1L.
Preferably, the organic solvent includes at least one of ethanol, benzyl alcohol and isopropyl alcohol.
Preferably, the fluorine Lei Lana is 0.5-2.5g and the antioxidant is 0.01-0.05g; 2.5-12.5g of transdermal agent and 5-10g of odor-expelling agent, wherein the organic solvent is filled up to 100ml.
Preferably, the fluorine is Lei Lana g, and the antioxidant is 0.03g; 7.5g of transdermal agent and 7.5g of odor-expelling agent, the organic solvent being supplemented to 100ml.
Firstly, transferring a proper amount of organic solvent into a clean glass container, weighing a proper amount of the fluororalston raw material medicine, gradually adding the fluororalston raw material medicine, heating and dissolving the fluororalston raw material medicine in a water bath at 60 ℃, and rapidly and uniformly stirring the fluororalston raw material medicine;
sequentially weighing a proper amount of antioxidant, transdermal agent and odor-removing agent, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
and thirdly, cooling to room temperature, then removing the organic solvent to fix the volume, and performing ultrasonic dissolution to obtain the fluorine Lei Lana insecticidal and odor-expelling spray.
By adopting the scheme, the invention has the beneficial effects that: the organic solvent can better dissolve fluorine Lei Lana, and can form good solution stability with the antioxidant, so that the shelf life of the product can be prolonged; the proper transdermal agent can promote the rapid absorption of the medicine and reduce the usage amount; the invention has simple and safe components, promotes wide use, greatly reduces the environmental pollution hazard, and can expel the peculiar smell of pets by adding the natural essential oil.
Detailed Description
The present invention will be described in further detail with reference to the following examples in order to make the objects, technical solutions and advantages of the present invention more apparent. It should be understood that the specific embodiments described herein are for purposes of illustration only and are not intended to limit the scope of the invention.
The fluorine Lei Lana spray comprises fluorine Lei Lana, an organic solvent, an antioxidant, a transdermal agent and a smell-expelling agent; the antioxidant comprises one or more of BHT, BHA and propyl gallate; the transdermal agent comprises one or more of propylene carbonate, diethylene glycol monoethyl ether and isopropyl myristate; the odor-expelling agent comprises one or more of Fendol essential oil, lemon essential oil and sandalwood essential oil.
Example 1
The spray comprises Lei Lana 0.5.5 g of fluorine, 0.01g of BHT, 2.5g of propylene carbonate, 5g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 0.5.5 g of fluorine, heating in water bath at 60 ℃ for dissolution, and rapidly stirring uniformly;
(2) Weighing 0.01g of BHT, 2.5g of propylene carbonate and 5g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 2
The spray comprises Lei Lana 0.5.5 g of fluorine, 0.01g of BHT, 2.5g of propylene carbonate, 6g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 0.5.5 g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.01g of BHT, 2.5g of propylene carbonate and 6g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 3
The spray comprises Lei Lana 0.5.5 g of fluorine, 0.01g of BHT, 2.5g of propylene carbonate, 7g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 0.5.5 g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.01g of BHT, 2.5g of propylene carbonate and 7g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 4
The spray comprises Lei Lana 0.5.5 g of fluorine, 0.01g of BHT, 2.5g of propylene carbonate, 8g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 0.5.5 g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.01g of BHT, 2.5g of propylene carbonate and 8g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 5
The spray comprises Lei Lana 0.5.5 g of fluorine, 0.01g of BHT, 2.5g of propylene carbonate, 9g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 0.5.5 g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.01g of BHT, 2.5g of propylene carbonate and 9g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 6
The spray comprises Lei Lana 0.5.5 g of fluorine, 0.01g of BHT, 2.5g of propylene carbonate, 10g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 0.5.5 g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.01g of BHT, 2.5g of propylene carbonate and 10g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 7
The spray comprises Lei Lana g of fluorine, 0.03g of BHT, 7.5g of propylene carbonate, 7.5g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.03g of BHT, 7.5g of propylene carbonate and 7.5g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Example 8
The spray comprises Lei Lana 2.5.5 g of fluorine, 0.05g of BHT, 12.5g of propylene carbonate, 10g of fenprox essential oil and 100ml of ethanol.
(1) Transferring a small amount of ethanol, adding Lei Lana 2.5.5 g of fluorine, heating in a water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(2) Weighing 0.05g of BHT, 12.5g of propylene carbonate and 10g of fendol essential oil;
(3) Adding (2) into (1), adding proper amount of ethanol, heating in water bath at 60 ℃ for dissolution, and rapidly and uniformly stirring;
(4) Cooled to room temperature and then fixed to volume of 100ml by ethanol.
Stability test
1. Long-term test
The solutions prepared in examples 1 to 8 of the present invention were left at room temperature for 6 months, sampled and assayed for major content and impurities, and observed for properties.
2. High temperature test
The solutions prepared in examples 1 to 8 of the present invention were left at 40℃for 10 days, and the relevant index was measured on the day, 5 days, and 10 days, respectively:
3. evaluation of drug efficacy
In a rough dog base in Jiujiang city of Jiangxi province, 32 natural infection cases (4 cases per example) are selected for drug effect evaluation. The drug effect evaluation of the invention takes the index of change of the number of ectoparasites in the skin (or ear) and clinical symptoms as judgment standards. The ectoparasite number (and egg number) of each dog was examined in turn, the reduction rate of the parasite (egg) was calculated, and the efficacy of each group was judged according to the following principle:
1. the medicine is effective in that after the medicine is used, the average reduction rate of the ectoparasites (and ova) of the skin (or the ear) is more than 90 percent, and the affected part has no itching, no erythra, no dander or no damage caused by the self biting of test animals.
2. The medicine is ineffective, after the medicine is used, the average reduction rate of the ectoparasites (and insects) on the skin (or ear) is less than 90 percent, and the affected part still has cancer itch, erythra, dander and the like, and the self biting injury of animals is obvious.
| Examples | Effectiveness of the method | Clinical response |
| 1 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 2 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 3 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 4 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 5 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 6 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 7 | Has the following components | Has no obvious itching, erythra and other phenomena |
| 8 | Has the following components | Has no obvious itching, erythra and other phenomena |
From the above examples 1 to 8, it is evident that the effect in example 7 is most remarkable, and the effect in the application of adjuvant treatment of allergic dermatitis caused by fleas is most remarkable in the treatment of fleas and tick infections on canine body surfaces, and the product stability is stronger and the impurities are minimized by the above examples.
The previous description of the embodiments is provided to facilitate a person of ordinary skill in the art in order to make and use the present invention. Various modifications to these embodiments will be readily apparent to those skilled in the art, and the generic principles described herein may be applied to other embodiments without the use of the inventive faculty. Therefore, the present invention is not limited to the above-described embodiments. It will be understood by those skilled in the art that the foregoing and various other changes, modifications and variations can be made in the present invention without departing from the spirit and scope of the invention, and it is intended that the invention is limited only to the preferred embodiments of the invention.
Claims (7)
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104994852A (en) * | 2012-12-18 | 2015-10-21 | 唐纳吉有限公司 | Transdermal parasiticidal formulations |
| CN106806369A (en) * | 2017-01-18 | 2017-06-09 | 佛山市南海东方澳龙制药有限公司 | Pet external application desinsection drops containing natural plant essential oils and its preparation method and application |
| CN111050557A (en) * | 2017-09-06 | 2020-04-21 | 拜耳动物保健有限责任公司 | Topically applicable formulation for controlling and preventing parasites in animals |
| CN115671040A (en) * | 2021-07-21 | 2023-02-03 | 瑞普（天津）生物药业有限公司 | An external preparation for controlling parasitic infection in animals |
| CN117064851A (en) * | 2023-09-20 | 2023-11-17 | 中国农业大学 | Preparation method of isoxazoline anthelmintic preparation |
-
2023
- 2023-11-22 CN CN202311565322.6A patent/CN117547530A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104994852A (en) * | 2012-12-18 | 2015-10-21 | 唐纳吉有限公司 | Transdermal parasiticidal formulations |
| CN106806369A (en) * | 2017-01-18 | 2017-06-09 | 佛山市南海东方澳龙制药有限公司 | Pet external application desinsection drops containing natural plant essential oils and its preparation method and application |
| CN111050557A (en) * | 2017-09-06 | 2020-04-21 | 拜耳动物保健有限责任公司 | Topically applicable formulation for controlling and preventing parasites in animals |
| CN115671040A (en) * | 2021-07-21 | 2023-02-03 | 瑞普（天津）生物药业有限公司 | An external preparation for controlling parasitic infection in animals |
| CN117064851A (en) * | 2023-09-20 | 2023-11-17 | 中国农业大学 | Preparation method of isoxazoline anthelmintic preparation |
Non-Patent Citations (1)
| Title |
|---|
| 刘冠麟, 等.: ""氟雷拉纳在动物寄生虫疾病控制中的应用进展"", 《中国兽药杂志》, vol. 56, no. 09, 20 September 2022 (2022-09-20), pages 58 - 65 * |
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