KR101942801B1 - Mosquito repelling composition - Google Patents

Abstract

The present invention relates to a mosquito-repellent composition, which uses fennel oil and rosemary oil together as active ingredients, and as a result of a synergistic effect, the compotiison exhibits excellent mosquito repellent activity and temporal repulsion persistence, and is environmentally friendly and practically harmless to human body, thereby being able to effectively replace DEET, which is a conventional organic synthetic repellent.

Description

[0002] MOSQUITO REPELLING COMPOSITION [0003]

The present invention relates to a mosquito repellent composition, and more particularly, to a mosquito repellent composition which has excellent repellent activity and repellency duration against mosquito which is one of the blood-circulating arthropods, rosemary oil) as a main ingredient, and thus it is environmentally friendly and does not harm human body.

Mosquito is a complete metamorphic insect belonging to the paralyzed mosquito of the insect fauna of the arthropods. It has the life cycle of eggs, larvae, pupa and adults. There are about 3500 species in the world and 56 species in 9 genera.

The female adult of the mosquito obtains proteins necessary for egg maturation from human or animal blood and injects protein anticoagulant during the vomiting process, causing an inflammatory reaction to the foreign invasive substance. In this process, histamine is released and the immune system Mosquitoes are very annoying causing pain to humans and livestock as well as diseases such as dengue hemorrhagic fever, yellow fever, fever, a microcephaly caused by yellow fever, encephalitis, plasmodium, West Nile fever, Chikungunya fever, filariasis, Zika virus, , Which is a very important hygienic insect that mediates a variety of serious diseases, Omgimyeo to the disease, have been reported, especially it killed more than one million people every year by malaria mosquitoes.

Due to the expansion of mosquito habitat due to global warming, an increase in large civil engineering buildings suitable for wintering mosquitoes, and an increase in overseas travelers to Southeast Asia, South America and Africa, an average of 2,200 or more mosquito- In recent years, it has been found that the white mulberry mosquito, which can be a mediator of Zicca virus, dengue fever, and mites, occupies about 10% of the mosquito species in Korea, I have to.

As a means of controlling mosquitoes, it is possible to maintain an ecosystem balance and enduring effect by suppressing or suppressing the propagation by means of hospital microorganisms, genetically engineered microorganisms or radioactive treatments, but it is difficult to maintain and release the mass Biological control with excessive time and expense; The effect is accurate and rapid, it can prevent effective damage in the early stage. It is easy to purchase and well-developed anti-pollution equipment, so it can be used with relatively little effort. However, it has a large side effect on ecosystem and damage caused by rapid recovery of pest density Of recurrent and resistant pests and secondary pest problems; Mechanical control such as capturing or suicide by attracting mosquitoes with traps and then removing them electrically, chemically, and / or mechanically.

Recently, it has been reported that a male mosquito infected with a Wolbachia bacterium that has a mosquito as a host can be used to kill an offspring or change it into a female to prevent propagation by sex disturbance, A method of releasing pre-treated mosquitoes as described above in a small area in a chamber cooled at 4 to 8 ° C; a method of releasing 'OX513A' genetically engineered male mosquitoes by Oxytec UK Method, a method of insecticide using fungi manipulated with a gene for producing a spider toxin, etc., has attracted attention, but in addition to the above-mentioned problems, there is still a problem that it is difficult to secure biological and environmental safety, Is not being attempted.

Thus, among the aforementioned means of controlling mosquito damage, mosquito insecticides, mosquito-inducing agents using traps, and mosquito repellents are currently widely used.

As mosquito insecticides, chemical compounds such as allethrin, trans fluthrin, metho fluthrin, Di-cis or trans allethrin, etc., An aerosol insecticide spraying the insecticidal component in the form of a mist; a liquid electronic mosquito repellent insecticidal component which contains a liquid in which insecticidal components are dissolved in a bottle in which the wick is plugged and heats the core; Mosquito repellent mattresses which are placed on an electric hot plate and volatilized are widely used. However, these mosquito insecticides have a wide range of insecticides and their advantages are rapid, There is a problem that there is a risk of harming the human body, pollution of the surrounding environment, and food contamination.

On the other hand, mosquito attractants are made by replicating potential hosts such as humans or animals, and they can be visual signals such as color, pattern or shape, physical signals such as body heat and moisture of about 35-40 ° C, (octenol), lactic acid, and usually utilizing a chemical signal such as the CO ₂ contained in the body odor or exhalation, such as ammonia, it may also be used rarely visible light or ultraviolet light of a particular wavelength.

The mosquito-attracted traps described above are designed to catch or prevent the attracted mosquitoes from escaping or to kill in a short time, to be strongly sucked into the chamber by a fan or to be surrounded by a tacky sheet or plate, Or it is common to combine these methods appropriately.

However, because mosquito attractants induce mosquitoes by providing a favorable environment for mosquitoes, inevitably mosquito densities within the residential or living environment where the mosquito attractant is located are increased, thereby increasing the frequency or possibility of being affected by mosquitoes There is a problem that there is a concern.

Then, the mosquito repellent agent does not have a mosquito insecticidal effect, but the formulation containing the chemical component avoided by the mosquito is applied or sprayed on the human body or the cloth to prevent the approach of the mosquito to reduce the risk of contact with the mosquito. As a typical example, (DEET), pyramentane-3,8-diol, linarul, pemetrein, indalone, icaridin (Icaridin) or picaridin, dimethyl phthalate, IR3535 (ethyl 3- [acetyl (butyl) amino] propanoate, dimethyl carbate, and ethyl hexanediol. The most widely used products in the past have been DEET (for example, Rifenans for Shinsein Pharm, OFF lotion for SC Johnson, Mikkipa for Henkel, Sof for Sof fell, etc.) and excellent mosquito repellent effect, it can cause delirium caused by vomiting, rash, convulsions and nervous system disturbance due to excessive use due to unpleasant odor and high penetration of the skin. Especially, it can damage plastic frames and synthetic fibers , And mosquitoes with a resistance gene for DEET are also reported to be in an increasing trend.

The above-mentioned chemosynaptic repellents are mostly used for children, pregnant women, hypotensive patients, or people with sensitive skin, and even in the case of icaridine, which is known to be relatively safe, Use is limited for infants or children under 6 years of age.

The mosquito repellent also has the problem of inhalation of human body into aerosol state, contamination of food or clothing, possibility of inflow into human body through the repellent agent in hand, and also environmental pollution problem.

Therefore, although a natural component repellent agent mainly composed of citronella oil, cinnamon, and clove oil, which is not a chemical compound, has been proposed as an effective ingredient of a mosquito repellent agent, Citronella oil contains a methyl-eugenol component The use of unlunged clove oils is a problem of skin damage or burning, and there is a fear of blindness in the case of getting into eyes, Shinamon has a unique scent.

Typical conventional techniques of natural mosquito repellents include the following.

Korean Registered Patent No. 10-0407605 (registered on November 18, 2003) and Korean Patent Application No. 10-0407604 (registered on November 18, 2003), which is a divisional applicant, discloses a methanol extract of Fenniculum vulgare fruit, A hexane fraction of a fruit methanol extract, especially a fungicide or octadecenoic acid, has been proposed. However, the experimental results of Tables 1 to 3 show that the effect is not satisfactory to DEET as a whole.

Also, Korean Patent Registration No. 10-1517479 (registered on Apr. 28, 2014) contains 1-10% by weight of a mixed oil of Clove Oil, Orange Oil and Eucalyptus Oil as an active ingredient However, mosquito repellent effect and escape duration are still unsatisfactory.

Korean Patent Laid-Open Publication No. 10-1999-0034611 (published on Mar. 5, 2001) proposes a natural mosquito repellent containing eucalyptus leaf extract oil, lavender leaf extract oil, rosemary leaf extract oil, or thyme extract oil However, it can be confirmed from the description of Example 3 and Table 1 that the mosquito-repelling effect and the repulsive duration of the rosemary leaf extract oil or other plant extract oils containing it are unsatisfactory.

Korean Patent Registration No. 10-0407605 (registered on November 18, 2003) Korean Patent Registration No. 10-0407604 (registered on November 18, 2003) Korean Registered Patent No. 10-1517479 (registered on Apr. 28, 2014) Korean Patent Publication No. 10-1999-0034611 (published on Mar. 5, 2001)

The first object of the present invention is to provide a mosquito repellent composition which exhibits excellent mosquito repellent activity as well as temporal repellency as synergy effect of the combination of fennel oil and rosemary oil.

A second object of the present invention is to provide a safer mosquito-repellent composition that is environmentally friendly and practically harmless to human beings and can effectively replace DEET, which is a conventional organic synthetic detergent.

The first and second object of the present invention is to provide a lubricating oil composition comprising 1 to 5% by weight, preferably 2 to 4% by weight, especially 3% by weight, of fennel oil; 1 to 4% by weight, preferably 1 to 3% by weight, in particular 2% by weight, of rosemary oil; 8 to 12% by weight of ethanol as an excipient; 5 to 9% by weight of a nonionic surfactant; Purified water is composed of the remainder: the above-mentioned fenel oil and rosemary oil can be smoothly achieved by the liquid mosquito-repellent composition which is an essential oil by the steam distillation method.

Optionally, the mosquito-repelling composition may further comprise from 0 to 2% by weight, in particular 1% by weight, of vanillin oil.

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The nonionic surfactant may be Tween 80.

The mosquito-repellent composition according to the present invention exhibits excellent mosquito repellent activity and long-term perspiration persistence as a synergistic effect due to the combined use of Fenel oil and rosemary oil, while being environmentally friendly and practically harmless to human body, Can be effectively replaced.

Figure 1 is a schematic view of a red house mosquito ( Culexpipiens (%) and a complete protection time (CPT) for the repellent activity of the Example 2 against paracetamol , pallens .
Figure 2 is a schematic view of a red house mosquito ( Culexpipiens (%) and avoidance effect duration time of DEET for P. pallens .
Fig. 3 is a graph showing the repelling activity of Example 2 against Aedes albopictus as a percentage of avoidance and duration of avoiding effect.
FIG. 4 is a graph showing the repellent activity of DEET against Aedes albopictus in terms of the avoidance rate (%) and the duration of the avoidance effect.

Hereinafter, the present invention will be described in detail.

First, the mosquito-repellent composition according to the present invention comprises a fennel oil and a rosemary oil as mosquito-repellent active ingredients, and may optionally further include a vanillin oil as a disabling aid.

Fennel (fennel: Foeniculum vulgare) is fennel obtained by evaporation of the unique and the flavor is known to have the stomach, anthelmintic, antispasmodic action, antibacterial action, diuretic action, excretory action and geodam effect in one shot, fennel fruit as a perennial plant of the mountain-shaped reconciled acid type Oils are used in fragrance aroma therapy.

Rosmarinus officinalis ) is a plant of the family Lamiaceae, and dried leaves and fresh leaves have been mainly used as a seasoning. In private medicine, they have been used as tonic and ointment. Directional oils have also been used in soaps and shampoos.

Vanilla fragrans Ames, which can be used as a disabling adjuvant in the present invention, is widely used as a spice, a perfume, a fragrance additive and the like as a component of about 3% or more in plants of an orchid tree orchid.

The above-mentioned natural oil as the mosquito repellent active ingredient used in the present invention can be extracted and used in the form of essential oil by a conventional steam distillation method or a pressing method, or can be used by purchasing a commercially available essential oil.

The content of the fennel oil used in the mosquito repellent composition according to the present invention is 1 to 5% by weight, preferably 2 to 4% by weight, particularly 3% by weight based on the total weight of the composition, There is a fear that the mosquito repellent effect can not be obtained. Conversely, if it exceeds 5 wt%, economical efficiency may not be secured.

In the mosquito-repellent composition according to the present invention, the content of rosemary oil, which is used together with the above-described Fenel oil to exhibit synergistic effects of mosquito repellency, is 1 to 4% by weight, preferably 1 to 3% If the amount is less than 1% by weight, the synergistic effect of preventing mosquitoes may become insufficient, which is undesirable. Conversely, even if the amount exceeds 4% by weight, synergistic effects can not be expected, It is also undesirable.

Meanwhile, the vanillin oil which can be used as an unwanted auxiliary agent in the mosquito-repellent composition according to the present invention is capable of controlling the volatilization power of the fenel oil and the rosemary oil during the application such as spraying of the mosquito repellent composition, And can be contained in an amount of 0 to 2% by weight, specifically 1% by weight based on the total weight of the composition, and even if it is more than 2% by weight, it is difficult to expect a sufficient effect as well as economically undesirable.

In addition, the mosquito-repellent composition according to the present invention is formulated into a liquid form, and in addition to the above-mentioned oil components, excipients, nonionic surfactants and purified water are included.

Specifically, 8 to 12% by weight of the excipient and 5 to 9% by weight of the nonionic surfactant are based on the total weight of the composition, and the purified water is the balance (balance).

In the mosquito-repellent composition of the present invention, the above-mentioned excipient is preferably ethanol in terms of ease of use and effect, and the kind of the nonionic surfactant is not particularly limited, but usually Tween 80 can be used.

The mosquito repellent composition according to the present invention may be used as a liquid formulation as described above, but it is not limited thereto. If necessary, a suitable diluent or excipient may be added according to various parameters such as purpose of use, environment, But it is also within the scope of the present invention.

If necessary, it may also contain an inert filler gas for spraying, a wetting agent, or various other types of nonionic surfactants, preservatives, phase stabilizers, saline, and the like.

The above-described mosquito-repelling composition according to the present invention may be formulated into a suitable form taking into consideration the purpose of use, use, or use, and may be, for example, a liquid preparation, an aerosol preparation, a spray, an ointment, A liquid preparation, an aerosol preparation, a spray, an emulsion, a lotion, a suspension and the like may be preferable from the viewpoint of ease of use of the mosquito repellent composition and development of sustainable effect.

Hereinafter, the present invention will be described in more detail with reference to Examples, Comparative Examples and Test Examples, but the present invention is not limited thereto.

Example 1

3% by weight of fennel oil commercially available from Berje, Bloomfield, NJ and 2% by weight of rosemary oil were dissolved in 10% by weight of ethanol, and purified water and a nonionic surfactant Tween 80 were added in small amounts A mosquito repellent composition having a purified water content of 78% by weight and a nonionic surfactant of 7% by weight was prepared.

Example 2

A mosquito repellent composition was prepared by the same procedure and with the exception that 1% by weight vanillin oil was added and the purified water content was 77% by weight in Example 1.

Comparative Example 1

Instead of using 3 wt.% Of fenel oil and 2 wt.% Of rosemary oil in Example 1, a commercially available DEET 7% solution from Sigma-Aldrich (MO) was used by the same procedure and method, This was regarded as Comparative Example 2.

Comparative Examples 2 to 4

In Example 2, only 3 wt% of Fenner oil alone was used instead of 3 wt% of Fenner oil, 2 wt% of rosemary oil, and 1 wt% of vanillin oil. In Comparative Example 2, only 2 wt% of rosemary oil was used alone , Comparative Example 3, and only 1% by weight of vanillin oil were used alone.

Test example:

Based on the guideline for evaluating mosquito repellent efficacy (Food and Drug Administration Notice), the repellent activity test in the room was evaluated by the mosquito repellency rate and the mosquito repellency duration (Complete Protection Time, CPT) During the test, perfume and other repellent were not used, and no smoking was allowed 12 hours before the test and during the test.

1. Selection and preparation of test mosquito

Culexpipiens pallens group and Aedes albopictus group were used in Korea.

Two species of mosquitoes were used as insecticides in the insecticides of physiologically active natural products / medicinal entomology research at Seoul National University.

The larvae were fed with the sedimentation water settled in a plastic tray (30 cm x 50 cm x 10 cm) for 2-3 days, and the recovered larvae were put into water and fed larvae. The larvae fed artificial diet (fry feed + dried yeast (1: 1)) were mixed and supplied. The temperature condition of the breeding room was maintained at 27 ± 2 ℃ and the relative humidity was maintained at 80 ± 10%. Light condition was maintained at 12h: 12h intervals.

Breeding of adult mosquitoes was carried out in an insect breeding box (45cm x 45cm x 45cm) and 10% sugar water was fed with food. Animal blood was supplied to artificial blood supply device for the induction of mosquito adults and eggs were recovered.

2. Investigation of repayment duration (CPT)

The used calli were from the same age group on the 5th to 7th day of adulthood.

250 test female mosquitoes that did not acquire blood (Test mosquitoes were fed 5 times for 5 tests with a sugar solution instead of blood and starved for 12 hours or more before use) in a test cage, The kennels were prepared and one was used to test Example 1 and the other four were used to test controls and positive controls.

During the test, the subject's hands were protected by wearing gloves of mosquito-resistant material, and the subject's arms were kept from moving. The mosquito repellent was sprayed with 1 mL (6 times spray) per about 600 cm 2.

Ethanol was treated in both arms before the start of the test, and the dried arm was placed in a killing area for 3 minutes as a negative control. Then, 7% of N, N-diethyl-3-methylbenzamide (Comparative Example 2) DEET) and the mosquito repellents of Example 1 and Comparative Examples 2 to 4 were applied to the same arms in the same arms, and after 60 minutes, they were placed in the test field for 3 minutes to measure the landing and blood-sucking activity of the mosquito. This was carried out 8 times at 60-minute intervals for a total of 8 hours. When the control group, ethanol-only arm, was placed in the breeding ground for 30 seconds, when the number of mosquitoes landed or vomited was not more than 10 (times), the test strips were used again for the experiment. All the tests were repeated three times for each repellent.

3. Calculate the avoidance effect percentage

Repellent Ratio was the ratio of the number of mosquitoes landed or vomited (T) to the arm treated with the repellant compared to the number of mosquitoes landed or vomited (C) in the control arm of each subject.

Repellent Ratio = ((C-T) / C) X 100

(T: average number of mosquitoes collected from subjects who have been treated with repellents within the test time, C: average number of mosquitoes collected from negative or positive control subjects at the same time)

4. Results

4-1. The avoidance rate of the repellents of Example 1 and Comparative Examples 1 to 4

In order to confirm the cumulative synergistic effect of 3% by weight of the penne oil of Example 1 and 2% by weight of the rosemary oil, Comparative Example 1 of 7% DEET, Comparative Example 2 of only 3% by weight of the penne oil alone, Comparative Example 3 in which only 2% by weight was used alone, and Comparative Example 4 in which only 1% by weight of vanillin oil alone were used, was evaluated. The results are shown in Table 1 below.

Average Avoidance Rate (%) Avoidance rate (%) 1h 2h 3h 4h Example 1 100 100 100 100 Comparative Example 1 100 100 100 100 Comparative Example 2 81 64 52 43 Comparative Example 3 74 55 48 41.6 Comparative Example 4 15 10 8 2

The results shown in Table 1 show that the mosquito-repellent composition of Example 1 in which 3% by weight of fennel oil and 2% by weight of rosemary oil are used as mosquito repellent agents is superior to the case of using only fennel oil or rosemary oil by an unexpected synergy effect Indicating that it exhibits remarkably superior mosquito repellent activity.

4-2. Red house mosquito ( Culexpipiens < / RTI > pallens )

The same amount of the mosquito repellent of Comparative Example 1 using 7% DEET as the positive control group and the same amount of the same amount of the mosquito repellent of Example 1 were measured and the number of mosquitoes landed and blood-sucking times were measured for 8 times in 60- Respectively.

The repellency effect duration (CPT) of Comparative Example 1 using the positive control group 7% DEET was found to be 4 hours, while the repelling effect duration of Example 1 was found to be 6 hours and the repellency effect percentage was 8 And maintained more than 85% until after the time (see Table 2 and Figs. 1 and 2).

In conclusion, although the mosquito-resistant composition of Example 1 had a lower concentration of active ingredient than the concentration of DEET in Comparative Example 1, which is a positive control, the avoidance effect of Example 1 is significantly superior to that of Comparative Example 1 Proved.

Red house mosquito ( Culexpipiens < / RTI > pallens ) Processing time Number of landing and vomiting Percentage of avoided effect ± average error (%) Subject 1 Subject 2 Subject 3 Test Products 7% DEET Test Products 7% DEET Test Products 7% DEET Test Products 7% DEET 1 hours 0 0 0 0 0 0 100 100 2 hours 0 0 0 0 0 0 100 100 3 hours 0 0 0 0 0 0 100 100 4 hours 0 One 0 2 0 0 100 97.5 ± 2.5 5 hours 0 3 0 3 0 2 100 90.0 ± 2.5 6 hours 0 4 One 5 0 6 98.3 ± 1.7 83.3 ± 1.7 7 hours One 6 One 6 One 7 96.7 ± 1.3 77.5 ± 2.5 8 hours 4 8 3 8 2 7 85.0 ± 2.9 73.3 ± 1.7

4-3. Repellent activity against Aedes albopictus

The same amount of the mosquito repellent of Comparative Example 1 using 7% DEET as the positive control group and the same amount of the same amount of the mosquito repellent of Example 1 were measured, and the number of mosquitoes landed and blood-sucking times were measured at 8- Respectively.

The CPT of Comparative Example 1 using the 7% DEET positive control group was confirmed to be 4 hours, while the repelling effect duration of Example 1 was found to be 5 hours, and the repelling effect percentage was 6 hours (Fig. 3 and Fig. 3 and Fig. 4).

In conclusion, although the mosquito-resistant composition of Example 1 had a lower concentration of active ingredient than the DEET of Comparative Example 1, which is a positive control, the avoidance effect of Example 1 is better than that of Comparative Example 1 Proved.

Repellent activity against Aedes albopictus Processing time Number of landing and vomiting Avoidance rate Mean ± mean error Subject 1 Subject 2 Subject 3 Test Products 7% DEET Test Products 7% DEET Test Products 7% DEET Test Products 7% DEET 1 hours 0 0 0 0 0 0 100 100 2 hours 0 0 0 0 0 0 100 100 3 hours 0 0 0 0 0 0 100 100 4 hours 0 One One One 0 2 98.3 ± 1.7 93.3 ± 1.3 5 hours 3 3 2 3 2 4 90.0 ± 2.5 90.0 ± 2.5 6 hours 5 6 6 5 4 6 83.3 ± 1.7 81.3 ± 1.7 7 hours 6 9 6 8 5 8 80.0 ± 2.5 73.3 ± 1.7 8 hours 8 10 10 9 9 9 75.0 ± 2.5 70.0 ± 2.5

4-4. conclusion

The duration of the avoidance effect in Example 1 was 6 hours and the duration of the avoidance effect was 5 hours in the red house mosquito and the duration of the avoidance effect in Comparative Example 1 as the positive control was the red house mosquito All of the forest mosquitoes were confirmed as 4 hours.

As a result, it was confirmed that the mosquito-resistant composition of Example 1, which used the fenel oil and the rosemary oil as an effective ingredient, exhibited a better mosquito repellent activity even at a lower concentration in the positive control group 1 due to the remarkable synergistic effect I could.

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Claims (5)

2 to 4% by weight of fennel oil, 1 to 3% by weight of rosemary oil, 8 to 12% by weight of ethanol as an excipient, 5 to 9% by weight of a nonionic surfactant, ;
Wherein the above-mentioned fenel oil and rosemary oil are essential oils by the steam distillation method. The liquid mosquito-repellent composition according to claim 1, further comprising 1% by weight of vanillin oil. delete delete The liquid composition according to claim 1, wherein the nonionic surfactant is Tween 80.

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