KR100821879B1 - Mosquito repellent composition - Google Patents

Abstract

A mosquito repellent composition is provided to show very high mosquito repellent rate and maintain the duration time for a long time of at least 6 hours. A composition for repelling mosquito comprises 1.5-2.5 wt.% of linalool and an excipient consisting of 0.15-0.20 wt.% of stearic acid, 0.50-0.55 wt.% of propylene glycol, 14.0-15.5 wt.% of ethyl alcohol, 0.1-0.3 wt.% of methyl paraben, and 84-85 wt.% of liquid propane gas. The composition further comprises 0.05-0.5 wt.% of at least one selected from the group consisting of citronella oil, eucalyptus oil, lavender oil, rosemary oil, thyme oil, and cinnamon oil.

Description

Mosquito repellent composition

The present invention relates to a mosquito repellent composition containing linalool as a main component.

Specifically, the present invention relates to a mosquito repellent composition containing linarul as an active ingredient having excellent mosquito repellent activity and sustaining effect.

Mosquitoes are not only blood-sucking humans or animals, but also mediate various diseases such as malaria, encephalitis, yellow fever, and dengue, and are one of the pests that directly or indirectly damage such as disturbing sleep and limiting outdoor activities. About 53 species of mosquitoes are known in Korea. Among them, Anopheles sinensis mediates malaria and Inland Brugian Filariasis, and Aeded togoi in the southwestern region. The red mosquitoes (Culex triaeniorhynchus) spread Japanese encephalitis, and the red mosquitoes (Culex pipiens pallens) and the underground mosquitoes (Culex pipiens molestus), which belong to the mosquitoes, have recently been prevented by bloodsucking problems in apartment complexes Is inevitable.

In order to control such mosquitoes, the control of insecticides obtained by conventional chemical synthesis is mainly used. However, these synthetic chemical insecticides cause side effects such as toxicity to humans or animals and environmental pollution. There has been a need for the development of new control or alternative drugs that can effectively protect humans from mosquitoes with minimal impact (Geroghiou and Saito, 1983; National Research Council, 1986; Brown, 1078).

Under these circumstances, the demand for mosquito repellents that can effectively prevent insect-borne diseases and have less environmental impact has increased. Conventionally known repellents include citronella oil, dimethylphthalate (DMP), etc., but lack repellent activity. Since then, N, N-diethyl-m-toluamide (DEET) with excellent repelling activity has been developed and used throughout pests such as mosquitoes, mosquitoes, flies, teeth, fleas and ticks. However, DEET is a synthetic repellent prepared by reacting m-toluoyl chloride and diethylamine in benzene or ether, but it has an excellent mosquito repellent effect, but it has an unpleasant irritant odor, plastics and synthetics. In addition to damage to rubber, eyeglass frames or watch bands, there is a problem that causes the skin penetration is large, causing brain diseases, cardiovascular toxicity, hypersensitivity. Therefore, pyridostigmine bromide or chloropyrifos in combination with DEET is used to suppress such side effects, but it is difficult to apply to children, patients with hypotension, and those who are sensitive to skin (Hongchun). et al., 1998. Pharmacokinetic, formulation, and safety of insect repellent N, N-diethy-3-methylbenzamide (DEET): a review.J.Am.Mosq.Control Assoc. 14 (1): 12-27)

Therefore, in recent years, research on natural extracts or compounds derived from natural products has been actively conducted. Korean Patent No. 10-0341056 discloses citronella oil, cicalella oil, eucalyptus oil, lavender oil, thyme oil, rosemary oil, rosemary oil or cinnamon oil. selected from the group consisting of p-cymene, α-terpinene, linalool, carvacrol and thymol isolated from cinnamon oil or thyme oil. Mosquito repellents containing one or more compounds are disclosed.

Compounds derived from natural products are known to have mosquito repellent effects.

The patent is proposed by the inventor. However, the mosquito repellents derived from natural products obtained from plants have an excellent effect on the mosquito repellency rate, but the problem is that the duration of the drug is short for about 1 hour, which is not suitable for industrial use.

When comparing the mosquito repellent rate and the duration of the mosquito repellents derived from natural products described in the Republic of Korea Patent No. 10-0341056 as follows.

Table 1 compares the total number of bites and the control for 1 hour of each mosquito repellent and calculated the evasion rate (%). The formula for evasion rate (%) is shown in Equation 1. In addition, the avoidance time was to avoid the mosquito bites three times.

Here, as a mosquito repellent, the control used only 0.1% ethanol, and other mosquito repellents were dissolved in 0.1% ethanol.

TABLE 1

Mosquito repellent Total number of bites Evasion rate (%) Evasion time until 3 bites p-cymen 2.6 ± 0.98 85 59.1 ± 9.22 min α-terpinene 1.7 ± 1.30 90 62.7 ± 10.27 min Linarul 1.9 ± 1.54 89 60.3 ± 11.15 min Kabakrole 1.1 ± 1.23 96 70.0 ± 13.21 min Thymol 1.0 ± 1.43 97 72.1 ± 12.32 min Control 17.2 ± 1.64 - 17.8 ± 1.92 min

※ The control does not use mosquito repellent.

[Equation 1]

 Evasion rate = number of bites in rats treated with 1-extract oil / Control  Number of bites × 100

[Table 2] shows the results of mixing the natural mosquito repellent linarul and the existing synthetic mosquito repellent (DEET) test results in [Table 2] the evasion rate was 86-93%, until the 3 bites Evasion time was about 45-70 minutes.

TABLE 2

Mixing ratio of treated materials Total number of bites Evasion rate (%) Evasion time until 3 bites 1: 0.1 1.1 ± 1.11 93 70.2 ± 3.70mm 1: 0.2 1.2 ± 0.93 91 67.5 ± 11.40mm 1: 0.3 1.8 ± 2.01 88 60.1 ± 8.17mm 1: 0.4 1.9 ± 0.86 86 47.8 ± 9.48 mm

DEET is the most representative drug as a synthetic mosquito repellent. Generally, in order to make a form suitable for use when preparing a prescription drug, it is prepared by adding an excipient to the prescription drug.

Conventionally, as an excipient of DEET, ethyl alcohol is used alone or a mixture of ethyl alcohol, lavender oil, citronella oil, and glycerin is used. To make them spray type, a mixture of liquefied gases such as liquified propane gas is used.

Ethyl alcohol is used as a solvent of DEET, lavender oil or citronella oil is used as a flavoring agent, and glycerin is used as a coating agent (a chemical that maintains adhesion to skin). .

Drugs prepared by using a mosquito repellent derived from natural substances such as linarul using an excipient which is conventionally applied to mosquito repellents have a problem in that it is inconvenient to use as a real mosquito repellent because the duration of the mosquito repellency is short as about 1 hour.

Therefore, in this field, it is necessary to develop a mosquito repellent which lasts a long time while using a mosquito repellent derived from natural materials.

SUMMARY OF THE INVENTION An object of the present invention is to provide a mosquito repellent composition mainly comprising mosquito repellents derived from natural substances such as linarul, which has a duration of about 6 hours while using natural substances as an active ingredient of the mosquito repellent.

The present inventors show that linarul, a mosquito repellent derived from natural substances used in combination with conventional ethanol or DEET, has an excellent effect on the mosquito repellency rate, but there is a problem of short duration and the mosquito repellency effect of the conventionally used mosquito repellents. In view of the fact that a short time of about 1 hour is applied to the skin and high volatility of the repellent is an important factor, the mixture containing stearic acid and methyl paraben is used as an excipient ( Excited mosquito repellent in the form of a composition to confirm that it can extend the repellent duration of about 6 hours without inhibiting the mosquito repellent efficacy of linarul was completed the present invention.

The present invention relates to a mosquito repellent composition containing linarul as a mosquito repellent which can maintain the duration of the drug for at least 6 hours while maintaining the mosquito repellent activity of linarul.

Mosquito repellent composition of the present invention

Stearic acid 0.15 ~ 0.20 wt%

Propylene Glycol 0.50 ~ 0.55 wt%

Ethyl alcohol 14.0 ~ 15.5 wt%

Methylparaben 0.1 ~ 0.3 wt%

Liquefied Propane Gas 84 ~ 85 wt%

The present invention relates to a mosquito repellent composition composed mainly of linarul formed by mixing 1.5 to 2.5 wt% of linarul to a composition excipient. In the present invention, wt% is based on the total amount of excipients.

The purpose of the present invention is a mosquito repellent derived from natural substances as shown in the results of [Table 1] and [Table 2] has a good repellent rate, but the repellent time is shorter to about 1 hour until the 3 times bite repellent 1 There is a disadvantage to spray every hour

The present invention provides a mosquito repellent composition comprising linarul as a main component of which the repelling time is maintained for about 6 hours by changing the components of natural mosquito repellents and adding various excipients other than ethanol to compensate for this drawback.

When the present invention is described in more detail, by using linarul alone as a natural mosquito repellent, or by mixing cilanella oil, eukaryptus oil, lavender oil, rose mario oil or thyme oil with lina rule and mosquito repellent effect Used. As a result, a small amount of linarul and citronella or linarul, citronella, eucarriptus oil, lavender oil, rosemary oil and thyme oil were used, as shown in [Table 4]. The evasion rate was 82-87% and the evasion time was increased to 2-3 hours.

The present invention will be described in detail with reference to the following Examples.

<Production of Excipients>

Example  One

15 g of stearic acid was dissolved in 1425 g of ethyl alcohol, and 50 g of propylene glycol and 10 g of methyl paraben were added thereto and mixed with 8500 g of liquefied propane gas to obtain a mixture (excipient A).

The mixture is composed of 0.15 wt% stearic acid, 14.25 wt% ethanol, 0.5 wt% propylene glycol, 0.1 wt% methyl paraffin and 85 wt% liquefied propane gas. Liquefied propane gas is used here as a prolellant.

<Production of Mosquito Repellent Composition>

Example  2

An excipient was prepared in the same manner as in Example 1, and 100 g of the excipient of Example 1 and 2.0 g of linarul were mixed to obtain 102 g of a mosquito repellent. The mosquito repellent effect test was carried out using the mosquito repellent composition obtained here, and the result is shown in the following [Table 3].

Example  3

An excipient was prepared in the same manner as in Example 1, and 100 g of the excipient was mixed with 2.5 g of linarul and 0.5 g of citronella to obtain 103.0 g of a mosquito repellent. The mosquito repellent effect of the mosquito repellent composition obtained here is shown in the following [Table 3].

Example  4

Excipients are prepared in the same manner as in Example 1, take 100 g of linarul 2.0g, citronella 0.525g, eucalyptus oil 0.035g, lavender oil 0.15g, rose mario oil 0.035g and time oil 0.05g to prepare 102.80g of mosquito repellent Got it. The mosquito repellent effect of the mosquito repellent composition obtained here is shown in the following [Table 3].

Comparative example  One

10 g of ethanol was added to 990 g of water to obtain a solution of 0.1 wt% of ethanol. 100 g of this solution and 2.0 g of linalule were mixed to obtain 102 g of a mosquito repellent.

Comparative example  2

100 g of the excipient of Comparative Example 1, 2.5 g of linarul and 0.5 g of citronella were mixed to obtain 102.5 g of a mosquito repellent.

Comparative example  3

100 g of excipient of Comparative Example 1, 2.0 g of linalul, 0.525 g of citronella, 0.035 g of eucalyptus oil, 0.15 g of lavender oil, 0.035 g of cassia oil and 0.05 g of time oil were mixed to obtain 102.80 g of a mosquito repellent.

<Mosquito avoidance test method>

Larvae of 1000 female red-eared mosquitoes (Culex pipiens pallens Coquillett) were purchased from KFDA (Korea Food and Drug Administration), and the temperature of 27 ± 2 ° C, 75-80% relative humidity, and 8% sugar / water under natural light conditions. Pads were used as experimental materials while subcultured. Of these, 6 to 7 days old female mosquitoes were placed in a wire mesh cut to 30 × 30 × 30 cm, each with 100 mosquitoes. The sugar / water pad was removed from the wire net 12 hours before the experiment. 25 male rats (SKH-1 HRBR Hairless mice, 7 weeks old, 26-38 g, Charles River, Japan) were placed in a cage in a temperature- and humidity-controlled room with five dogs and feed (Samyang Corporation). And water were paid indefinitely. Mice were identified by marking on the tail. Five rats were treated indiscriminately with 0.1wt% of ethanol, DEET agent (Lipperans) and Examples 1-6. Treated mice were transferred to a net containing 100 mosquitoes. The wire mesh was placed 10 cm above the workbench to ensure good air circulation during the test. The number of mosquito bites was recorded every 5 minutes to check the number of bites. The number of bites in three hours and the evacuation time until three bites were measured. All experiments were repeated five times and the average is shown in the following [Table 3] and [Table 4]. Protection rate was calculated according to the following Table 3 and Table 4.

TABLE 3

Number of bites in 3 hours ^** Evasion rate (%) Time to bite 3 times Control 19.2 ± 1.8 - 11.0 ± 3.0 DEET product 4.2 ± 1.0 78.1 124.0 ± 58.0 Example 2 2.6 ± 1.8 86.3 193.1 ± 51.6 Example 3 1.9 ± 0.6 90.0 219.8 ± 67.1 Example 4 1.1 ± 1.0 94.3 342.2 ± 35.0

[Table 4] Mosquito Efficacy

Number of bites in 3 hours ^** Evasion rate (%) Time to bite 3 times Control 18.8 ± 1.2 - 12.0 ± 3.0 DEET product 4.3 ± 1.6 77.1 131.0 ± 16.0 Comparative Example 1 3.4 ± 0.8 82.2 169.1 ± 11.6 Comparative Example 2 2.5 ± 1.2 86.7 171.4 ± 16.1 Comparative Example 3 2.4 ± 1.2 87.2 183.6 ± 16.7

As shown in Table 3, citronella oil, lavender oil, rose mario oil, and thyme oil, which are the essential oil components of mosquito repellent effect, are mixed with linarul 1.5 to 2.5 wt% in the excipient of the present invention alone. And when at least one of cinnamon oil is added to the composition by adding 0.05 ~ 0.5wt% mosquito repellent effect was maintained without change to 86-94% and the duration was increased to about 6 hours.

In order to compensate for the shortage of the repellency or short duration which was a problem in the conventional mosquito repellent, the change of the formulation of the natural mosquito repellent mixture and the excipient is maintained for about 6 hours and the new high repellency rate is very high. The natural mosquito repellent formulation was developed.

The present invention relates to a mosquito repellent composition containing linarul as a mosquito repellent which can maintain the duration of the drug for at least 6 hours while maintaining the mosquito repellent activity of linarul. The mosquito repellent composition of the present invention is a mixture of linalul, linalul and citronella, or a mixture of linalul, citronella, eucalyptus oil, lavender oil, rosemary oil and time oil, and the excipients used to increase the duration The composition is 0.15 to 0.20 wt% of stearic acid, 0.50 to 0.55 wt% of propylene glycol, 14.0 to 15.5 wt% of ethyl alcohol, 0.1 to 0.3 wt% of methylparaben, and 84 to 85 wt% of liquefied propane gas. The present invention relates to a natural mosquito repellent composition prepared by adding 1.5 to 2.5 wt% of linalul.

When the mosquito repellent of the present invention is injected from the hermetically sealed container, stearic acid exhibits a fine particle form in the air.

When the stearic acid content is more than 2.0wt%, clogging of the injection nozzle occurs. Therefore, stearic acid is suitable for 0.15 ~ 0.20wt%, methylparaben is suitable for 0.1 ~ 0.3wt%. Methylparaben is a substance used as a preservative in cosmetics, food, and beverages. In general, the liquefied gas content of the injection-type mosquito repellent is 80 ~ 90wt%. In the case of spray composition, the content of linalule is 2.0 to 3.0wt%.

Stearic acid is a white solid that is insoluble in water. It is a substance which is not used as a liquid excipient. When dissolved in ethyl alcohol it shows a high viscosity plays a role in suppressing the volatility of linarul.

Methyl paraben is a white acicular crystal that is poorly soluble in water but ethyl alcohol is soluble. It is mainly used as a preservative in cosmetics, food and beverages.

Propylene glycol is used as a food additive and has a high moisture absorption point.

The mosquito repellent composition of the present invention is added to linarul and plant essential oils citronella, eukariptus oil, lavender oil, rose mario oil and thyme oil and added as excipients stearic acid, propylene glycol, ethyl alcohol, methyl paraben and liquefied propane As a result of mixing the gas, the repellency rate of the mosquito repellent is very high and has an effect of maintaining the duration for at least 6 hours or longer.

Claims (2)

In the mosquito repellent composition whose main component is linalule, Stearic acid 0.15 ~ 0.20 wt% Propylene Glycol 0.50 ~ 0.55 wt% Ethyl alcohol 14.0 ~ 15.5 wt% Methylparaben 0.1 ~ 0.3 wt% Liquefied Propane Gas 84 ~ 85 wt% A mosquito repellent composition formulated by mixing 1.5 to 2.5 wt% of linalul to an excipient composed of a mixture. In the excipient of claim 1, at least one of Linarul 1.5 to 2.5wt% and at least one of citronella oil, eukaryptus oil, lavender oil, rose mario oil, thyme oil and cinnamon oil as plant essential oils are 0.05 to 0.5 wt%. Mosquito repellent formulated by mixing.