CN111643419A

CN111643419A - Mosquito-repelling itching-relieving floral water and preparation method thereof

Info

Publication number: CN111643419A
Application number: CN202010676778.XA
Authority: CN
Inventors: 张建广
Original assignee: Shandong Guangyuyuan Environmental Protection Technology Co ltd
Current assignee: Shandong Guangyuyuan Environmental Protection Technology Co ltd
Priority date: 2020-07-14
Filing date: 2020-07-14
Publication date: 2020-09-11
Anticipated expiration: 2040-07-14
Also published as: CN111643419B

Abstract

The invention discloses mosquito-repellent itching-relieving floral water and a preparation method thereof. Specifically, the invention provides a composition, which is an emulsion, and the emulsion comprises: (A) an aqueous phase comprising water and extracts, said extracts being aqueous extracts of chrysanthemum, plantain and bay leaves; (B) an oil phase comprising essential oil of mugwort, palm oil, castor oil, and stearic acid; (C) and the emulsifier comprises sorbitan monooleate and glyceryl monostearate. The composition can effectively prolong the mosquito repelling time, reduce swelling and relieve pain, and effectively treat skin inflammation after biting.

Description

Mosquito-repelling itching-relieving floral water and preparation method thereof

Technical Field

The invention relates to the field of medicine, and particularly relates to floral water and a preparation method thereof.

Background

In summer, mosquito bites not only affect sleep, but also can infect various diseases, thereby bothering people's life. Floral water is the main finished product for repelling mosquitoes in the existing market. The effective component of most of the prior toilet water is anophelifuge ester which has certain toxicity and is not beneficial to health, moreover, the toilet water in the prior market has short action time, needs to be used for many times, can not reach the mosquito repellent effect for a long time, and especially falls asleep at night, because the mosquito repellent time of the toilet water is short, a user is bitten and awakened for many times at night, the sleep quality of the user is seriously influenced, and the sleep quality is reduced. In addition, for the skin bitten by mosquitoes, the existing floral water is difficult to effectively relieve swelling and pain, and is also difficult to effectively treat skin inflammation caused by the mosquito bites, so that the skin injury is caused.

Therefore, there is a need in the art to develop a preparation that can prolong mosquito repelling time, effectively relieve swelling and pain, and effectively treat skin inflammation after stinging.

Disclosure of Invention

The invention aims to provide a composition which can effectively prolong mosquito repelling time, reduce swelling and relieve pain and effectively treat skin inflammation after biting.

In a first aspect of the present invention, there is provided a composition, said composition being an emulsion, said emulsion comprising:

(A) an aqueous phase comprising water and extracts, said extracts being aqueous extracts of chrysanthemum, plantain and bay leaves;

(B) an oil phase comprising essential oil of mugwort, palm oil, castor oil, and stearic acid;

(C) and the emulsifier comprises sorbitan monooleate and glyceryl monostearate.

Preferably, the extract is water extract of mixed medicinal materials of chrysanthemum, plantain herb and laurel leaf.

Preferably, the composition further comprises artemisinin and/or borneol.

Preferably, the oil phase further comprises artemisinin.

Preferably, the artemisinin is 1-3 parts by weight.

Preferably, the aqueous phase further comprises borneol.

Preferably, the borneol is 1-3 parts by weight.

Preferably, the composition is toilet water.

Preferably, the composition is prepared as a floral water.

Preferably, the aqueous phase further comprises a wetting agent.

Preferably, the humectant comprises one or more of glycerol, propylene glycol and polyethylene glycol.

Preferably, the emulsion is a water-in-oil emulsion.

Preferably, the extract is a dry extract.

Preferably, the extract is a water-soluble dry extract.

Preferably, the weight ratio of the chrysanthemum to the plantain to the laurel leaf is (1-5): (3-7): (0.5-4), preferably (2-4): (4-6): (1-3).

Preferably, the weight ratio of the chrysanthemum to the plantain is (1-5): (3-7), preferably (2-4): (4-6).

Preferably, the weight ratio of the chrysanthemum to the laurel leaf is (1-5): (0.5-4), preferably (2-4): (1-3).

Preferably, the weight part of the water is 300-380 parts, preferably 330-350 parts, and preferably 335-345 parts.

Preferably, the weight part of the argyi leaf essential oil is 20-40 parts, preferably 25-35 parts, and more preferably 27-33 parts.

Preferably, the weight portion of the palm oil is 160-240 weight portions, preferably 180-220 weight portions, preferably 190-210 weight portions.

Preferably, the weight part of the castor oil is 150-210 parts, preferably 170-190 parts, preferably 175-195 parts.

Preferably, the stearic acid is 70 to 110 parts by weight, preferably 80 to 100 parts by weight, and preferably 85 to 95 parts by weight.

Preferably, the sorbitan monooleate is used in an amount of 60 to 100 parts by weight, preferably 70 to 90 parts by weight, more preferably 75 to 85 parts by weight.

Preferably, the weight part of the glyceryl monostearate is 10-30, preferably 15-25, preferably 17-23.

Preferably, the weight portion of the extract is 20-60 weight portions, preferably 35-45 weight portions, preferably 37-43 weight portions based on the dry weight of the extract.

Preferably, the humectant (e.g., glycerin) is present in an amount of 10 to 30 parts by weight, preferably 15 to 25 parts by weight, preferably 17 to 23 parts by weight.

Preferably, the unit of parts by weight is grams (g).

Preferably, the extract is prepared by the following method:

mixing flos Chrysanthemi, herba plantaginis and laurel leaf, pulverizing, extracting with water, filtering, concentrating, and drying to obtain the extract.

Preferably, the extract is prepared by the following method:

mixing flos Chrysanthemi, herba plantaginis and laurel leaf, pulverizing, adding 4-6 times of water, extracting at 65-75 deg.C for 8-14 hr, filtering, concentrating the filtrate, and drying to obtain the extract.

Preferably, the drying is concentration drying under reduced pressure.

Preferably, the formulation of said emulsion comprises:

prescription components	Parts by weight
		Folium artemisiae argyi essential oil	20-40
Palm oil	160-240
		Castor oil	150-210
Stearic acid	70-110
		Sorbitan monooleate	60-100
Glyceryl monostearate	10-30
		Extract of plant	20-60
Glycerol	10-30
		Distilled water	300-380；

The extract is a water extract of mixed medicinal materials of chrysanthemum, plantain herb and laurel leaf, wherein the weight ratio of the chrysanthemum to the plantain herb to the laurel leaf is (1-5): (3-7): (0.5-4).

Preferably, the formulation of said emulsion comprises:

the extract is a water extract of mixed medicinal materials of chrysanthemum, plantain herb and laurel leaf, wherein the weight ratio of the chrysanthemum to the plantain herb to the laurel leaf is (2-4): (4-6): (1-3).

Preferably, the formulation of said emulsion comprises:

prescription components	Parts by weight
		Folium artemisiae argyi essential oil	27-33
Palm oil	190-210
		Castor oil	175-195
Stearic acid	85-95
		Artemisinin	1-3
Sorbitan monooleate	75-85
		Glyceryl monostearate	17-23
Extract of plant	37-43
		Glycerol	17-23
Borneol (borneol)	1-3
		Water (W)	335-345；

Preferably, the emulsion has an average particle size of 70-90 nm.

In a second aspect of the invention, there is provided a process for preparing a composition according to the first aspect of the invention, said process comprising the steps of:

(a) mixing the components of the water phase, and mixing at 65-80 ℃ to obtain a water-based phase A;

(b) mixing the components of the oil phase and the emulsifier, and mixing at 65-80 deg.C to obtain oily phase B;

(c) slowly adding the phase A into the phase B under stirring, continuing to stir uniformly for 4-6min, homogenizing for 4-6min at 8000-.

In a third aspect of the invention, there is provided a use of a composition according to the first aspect of the invention for the preparation of a formulation for repelling mosquitoes, reducing swelling, relieving itching and/or resisting inflammation.

Preferably, the inflammation is inflammation of the skin caused by mosquito bites.

Preferably, the anti-inflammatory is by reducing inflammatory factors.

Preferably, the inflammatory factor is IL-1 beta, IL-6 and/or TNF-alpha.

It is to be understood that within the scope of the present invention, the above-described features of the present invention and those specifically described below (e.g., in the examples) may be combined with each other to form new or preferred embodiments.

Detailed Description

The invention develops a composition which is an emulsion, the emulsion comprises a water phase, an oil phase and an emulsifier, the water phase comprises water extracts of chrysanthemum, plantain and bay leaves, the oil phase comprises argy wormwood leaf essential oil, palm oil, castor oil and stearic acid, and the emulsifier comprises sorbitan monooleate and glyceryl monostearate. Experimental research shows that the emulsion composition can effectively prolong mosquito repelling time, relieve swelling and pain, and effectively treat skin inflammation after biting.

Term(s) for

Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.

As used herein, the terms "comprising," including, "and" containing "are used interchangeably and include not only open-ended definitions, but also semi-closed and closed-ended definitions, and include" consisting of … …, "" consisting essentially of … ….

As used herein, sorbitan monooleate is also known as Span 80, Span-80.

As used herein, mugwort leaf is a dried leaf of Artemisia argyi Levl. et Vant.

As used herein, plantain is a dried or fresh whole plant of the Plantago asiatica l.

As used herein, laurel leaf is the leaf of Laurus nobilis l.

Composition and preparation method thereof

The invention provides a composition which can be used for repelling mosquitoes, reducing swelling, relieving itching and/or resisting inflammation. The composition of the invention is preferably floral water.

Typically, the composition is an emulsion comprising:

(C) and the emulsifier comprises sorbitan monooleate and glyceryl monostearate.

In a preferred embodiment of the present invention, the oil phase further comprises artemisinin.

In another preferred embodiment of the present invention, the aqueous phase further comprises borneol.

In another preferred embodiment of the present invention, the aqueous phase further comprises a wetting agent. For example, the humectant may include one or more of glycerin, propylene glycol, and polyethylene glycol.

In the present invention, sorbitan monooleate and glyceryl monostearate are used as water-in-oil emulsifiers, and the emulsion of the present invention is made into a water-in-oil emulsion by emulsification.

In another preferred embodiment of the present invention, the extract is a dried extract.

In the extract of the invention, the weight ratio of the chrysanthemum to the plantain to the laurel leaf is (1-5): (3-7): (0.5-4), preferably (2-4): (4-6): (1-3).

A preferred formulation of the composition of the present invention comprises:

More preferably, the formulation of said emulsion comprises:

prescription components	Parts by weight
		Folium artemisiae argyi essential oil	27-33
Palm oil	190-210
		Castor oil	175-195
Stearic acid	85-95
		Sorbitan monooleate	75-85
Glyceryl monostearate	17-23
		Extract of plant	37-43
Glycerol	17-23
		Water (W)	335-345。。

In another preferred embodiment of the present invention, the extract is prepared by the following method:

The present invention also provides a method for preparing said composition, said method comprising the steps of:

Use of

The invention also provides application of the composition in repelling mosquitoes, diminishing swelling, relieving itching and/or resisting inflammation.

Typically, the inflammation is inflammation of the skin caused by mosquito bites.

The anti-inflammatory agent of the present invention may be an agent that reduces inflammatory factors. The inflammatory factor may be IL-1 beta, IL-6 and/or TNF-alpha.

The main technical effects of the invention comprise:

1. the invention develops the mosquito repellent lotion which is prepared from natural materials, has no side effect, can effectively prolong mosquito repellent time, relieve swelling and pain, and effectively treat skin inflammation after biting.

2. The emulsion composition of the invention can also contain artemisinin and is used for preventing and treating the transmission of malaria.

3. The emulsion composition can also contain borneol, achieves a cooling effect, and can effectively improve the use comfort.

The invention will be further illustrated with reference to the following specific examples. It should be understood that these examples are for illustrative purposes only and are not intended to limit the scope of the present invention.

Example 1

This example prepared an emulsion (which could be used in floral water) as follows:

preparing the folium artemisiae argyi essential oil:

pulverizing folium Artemisiae Argyi, adding deionized water, and distilling with steam to obtain folium Artemisiae Argyi essential oil.

Preparing a water-soluble dry extract:

mixing and crushing 3 parts by weight of chrysanthemum, 5 parts by weight of plantain and 2 parts by weight of bay leaves, adding 5 times of water, extracting at 70 ℃ for 12 hours, filtering, and concentrating and drying the filtrate under reduced pressure to obtain the water-soluble dry extract.

The formulation of the emulsion of this example is shown in table 1:

TABLE 1 formulation composition of the emulsion

The preparation method comprises the following steps:

the preparation method of the emulsion of the embodiment 1 of the invention is the same, and comprises the following steps:

(1) mixing the water-soluble dry extract, glycerol and distilled water, heating to 70 ℃, stirring, mixing and dissolving to obtain a water-based phase A;

(2) mixing folium Artemisiae Argyi essential oil, palm oil, oleum ricini, stearic acid, sorbitan monooleate and glyceryl monostearate, heating to 70 deg.C, stirring, mixing and dissolving to obtain oily phase B;

(3) slowly injecting the aqueous phase A into the oily phase B under stirring, stirring for 5min, homogenizing at 10000 rpm for 5min with a homogenizer, and emulsifying to obtain water-in-oil emulsion.

And (3) particle size performance measurement:

the average particle size of the emulsion measured by a Malvern laser particle sizer is 80.6 +/-10 nm.

Example 2

This example is different from example 1 in that,

preparing a water-soluble dry extract:

mixing and crushing 7 parts by weight of chrysanthemum, 2 parts by weight of plantain and 1 part by weight of bay leaf, adding 5 times of water, extracting at 70 ℃ for 12 hours, filtering, and concentrating and drying the filtrate under reduced pressure to obtain the water-soluble dry extract.

The formulation of the emulsion is shown in table 2:

TABLE 2 formulation composition of the emulsion

Example 3

This example is similar to example 1, except that the formulation of the emulsion is shown in Table 3:

TABLE 3 formulation composition of the emulsion

Example 4

This example is similar to example 1, except that the formulation of the emulsion is shown in table 4:

TABLE 4 formulation composition of the emulsion

Example 5

This example is similar to example 1, except that the formulation of the emulsion is shown in Table 5:

TABLE 5 formulation composition of the emulsion

The preparation method comprises the following steps:

the preparation method of the emulsion (floral water) in the embodiment 1 of the invention is the same, and comprises the following steps:

(1) mixing water soluble dry extract, glycerol, Borneolum Syntheticum and distilled water, heating to 70 deg.C, stirring, mixing and dissolving to obtain aqueous phase A;

(2) mixing folium Artemisiae Argyi essential oil, palm oil, oleum ricini, stearic acid, sorbitan monooleate, glyceryl monostearate and artemisinin, heating to 70 deg.C, stirring, mixing and dissolving to obtain oily phase B;

Effect test

Repelling experiment

Test samples: the emulsion prepared in the embodiment 1-4 of the invention is the Liushen mosquito-repellent toilet water sold in the market;

test insect species and strains: aedes albopictus (Aedesalbopictus), a standard test insect of sensitive strain, a female adult that did not take blood 3-5 days after emergence.

The test method comprises placing 300 female mosquitoes in a mosquito cage of 30cm × 30cm × 40cm, comparing the emulsion prepared in the examples 1-4 with the commercial Liushen mosquito-repellent toilet water, selecting 100 healthy volunteers, before the age of 15-60, half of male and female, and smearing about 0.12ml/cm on the back of the hand of the subject²The emulsion or Liushen mosquito-repellent toilet water is prepared by putting hands into a mosquito cage, exposing for 5min every hour, observing for 6h, recording the number of mosquito bites and calculating the effective protection rate. The test temperature is 27-32 ℃, the humidity is 40-55%, and the light is dark. The average number of bites by an untreated human hand is 30.

The effective protection rate is the number of effective lures/the total number of applied lures multiplied by 100 percent (the effective lures number refers to the number of lures which are not bitten by mosquitoes, and the lures are failed when being bitten by the first mosquito), and the results are shown in table 6:

TABLE 6 effective protection against mosquito bites

Test group	Effective protection rate
		Example 1	100％
Example 2	91.5％
		Example 3	95.7％
Example 4	94.3％
		Liushen mosquito-repellent toilet water	68.8％

As can be seen from table 6, the emulsions prepared in examples 1 to 4 were able to significantly repel the bite of mosquitoes, and particularly the emulsion prepared in example 1 was able to be very effective for the second time repelling the bite of mosquitoes, compared to the commercial toilet water.

Testing mosquito repelling effect time

The test method comprises the following steps: the test was carried out according to the test method of GB/T13917.9-2009 (pesticide registration sanitary insecticide indoor efficacy test and evaluation part 9: repellent), wherein 20 volunteers with qualified offensive power were selected for each group of the repellent test and tested, and the results are shown in Table 7 for each half of men and women.

TABLE 7 mosquito repelling time

As can be seen from table 7, the emulsions prepared in examples 1 to 4 were able to repel mosquitoes for a significantly longer time than commercially available toilet water, and particularly, the emulsions prepared in example 1 were able to repel mosquitoes for as long as 18.6 hours.

Detumescence and itching-relieving test

The test method comprises the following steps: volunteers bitten by mosquitoes were selected, aged 12-56 years, and randomly divided into 5 groups of 30 persons each, namely the emulsion prepared in examples 1-4 and a positive control group (compound menthol ointment, manxileidun (china) pharmaceutical co. After the skin is bitten by mosquitoes, toilet water or ointment is uniformly applied to the red and swollen part of the skin, the application dosage is adjusted according to the size of the swelling, and the number of volunteers taking the effect of the emulsion or the ointment on relieving swelling and itching and the effect of relieving itching within 3min are recorded.

And (3) evaluating the curative effect:

the effect is shown: the symptoms of red swelling, heat, pain and itch of the skin can be quickly relieved;

the method has the following advantages: the symptoms of red swelling, heat, pain and itching of the skin are relieved;

and (4) invalidation: the detumescence and itching relieving effects are not obvious or aggravated.

And (3) test results: see table 8.

TABLE 8 number of people with different therapeutic effects and their ratio

Test group	Display effect (rate)	Effective (rate)	Ineffectiveness (rate)
				Example 1	28(93.3％)	2(6.7％)	0(0％)
Example 2	22(73％)	5(16.7％)	3(10％)
				Example 3	25(83％)	4(13.3％)	1(3.3％)
Example 4	24(80％)	5(16.7％)	1(3.3％)
				Compound menthol ointment	19(63.3％)	9(30％)	3(10％)

As can be seen from table 8, compared with the commercially available compound menthol ointment, the emulsion prepared in examples 1 to 4 can significantly reduce swelling and relieve itching, and particularly, the emulsion prepared in example 1 has very excellent swelling and relieving itching effects.

Anti-inflammatory assay

Test samples: the emulsions prepared in examples 1-4 of the present invention;

The test method comprises the following steps: the four limbs of a BALB/c mouse are fixed on a mouse board, the head of the BALB/c mouse can be shaken, hairs in 2 same areas on two sides of the back of the BALB/c mouse are removed, the skin is exposed, other parts containing the hairs are pasted by using an adhesive tape, the fixed mouse is placed into mosquito cages, one mouse and 50 female mosquitoes (the test temperature is 27-32 ℃, the humidity is 40-55%, the light is dark), after the mouse is bitten for 6 hours, the hairless skin part is visible to be red and swollen, the mouse is taken out and randomly divided into 4 groups, each group comprises 10 mice, and half of the female mosquitoes.

The emulsion prepared in the embodiment 1-4 is respectively smeared on the red and swollen skin on one side of the back of 4 groups of bitten mice, the normal saline is smeared on the red and swollen skin on the other side of the back of the mice as a negative control, the emulsion is smeared on the red and swollen part of the hairless skin of the mice for 2.5h, the emulsion on the two sides of the back of the same mouse and the hairless skin tissue smeared with the emulsion are respectively homogenized, the supernatant tissue is taken after centrifugation, each sample is subjected to protein quantification, and the expression levels of inflammatory factors IL-1 beta (interleukin 1 beta), IL-6 (interleukin 6) and TNF-alpha (tumor necrosis factor alpha) in the skin tissue are detected by an ELISA method (according to the kit operation instruction).

The reduction rate of inflammatory factors in the cream-applied glabrous skin tissue compared to the glabrous skin without cream application (negative control) is shown in table 9:

TABLE 9 reduction ratios (%) of inflammatory factors IL-1. beta., IL-6 and TNF-. alpha.

Test group	IL-1β	IL-6	TNF-α
				Example 1	90.7％	85.1％	87.3％
Example 2	85.2％	72.6％	74.8％
				Example 3	43.5％	37.8％	34.7％
Example 4	36.6％	35.9％	32.9％

Remarking: the reduction rate (%) of inflammatory factors in the same mouse was ═ the (amount of inflammatory factors in hairless skin without cream application-inflammatory factors in hairless skin tissue with cream application)/the amount of inflammatory factors in hairless skin without cream application.

As can be seen from table 9, the emulsions prepared in examples 1 to 4 can significantly treat skin inflammation caused by mosquito bites, and it can be found from the comparison of the data in examples 1, 3 and 4 that palm oil and castor oil as oil phase components can synergistically enhance the therapeutic effect of the emulsions on inflammation.

The above description is only a preferred embodiment of the present application and is not intended to limit the present application, and various modifications and changes may be made by those skilled in the art. Any modification, equivalent replacement, improvement and the like made within the spirit and principle of the present application shall be included in the protection scope of the present application.

Claims

1. A composition characterized in that said composition is an emulsion, said emulsion comprising:

(C) and the emulsifier comprises sorbitan monooleate and glyceryl monostearate.

2. The composition of claim 1, wherein the oil phase further comprises artemisinin; and/or

The water phase also comprises borneol.

3. The composition of claim 1, wherein said composition is formulated as a floral water.

4. The composition of claim 1, wherein said aqueous phase further comprises a wetting agent,

the humectant comprises one or more of glycerol, propylene glycol and polyethylene glycol.

5. The composition of claim 1, wherein the weight ratio of chrysanthemum, plantain and bay leaves is (1-5): (3-7): (0.5-4).

6. The composition of claim 1, wherein said extract is prepared by the following method:

7. The composition of claim 1, wherein the emulsion is formulated by:

8. The composition of claim 1, wherein the emulsion is formulated by:

9. A method of preparing the composition of claim 1, comprising the steps of:

10. Use of a composition according to claim 1 for the preparation of a formulation for repelling mosquitoes, reducing swelling, relieving itching and/or resisting inflammation.