WO2006006283A1

WO2006006283A1 - Composition for nasal cavity

Info

Publication number: WO2006006283A1
Application number: PCT/JP2005/006391
Authority: WO
Inventors: Toshihiko Tsuda
Original assignee: Kobayashi Pharmaceutical Co., Ltd.
Priority date: 2004-09-30
Filing date: 2005-03-31
Publication date: 2006-01-19
Also published as: JP2006104076A

Abstract

[PROBLEMS] To provide a composition for the nasal cavity which can effectively mitigate unpleasant nasal symptoms such as nasal occlusion, sneezing, and itching, is highly safe, and has a lasting effect. [MEANS FOR SOLVING PROBLEMS] A distilled water obtained by the steam distillation of lavender is used to prepare a composition for the nasal cavity.

Description

Specification

Nasal composition

Technical field

[0001] The present invention relates to a composition for nasal cavity. More specifically, the present invention relates to a composition for nasal cavity that improves nasal discomfort such as nasal congestion, sneezing and sneezing.

Background art

[0002] When allergens such as bacteria, viruses and pollen adhere to the nasal mucosa, chemical substances such as histamine are released from the mucosal tissue, and the blood flow in the nasal mucosa increases dramatically. This causes the nasal mucosa to become congested and swollen, and a large amount of mucus is secreted, narrowing and clogging the nasal cavity. This results in nasal discomfort such as stuffy nose, sneezing and itching.

[0003] To date, the use of various drugs such as anti-inflammatory drugs and antihistamines has been proposed as means for improving nasal discomfort. However, these conventional drugs are safe and effective.

However, what satisfies all the points of sustainability and feeling of use can satisfy the demands of users and users, and it is the current situation.

[0004] Conventionally, plant-derived essential oil components such as lavender have been found to have the effect of improving nasal discomfort due to allergies, etc., and have been volatilized as a method using the action of this essential oil. A method of improving nasal discomfort by aspirating the essential oil component into the nasal cavity has been proposed (see, for example, Patent Document 1). However, in such a method, since the essential oil component is used in a volatilized state, not only a sufficient discomfort improvement effect cannot be obtained, but it also takes time to manifest the effect and has a drawback in terms of immediate effect.

[0005] By the way, the water-soluble fraction (steam-distilled water) obtained by steam-distilling lavender is not known for its characteristics and effective use, and the steam-distilled water is a nasal discomfort. What kind of influence it will have on you?

Patent Document 1: Special Table 2004-513875

Disclosure of the invention

Problems to be solved by the invention

[0006] Accordingly, an object of the present invention is to solve the above-described problems of the prior art. That is, this departure Ming aims to provide a composition for nasal cavity that can effectively improve nasal discomfort such as nasal congestion, sneezing, and itchiness, and has a long-lasting safety effect.

Means for solving the problem

[0007] The present inventors diligently studied to solve the above problems, and as a result, steam distilled water obtained by steam distillation of lavender has an action of suppressing histamine release, nasal congestion, It has been found that nasal discomfort such as sneezing and itchiness can be effectively improved, and that the discomfort improvement effect is persistent. The present invention has been developed based on further research and further studies.

That is, the present invention provides the following inventions:

Item 1. A nasal composition containing lavender steam distilled water.

Item 2. The composition for nasal cavity according to Item 1, wherein the lavender steam-distilled water is obtained from the above-ground part or whole plant power of lavender.

Item 3. The nasal composition according to Item 1 or 2, wherein the lavender is Okamurasaki or an improved variety thereof.

[0009] The present invention is described in detail below. The composition for nasal cavity of the present invention is characterized by containing lavender steam-distilled water.

[0010] Lavender is a plant species belonging to the family Labiatae and Lavandula, and is an authentic lavender (scientific name; Lavandula).

L. officinalis ^ vera), Sno 《Icraventer (scientific name; L.spica), Stokes (scientific name; L.stoechas), Labandin (scientific name; L.hybrida) And so on. In the present invention, the type of lavender to be used is not particularly limited. Particularly preferred examples include various varieties such as Okamurasaki, Hanamoiwa, dark purple early bloom, and Yodei, and more preferred are Okamurasaki or improved varieties thereof, particularly those produced in Hokkaido, Japan. The lavender may be a wild species or a cultivated species.

[0011] As a raw material of lavender steam-distilled water, lavender flowers, spikes, fruits, pericarp, stems, leaves, branches, branches and leaves, stems, crusts, rhizomes, root barks, seeds, either alone or in combination You can also use lavender whole plants. Preferably above ground (excluding root (Whole plant) or whole plant.

[0012] The steam distilled water of lavender is a distilled liquid collected by steam distillation using 0.6 to 2 parts by weight, preferably 0.8 to 1 part by weight of water with respect to 1 part by weight of lavender. It is prepared by recovering the aqueous phase. The method for steam distillation is not particularly limited, but a pressurized steam distillation method is preferable.

[0013] The composition for nasal cavity of the present invention may be lavender steam distilled water alone, but contains other components such as a pharmaceutically acceptable base material additive. It's good. The blending ratio of lavender steam distilled water in the composition for nasal cavity of the present invention may be appropriately set according to the purpose of use, the degree of symptoms, the form of the composition, etc., but as an example, the composition The ratio of the lavender steam distilled water is 0.01 to: LOO wt%, preferably 0.1 to L00 wt%, more preferably 1 to L00 wt% with respect to the total amount.

[0014] The shape of the composition for nasal cavity of the present invention is appropriately adjusted according to the usage form. Examples of the shape of the composition for nasal cavity include liquid, ointment, sol and the like. Of these, liquid is preferred.

[0015] Other components that can be blended in the nasal composition of the present invention include, for example, ethanol, alcohol such as methanol, water, base material components such as ointment base material, and surfactant, buffer, pH Examples thereof include additives such as regulators, isotonic agents, thickeners, dyes, preservatives, preservatives, anti-inflammatory agents, antibacterial agents, vasoconstrictors, steroids and the like.

[0016] The nasal composition of the present invention is employed in general nasal compositions as long as the pH and osmotic pressure do not impede the effects of the present invention. Should be set as appropriate.

[0017] The use of the composition for nasal cavity of the present invention is not particularly limited as long as it is applied directly into the nasal cavity. Can be used.

[0018] The daily dose of the nasal composition of the present invention includes the shape of the composition, the concentration of lavender steam distilled water, the age and sex of the user, the shape of the composition, the method of administration, It can be set as appropriate according to the expected degree. The nasal composition of the present invention is It is usually administered by spraying, applying, dripping or flowing into the nasal cavity one to several times at a suitable dose.

[0019] As shown in the following test examples, the composition for nasal cavity of the present invention has an action of suppressing the release of histamine and an effect of suppressing the growth of various bacteria in the nasal cavity. It can also be used as a composition for inhibiting histamine release or an antibacterial composition for the nasal cavity.

The invention's effect

[0020] The composition for nasal cavity of the present invention is excellent in the effect of improving nasal discomfort such as nasal congestion, sneezing and itchiness. In addition, the composition for nasal cavity of the present invention can remain in the nasal mucosa for a long time and is excellent in sustainability of the effect, so that discomfort can be improved over a long period of time. In particular, the effect of the present invention is excellent when using steam distilled water that can obtain the above-ground part of lavender or the total plant power.

In addition, the composition for nasal cavity of the present invention can be used as a preventive or therapeutic agent for inflammation in the nasal cavity because it stays in the nasal mucosa for a long time and can prevent the propagation of bacteria and suppress the occurrence of inflammation. It is.

[0022] Furthermore, the composition for nasal cavity of the present invention releases a pleasant aroma that has a restful and sedative effect on human beings, so that a relaxing effect can be enjoyed and a good feeling of use can be obtained. In addition, such an effect can enhance the user's or user's sense of use.

[0023] The composition for nasal cavity of the present invention uses lavender steam distilled water, which is a naturally derived component, and has extremely low irritation to nasal mucosa and high safety.

Brief Description of Drawings

FIG. 1 is a diagram showing the results (chromatograph) of lavender steam distilled water obtained in Example 1 analyzed by gas chromatography.

FIG. 2 is a diagram showing the results (chromatograph) of lavender essential oil analyzed by gas chromatography.

BEST MODE FOR CARRYING OUT THE INVENTION

Hereinafter, the present invention will be described with reference to examples and test examples. However, the present invention is not limited to these examples. It is not limited to.

Example 1

About 60 kg of lavender (Okamurasaki) above ground (whole plant excluding roots) was subjected to pressurized steam distillation using about 50 kg of water to produce a distillate containing 36 kg of water phase and 0.36 kg of oil phase. The aqueous phase was recovered from the distillate to obtain lavender steam distilled water.

[0026] Test Example 1 Evaluation of irritation

The lavender steam distilled water obtained in Example 1 was evaluated for irritation to the nasal mucosa by the following method.

[0027] With 6 adult males (3 healthy subjects and 3 hay fever patients) as subjects, 20 g of lavender steam distilled water obtained in Example 1 was allowed to flow into the nasal cavity and then discharged. (Test Example 1). After administration, irritation was evaluated according to the following criteria. For comparison, purified water (manufactured by Otsuka Pharmaceutical Co., Ltd.) (Comparative Test Example 1-1) instead of lavender steam distilled water; physiological saline (manufactured by Otsuka Pharmaceutical Co., Ltd.) (Comparative Test Example 1-2) Lavender essential oil-containing solution (lavender essential oil 1% by weight, surfactant 5% by weight, balance water) (Comparative Test Example 1-3); or lavender essential oil-containing solution (lavender essential oil 1% by weight, surfactant 5% by weight) The test was conducted in the same manner as described above using Comparative Example 1-4).

(Score)

0: No unpleasant irritation

1: Somehow, there is no unpleasant irritation

2: I can say neither

3: Somewhat unpleasant stimulus

4: Uncomfortable irritation.

[0028] Table 1 shows the obtained results. In Test Example 1, it was confirmed that an unpleasant stimulus was shown, but in Comparative Test Examples 1-1, 1-3, and 1-4, an unpleasant stimulus was observed. Further, the unpleasant irritation disappeared in about 15 minutes after administration in Comparative Test Example 1-1, but in Comparative Test Examples 3 and 1-4, unpleasant irritation remained even 60 minutes after administration. On the other hand, in Comparative Example 2 Irritated and irritated by hay fever patients.

[0029] [Table 1]

In the table, each numerical value shows the average value of the score. Test Example 2 Evaluation test of nasal discomfort improvement effect

The lavender steam distilled water obtained in Example 1 was evaluated for the effect of improving nasal discomfort by the following method.

[0030] 5 adult males suffering from hay fever! Were administered by letting 20g of lavender steam-distilled water obtained in Example 1 flow into the nasal cavity and then draining it. (Test Example 2). After administration, the degree of improvement in discomfort (nasal congestion and nasal itchiness) was evaluated according to the following criteria. The evaluation was performed immediately after administration, 5 minutes, 10 minutes, 30 minutes, 1, 2, 4 and 12 hours. In addition, the ability to reduce stress (irritability), which also causes nasal discomfort, was evaluated according to the following criteria. The evaluation was performed immediately after administration, 2 and 4 hours later. For comparison, instead of lavender steam distilled water, physiological saline (manufactured by Otsuka Pharmaceutical Co., Ltd.) (Comparative Test Example 2-1) or lavender essential oil-containing solution (lavender essential oil 1% by weight, surfactant 5% by weight) %, Remaining water) (Comparative Test Example 2-2).

(Score)

4: Improved

3: Improved rather

2: I can say neither

1: Somehow!

0: Not improved

1: Slightly worse —2: Deteriorated

(Score)

2: Reduced stress

1: Rather, stress was reduced

0: Neither

-1: Somehow, the stress increased.

2: Stress increased.

[0031] The results obtained are shown in Tables 2 and 3. As shown in Table 2, in Test Example 2, the effect of improving nasal discomfort immediately after administration was observed in Test Example 2. On the other hand, in Comparative Test Examples 2-1 and 2-2, the effect of improving discomfort was not recognized. In particular, Comparative Test Example 2-2 was confirmed to have an adverse effect on improving nasal discomfort, which is strongly stimulated by lavender essential oil. In addition, as is clear from Table 3, it was confirmed that stress (irritability) was reduced with improvement of nasal discomfort.

[0032] [Table 2]

In the table, each numerical value shows the average value of the score.

[0033] [Table 3]

In the table, each numerical value shows the average value of the score. Test Example 3 Confirmation test of histamine release inhibition

This test was conducted using a test method (J. So Cosmet. Japan, Vol. 25, No. 4, P246 (1992)) that releases compound histamine from rat mast cells using compound 48/80, a histamine release reagent. The histamine release inhibitory effect of lavender steam distilled water obtained in Example 1 was evaluated.

[0034] 1.2 mL of mast cell suspension collected from the abdominal cavity of rats (Slc: Wister male rats, about 4 to 9 weeks old) together with 0.2 mL of the lavender steam distilled water obtained in Example 1, compound48 / 80 was added to a final concentration of 1.0 / g / mL and incubated at 37 ° C for 15 minutes. Next, the reaction was stopped by cooling with ice, and then the reaction solution was centrifuged. The amount of histamine released from the supernatant was extracted and purified according to a conventional method, colored with 0-phthaldialdehyde, and the excitation wavelength. Measurement was performed by measuring fluorescence intensity at 360 nm and a fluorescence wavelength of 450 nm. For comparison, a lavender essential oil-containing solution (1% by weight of lavender essential oil, 5% by weight of surfactant, remaining water) (comparative test example 3) (Comparative Test Example 3) was used instead of lavender steam distilled water, and as a control, lavender was used. The test was conducted in the same manner as described above using physiological saline (manufactured by Otsuka Pharmaceutical Co., Ltd.) (control) instead of the steam distilled water. From the following formula, the inhibition rate of histamine release was calculated.

[0035] [Equation 1] Histamine release inhibition rate (%) = {1-(A-C) / (B-C)} X 1 0 0 A: Fluorescence intensity obtained in Test Example 3 or Comparative Test Example 3 Measured value of

B: Measured fluorescence intensity of control

C: Blind value Table 4 shows the results obtained. From this result, it was confirmed that the steam-distilled water of lavender obtained in Example 1 has an excellent inhibitory effect on histamine release.

[0036] [Table 4]

Test Example 4 Antibacterial evaluation test About 1 X 10 ⁶ cells / mL of Escherichia coli ATCC 8739, Staphylococcus aureus ATCC 6538 or Pseudomonas aeruginosa ATCC 9027 in the steam distilled water of lavender obtained in Example 1 I added it to become. After the addition of the bacteria, the mixture was thoroughly stirred, and then allowed to stand at 37 ° C. After 12 hours, sampling was performed to measure the concentration of the bacteria in the liquid. The concentration of the bacteria was measured by culturing at 37 ° C for 18 hours using a blood agar plate for DD bacteria and general bacteria. For comparison, a test was performed in the same manner as described above, using physiological saline (manufactured by Otsuka Pharmaceutical Co., Ltd.) (Comparative Test Example 4) instead of Lavender's steam distilled water.

[0037] Table 5 shows the obtained results. As a result, it was confirmed that lavender steam distilled water has an excellent antibacterial action.

[0038] [Table 5]

Test Example 5 Evaluation test of sedation effect

Three subjects with hay fever with nasal discomfort were selected as subjects. Three subjects were administered by allowing 20 g of the lavender steam distilled water obtained in Example 1 to flow into the nasal cavity and then draining it. After administration, subjects were immediately put to bed and evaluated how lavender steam-distilled water had an effect on sleep! // (Study Example 5). The evaluation was performed according to the following evaluation criteria for (1) falling asleep, (2) depth of sleep, (3) awakening during sleep, and (4) awakening. For comparison, instead of lavender steam-distilled water, physiological saline (manufactured by Otsuka Pharmaceutical Co., Ltd.) (Comparative Test Example 5-1) or lavender essential oil-containing solution (1% by weight of lavender essential oil, surfactant 5) The test was conducted in the same manner as described above using (weight%, balance water) (Comparative Test Example 5-2).

A: V, better than Tsum

B: V, no change compared to Tsumo!

C: Bad compared to usual. [0039] Table 6 shows the obtained results. As a result, it was confirmed that the composition for nasal cavity of the present invention has an excellent sleep inducing effect. From this result, since the composition for nasal cavity of the present invention can stay in the nasal cavity for a long time, it improves nasal discomfort during sleep, and furthermore, the problem of sleeping due to the fragrance component of the present invention. It was suggested that

[0040] [Table 6]

The numbers in the table indicate the number of people. Participant example Composition analysis

The lavender steam distilled water and lavender essential oil obtained in Example 1 were subjected to component analysis by gas chromatography. As the lavender essential oil to be analyzed, the oil phase in which the distillate power produced by steam distillation was recovered in Example 1 was used. For the analysis, 47.5 g of lavender steam distilled water obtained in Example 1 was mixed with 2.5 g of hexane, and the lavender essential oil diluted to 1% by weight with methanol was used as samples. . The analysis conditions are as follows.

Gas chromatograph

Hewlett Packard

HP6890 series

DB-5MS

Length 30m

ID 0.25 mm

Film thickness 0.25 / x m

oven Initial temperature 50 ° C 7 minutes

Heated up to 100 ° C at 5 ° C per minute

Heated up to 250 ° C at 20 ° C per minute

250. C constant temperature 10.5 min

Total analysis time 45 minutes

Inlet

Temperature 250 ° C

Split ratio 10: 1

Total flow rate 9.8mlZ min

Carrier gas Ultra high purity helium

Sample ft

2 μ \

FID (hydrogen flame ionization) detector.

Figure 1 shows the chromatograph obtained for lavender steam distilled water, and Figure 2 shows the chromatograph obtained for Lavender mono essential oil. The peak patterns are different between Fig. 1 and Fig. 2, and it was confirmed that the composition of lavender steam distilled water and lavender essential oil differ.

Claims

The scope of the claims

[1] A composition for nasal cavity containing lavender steam distilled water.

[2] Steam-distilled hydropower of lavender The nasal composition according to claim 1, wherein the above-ground or whole-plant power of lavender is obtained.

[3] The composition for nasal cavity according to claim 1 or 2, wherein the lavender is Okamurasaki or an improved variety thereof.