JPH0640911A - Sleep inducing stimulating agent - Google Patents

Abstract

PURPOSE:To provide a sleep inducing agent capable of being absorbed from a nasal membrana mucosa, oral membrana mucosa or lung to advantageously stimulate the sleeping. CONSTITUTION:The sleep inducing agent is characterized by containing jasmine lactone as an active ingredient and preparing the mixture into such a shape that the active ingredient is absorbed from a nasal membrana mucosa, oral membrana mucosa or lung.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a sleep onset promoter containing jasmine lactone as an active ingredient.

[0002]

2. Description of the Related Art In recent years,
There have been numerous reports that scents have various effects on physiological and psychological states, and the psychophysiological effects of aroma substances have come to the forefront. Aromatherapy has long been well known in Europe as a method for recovering or preventing various physiological functions caused by scents (Theory and practice of aromatherapy <fragrance therapy> by Robert Tisland, Fragrance Journal. Company 198
7).

In particular, various methods have been described in the literature for eliminating insomnia by using scents ("Practical aromatherapy", written by Shirley Price; "Plant aromatherapy", written by Jean Barnet). Further, as an example of physiological evaluation using humans, JP-A-4-128234 discloses that bitter orange essential oil has an effect of promoting sleep onset.

On the other hand, jasmine lactone is a component contained in essential oil of jasmine and is known as a component characterizing jasmine aroma. Jasmine oil, as a mixture,
It is said that it has an action of increasing arousal level, and it has been proved that it has an excitatory action by an electroencephalogram CNV method using humans [Torii, Shigeo et al., Fragrance Journal, No86.
(1987)].

However, looking at the component level,
Kubota et al. Reported that the high boiling point composition of jasmine oil showed a sedative effect in the evaluation by human EEG CNV method [23rd Symposium on Taste and Odor, p.
317-320 (1989)]. However, these reports do not specify the active ingredient, and
It has not been evaluated to enhance the decrease in wakefulness and promote sleep onset.

[0006]

Under such circumstances, the present inventors have examined the effects of many aroma substances on their physiological actions, and found that jasmine lactone was absorbed from nasal mucosa, oral mucosa or lung. It was found that when administered in such a manner, at a low concentration and with a fast-acting effect, the reduction in arousal level that occurs during simple task work is enhanced and sleep onset is promoted, and the present invention was completed.

That is, the present invention provides a sleep-promoting agent which comprises jasmine lactone as an active ingredient and is formulated into a form in which the active ingredient is absorbed from nasal mucosa, oral mucosa or lung. It is provided.

In the present invention, the jasmine lactone may be of any purity as long as it can provide the effective concentration described below, and it may be any other essential oil component such as, for example, as long as its action is not impaired. It can also be used as a mixture with aroma components such as bergamot, bitter orange, linden, fennel, ginger, lavender, clary sage, rosemary, geranium and juniper.

Since the sleep-promoting effect of the present invention is exhibited by absorption of jasmine lactone from the nasal mucosa, oral mucosa or lung, the sleep-promoting agent of the present invention is formulated in such an absorbable form. It is necessary to be

The method of formulation is not particularly limited, and jasmine lactone may be absorbed as an aroma component from the nasal mucosa, oral mucosa or lungs. As such a form,
Spray agent that is diffused in the air and inhaled, volatile fragrance, emulsion that is applied and absorbed on the face and body, lotion, makeup powder, cream, body lotion, deodorant stick, hair products, etc. Gum to be absorbed, confectionery such as candy, troche, mouthwash, dentifrice, alcohol such as jelly and liqueur, soft drinks, sublingual tablets or additives to be used by adding to coffee, tea, etc. To be Further, jasmine lactone may be encapsulated and used.

In the case of the form of being diffused in the air and inhaled, the air concentration of jasmine lactone should be at least 0.5 ng / l or more in order to obtain the effects of the present invention. Even if the concentration is further increased beyond this range, no significant increase in the effect is observed, so that the concentration is usually 0.5-
It is preferable to adjust to 10 ng / l. For this purpose, in the case of a spray agent, it is necessary to dissolve it in a solvent such as alcohol to a concentration of 0.1 to 10%, and to fill it in a container together with a propellant. It is preferably dissolved or dispersed in a solution or gel such as isoparaffin.

Further, in the case of the form of diffusing in the mouth, it is sufficient to contain jasmine lactone in an amount of 5.0 × 10 ^-7 % or more. The sleep onset promoter of the present invention was evaluated by the following method.

A. Objective physiological evaluation by humans (evaluation using background EEG activity) Background EEG activity when given a monotonous task task that induces drowsiness in humans, for example, a reaction task to a visual stimulus randomly presented on the CRT. It is evaluated according to the degree of change. The relationship between decreased arousal level and background EEG activity has been proved by the reports by Yoshioka et al. And Ninomiya et al. [Yoshioka et al., Ergonomics Society 2nd
0th Conference Proceedings, 19, 182-183; Ninomiya et al., Medical Electronics and Biotechnology vol29, Suppl (1991)]
Generally, as the level of alertness decreases, the EEG α wave at eye opening,
It is known that the θ wave shows an increasing tendency, but it can be evaluated by whether or not such a physiological reaction is enhanced by giving a scent.

B. Evaluation using mouse The increase / decrease in spontaneous locomotor activity of the mouse is evaluated using a rotating basket. The correlation between changes in spontaneous locomotor activity in mice and central effects has been clarified by Hirabayashi et al. [Hirabayashi, Iizuka, Tadokoro, Nikaku Jpn Jpn, 74 , p629-639 (1978)]. It can be concluded that central depression, that is, a sedative effect is observed if a clear decrease in spontaneous motor activity is observed when a scent is given.

[0015]

EXAMPLES Next, examples will be described.

Example 1 14 subjects (6 males, 8 females, average age 23 years)
Was placed in an electromagnetically shielded room of constant temperature (24 ° C.) and constant humidity (60%), and background electroencephalography was performed for 3 minutes each with the eyes closed and the eyes closed. Subsequently, in order to raise the awakening level to a constant level, a calculation work (keyboard input calculation work task using a personal computer) was performed for 20 minutes. Next, as a simple visual discrimination task, for a red (presentation probability 20%) or blue (presentation probability 80%) color stimulus presented at random (1.5 to 3 second intervals) on the CRT,
The subject was made to perform the task of pressing the button with the right hand only for the red visual stimulus continuously for 40 minutes. During this time, background electroencephalogram recording and eyeblink waveform detection by electrooculogram were performed to measure sleepiness induced by the task.

This trial was carried out twice for each test subject, with and without administration of jasmine lactone. The administration of jasmine lactone was carried out by releasing it into the shielded room under the following conditions.

Jasmine lactone (Hasegawa fragrance SA-5
774) 4.0 ml of liquid paraffin was dissolved in 40 ml of liquid paraffin, put in a gas washing bottle, and 4.0 l / min of dry air was sent from the outside to start emission at the same time when the task work was started. The concentration of jasmine lactone in the air in the shield room was 1.
It was set to 5 ng / l.

Background EEG activity evaluation: The measurement site was derived from the central part (Cz) according to the International 10-20 Electrode Arrangement Method, and was amplified with a high-cut filter 70 Hz with a time constant of 0.3 seconds (NEC Saneisha, Multipurpose EEG 1A98),
From the obtained electroencephalogram recording, frequency analysis was performed by the fast Fourier transform method (FFT method) at 1024 points every 5 seconds. (NEC Saneisha, signal processor 7T1
8). The total power values of the θ wave (4 to 8 Hz) and α wave (8 to 13 Hz) were obtained from the obtained power spectrum data of the frequency distribution, and the jasmine lactone administration group and the non-administration group were compared. Note that the α and θ wave power values every 5 seconds are 6
00 seconds, that is, 120 pieces of data were added and averaged, and the average value was used as the α and θ wave power values at that time.

Based on the power values of the α wave and the θ wave at the time of resting eyes open before the task work, 0 to 10 minutes, 10 to 2 during the task work
The results of comparing the increase and decrease in the power values of the α-wave and the θ-wave for 0 minutes, 20-30 minutes, and 30-40 minutes are as shown in FIGS. 1 and 2.

As shown in FIGS. 1 and 2, in the jasmine lactone non-administration group, the power values of the α wave and the θ wave increase with drowsiness, whereas in the jasmine lactone administration group,
The increase in power values of α-wave and θ-wave was significantly enhanced as compared with the non-administered group, and the decrease in arousal level induced during the simple visual task was promoted.

Example 2 Jasmine lactone (same as in Example 1) was allowed to diffuse its aroma in an inhalation box at a rate of 100 μl per hour, and 8 male ICR mice were placed in this and left for 60 minutes. The number of rotations was measured by a rotating basket (Muromachi Kikai Co., Ltd.), and the amount of exercise was compared with that of a group not given jasmine lactone aroma (non-administered group, 11 animals). The results are shown in FIG. 3, and a significant decrease in the amount of exercise was observed by the administration of jasmine lactone.

[0023]

Table 1 Example 3 (gum) Gum base 20 (parts by weight) Calcium carbonate 2 Stevioside 0.1 Jasmine lactone 1 Lactose 76.895 Flavor 0.005 Total amount 100

[0024]

Table 2 Example 4 (candy) powdered sorbitol 99.93 (parts by weight) jasmine lactone 0.01 fragrance 0.01 sorbitol seed 0.05 total amount 100

[0025]

Table 3 Example 5 (troche) Gum arabic 6 (parts by weight) Glucose 73 Jasmine lactone 0.005 Dibasic potassium phosphate 0.2 Dibasic potassium phosphate 0.1 Lactose 17 Perfume 0.005 Magnesium stearate Residue The amount Total 100

[0026]

Table 4 Example 6 (Mouthwash) Sodium lauryl sulfate 0.8 (parts by weight) Glycerin 7 Ethyl alcohol 15 Jasmine lactone 0.01 Sorbitol 5 Perfume 0.01 Saccharin sodium 0.01 Water Remaining total amount 100

[0027]

Table 5 Example 7 (liqueur) Neutral spirits 30 (parts by weight) Stevioside 0.1 Orange juice 5 Jasmine lactone 0.01 Perfume 0.01 Water Remaining total amount 100

[0028]

[Table 6] Example 8 (soft drink) Orange juice 5 (parts by weight) Sodium citrate 0.2 L-Ascorbic acid 0.02 Jasmine lactone 0.01 Perfume 0.01 Citric acid 0.2 Carbonated water Remaining total amount 100

[0029]

[Table 7] Example 9 (juice) Frozen orange juice concentrate 5.0 (parts by weight) Sugar 11.0 Citric acid 0.2 L-Ascorbic acid 0.02 Jasmine lactone 0.1 Water 83.68 Total amount 100

Example 10 (Black Tea) 1.2 parts by weight of tea leaves were put into an appropriate amount of hot water (80 ° C.) and sufficiently leached, and then the tea leaves were filtered off, and 3.0 parts by weight of sugar and sodium bicarbonate were added to the leaching solution. 0.08 parts by weight, L-ascorbic acid 0.1 parts by weight, jasmine lactone 1.0 parts by weight were added, and the remaining water (20 ° C.) was added to 100 parts by weight.

Example 11 (Oolong Tea) 1.2 parts by weight of tea leaves were put into an appropriate amount of hot water (80 ° C.) and sufficiently leached, and then the tea leaves were filtered off. 0.03 parts by weight of sodium hydrogencarbonate, L -0.1 parts by weight of ascorbic acid,
1.0 parts by weight of jasmine lactone was added and the remaining water (2
(0 ° C.) was added to make 100 parts by weight.

[0032]

Table 8 Example 12 (jelly) Jasmine lactone 0.3 (parts by weight) Sugar 15.0 Sodium citrate 0.3 Gelatin 1.1 Water 73.0 Orange juice 10.0 Citric acid 0.3 Total amount 100

[0033]

Table 9 Example 13 (Emulsion) Stearic acid 2.0 (parts by weight) Cetanol 1.0 Vaseline 3.0 Lanolin alcohol 2.0 Liquid paraffin 8.0 Squalane 3.0 Escalol 507 2.0 Jasmine lactone 5 0.0 POE (10) monooleate 2.5 triethanolamine 1.0 propylene glycol 5.0 preservative appropriate amount distilled water remaining total amount 100

[0034]

Table 14 Example 14 (nutrition cream) Stearic acid 2.0 (parts by weight) Stearyl alcohol 7.0 Reduced lanolin 2.0 Squalane 5.0 Octyldodecanol 6.0 POE (25) Cetyl ether 3.0 Glyceryl Monostearate 2.0 Preservative Suitable amount Jasmine lactone 2.0 Propylene glycol 5.0 Distilled water Remaining amount 100

[0035]

Table 15 Example 15 (ointment) Stearyl alcohol 18.0 (parts by weight) Mokurou 20.0 Jasmine lactone 0.5 Polyoxyethylene monooleate ester 0.25 Glycerin monostearate ester 0.25 Vaseline 40.0 Purified water Total remaining amount 100

[0036]

Table 16 Example 16 (lotion) Jasmine lactone 1.0 (parts by weight) Propylene glycol 1.0 Citric acid 0.2 95% Ethanol 10.0 POE (20) Lauryl ether 0.5 Distilled water Total amount 100

[0037]

Table 13 Example 17 (Lip treatment) Candelilla wax 9.0 (parts by weight) Solid paraffin 8.0 Beeswax 5.0 Carnauba wax 5.0 Lanolin 11.0 Castor oil Remaining amount Jasmine lactone 1.0 Isopropyl myristate 10.0 Antioxidant Suitable amount Total 100

[0038]

Table 14 Example 18 (Spraying agent) Ethanol 50 (parts by weight) Dichlorodifluoromethane 49.5 Jasmine lactone 0.5 Total amount 100

[0039]

Table 15 Example 19 (fragrance) Isoparaffin 80 (parts by weight) Jasmine lactone 20 Total amount 100

[0040]

Table 16 Example 20 (fragrance) K-carrageenan powder 1.1 (parts by weight) Locust bean gum 1.0 Jasmine lactone 5.0 Water Total amount of remaining amount 100

Example 21 (soft capsule) Jasmine lactone and gelatin solution (gelatin 35%,
A gelatin capsule having a particle size of 1 mm was produced from glycerin 15% and water 50%) using a seamless capsule production apparatus.

[0042]

EFFECTS OF THE INVENTION By absorbing the sleep onset promoter of the present invention from the nasal mucosa, oral mucosa or lung, sleep onset can be advantageously promoted.

[Brief description of drawings]

FIG. 1 shows a comparison of α-wave power values in a jasmine lactone administration group and a non-administration group.

FIG. 2 shows a comparison of θ wave power values between a jasmine lactone administration group and a non-administration group.

FIG. 3 shows a comparison of spontaneous locomotor activity in mice between a jasmine lactone administration group and a non-administration group.

Claims (1)

[Claims] 1. A hypnagogic agent which comprises jasmine lactone as an active ingredient and is formulated into a form in which the active ingredient is absorbed from the nasal mucosa, oral mucosa or lung.