JP2014218483A - Composition for sleepiness prevention containing gardenia extract - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition which has high sleepiness prevention effect and contains a capsicum extract or a ginger extract as an active ingredient, and a composition with reduced volume which contains the capsicum extract and the ginger extract and has sufficient awakening effect while reducing the content of the capsicum extract and the ginger extract.SOLUTION: A composition containing a capsicum extract and a ginger extract has high awakening effect by blending a gardenia extract with the capsicum extract and the ginger extract. A composition with reduced volume has high awakening effect while reducing the blending content of the capsicum extract and the ginger extract.

Description

  The present invention provides a composition comprising gardenia extract, pepper extract and ginger extract for preventing or eliminating drowsiness.

  Conventionally, various drowsiness preventives containing a pepper extract or a ginger extract as an active ingredient have been proposed. For example, Patent Document 1 discloses a water-soluble polymer, a cooling sensation agent such as menthol, and a stimulation agent that is one or more of a warm sensation agent that may be a plant extract such as pepper and ginger. A palatal sticking film for preventing drowsiness is disclosed. Patent Document 2 discloses a drowsiness preventive agent (coating agent) characterized in that a soft kneaded product is obtained by mixing a mixture of ginger, yam seed, chili, and coconut extract with appropriate amounts of mint oil and petrolatum. Is disclosed.

  However, the conventional anti-drowsiness agents containing a chili pepper extract or a ginger extract as an active ingredient have low convenience in use, and it has been difficult to obtain satisfactory drowsiness prevention effects and arousal effects.

  The present inventors have so far developed a sleepiness preventive agent (solution) containing capsicum extract, ginger extract, arginine, and caffeine as active ingredients, and ingesting the sleepiness preventive agent. It has been reported that a high sleepiness prevention (awakening) effect can be obtained (Patent Document 3).

  However, there is still a need in the art for a composition comprising a chili pepper extract or a ginger extract having an even higher drowsiness prevention (awakening) effect.

  On the other hand, crocin and crocetin are types of carotenoids and yellow pigments. These pigments are contained in the fruits of the Gardenia jasminoides and the female head of the saffron genus Saffron (Crocus sativus LINNE), and have been used as food colors for a long time. Also, today, these pigments improve brain function, antioxidants, antidepressants, cancer prevention, mental function improvement, low cholesterol, inflammation prevention, sleep improvement agent, sedative, eye strain improvement composition It is known to have such effects (Patent Documents 4-8).

JP 2007-99689 Japanese Patent Laid-Open No. 2001-2580 JP 2010-195761 Japanese Patent No. 2704356 JP 2008-273939 A JP 2010-195779 JP 2011-246357 JP JP 2007-215465 A

  As described above, there is still a need in the art for a composition comprising a chili extract or a ginger extract having an even higher drowsiness prevention effect as an active ingredient.

  In addition, caffeine-containing beverages that have been provided as anti-drowsiness agents in the past have been concentrated in a relatively small amount (50 ml) by concentrating active ingredients, and are gaining popularity due to factors such as ease of consumption. . The present inventors concentrated the active ingredient on the anti-drowsiness agent (liquid preparation) containing the above-mentioned pepper extract and ginger extract as an active ingredient, and reduced the volume while maintaining the compounding amount of the active ingredient. It was found that the pungent taste caused by the pepper extract and the ginger extract was increased and the intake was difficult. On the other hand, in order to suppress the pungency attributed to the pepper extract and the ginger extract, the amount of these active ingredients was reduced to reduce the volume, and it was found that a sufficient drowsiness prevention effect could not be obtained.

  Then, an object of this invention is to provide the composition which has a chili pepper extract and a ginger extract which has a high sleepiness prevention effect as an active ingredient. Furthermore, the present invention is a composition comprising the above-mentioned pepper extract or ginger extract as an active ingredient, and it is possible to obtain a sufficient drowsiness prevention effect while reducing the content of the pepper extract and the ginger extract. It is an object to provide a composition with a small volume.

  As a result of intensive studies to solve the above problems, the present inventors have found that a composition having a high arousal effect can be obtained by blending a gardenia extract together with a pepper extract and a ginger extract. In addition, by combining the gardenia extract together with the pepper extract and the ginger extract, it is possible to obtain a small-volume composition having a high arousal effect while reducing the amount of the pepper extract and the ginger extract. I found. The present invention is based on these findings.

That is, the present invention has the following features.
[1] A composition containing a gardenia extract, a red pepper extract, and a ginger extract.
[2] The composition according to [1], which is liquid.
[3] The pepper extract is contained so that capsaicin is 5 μg to 15 μg,
The composition according to [1] or [2], wherein the ginger extract is contained so that gingerol is 0.5 mg to 1.2 mg.
[4] Drowsiness prevention agent containing gardenia extract, red pepper extract, and ginger extract.
[5] The sleepiness preventive agent according to [4], which is liquid.
[6] A capsicin extract is contained so that capsaicin may be 5 micrograms-15 micrograms,
The sleepiness preventive agent according to [4] or [5], wherein the ginger extract is contained so that gingerol is 0.5 mg to 1.2 mg.

  ADVANTAGE OF THE INVENTION According to this invention, the composition containing a red pepper extract and a ginger extract which has a high arousal effect can be provided. In addition, according to the present invention, a composition containing a capsicum extract and a ginger extract, which can obtain a sufficient awakening effect while reducing the content of the capsicum extract and the ginger extract. A volumetric composition can be provided.

FIG. 1 shows the test protocol of Example 1. FIG. 2 shows the evaluation result by the VAS method regarding “improvement of sleepiness” in Example 1. * 1: Test food 1 is significantly different from test food 2 at P> 0.05. * 2: Test food 1 is significantly different from test food 3 at P> 0.05. FIG. 3 shows an evaluation result by the VAS method regarding “improvement of the head sag” in the first embodiment. * 2: Test food 1 is significantly different from test food 3 at P> 0.05. +1: Test food 1 tends to be P> 0.1 compared to test food 2. +2: Test food 1 tends to be P> 0.1 compared to test food 3. FIG. 4 shows the test protocol of Example 2. FIG. 5 shows the evaluation result by the VAS method regarding “clean feeling” in Example 2. * 4: Test food 4 is significantly different from test food 6 at P> 0.05. +5: Test food 5 tends to be P> 0.1 compared to test food 6. FIG. 6 shows the evaluation result by the VAS method regarding “crisp” in Example 2. +5: Test food 5 tends to be P> 0.1 compared to test food 6. FIG. 7 shows the evaluation result by the VAS method regarding “fatigue” in Example 2. * 5: Test food 5 is significantly different from test food 6 at P> 0.05. FIG. 8 shows the evaluation result by the VAS method regarding “head is dull” in Example 2. * 4: Test food 4 is significantly different from test food 6 at P> 0.05. +5: Test food 5 tends to be P> 0.1 compared to test food 6.

1. Gardenia extract Gardenia extract is obtained by extracting the fruit part of gardenia with a solvent that is an organic solvent, water, a supercritical fluid or a subcritical fluid. Gardenia extract contains carotenoid pigments crocin and / or crocetin.

  The gardenia extract may be used as it is as an extract with a solvent, or a concentrated or diluted extract, or a product obtained by purifying or roughly purifying crocin and / or crocetin from the extract. Can also be used.

  The extraction solvent is not particularly limited as long as it can extract crocin and / or crocetin, but it is preferable to use alcohol or water as the extraction solvent for the extraction of crocin. Ethanol is preferred as the alcohol. The mixing ratio when using a mixture of alcohol and water is not particularly limited, but for example, the weight ratio is preferably in the range of 10:90 to 90:10, and more preferably in the range of 20:80 to 50:50. It is particularly preferable to use water as an extraction solvent for the extraction of crocin. Since crocin is water-soluble, crocetin is insoluble in water. Therefore, crocin can be efficiently extracted by using water as an extraction solvent. When water is used as the extraction solvent, hot water (about 90 to 100 ° C.) is preferably used. On the other hand, it is preferable to use alcohol as an extraction solvent for the extraction of crocetin. Although the amount of crocetin contained in the fruit portion of gardenia is very small, crocetin can be produced by hydrolyzing crocin. Therefore, when extracting crocetin, crocetin can be efficiently extracted by subjecting the gardenia extract containing crocin to hydrolysis, and then extracting it with alcohol. The hydrolysis treatment can be performed by a known method, using a hydrolase (eg, β-glucosidase), an acid (eg, hydrochloric acid, sulfuric acid, etc.), or an alkali (eg, sodium hydroxide, sodium carbonate, etc.). Can be done.

  In the composition or sleepiness prevention agent of the present invention, preferably the amount that crocin or crocetin is 3 mg or more per one oral intake, for example, the amount that is 3.5 mg or more, more preferably 3.5 mg to 30 mg, More preferably, the gardenia extract in an amount of 3.5 mg is blended. The crocin or crocetin concentration in the composition can be measured by a high performance liquid chromatography (HPLC) method.

  In the present invention, the term “single oral intake” refers to the amount of the composition of the present invention or the sleepiness inhibitor that is taken orally at a time, or a short time interval (for example, 10 minutes or less, preferably 5 minutes or less). It means the total amount that is taken orally continuously multiple times. When the composition of the present invention or the sleepiness prevention agent is in the form of a liquid composition, the amount is, for example, 50 ml to 200 ml (typically 50 ml, 100 ml, 150 ml, 200 ml). When in the form, the amount is, for example, 20 ml to 100 ml (typically 20 ml, 50 ml, 75 ml, 100 ml), more preferably 20 ml to 75 ml (typically 20 ml, 50 ml, 75 ml). For example, 5g to 200g (typically 5g, 10g, 20g, 30g, 40g, 50g, 100g, 150g, 200g) is the amount in the case of other forms such as jelly or the like . Hereinafter, “single oral intake” is used in this sense.

2. Capsicum extract Capsicum extract is obtained by extracting the fruit portion of pepper with an organic solvent, water, a supercritical fluid or a subcritical fluid. The capsicum extract contains capsaicin that acts on the TRV1 receptor, which is a pungent receptor, to make it feel pungent. As the pepper extract, a solvent extract can be used as it is, a concentrate obtained by concentrating or diluting the extract, or a capsaicin purified or roughly purified from the extract can be used. You can also. The extraction solvent is not particularly limited as long as it can extract capsaicins, but ethanol is preferable. In capsicum extract, capsaicins are usually contained in an amount of 0.7 to 0.9% by weight. Capsaicin concentration can be measured by HPLC method. The amount of capsaicin (capsaicin amount) is the total amount of capsaicin and dihydrocapsaicin. In the present invention, capsaicin and dihydrocapsaicin are sometimes collectively referred to as “capsaicins” or simply “capsaicin”.

  The pepper extract is blended in the composition of the present invention or the sleepiness preventive agent in an amount that makes a pungent taste. As such an amount, for example, in the final composition, the amount that capsaicins are 5 μg or more, preferably 5 μg to 15 μg, more preferably 9 μg per oral intake, for example. Of red pepper extract.

In addition, the above-mentioned pepper extract is combined with the ginger extract,
A pungent pattern suitable for oral intake.

3. Ginger extract Ginger extract is obtained by extracting the rhizome part of ginger with organic solvent, water, supercritical fluid or subcritical fluid solvent. The ginger extract contains gingerol that acts on the TRV1 receptor, which is a pungent receptor, to make it feel pungent. As a ginger extract, an extract with a solvent can be used as it is, or an extract obtained by concentrating or diluting the extract can be used, or a gingerol purified or roughly purified from the extract can be used. It is also possible to use a preparation in which purified gingerol is emulsified and solubilized. The extraction solvent is not particularly limited as long as it can extract gingerol, but a supercritical fluid such as carbon dioxide is preferable. The ginger extract usually contains 1.7 to 2.1% by weight of gingerol. The gingerol concentration can be measured by the HPLC method.

  The ginger extract is blended in the composition of the present invention or the drowsiness preventive in an amount that makes it feel pungent. Such amount is, for example, in the final composition, preferably in an amount such that gingerol is 0.5 mg or more, more preferably 0.5 mg to 1.2 mg, more preferably 0.75 mg per oral intake. The amount of ginger extract is blended.

4. Caffeine In addition to the above active ingredients, the composition or drowsiness inhibitor of the present invention may further contain caffeine. Commercially available caffeine can be used as caffeine. For example, caffeine having a high concentration (for example, 98.5% by weight or more) produced by extraction from coffee beans can be used.

  In the composition of the present invention or the drowsiness preventive agent, caffeine may be formulated in an effective amount that exerts a spontaneous motor excitability by eating.For example, in the final composition, preferably 100 mg per oral intake. For example, 100 mg to 300 mg, preferably 100 mg is blended.

5. Arginine In addition to the above active ingredients, the composition or anti-drowsiness agent of the present invention may further contain arginine. L-arginine is preferably used as arginine, and may be in the form of a salt. As arginine, commercially available arginine can be used. For example, arginine having a high concentration (for example, 98.0% by weight or more) produced from a sugar source by a fermentation method can be used.

  Arginine is used in the composition of the present invention or the drowsiness preventive in an amount that enhances the spontaneous movement excitatory action of caffeine used in combination. Such an amount is, for example, preferably 500 mg or more, for example 500 mg to 1500 mg, preferably 500 mg per single oral intake in the final composition.

6. Other ingredients In addition to the above active ingredients, the composition or sleepiness inhibitor of the present invention is an ingredient that is acceptable in the final form of foods and drinks, pharmaceuticals, etc., and other ingredients that can be taken orally. Further can be included. In particular, when the composition or drowsiness preventive agent of the present invention is in the form of a liquid composition or a semi-solid composition (such as a jelly), in addition to the above components, fruit juice, sweetener, acidulant in water Antioxidants, thickeners, salt, flavorings, vitamins, extracts, cyclic oligosaccharides, carbonic acid, starch, agar, and other food additives can be added.

Examples of the fruit juice include apple juice, lemon juice, orange juice, and concentrated juices thereof.
Examples of the sweetener include sugars such as fructose, glucose, liquid sugar and granulated sugar, and high-intensity sweeteners such as honey, sucralose, acesulfame potassium and aspartame.

Examples of the acidulant include citric acid, malic acid, gluconic acid, tartaric acid, ascorbic acid and the like.
Examples of the antioxidant include vitamin C, catechin, enzyme-treated rutin and the like.

  Thickeners include thickening polysaccharides such as gellan gum, xanthan gum, pectin, guar gum and the like. The viscosity of the beverage composition of the present invention can be adjusted to about 2.5 mPa · s with the thickening polysaccharide.

Examples of the fragrance or extract include fragrances or extracts such as ginger, cinnamon, clove, turmeric, jujube, l-menthol, and menthol analogs.
Vitamins include vitamin B1, vitamin B6, niacin and the like.

7. Composition and use thereof The composition of the present invention can be used as a food / beverage composition or a pharmaceutical composition having a drowsiness-preventing action.

  The form of the composition of the present invention is not particularly limited, but a liquid, solid, or semi-solid composition suitable for oral intake is preferable, and a liquid composition or a solid composition is particularly preferable.

  The liquid composition may be provided as a liquid food (beverage) or a liquid pharmaceutical for oral administration, but is preferably a beverage. The liquid composition is a composition based on water, and can be produced by mixing the above components with water. The amount of each component is as described above. Such a liquid composition can be contained in a container used as a beverage container. Examples of beverage containers include polyethylene terephthalate (PET) containers, so-called PET bottles, metal can containers, and the like. The form of the container is not particularly limited. Further, the capacity of the container is not particularly limited, but for example 50 ml to 500 ml (typically 50 ml, 100 ml, 150 ml, 200 ml, 250 ml, 300 ml, 350 ml, 400 ml, 450 ml or 500 ml), preferably 50 ml to 200 ml. it can. For a small volume type, for example, 20 ml to 100 ml (typically 20 ml, 25 ml, 30 ml, 40 ml, 50 ml, 60 ml, 70 ml, 80 ml, 90 ml, or 100 ml), more preferably 20 ml to 75 ml (typically 20 ml) , 50 ml, 75 ml). The means for accommodating the liquid composition in the container is arbitrary.

  The solid composition is provided as, for example, a pharmaceutical having a form such as a granule, capsule, tablet, fine granule, caplet, powder, pill, health food, nutritional supplement (supplement), chewing gum, and the like. . In the solid composition, the active ingredient (the amount of each component is as described above) is mixed with an excipient such as an excipient, a filler, a binder, a disintegrant, a lubricant, and a gum base, It can be molded and produced according to a conventional method.

[Example 1]
1. Test method The test was conducted by three groups of crossover test methods (single administration) for 10 healthy men aged 20 to 49 years old.

The test was carried out in a room where a 60W standlight was installed and external light was blocked by a blackout curtain.
The room temperature was set to 25 ° C. ± 1 ° C.

  The subject was seated on a reclining seat installed indoors, and no particular work was performed during the test except during the examination.

なお、「カプサイシン」にはカプサイシンとジヒドロカプサイシンを包含した。 2. Inspection sample

“Capsaicin” includes capsaicin and dihydrocapsaicin.

(i) Test food 1
Test food 1 is water, the amount of crocin is 3.5 mg of capsicum extract, the amount of capsicin is 9 μg of capsicum extract, the amount of gingerol is 0.75 mg of ginger extract, 100 mg of caffeine, and 500 mg of arginine A non-carbonated beverage having a content weight of 50 ml was prepared.

(ii) Test food 2
Test food 2 contains an amount of capsaicin in an amount of 18 μg of capsicin, an amount of gingerol in an amount of 1.5 mg of ginger extract, 100 mg of caffeine, and 500 mg of arginine in water, and does not contain a gardenia extract. A 100 ml carbonated beverage was used.

(iii) Test food 3
Test food 3 was a non-carbonated beverage with a content weight of 50 ml containing 120 mg of caffeine alone in water.

The following commercially available products were used as the raw materials used in the test food.
Gardenia extract: An extract obtained by extracting the fruit portion of gardenia with water-containing ethanol and then spray-dried with an excipient.
Capsicum extract: An extract of capsicum fruit part with ethanol, capsaicin content is 0.7-0.9 wt%.
Ginger extract: A spice extract preparation obtained by purifying and emulsifying the extract obtained by supercritical extraction of carbon dioxide as a solvent for the underground stem portion of ginger, and the gingerol content is 1.7 to 2.1% by weight.
Caffeine: Coffee beans based on coffee beans with a caffeine content of 98.5% by weight or more.
Arginine: L-arginine obtained by fermentation and isolation and purification of sugar. The L-arginine content is 98.0% by weight or more.

(iv) Manufacturing method Each test food is the water added to the above raw materials, sterilized by heating at around 100 ° C, then cooled, and for test food 2, after filling with carbonic acid, sealed in a container and heated again. Manufactured by sterilization and cooling.

3. Test items
(1) Evaluation of subjective symptoms
VAS (Visual Analog Scale) method is a test that evaluates the degree of subjective symptoms by quantification. In this method, the highest possible state is set to the right end and the lowest is set to the left end in a straight line. It is also widely used in clinical medicine for subjective evaluation, and is used especially for comparison of the condition before and after administration between subjects. The VAS method was used to evaluate “improving drowsiness” and “improving headiness”.
Measurements were taken immediately before and after ingestion of the test food, and 60 minutes after ingestion.

(2) Statistical analysis Statistical processing was performed using a paired t-test as a comparison before and after intake, and a paired t-test was used for comparison between controls. In both cases, the significance level was set at 5% by the two-sided test.

4. Test protocol Figure 1 shows the test protocol.

5. Results
(1) Evaluation of subjective symptoms
FIG. 2 and FIG. 3 show the evaluation results of “improvement of drowsiness” and “improvement of dullness” by the VAS method.
Immediately after the test meal, test food 1 (invention) has a higher improvement effect (wakefulness effect) in “drowsiness” and “head is dull” than test food 2 and test food 3. It was.

(2) Conclusion It was confirmed that the intake of test food 1 (the present invention) reduced “drowsiness” and “head tingling”, and a high arousal effect was obtained. Moreover, since the arousal effect was recognized even 60 minutes after ingestion of the test food 1, it was confirmed that it was persistent.

  It was confirmed that foods with crocin added with capsaicin and gingerol have a high arousal effect, and foods with crocin added have a high arousal effect even if the content of capsaicin and gingerol is reduced. .

[Example 2]
Subsequently, the arousal effect of crocin and crocetin was evaluated.

1. Test Method The test was conducted by the crossover test method of 3 groups (single administration) as in Example 1.

なお、「カプサイシン」にはカプサイシンとジヒドロカプサイシンを包含した。 2. Inspection sample

“Capsaicin” includes capsaicin and dihydrocapsaicin.

(i) Test food 4
Test food 4 is an amount in which the gardenia extract is crocin 3.5 mg, capsicum extract is 18 μg capsaicin, ginger extract is 1.5 mg gingerol, caffeine 100 mg, arginine 500 mg, A carbonated beverage with a content weight of 100 ml containing 2.5 mg of vitamin B1 was prepared.

(ii) Test food 5
Test food 5 was prepared in water such that the gardenia extract had an amount of crocetin of 3.5 mg, the pepper extract had an amount of capsaicin of 18 μg, the ginger extract had an amount of 1.5 mg of gingerol, caffeine 100 mg, arginine 500 mg and A carbonated beverage with a content weight of 100 ml containing 2.5 mg of vitamin B1 was prepared.

(iii) Test food 6
The test food 6 was a non-carbonated beverage containing 2.5 mg of vitamin B1 in water and having a content weight of 100 ml.

The following commercially available products were used for crocetin and vitamin B1 used in the test food.
Vitamin B1: Vitamin B1 nitrate.
Crocetin: obtained by hydrolyzing crocin.
The other raw materials were those described in Example 1 above.

3. Test items
(1) Evaluation of subjective symptoms
The VAS method was used to evaluate “clean feeling”, “crisp feeling”, “fatigue”, and “head-feeling”.
Measurements were taken immediately before and immediately after intake of the test food, and at 15, 30, and 60 minutes after intake.

(2) Statistical analysis Statistical processing was performed using the t-test in the same manner as in Example 1 above, and the significance level was determined to be 5%.

4. Test protocol Figure 4 shows the test protocol. The “PC work” is performed by typing (inputting) a character string in which alphabets (including lowercase letters and uppercase letters) are randomly listed on a Microsoft Word (registered trademark) document.

5. Results
(1) Evaluation of subjective symptoms
FIG. 5, FIG. 6, FIG. 7 and FIG. 8 show the evaluation results of “clean feeling”, “crisp feeling”, “fatigue”, and “head tingling” by the VAS method, respectively.

  Immediately after the test meal, the test food 4 and the test food 5 improved in comparison with the test food 6 in “clean feeling”, “crisp feeling”, “fatigue” and “heady” The effect (wakefulness effect) was observed.

(2) Conclusion As with the food with crocin, the arousal effect was confirmed with the food with crocetin.

Claims (6)

  A composition comprising a gardenia extract, a red pepper extract, and a ginger extract.   The composition according to claim 1, which is liquid. Capsicum extract is contained so that capsaicins may be 5 μg to 15 μg,
The composition of Claim 1 or 2 containing a ginger extract so that a gingerol may be 0.5 mg-1.2 mg.   An anti-drowsiness agent comprising a gardenia extract, a pepper extract, and a ginger extract.   The sleepiness preventive agent according to claim 4, which is liquid. Capsicum extract is contained so that capsaicins may be 5 μg to 15 μg,
The sleepiness inhibitor of Claim 4 or 5 which contains a ginger extract so that a gingerol may be 0.5 mg-1.2 mg.

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