JP7451124B2 - Oral composition and method for suppressing moisture absorption thereof - Google Patents

Description

The present invention relates to an internal composition containing at least one of a Chinese herbal extract and a herbal medicine extract, which effectively prevents deterioration over time and maintains excellent medicinal efficacy over a long period of time, and a method for suppressing moisture absorption thereof.

In general, internal compositions containing Chinese herbal extracts and herbal medicine extracts have high hygroscopicity, so it is necessary to take measures to prevent discoloration and deterioration due to absorption of moisture (for example, Patent Document 1).

Japanese Patent Application Publication No. 2016-222729

An object of the present invention is to provide a novel internal composition and a method for suppressing moisture absorption thereof.

In order to achieve the above object, the present invention has the following points [1] to [8].
[1] An internal composition containing at least one of a Chinese herbal extract and a crude drug extract, and terpenes.
[2] The internal composition according to [1], wherein the content of the terpenes is 0.0005 to 20% by mass based on the entire internal composition.
[3] The content ratio of terpenes to at least one of the herbal medicine extract and herbal medicine extract (terpenes/herbal medicine extract) is 0.00001 to 10 in mass ratio, [1] or [2]. Oral composition.
[4] The internal composition according to any one of [1] to [3], wherein the terpene is menthol.
[5] At least one of the above-mentioned Chinese herbal extract and herbal medicine extract uses a herbal medicine derived from at least one selected from the group consisting of roots, rhizomes, and flower buds as a constituent herbal medicine, [1] to [4] The internal composition according to any one of the above.
[6] The above-mentioned Chinese herbal extract formulations include Keishigomotsuto, Kanrodon, Kyoseihabuemaru, Hankashashinto, Hankakobokuto, Hainoshankyoto, Shinisheilungto, Chikuba Seikyuto, The internal composition according to any one of [1] to [5], which is at least one selected from the group consisting of Yokukansan and Rikkunshito.
[7] A method for suppressing moisture absorption of an internally administered composition, which comprises incorporating terpenes into an internally administered composition containing at least one of a Chinese herbal extract and a crude drug extract.

That is, the present inventors have conducted various studies in order to suppress moisture absorption of internal compositions containing Chinese herbal extracts and herbal medicine extracts. Normally, when an ingredient derived from a herbal medicine other than the herbal formula or herbal medicine is added to an oral composition containing at least one of a herbal medicine extract and a herbal medicine extract, the expression of the desired efficacy derived from the herbal medicine extract may be inhibited. , there is a tendency to avoid using Chinese herbal medicine as it may lead to a disruption of traditional Chinese medicine prescriptions. However, the present inventors broke down such preconceptions and unexpectedly discovered that when a Chinese herbal extract or a crude drug extract is included together with terpenes, excellent moisture absorption can be suppressed. Furthermore, preparations containing Chinese herbal extracts and herbal medicine extracts have poor membrane permeability and foam formation when suspended, but by incorporating terpenes, oral compositions can be suspended in water, etc. It has been found that membrane permeability is improved when a suspension or oral composition is made into a liquid formulation, and it is possible to suppress a decrease in the feeling of taking the drug due to the generation of bubbles.

As described above, although the oral composition of the present invention contains at least one of a Chinese herbal extract and a crude drug extract, it is excellent in suppressing moisture absorption, so discoloration and deterioration due to moisture absorption are less likely to occur, and the quality of the oral composition is improved. can be guaranteed for a long period of time. Furthermore, the oral composition of the present invention can improve membrane permeability and suppress the generation of bubbles when the oral composition is suspended in water or the like, or when the oral composition is in the form of a liquid. .

Next, a mode for carrying out the present invention will be described. However, the present invention is not limited to the following embodiments.

The present invention includes at least one of a Chinese herbal extract and a crude drug extract, and terpenes. Details will be explained below.

The "Chinese herbal extract" used in the oral composition according to the present embodiment refers to all extracts derived from herbal medicines according to the Chinese herbal prescription using water, organic solvents such as ethanol, or mixtures thereof. It is intended to include any form such as the extract itself, a soft extract obtained by concentrating the extract, and a dry extract obtained by drying the extract or soft extract.
In addition, "crude drug extract" refers to all extracts obtained by extracting a single or multiple types of crude drugs with water or organic solvents, including the extract itself, a soft extract obtained by concentrating the extract, and a dried extract or soft extract. It is intended to include any form such as a dry extract or the like.
Both Chinese herbal extracts and crude drug extracts can be used alone or in combination of two or more, and Chinese herbal extracts and crude drug extracts may also be used in combination.

The above-mentioned Chinese herbal extracts and crude drug extracts can be those manufactured according to the method for producing crude drug-related preparations "extract preparations" as described in the General Rules for Preparations of the 17th Edition of the Japanese Pharmacopoeia. The above methods include, for example, adding an appropriate extractant to an appropriately sized herbal medicine, cooling and soaking it for a certain period of time to obtain an extract, or measuring an appropriately sized herbal medicine in fixed amounts according to a prescription. An example of this method is to add about 10 to 20 times the amount of water to the total amount and heat it for a certain period of time to obtain an extract. Note that the obtained extract is usually subjected to solid-liquid separation such as centrifugation or filtration to remove solid content before use.

The term "crude drug" in the oral composition according to the present embodiment means those listed as "crude drug" in the Japanese Pharmacopoeia and the standards for crude drug outside the Japanese Pharmacopoeia. Furthermore, "Kampo prescription" refers to a combination (recipe) of crude drugs based on the concept of Chinese medicine.

The oral composition according to the present embodiment preferably contains a herbal medicine derived from at least one selected from the group consisting of roots, rhizomes, and flower buds as the herbal medicine constituting the Chinese herbal prescription, and two types of these are preferably used. It is preferable to contain the above amount. Crude drug extracts consisting of herbal medicines derived from roots, rhizomes, and flower buds and herbal medicine extracts containing herbal medicines derived from these usually tend to be highly hygroscopic, and therefore can exhibit a greater moisture absorption suppressing effect. In addition, since herbal medicines derived from these substances tend to contain a large amount of polysaccharides, preparations containing these substances have poor membrane permeability when suspended, and have a marked tendency to generate bubbles. The oral composition according to the present embodiment effectively improves membrane permeability against these, and reduces the feeling of taking it when taken with water due to the generation of bubbles in solid preparations such as granules. can suppress foam generation. Among such herbal medicines, those containing Scutellaria scutellariae, Scutellaria scutellariae, Ginkgo, Rhubarb, Licorice, Carrot, and Ginseng are preferable, those containing Scutellaria scutellariae, Scutellaria scutellariae, Glycyrrhiza, and Carrot are more preferable, and those containing at least one of Scutellaria scutellariae and Scutellaria scutellariae are preferred. It is even more preferable that you do so.

The above-mentioned Kampo prescriptions include, for example, "Shokanron", "Kinki Yoryaku", "Revised Guide to General Use Kampo Prescriptions" (supervised by the Japan Official Book Association, Japanese Traditional Chinese Herbal Medicine). (edited by Japan Pharmaceutical Association, published by Jihousha).
In addition, there are no limitations to the herbal medicines that contain herbal medicines derived from at least one selected from the group consisting of roots, rhizomes, and flower buds, such as, but not limited to, keishigomotto, kanro-n, Seinetsu Hokito, Seinetsu Hoketsuto, Seiryuto, Shin'i Seiketsuto, Hainosankyoto, Kyoseihabuemaru, Hankashashinto, Hankakobokuto, Chikuba Seikyuto, Yokukansan, Rikkunshi Among them, Keishigomonto, Kanro-n, Hibosei-habu-maru, Hankashashin-to, Hankakoboku-to, Haiyu-sankyo-to, Shin-ishei-lung-to, Chikuba-seikyu-to, and Inhibito. Kinsan and Rikkunshito are preferred. Examples of Chinese herbal medicine prescriptions containing at least one of Scutellaria scutellariae and Scutellaria scutellariae as herbal medicines include Keishigomotto, Kanrodon, Gorinsan, Shiketsu Junchoto, Seiryuto, Shin'i Seiryuto, and the like. Further, examples containing both scutellariae and scutellariae include keishigomotto, kanro-drink, and gorinsan.

The above-mentioned Chinese herbal extract can normally contain, but is not limited to, a daily dose of 1 mg to 100 g, preferably 10 mg to 50 g, more preferably 10 mg to 10 g. In addition, in the case of a solid preparation, the amount in the preparation is usually 1 to 99% by weight, preferably 10 to 95% by weight, and more preferably 20 to 90% by weight, although there is no limitation. In the case of a liquid preparation, the amount in the preparation is usually 0.01 to 100% by weight, preferably 0.1 to 95% by weight, and more preferably 1 to 90% by weight, although there is no limitation.

The above-mentioned herbal medicine extract can normally contain, but is not limited to, a daily dose of 1 to 10,000 mg, preferably 1 to 2,000 mg, and more preferably 5 to 1,000 mg. It is.

The terpenes used in the oral composition according to the present embodiment refer to a group of natural organic compounds in general whose chemical structure is formed from units of the carbon skeleton of isoprene, such as terpenoids, terpenoids, and terpenoid compounds. etc. can be mentioned. Among them, menthol, camphor, and borneol are preferably used, and menthol is more preferably used. These can be used alone or in combination of two or more.

The above-mentioned terpenes can be contained in a range of usually 0.00001 to 40% by weight, preferably 0.0005 to 20% by weight, and preferably 0.001 to 5% by weight, based on the entire oral composition. %, and more preferably 0.01 to 2% by mass from the viewpoint of comfort upon taking.
The content ratio of terpenes to at least one of the above-mentioned Chinese herbal extract and herbal medicine extract (terpenes/herbal medicine extract) can be contained in a mass ratio of usually 0.00001 to 20, but 0.00001 to 20. It is preferably contained in a ratio of 0.00001 to 10, more preferably 0.0001 to 2, and even more preferably contained in a ratio of 0.0005 to 0.2 from the viewpoint of feeling of taking. It is even more preferable to set the ratio to 0.1. In addition, when a Chinese herbal extract and a herbal medicine extract are contained in the internal composition, the content ratio of the terpenes (terpenes/herbal medicine extract and herbal medicine extract) is relative to the total amount of the herbal medicine extract and herbal medicine extract.

Examples of the above-mentioned menthol include l-menthol and dl-menthol, but l-menthol is preferably used because it has excellent stability over time. These can be used alone or in combination of two or more.
The above-mentioned menthol can be contained generally in the range of 0.00001 to 20% by mass, but preferably 0.0005 to 10% by mass, based on the overall oral composition, and 0.0005% to 10% by mass is preferable from the viewpoint of feeling of taking it. The content is more preferably 0.01 to 5% by mass, and even more preferably 0.01 to 2% by mass.
The content ratio of menthol to at least one of the above-mentioned Chinese herbal extract and herbal medicine extract (menthol/herbal medicine extract and herbal medicine extract) can be contained in a mass ratio of usually 0.00001 to 10, but 0.0001 to 10. It is preferably contained at a ratio of 0.1 to 1, and more preferably from 0.0005 to 0.1 from the viewpoint of the feeling of taking it. In addition, when the internal medicine composition contains a Chinese herbal extract and a crude drug extract, the above-mentioned content ratio of menthol (menthol/herbal medicine extract and crude drug extract) is based on the total amount of the Chinese herbal extract and the crude drug extract.

In the internal composition according to the present embodiment, the internal composition includes all orally administered compositions, such as foods, food additives, feeds, feed additives, pet foods, pharmaceuticals, and pharmaceuticals. Examples include external products, supplements, functional foods, and beauty foods. Dosage forms include solid preparations and liquid preparations. Examples of solid preparations include granules, powders, tablets, capsules, pills, chewable preparations, jelly preparations, preparations for dissolution at the time of use (forms taken by dissolving in liquid such as dry syrup), and the like.

The internal composition according to this embodiment may contain components other than Chinese herbal extracts, crude drug extracts, and terpenes as optional components. Examples of such optional ingredients include additives, medicinal ingredients, crude drug ingredients, and the like.

Examples of the above-mentioned additives include stabilizers, stabilizers, surfactants, lubricants, lubricants, solubilizing agents, buffers, sweeteners, bases, adsorbents, flavoring agents, Binding agents, suspending agents, hardening agents, antioxidants, brightening agents, fragrances, coating agents, coatings, wetting agents, moisture regulators, fillers, antifoaming agents, cooling agents, masticating agents antistatic agents, flavoring agents, coloring agents, sugar coating agents, tonicity agents, softeners, emulsifiers, adhesives, tack enhancers, viscosity agents, foaming agents, pH adjusters, Examples include pH adjusters, excipients, dispersants, disintegrants, disintegration aids, fragrances, moisture proofing agents, preservatives, preservatives, solubilizers, solubilization aids, solvents, and fluidizing agents. These can be used alone or in combination of two or more.

Specific examples of the additives include refined white sugar, glucose, trehalose, lactose, maltose, mannitol, sorbitol, xylitol, erythritol, granulitol, sodium saccharin, aspartame, acesulfame potassium, sucralose, licorice extract, stevia extract, Lakanka extract, corn starch, potato starch, wheat starch, sodium bicarbonate, potassium bicarbonate, sodium carbonate, magnesium aluminate metasilicate, magnesium aluminate silicate, magnesium oxide, magnesium hydroxide, magnesium alumina hydroxide, magnesium carbonate , calcium carbonate, anhydrous calcium hydrogen phosphate, sodium chloride, crystalline cellulose, methylcellulose, ethylcellulose, hypromellose, hydroxypropylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, calcium carboxymethylcellulose, carmellose calcium, croscarmellose sodium, hypromellose phthalate Acid ester, cellulose acetate phthalate, dextrin, pregelatinized starch, gum arabic, gelatin, sodium alginate, polyvinylpyrrolidone, crospovidone, polyvinyl alcohol, polyethylene glycol, casein, sodium caseinate, carboxyvinyl polymer, tartaric acid, light anhydrous silicic acid, water content Silicic acid dioxide, magnesium stearate, calcium stearate, sodium stearate, sodium lauryl sulfate, talc, hydrogenated vegetable oil, macrogol, silicone oil, agar, shellac, glycerin, aromatic essential oils, water-soluble food coloring, yellow iron oxide , yellow iron sesquioxide, iron sesquioxide, brown iron oxide, black iron oxide, titanium dioxide, lake pigment, benzoic acid, sodium benzoate, paraoxybenzoic acid, cyclodextrin, polysorbate 80, glycerin fatty acid ester, propylene glycol fatty acid ester, Lecithin, white beeswax, medium chain fatty acid triglycerides, ascorbic acid, tocopherol, sodium thiosulfate, sodium edetate, plant-derived flavors (fruit flavors such as orange and lemon, coffee flavors, tea flavors), chocolate flavors, yogurt Examples include plant essential oils such as peppermint oil, lemon oil, peppermint oil, spearmint oil, and spice oil. These can be used alone or in combination of two or more.

The above-mentioned medicinal ingredients include, for example, prescriptions of Chinese herbal extracts, herbal ingredients that do not constitute herbal extracts, analgesic ingredients, antihistamine ingredients, antitussive ingredients, bronchodilator ingredients, expectorant ingredients, mucosal protective ingredients, antacid ingredients, stomach-healthy ingredients, Examples include intestinal regulating ingredients, antidiarrheal ingredients, sympathetic nerve stimulating ingredients, parasympathetic nerve blocking ingredients, caffeine, vitamins, and anti-inflammatory enzymes. These can be used alone or in combination of two or more.

The formulation of the above-mentioned Chinese herbal extract and herbal drug components that do not constitute the herbal medicine extract include not only the herbal medicine itself (herbal medicine), but also powdered herbal medicine, herbal medicine and herbal medicine powder, water, organic solvents such as ethanol, or mixtures thereof. It refers to all substances derived from extracts extracted using be. These can be used alone or in combination of two or more.

The internal composition according to the present embodiment can be obtained by mixing at least one of a Chinese herbal extract and a crude drug extract, terpenes, and other materials if necessary by a conventional method. That is, first, at least one of the above-mentioned Chinese herbal extract and herbal medicine extract (hereinafter sometimes referred to as "Chinese herbal extract, etc.") and terpenes may be mixed, and other materials may be mixed with this mixture, All the ingredients containing terpenes, such as the above-mentioned Chinese herbal extract, may be mixed at once. Alternatively, the mixed materials may be dried, sized, etc. to form a composition for internal use.

According to the internal composition according to the present embodiment, since it is excellent in suppressing moisture absorption, discoloration and deterioration due to moisture absorption are unlikely to occur, and the quality of the internal composition can be ensured for a long period of time. Furthermore, there are various types of oral compositions containing Chinese herbal extracts, such as those that are taken with water, those that are suspended in water, etc., those that are taken without water, and those that are provided as liquid preparations. Some of them produce bubbles when they come into contact with water or saliva, making them uncomfortable to take. However, the oral composition according to the present embodiment suppresses the generation of bubbles, so even in the oral composition in the form of granules, powders, liquids, etc., the feeling of taking it in the mouth is improved, It is now possible to provide it to a wide range of users. Furthermore, when it comes into contact with water or the like, the particles of the oral composition become finer, and it is expected that the absorption rate of medicinal ingredients and the like will be improved and the absorption rate will be increased. And, if it contains a Chinese herbal extract or the like, effects due to the Chinese herbal extract or the like can be expected.

Next, examples will be described together with comparative examples. However, the present invention is not limited to this. In addition, all the component compositions shown below are shown on a mass basis unless otherwise specified. Details of the Chinese herbal extract and herbal medicine extract used in the Examples and Comparative Examples are as follows.
- Keishigomototo extract, Kanrodon extract, Chikuba Seikyuto extract, Yokukansan extract, Rikkunshito extract, and Shinyi extract were manufactured according to the conventional method described in paragraph [0011].
- Hibisei Habuemaru Extract manufactured by JPS Pharmaceuticals (Kyosei Habuemaru Extract Granules G) was used.
- Hankashashinto extract manufactured by Toyo Yakushosha ([Toyo] Hankashashinto extract fine granules) was used.
- Hankakobokuto extract manufactured by Toyo Yakushosha ([Toyo] Hankakobokuto extract fine granules) was used.
- Haino-sankyu-to extract manufactured by Tsumura (Tsumura Haino-sankyu-to extract granules (medical use)) was used.

<Moisture absorption suppression rate>
[Examples 1 to 17]
Then, to 10 g of each Chinese herbal extract (dried) or herbal medicine extract (dried), l-menthol, which has been ground into powder using a mortar, is added in the amount shown in Tables 1 to 4 below, mixed, and taken internally. A composition was obtained.
Each of these internal compositions was placed in a petri dish, and the mass of each was measured immediately after the start of the experiment and 4 days after the start of the experiment under conditions 1 and 2 below.
Separately, 10 g of l-menthol alone, herbal extract (dried), or crude drug extract (dried) was placed in a petri dish and placed under conditions 1 and 2, and the mass of each was measured in the same manner.
These measurement results were applied to the following equation (1) to calculate the moisture absorption suppression rate (%) of each internal composition. The calculated results are also shown in Tables 1 to 4 below.
Condition 1: 25℃, 75%RH
Condition 2: 60℃, normal humidity

・Moisture absorption suppression rate (%) = {(B-A)-[(FE)/10]×[L-menthol addition amount (g)]}/(D-C)×100...(1)
However, A to F shall be as follows.
A: Mass (g) of the oral composition immediately after the start of the experiment
B: Mass (g) of internal composition after 4 days
C: Mass (g) of Chinese herbal medicine (or herbal medicine) extract immediately after the start of the experiment
D: Mass (g) of Chinese herbal (or herbal medicine) extract after 4 days
E: Mass of l-menthol (g) immediately after the start of the experiment
F: Mass of l-menthol after 4 days (g)
Note that some of the Chinese herbal extracts and crude drug extracts used contained various additives for the purpose of formulation and quality assurance. Therefore, in order to eliminate the influence of additives, we calculated the moisture absorption inhibition rate of each of the three products that were included in the Chinese herbal extract, etc., corn starch, lactose, and reduced maltose syrup, in the same way as the above Chinese herbal extract, etc. . As a result, almost no moisture absorption was observed for any of the additives, which indicates that there is no need to consider the influence of various additives on moisture absorption in the above-mentioned Chinese herbal extracts (additives have almost no influence). confirmed.

(1-1) Keishigomotto extract Condition 1: L-menthol addition amount (mass% relative to extract mass)
0.3% by mass, 1% by mass, 3% by mass, 5% by mass, 10% by mass

(1-2) Keishigomotto extract Condition 2: L-menthol addition amount (mass% relative to extract mass)
0.3% by mass, 0.7% by mass, 1% by mass, 3% by mass, 5% by mass, 10% by mass

(2) Kyosei Habueumaru extract, Hankakobokuto extract, Hainosankyoto extract, Shinyi extract Condition 1: L-menthol addition amount 5% by mass (mass% relative to extract mass)

(3) Takeba Seikyuto extract, Yokukansan extract Condition 1: L-menthol addition amount 0.3% by mass (% by mass based on the mass of the extract)

The results in Tables 1 to 4 above indicate that the presence of a Chinese herbal extract or herbal medicine extract and l-menthol suppresses the amount of water absorbed per amount of Chinese herbal extract or herbal medicine extract. It was also found that as the amount of l-menthol added increased, the amount of moisture absorption suppressed increased, and Examples 1 to 17 all exhibited excellent moisture absorption suppression rates (%).

<Defoaming rate (%)>
[Examples 18 to 41, Comparative Examples 1 to 9]
Oral compositions containing 5 g of each Chinese herbal extract (dried) or crude drug extract (dry) and l-menthol in the amount shown in Tables 5 to 13 were added to 50 mL of ultrapure water, stirred with a stirrer for 5 minutes, and suspended. Made it muddy.
Regarding the obtained suspension and the generated foam, the thickness a of the suspension layer and the thickness b of the foam layer were measured from the outside of the container. The sum of the thickness a of the suspension layer and the thickness b of the foam layer is the total thickness. First, the thickness b of the foam layer is applied to the following equation (2) relative to the total thickness (a + b), and the thickness of the foam layer is The ratio c was calculated. Next, the calculated proportion c of the foam layer was applied to the following formula (3) to calculate the defoaming rate (%) of each internal composition. The calculated results are also shown in Tables 5 to 13 below.
・Proportion of foam layer c=[b/(a+b)]...(2)
・Defoaming rate (%) = [1-{ratio c of foam layer of each example/ratio c of foam layer of comparative example}]×100...(3)
In addition, for the additives (corn starch, lactose, reduced maltose starch syrup) that were included in the Chinese herbal extract, herbal medicine extract, etc., the defoaming rate (%) of each of these additives was calculated in the same way as the above Chinese herbal extract, etc. As a result, no change was observed depending on the amount of l-menthol added in any of the additives, so there is no need to consider the influence of the antifoaming effect of various additives in the above-mentioned Chinese herbal extracts (depending on the amount of l-menthol added). It was confirmed that the impact was negligible.

(1) Keishigomotto extract l-menthol addition amount: 0.015g, 0.25g, 5g

(2) Added amount of kanro drink extract l-menthol: 0.015g, 0.25g, 5g

(3) Kyosei Habuemaru Extract L-menthol addition amount: 0.015g, 0.25g, 5g

(4) Hankakobokuto extract l-menthol addition amount: 0.015g, 0.25g, 5g

(5) Hainosankyuto extract l-menthol addition amount: 0.015g, 0.25g, 5g

(6) Bamboo gypsum bath extract l-menthol addition amount: 0.25g, 5g

(7) Yokukansan extract l-menthol addition amount: 0.25g, 5g

(8) Rikkunshito extract l-menthol addition amount: 0.015g, 5g

(9) Shinyi extract l-menthol addition amount: 0.015g, 0.25g, 5g

From the results in Tables 5 to 13 above, it was shown that the generation of bubbles was suppressed in all Examples 18 to 41.

<Membrane permeation effect>
[Examples 42 to 46, Comparative Examples 10 to 13]
5 g of each Chinese herbal extract (dried) or crude drug extract (dry) was added to 50 mL of ultrapure water, and stirred with a stirrer for 5 minutes to suspend.
Each of these suspensions was brought into contact with l-menthol in the amounts shown in Tables 14 to 17 below to prepare an oral composition, and this oral composition was suction-filtered using filter paper (90 mm, ADVANTEC No. 1). The time (sec) until the entire amount of the suspension was filtered was measured. The measurement results are also shown in Tables 14 to 17 below.

(1) Keishigomotto extract l-menthol addition amount: 0.25g, 5g

(2) Kanrodrink extract L-menthol addition amount: 5g

(3) Rikkunshito extract l-menthol addition amount: 5g

(4) Shinyi extract l-menthol addition amount: 5g

From the results in Tables 14 to 17 above, it was found that Examples 42 to 46 all tended to take less time for filtration, and were superior in membrane permeation. By using the Chinese herbal extract or herbal medicine extract together with l-menthol, the particles derived from the Chinese herbal extract or herbal medicine extract that had been in an aggregated state may have separated and become smaller, or the particles themselves may have become finer. .
Generally, the finer the particles, the faster they are absorbed into the body, and the absorption rate tends to be higher. It is presumed that this tendency was also observed in each of the Examples.

[Formulation example]
Oral compositions of the present invention (Formulation Examples 1 to 33) were prepared using the materials shown in Tables 18 to 25 below. Note that the materials for Formulation Examples 1 to 33 were all listed in the Japanese Pharmacopoeia. Furthermore, in the table, tablet (uncoated tablet) means an uncoated tablet, and tablet (film) means a film-coated tablet.

Formulation examples 1 to 33 shown in Tables 18 to 25 above were evaluated in the same manner as in the examples in terms of three items: moisture absorption suppression rate, defoaming rate (%), and membrane permeation effect. As a result, in all Formulation Examples 1 to 33, the same trends as in Examples were observed. Note that the moisture absorption suppression rate was not evaluated for the formulations in the form of jelly (Formulation Examples 6 and 15).

The present invention is an internal composition that effectively prevents deterioration over time and maintains excellent medicinal efficacy over a long period of time.

Claims (4)

An internal composition containing a Chinese herbal extract and terpenes,
Prescriptions of the above Chinese herbal extracts include Keishigomotsuto, Kanrodon, Hibisei Habuemaru, Hankashashinto, Hankakobokuto, Hainosankyoto, Shinyi Seilungto, Chikuba Seikyuto, Yokukansan, At least one selected from the group consisting of Rokukunshiyu,
The above terpene is l-menthol,
An internal composition characterized in that the shape of the internal composition is at least one selected from the group consisting of granules, fine granules, and powders . The internal composition according to claim 1, wherein the content of the terpenes is 0.0005 to 20% by mass based on the entire internal composition. The internal composition according to claim 1 or 2, wherein the content ratio of terpenes to the Chinese herbal extract (terpenes/herbal extract ) is 0.00001 to 10 by mass. A method for suppressing moisture absorption of an oral composition containing a Chinese herbal extract, comprising:
The formulations of the above Chinese herbal extracts include Keishigomotsuto, Kanrodon, Hibisei Habuemaru, Hankashashinto, Hankakobokuto, Hainosankyoto, Shinyi Seilungto, Chikuba Seikyuto, Yokukansan, At least one selected from the group consisting of Rikkunshiyu,
The above terpene is l-menthol,
The shape of the internal composition is at least one selected from the group consisting of granules, fine granules, and powders,
A method for suppressing moisture absorption of an internal composition , characterized by mixing the above-mentioned Chinese herbal extract and the above-mentioned terpenes without passing through an extrusion granulation process .