JP2015214530A - Gastrointestinal agent composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a new gastrointestinal agent composition having excellent prokinetic action.SOLUTION: A gastrointestinal agent composition comprises following components (A) and (B): (A) at least one selected from Perilla herb and Saussurea root and extract thereof; and (B) at least one selected from Swertia herb and extract thereof, Scopolia rhizome and extract thereof, and methylmethionine sulfonium chloride.

Description

  The present invention relates to a gastrointestinal drug composition comprising one or more selected from Soyo and Mokko and their extracts.

  Gastrointestinal drugs generally have the action of alleviating symptoms such as overeating, heartburn, leaning, stomach pain, nausea and vomiting, and are widely used to maintain or restore the gastrointestinal state to a healthy state It is subdivided into digestive drugs, stomachic medicines, antacids, compound gastrointestinal drugs, gastrointestinal analgesic drugs

Soyo (soyo) is a leaf and branch tip of perilla or chimpanzeo, has a slightly bitter taste, and is said to have excitatory sweating, antipyretic, antitussive, sedative, analgesic, diuretic, etc. In some cases, it is included in medicine.
Mokko is a root of Saussurea lappa Clarke and is used as a fragrance healthy stomach medicine. Moreover, it may be blended with gastrointestinal drugs.
On the other hand, assembly, rotcon, and methylmethionine sulfonium chloride are each used as a component of a gastrointestinal drug. Furthermore, about methylmethionine sulfonium chloride, the activation effect | action of gastrointestinal motility is also reported (patent document 1).
However, the effect of combining these has not been known so far.

International Publication No. 2006/115238

  The subject of this invention is providing the new gastrointestinal drug composition which shows the outstanding gastrointestinal motility activation effect | action.

The present inventors first confirmed the gastrointestinal motility activating action of Soyo or Moko or their extracts, and it was found that these alone do not show the gastrointestinal motility activating action.
However, as a result of diligent studies on what improves gastrointestinal motility activation when used in combination with assembly, rotcon, and methylmethionine sulfonium chloride, the above alone alone shows gastrointestinal motility activation. The present invention has been found by improving the gastrointestinal motility activating effect when used in combination with assembly, rotcon, and methylmethionine sulfonium chloride.

That is, the present invention includes the following components (A) and (B):
(A) One or more selected from Soyo and its extract (hereinafter also referred to as component (A-1)), and Moko and its extract (hereinafter also referred to as component (A-2));
(B) Assembly and extract thereof (hereinafter also referred to as component (B-1)), rotcon and extract thereof (hereinafter also referred to as component (B-2)), and methylmethionine sulfonium chloride (hereinafter referred to as component) One or more selected from (B-3));
A gastrointestinal drug composition containing the above is provided.

  The gastrointestinal composition of the present invention has a significantly enhanced gastrointestinal motility activation effect. Therefore, the gastrointestinal composition of the present invention exhibits an effect of improving symptoms such as leaning, stomach / abdominal fullness and stomach weight.

<Component (A-1)>
“Soyo” (Soyo) means leaves and branches of Perilla frutescens Britton var. Acuta Kudo or Perilla frutescens Britton var. Crispa Decaisne (Labiatae) as described in the 16th revision Japanese Pharmacopoeia. Means the destination. The shape of soyo can be adjusted as needed, and can be cut or crushed into small pieces, lumps, or pulverized into powder. In addition, in consideration of the convenience of handling at the time of production of the gastrointestinal composition, one obtained by subjecting Soyo to some kind of extraction treatment (hereinafter referred to as “Soyo extract”) may be used.
The “soyo extract” includes those subjected to processing such as heating, drying, and pulverization in addition to extraction processing. Specifically, after making soyo into an appropriate size as needed, a solution leached by adding an appropriate extraction solvent, a solution obtained by concentrating the leaching solution (soft extract, tincture, etc.), and these were further dried. Things (dry extract etc.) etc. are also included in the “soyo extract” of the present invention.
In the present invention, as one or more selected from Soyo and its extract, Soyo dry extract is preferable.

  The production method of Soyo extract is not particularly limited, for example, the description of `` Extract agent '', `` Dipping agent / decoction '', `` Tinching agent '', `` Flow extract '' in the 16th revised Japanese Pharmacopoeia It can manufacture with reference to the manufacturing method of a well-known plant extract. Specifically, for example, it can be produced by cutting, heating, drying, pulverizing, etc., if necessary, and extracting by adding an appropriate extraction solvent. The obtained extract may be further concentrated, dried, etc. as necessary.

Examples of the extraction solvent include lower monohydric alcohols such as methanol, ethanol, isopropanol, and n-butanol; lower polyhydric alcohols such as ethylene glycol, propylene glycol, 1,3-butylene glycol, and glycerin; ethers such as diethyl ether. Ketones such as acetone and ethyl methyl ketone; esters such as ethyl acetate; nitriles such as acetonitrile; alkanes such as pentane, hexane, cyclopentane and cyclohexane; halogenoalkanes such as dichloromethane and chloroform; benzene, toluene and the like And amides such as dimethylformamide; sulfoxides such as dimethyl sulfoxide; water (including hot water) and the like. These may be used alone or in combination of two or more. In the present invention, water, ethanol, or a mixture of water and ethanol is preferred.
The extraction operation is not particularly limited, and a known method used for the extraction operation from plants can be adopted. Specifically, for example, immersion in extraction solvent (cooling, digestion, percolation, etc.), super For example, extraction using a critical fluid or a subcritical fluid may be mentioned. In addition, in order to raise extraction efficiency, you may homogenize in stirring or an extraction solvent.
Although extraction temperature is not specifically limited, Although it changes with extraction solvents to be used, extraction operation, etc., it is preferable to set it as about 1 hour-14 days.

  Moreover, in this invention, you may use the Chinese prescription which contains these as a component as 1 or more types chosen from a soyo and its extract. Specific examples of such Kampo prescriptions include, for example, Kososan, Soko Shikito, Koka Shokisan (Cuckoo Shoxan), Sakai-Drinking Semi-Summer Hot Spring (Bukryo Ingou). Hangekou Bokuto), Hankakoubokuto, etc.

  In the present invention, a commercially available product can be used as one or more selected from Soyo and its extract, and specific commercial products include, for example, Soyo-style extract, dried soba extract (above, Japanese powder medicine ( Etc.).

  In the present invention, the content of one or more selected from Soyo and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, the total amount of the drug substance in terms of the active ingredient is 0 in total. 0.1 to 10% by mass is preferable, 0.1 to 5% by mass is more preferable, and 0.5 to 2% by mass is particularly preferable.

<Component (A-2)>
“Mokko” (Kika) means the root of Saussurea lappa Clarke (Compositae) as described in the 16th revision Japanese Pharmacopoeia. The shape of the mokko can be adjusted as necessary, and can be cut or crushed into small pieces, small lumps, or pulverized into powder. In addition, in consideration of the handling convenience at the time of production of the gastrointestinal composition, a product obtained by subjecting mokko to some kind of extraction treatment (hereinafter referred to as “mokko extract”) may be used.
The “mokko extract” includes those subjected to processing such as heating, drying, and pulverization in addition to extraction processing. Specifically, after the mokko was appropriately sized as necessary, a liquid that was leached by adding an appropriate extraction solvent, a liquid that concentrated the leaching liquid (soft extract, tincture, etc.), and these were further dried. Things (dry extract etc.) etc. are also included in the “mokko extract” of the present invention.
In the present invention, as the one or more selected from mokko and its extract, mokko soft extract is preferable.

  The method for producing the mock-up extract is not particularly limited, and for example, the extract can be produced by the same method as the method for producing the soy extract.

  Moreover, in this invention, you may use the Kampo prescription which contains these as a component as 1 or more types chosen from mokko and its extract. Specific examples of such Kampo prescriptions include, for example, Kuretsusanxan, Kishikunnitto, Kishito, Kikuchou blood drinking Kyotake Twin Daiichikagen), Kumi Bintoyu, Kosa Yoyoto, Koshikyosan, Gyutsusan, Shoumeto, Ginsou ), Shitsukushi-shi-to, Zenshi-byaku-jutsu-san, Ding-Kang-ta-yu, Nyoshin-san, Bunsho-to, Ki-Shi-to ) And the like.

  In the present invention, as one or more kinds selected from mokko and its extract, commercially available products can be used. Specific examples of commercially available products include wood powder, wood incense extract, wood incense extract (above, Nippon Powdery Chemical Co., Ltd.), Mokko soft extract (Ogi Pharmaceutical Co., Ltd.) and the like.

  In the present invention, the content of one or more selected from mokko and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, the total amount of the drug substance in terms of the active ingredient is 0 in total. It is preferable to contain 1-30 mass%, it is more preferable to contain 0.5-20 mass%, and it is especially preferable to contain 1-10 mass%.

  In the present invention, at least one selected from the component (A) soyo and mokko and their extracts is at least one selected from soyo and its extract from the viewpoints of gastrointestinal motility activation and bitterness suppression. It is preferable that the above is included.

<Component (B-1)>
“Assembly” (this drug) means the whole plant in the flowering period of the assembly (Swertia japonica Makino (Gentianaceae)) as described in the 16th revision Japanese Pharmacopoeia.

In addition, as shown in Test Example 4 below, the assembly exhibits an extremely strong bitter taste and is selected from the soyo and the extract thereof even though at least one kind selected from the soyo and the extract thereof exhibits a bitter taste. It became clear that 1 or more types have the effect | action which suppresses the bitter taste of the said assembly.
Therefore, the gastrointestinal composition of the present invention comprising at least one selected from Soyo and its extract as component (A) and at least one selected from assembly and its extract as component (B). It has an effect of activating the gastrointestinal motility, suppressing the bitter taste derived from the assembly, being easy to take, and excellent in compliance.

From another viewpoint, the present invention provides the following components (A-1) and (B-1):
(A-1) One or more selected from Soyo and its extract;
(B-1) one or more selected from assemblies and extracts thereof;
Is provided (preferably a gastrointestinal drug composition). Such a composition can be suitably used as a medicine (for example, a gastrointestinal drug) having good compliance with taking advantage of the pharmacological action of soyou and assembly because the bitterness derived from the assembly is suppressed and easy to take. In addition, the quantity of various components in the composition of such an aspect, a combination ratio, etc. are the same as that in the gastrointestinal medicine composition containing component (A) and (B).
Furthermore, from another point of view, the present invention is a method for suppressing bitterness derived from at least one selected from the assembly and the extract thereof (preferably characterized in that at least one selected from Soyo and the extract thereof is allowed to coexist. Is a pharmaceutical composition (preferably a gastrointestinal composition) containing at least one member selected from the assembly and its extract, characterized in that it contains at least one member selected from soyo and its extract. Bitterness control method). In addition, the amount of various components, the combination ratio, and the like in the method of this aspect are the same as those in the gastrointestinal composition containing components (A) and (B).

The form of the assembly can be adjusted as needed, and can be cut or crushed into small pieces, small chunks, or pulverized into powder. For example, “assembly powder” in which the assembly is powdered can also be used in the present invention. Can do. In addition, in consideration of the convenience of handling during production of the gastrointestinal composition, a product obtained by subjecting the assembly to some kind of extraction (hereinafter referred to as “assembly extract”) may be used.
The “assembly extract” includes those subjected to processing such as heating, drying, and pulverization in addition to extraction processing. Specifically, after the assembly was appropriately sized as necessary, a liquid leached by adding an appropriate extraction solvent, a liquid (such as a soft extract or tincture) obtained by concentrating the leached liquid, and these were further dried. Things (dry extract etc.) etc. are also included in the “assembly extract” of the present invention.
In the present invention, the assembly powder is preferably used as one or more selected from the assembly and its extract.

  The method for producing the assembly extract is not particularly limited, and for example, the assembly extract can be produced by a method similar to the method for producing the soy extract.

  In the present invention, as one or more kinds selected from the assembly and its extract, a commercially available product can be used. Specific examples of the commercially available product include assembly powder, Nisshin Sembly Sodasan (above, Nippon Powder Chemicals ( Etc.).

In the present invention, the content of one or more selected from the assembly and the extract thereof is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, the total amount of the drug substance in terms of the active ingredient is 0 in total. 0.001 to 10% by mass, preferably 0.01 to 7.5% by mass, more preferably 0.05 to 5% by mass, and 0.1 to 4% by mass It is more preferable to contain 0.25 to 3% by mass, and it is particularly preferable to contain 0.5 to 2% by mass.
Moreover, the combination ratio of one or more selected from Soyo and its extract and one or more selected from the assembly and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, bitterness suppression action, One or more selected from Soyo and its extract is 1 part by mass in terms of bulk drug, and one or more selected from assembly and its extract is 0.1 to 10 parts by weight in terms of bulk drug, more preferably Are preferably combined in a proportion of 0.1 to 5 parts by mass, particularly preferably 0.5 to 2 parts by mass.
Furthermore, the combination ratio of at least one selected from mokko and its extract and at least one selected from assembly and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, mokko and its extraction One or more selected from the product in terms of the amount of the active ingredient is 1 part by weight, and one or more selected from the assembly and the extract thereof is 0.01 to 5 parts by weight in terms of the amount of the active ingredient, more preferably 0.05. It is preferable to combine at a ratio of ˜2 parts by mass, particularly preferably 0.1 to 1.5 parts by mass.

<Component (B-2)>
The “rotcon” is a rhizome and root of a ashirodokoro (Scopolia japonica Maximowicz, Scopolia carniolica Jacquin or Scopolia parviflora Nakai (Solanaceae)) as described in the 16th revision Japanese Pharmacopoeia. The shape of the rotcon can be adjusted as necessary, and it can be cut or crushed into small pieces, lumps, or pulverized into powder. In addition, in consideration of the convenience of handling during production of the gastrointestinal composition, a product obtained by subjecting the funnel to some kind of extraction treatment (hereinafter referred to as “rotcon extract”) may be used.
The “rotcon extract” includes those subjected to processing such as heating, drying and pulverization in addition to the extraction. Specifically, after making the size of the rotocon as appropriate, a liquid that was leached by adding an appropriate extraction solvent, a liquid that concentrated the leachate (soft extract, tincture, etc.), and these were further dried. Things (dry extract etc.) etc. are also included in the “rotcon extract” of the present invention. Specific examples of such a rotocon extract include, for example, the “roto extract” described in the 16th revision of the Japanese Pharmacopoeia (the crude powder of “rotocon”, 35 vol% ethanol, “normal water”, “purified water”). Or “purified water (in a container)” as a leaching agent, and a soft extract by a method for producing an extract).
In the present invention, a funnel extract is preferred as at least one selected from rotocon and its extract.

  The production method of the rotcon extract is not particularly limited, and for example, it can be produced by the same method as the production method of the above-mentioned Soyo extract.

  In the present invention, a commercially available product can be used as one or more selected from rotocon and an extract thereof, and specific examples of commercially available products include, for example, Rohto extract Triplex (manufactured by Alps Pharmaceutical Co., Ltd.). Is mentioned.

In the present invention, the content of one or more selected from rotocon and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, the total mass of the gastrointestinal drug composition is 0.1 to 10 mass. % Content is preferable. In particular, when a funnel extract is used as one or more selected from rotocon and its extract, it is preferably contained in a total amount of 0.1 to 10% by mass, based on the total mass of the gastrointestinal composition, 0.1 to 5% by mass. % Is more preferable, 0.5 to 3% by mass is more preferable, and 0.5 to 2% by mass is particularly preferable.
Moreover, the combination ratio of at least one selected from Soyo and its extract and at least one selected from Rotocon and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, Soyo and its extraction It is preferable to combine 1 or more types selected from the product in a ratio of 0.1 to 10 parts by mass with respect to 1 part by mass in terms of bulk drug substance, based on one or more types selected from rotcon and its extract. In particular, when a funnel extract is used as one or more selected from rotocon and its extract, one or more selected from soyo and its extract is 0.1 to 1 part by mass in terms of the active ingredient, and 0.1 to 0.1 A combination of 10 parts by mass, more preferably 0.1 to 5 parts by mass, and particularly preferably 0.5 to 2 parts by mass is preferable.
Furthermore, the combination ratio of at least one selected from mokko and its extract and at least one selected from rotocon and its extract is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, mokko and its extraction It is preferable to combine 1 or more types selected from the product in a ratio of 0.5 to 5 parts by mass with respect to 1 part by mass in terms of the active ingredient. In particular, when a funnel extract is used as one or more selected from rotocon and its extract, 0.05 or more funnel extract is used with respect to 1 part by mass of the raw drug equivalent of one or more selected from mokko and its extract. It is preferable to combine at a ratio of 15 parts by mass, more preferably at a ratio of 0.1 to 10 parts by mass, particularly preferably at a ratio of 0.5 to 5 parts by mass.

<Component (B-3)>
“Methylmethionine sulfonium chloride” (hereinafter referred to as MMSC in the present specification) is a component also known as vitamin U. In the present invention, a commercially available product can be used as the MMSC. Specific examples of the commercially available product include U-bit “Hamawaiwai” (manufactured by Yonezawa Hamari Chemical Co., Ltd.).

In the present invention, the content of MMSC is not particularly limited, but it is preferably 0.1 to 10% by mass based on the total mass of the gastrointestinal drug composition, from the viewpoint of activating gastrointestinal motility, and 1 to 7%. The content is more preferably 5% by mass, and particularly preferably 2.5 to 5% by mass.
Moreover, the combination ratio of at least one selected from Soyo and its extract and MMSC is not particularly limited, but from the viewpoint of gastrointestinal motility activation action, at least one selected from Soyo and its extract is a crude drug. It is preferable to combine MMSC at a ratio of 0.1 to 15 parts by mass, more preferably 1 to 10 parts by mass, and particularly preferably 2.5 to 7.5 parts by mass with respect to 1 part by mass in terms of converted amount.
Furthermore, the combination ratio of one or more selected from Mkko and its extract and MMSC is not particularly limited, but from the viewpoint of activating gastrointestinal motility, one or more selected from Mkko and its extract is a crude drug. MMSC is combined at a ratio of 0.5 to 70 parts by mass, more preferably 1 to 50 parts by mass, further preferably 3 to 30 parts by mass, and particularly preferably 5 to 20 parts by mass with respect to 1 part by mass in terms of conversion amount. Is preferred.

  In the present invention, at least one assembly selected from the component (B) assembly and extract thereof, rotocon and extract thereof, and methylmethioninesulfonium chloride is at least assembly from the viewpoint of gastrointestinal motility activation action and bitterness suppression action. And at least one selected from the extract thereof, and more preferably a combination of at least one selected from the assembly and the extract thereof, and rotocon and the extract thereof or methylmethionine sulfonium chloride, A combination of at least one selected from the assembly and its extract, at least one selected from the rotocon and its extract, and methylmethionine sulfonium chloride is particularly preferable.

  The gastrointestinal drug composition of the present invention has an excellent gastrointestinal motility activation effect as shown in the following test examples. Therefore, the gastrointestinal composition of the present invention is suitable for use in activating gastrointestinal motility, and causes symptoms such as leaning, stomach / abdominal fullness, and stomach weight caused by retention of gastrointestinal contents. Especially suitable for use to ameliorate these symptoms caused by excessive drinking or eating.

The administration method of the gastrointestinal composition of the present invention is not particularly limited and includes oral administration and parenteral administration, but oral administration is preferable from the viewpoint of gastrointestinal motility activation action.
The dosage form of the gastrointestinal pharmaceutical composition of the present invention is not particularly limited, and may be appropriately formulated as a dosage form described in the 16th revision Japanese Pharmacopoeia according to the above administration method. Specific examples of such dosage forms include solid forms of gastrointestinal compositions such as powders, granules, tablets, pills, soft capsules, and hard capsules; and liquid forms such as drinks. Gastrointestinal composition; gastrointestinal composition in semi-solid form such as jelly. In the present invention, from the viewpoint of ease of administration, it is preferably a solid gastrointestinal composition, particularly preferably a powder, granule, or tablet.

  In the gastrointestinal composition of the present invention, in addition to the above-described components, pharmaceutically acceptable carriers (excipients, binders, disintegrants, lubricants, coloring agents, corrigents, etc. according to the above-mentioned dosage forms) 1 type or 2 types or more of a coating agent, etc.).

  Examples of the excipient include lactose, starches, crystalline cellulose, sucrose, mannitol, light anhydrous silicic acid and the like. Examples of the binder include hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, pregelatinized starch, polyvinylpyrrolidone, polyvinyl alcohol, pullulan and the like. Examples of the disintegrant include sodium carboxymethyl starch, carmellose, carmellose calcium, croscarmellose sodium, crospovidone, corn starch, and low-substituted hydroxypropylcellulose. Examples of the lubricant include magnesium stearate and talc. Examples of the colorant include tar pigments and iron sesquioxide. Examples of the corrigent include stevia and aspartame. Coating agents include film-forming polymers such as carboxymethyl ethyl cellulose, cellulose acetate phthalate, methacrylic acid copolymer S, methacrylic acid copolymer L, methacrylic acid copolymer LD, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate. Can be mentioned. When forming a film, a plasticizer such as triethyl citrate, triacetin, polyethylene glycol, talc, titanium oxide, yellow ferric oxide, ferric oxide, legal dye, light anhydrous silicic acid, hydrous silicon dioxide, etc. It can also be blended. In this invention, these 1 type (s) or 2 or more types can be mix | blended combining suitably.

  In addition to the above-mentioned components, the gastrointestinal composition of the present invention includes other pharmaceutical components (for example, local anesthetics, digestive agents (bilibrous agents), digestive enzymes, gastric mucosal repair agents (mucosal protective components)). 1 type or 2 types or more of herbal medicine ingredients, antacids, etc.).

  Examples of the local anesthetic include ethyl aminobenzoate, oxesasein and the like. Examples of the digestive agent (bile agent) include ursodeoxycholic acid, animal gall (bear gall, bovine gall) and the like. Examples of digestive enzymes include starch digestive enzymes (biodiastase, takadiastase), fat digestive enzymes (lipase) and the like. Examples of the gastric mucosa repair agent (mucosal protective component) include copper chlorofin sodium, copper chlorofin potassium, aldioxa, sucralfate, cetraxate hydrochloride, sofalcone, gefarnate, trimebutine maleate, and sodium azulene sulfonate. Herbal medicine ingredients include Asenya, Anise, Aloe, Fennel, Turmeric, Ubai, Uyaku, Engosaku, Life-grass, Ogon, Owaku, Auren, Processed Oyster, Gadju, Cuckoo, Karamus Root, Kankyo, Daylily, Pheasant, Kujin, Keihi , Ketsumeishi, Gentiana, Gennoshouko, Kojin, Koboku, Goshuyu, Pepper, Colombo, Conzurango, Hawthorn, Salamander, Yamana, Soshishi, Peonies, Shukusha, Shokyo, Shozukoku, Akatsuki, Red bud, Isodon, Centaurium grass , Otsuka, Daio, Chikutsu Carrot, Clove, Chinpi, Pepper, Spruce, Nigaki, Nikuzuku, Carrot, Pepper, Pepper, Papilio, Peacock, Hop, Homica, Sleeping Leaves, Yakuchi, Papilio, Ryu Crude drugs or extracts thereof such as emissions and Ryo ginger and the like. Antacids include proton pump inhibitors such as omeprazole, lansoprazole, and rabeprazole sodium; H2 receptor antagonists such as cimetidine, ranitidine hydrochloride, and famotidine; dry aluminum hydroxide gel, magnesium aluminate silicate, aluminate metasilicate Magnesium, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, magnesium oxide, magnesium alumina hydroxide, aluminum hydroxide gel, aluminum hydroxide / sodium bicarbonate coprecipitation product, aluminum hydroxide / magnesium carbonate mixed dry gel , Aluminum hydroxide / magnesium carbonate / calcium carbonate coprecipitation products, magnesium hydroxide, sodium bicarbonate, magnesium carbonate, precipitated calcium carbonate, magnesium aluminometasilicate Anhydrous calcium hydrogen phosphate, inorganic salts such as calcium hydrogen phosphate; cuttlefish bone, stone Ke'Akira, Borei, amino acid, dihydroxy aluminum aminoacetate, and the like. In this invention, these 1 type (s) or 2 or more types can be mix | blended combining suitably.

  The dose of the gastrointestinal composition of the present invention to humans may be appropriately adjusted according to the dosage form, the degree of disease, the age of the patient, etc., for example, one or more selected from Soyo and its extract When contained, based on this, it is sufficient to administer about 50 to 3000 mg / day, particularly about 100 to 2000 mg / day, in terms of bulk drug substance for normal adults. The dosage of other components can also be determined with reference to the combination ratio. In addition, for example, in the case of containing one or more selected from mokko and its extract, on the basis of this, it is preferably about 100 to 5000 mg / kg in terms of a crude drug, and particularly 500 to 3000 mg / kg. About kg is more preferable. In accordance with such a dose, the dose of other components can also be determined with reference to the combination ratio described above.

  EXAMPLES The present invention will be described in detail below with reference to examples, but the present invention is not limited to these examples.

[Test Example 1] Confirmation of gastrointestinal motility activation effect of Soyo extract alone 6 to 7-week-old ddY male mice fasted from the day before the test were 6 mice in each group so that the average body weight was equal 2 They were divided into groups, which were a test drug administration group and a control group, respectively.

  Mice in the test drug administration group received 30 mg / kg body weight (soy sauce dry extract: manufactured by Nippon Flour Pharmaceutical Co., Ltd.) dissolved in 0.5% methylcellulose aqueous solution (concentration of crude drug: 270 mg / kg body weight). The mice in the control group were each orally administered with a 0.5% methylcellulose aqueous solution, and 10 minutes later, 5% activated carbon powder suspension was orally administered at a dose of 0.1 mL / 10 g body weight.

Twenty minutes after administration of the activated carbon powder suspension, the mice were killed by cervical dislocation, and the intestinal tract from the stomach pylorus to the terminal ileum was removed. For each of the test drug administration group and the control group, calculate the average value of the migration rate of the carbon powder (the ratio of the migration distance from the pylorus to the total length of the extracted intestinal tract), and further calculate the average value of the migration rate of the control group. By calculating the relative index of the average value of the migration rate of the test drug administration group when set to 1, the presence or absence of activation of gastrointestinal motility by administration of the test drug was confirmed.
The results are shown in Table 1.

  Since the relative index of the migration rate of the test drug administration group was smaller than 1, it was confirmed that gastrointestinal motility was not activated when Soyo was administered alone at a dose of 270 mg / kg body weight (concentration of drug substance). .

[Test Example 2] Evaluation of gastrointestinal motility activation effect by combined administration of Soyo extract and other drugs: 6-7 week old ddY male mice fasted from the day before the test so that the average body weight becomes uniform Each group was divided into 2 groups of 6 animals, and they were designated as test drug A administration group (Group A) and test drug B administration group (Group B), respectively.

  The following test drug dissolved or suspended in 0.5% methylcellulose was orally administered to each group of mice, and 10 minutes later, 5% activated carbon powder suspension was orally administered at a dose of 0.1 mL / 10 g body weight. did.

  Twenty minutes after administration of the activated carbon powder suspension, the mouse was killed by cervical dislocation, and the intestinal tract from the stomach pylorus to the terminal ileum was removed, and then the carbon powder migration rate (movement distance from the pylorus) for each group. Of the total length of the isolated intestinal tract).

The test drug was as follows.
Group A: assembly (end of assembly: manufactured by Nippon Powder Chemical Co., Ltd.) 30 mg / kg body weight, rotokon extract (roth extract 3 times powder: manufactured by Alps Pharmaceutical Co., Ltd.) 90 mg / kg body weight (30 mg / kg as funnel extract) Body weight) and methylmethionine sulfonium chloride (Yonezawa Hamari Pharmaceutical Co., Ltd.) 150 mg / kg body weight combination Group B: Soyo extract (Suyo dried extract: Nippon Powdered Chemical Co., Ltd.) 30 mg / kg body weight (raw Table 2 shows the combined use results of the combination of 270 mg / kg body weight) and the group A as herbal medicine equivalent amount. The transfer rate of carbon powder was expressed as an average value.

From the results of Table 2, it is clear that even in a dose where gastrointestinal motility is not activated by Soyo alone, an excellent gastrointestinal motility activating effect is exhibited by combining with assembly, funnel extract and methylmethionine sulfonium chloride. became.
From the above test results, the combination of one or more selected from Soyo and its extract and one or more selected from assembly and its extract, rotcon and its extract, and methylmethionine sulfonium chloride is excellent digestion. It became clear that the tube movement activation effect was shown.

[Test Example 3] Evaluation of effect of gastrointestinal drug composition on abdominal indefinite complaints A male volunteer (41 years old) complaining of abdominal indefinite complaints (rest, stomach / abdominal fullness and stomach weight), with the following consent: Tablets containing the ingredients and general-purpose excipients were dosed 2 tablets at a time, 3 times a day for 2 days in the usage after each meal.
<Tablet components: 6 tablets>
Soyo Dry Extract 270mg (Drug equivalent)
Assembly powder 30mg
Rohto extract 90mg
Methylmethioninesulfonium chloride 150mg

After the medication, interviews were conducted regarding the above indefinite complaints, and an answer that all symptoms were alleviated was obtained.
From the above test results, it was revealed that the gastrointestinal pharmaceutical composition of the present invention is effective for leaning, stomach / abdominal fullness and abdominal indefinite complaints including stomach weight. In addition, it was guessed that such an effect | action was based on that the stay of the digestive tract contents was eliminated by the digestive tract exercise | movement activation effect | action confirmed by the said test examples 1 and 2. FIG.

[Test Example 4] Evaluation of Bitter Taste Inhibitory Action by Soyo Extract 10 Panelists feel the bitterness of bitter taste when 5mg each is placed on the tongue tip for 5 seconds each. Had enough time for evaluation.
Evaluation of the feeling of taking (bitter taste) was performed by scoring according to the following evaluation criteria.
(Evaluation criteria)
“I almost don't care about bitterness”: 2 points “I am slightly worried about bitterness”: 1 point “I feel bitter and my tongue numb”: 0 points

  The sensory test results (total score of all panelists) are shown in Table 3.

From the results in Table 3, it became clear that Soyo has the action of suppressing the bitter taste of the assembly.
From the above test results, the gastrointestinal composition containing at least one selected from Soyo and its extract and at least one selected from the assembly and its extract is taken with a bitter taste derived from the assembly suppressed. It became clear that it was excellent in feeling.

[Test Example 5] Confirmation of gastrointestinal motility activation effect of mock-up extract alone 6 to 7-week-old ddY male mice fasted from the day before the test were 5 mice in each group so that the average body weight was equal 2 They were divided into groups, which were a test drug administration group and a control group, respectively.

  The mice in the test drug administration group received 105 mg / kg body weight (mokkou soft extract: manufactured by Oshiro Seiyaku Co., Ltd.) dissolved in 0.5% methylcellulose aqueous solution (concentration in bulk drug: 808.5 mg / kg body weight). The mice in the control group were each orally administered with a 0.5% methylcellulose aqueous solution, and 30 minutes later, a phenol red solution (20% sucrose solution) was orally administered to the mice in both groups in a dose volume of 0.25 mL.

Fifteen minutes after administration of the phenol red solution, the mouse was killed by cervical dislocation, the gastric cardia and pylorus were ligated, and the stomach was removed. The excised stomach was cut into small pieces, and 10 mL of 0.1 M NaOH aqueous solution was added thereto and stirred. After standing for 30 minutes, 3 mL of the supernatant was collected. To the obtained supernatant, 0.3 mL of 20% trichloroacetic acid aqueous solution was added and stirred, and then centrifuged (3000 rpm, 20 minutes). An equal amount of 0.5 M NaOH aqueous solution was added to the obtained centrifugal supernatant, and 560 nm Absorbance was measured and used as an index of the amount of pigment in the stomach.
Separately, the amount of dye in the stomach (absorbance at 560 nm) immediately after administration of the dye solution was measured in the same manner, and the amount of dye in the stomach immediately after administration of the dye solution was determined for each of the test drug administration group and the control group. The average value of the gastric emptying rate of the pigment when calculated as%, and the relative index of the average value of the gastric emptying rate of the test drug administration group when the average value of the gastric emptying rate of the control group is 1 is calculated. The presence or absence of activation of gastrointestinal motility by administration of the test drug was confirmed by calculation.
The results are shown in Table 4.

  Since the relative index of the migration rate of the study drug administration group is less than 1, it is confirmed that the gastrointestinal motility is not activated when mokko is administered alone at a dose of 808.5 mg / kg body weight (raw drug substance equivalent) It was done.

[Test Example 6] Evaluation of gastrointestinal motility activation effect by co-administration of mokko extract and other drugs: 6-7 week old ddY male mice fasted from the day before the test so that the average body weight is uniform Each group was divided into 2 groups of 6 animals, and they were designated as test drug A administration group (Group A) and test drug B administration group (Group B), respectively.

  The following test drug dissolved or suspended in 0.5% methylcellulose was orally administered to each group of mice, and 10% later, 5% activated carbon powder suspension was orally administered at a dose of 0.1 mL / 10 g body weight. did.

  Twenty minutes after administration of the activated carbon powder suspension, the mouse was killed by cervical dislocation, and the intestinal tract from the stomach pylorus to the terminal ileum was removed, and then the carbon powder migration rate (movement distance from the pylorus) for each group. Of the total length of the isolated intestinal tract).

The test drug was as follows.
Group A: Assembly (end of assembly: manufactured by Nippon Powder Chemical Co., Ltd.) 90 mg / kg body weight, Rotcon extract (Roth extract 3 times powder: manufactured by Alps Pharmaceutical Co., Ltd.) 270 mg / kg body weight (90 mg / kg as funnel extract) Body weight) and methylmethionine sulfonium chloride (manufactured by Yonezawa Hamari Pharmaceutical Co., Ltd.) 450 mg / kg body weight Group B: Mockow extract (Mockow soft extract: manufactured by Ogi Seiyaku Co., Ltd.) 105 mg / kg body weight Table 5 shows the results of the combined use of the combination of group A and 808.5 mg / kg body weight). The transfer rate of carbon powder was expressed as an average value.

From the results of Table 5, it is clear that even in the doses in which gastrointestinal motility is not activated by Mokko alone, an excellent gastrointestinal motility activating effect is exhibited by combining with assembly, funnel extract and methylmethionine sulfonium chloride. became.
From the above test results, a combination of one or more selected from mokko and its extract and one or more selected from assembly and its extract, rotcon and its extract, and methylmethionine sulfonium chloride is excellent digestion. It became clear that the tube movement activation effect was shown.

[Test Example 7] Evaluation of effect of gastrointestinal drug composition on abdominal indefinite complaints Male volunteers (42 years old) complaining of abdominal indefinite complaints (rest and stomach / abdominal bloating) agreed with the following components: Tablets containing general-purpose excipients were dosed 2 tablets at a time, 3 times a day, after each meal for 2 days.
<Tablet components: 6 tablets>
Mokko soft extract 270mg (Drug equivalent)
Assembly powder 30mg
Rohto extract 90mg
Methylmethioninesulfonium chloride 150mg
After the medication, interviews were conducted regarding the above indefinite complaints, and an answer that all symptoms were alleviated was obtained.
From the above test results, it was revealed that the gastrointestinal composition of the present invention is effective against lean and indefinite complaints of the abdomen including the stomach / abdominal fullness. In addition, it was guessed that such an effect | action was based on the stay of the digestive tract contents having been canceled by the digestive tract exercise | movement activation effect | action confirmed by the said test examples 5 and 6. FIG.

[Production Example 1]
Tablets containing the following components in 6 tablets were produced by a conventional method.
Takadiastase T 150mg
Methylmethioninesulfonium chloride 150mg
Soyo Dry Extract 270mg (Drug equivalent)
Ursodeoxycholic acid 16mg
Rohto extract 30mg
Sodium bicarbonate 1500mg
Magnesium aluminate metasilicate 750mg
Tokyo 20mg
Keihi 20.5mg
Nutmeg 20mg
l-Menthol 3.5mg
Lactose hydrate 270mg
Corn starch 100mg
Crystalline cellulose 275mg
Hydroxypropylcellulose 24mg
Carmellose calcium 70mg
Magnesium carbonate 250mg
Methylcellulose 50mg
Talc 26mg
Macrogol 50mg
Magnesium stearate 5mg
Perfume

[Production Example 2]
Tablets containing the following components in 6 tablets were produced by a conventional method.
Methylmethioninesulfonium chloride 150mg
Soyo Dry Extract 270mg (Drug equivalent)
Rohto extract 90mg
Assembly powder 30mg
Keihi powder 20.5mg
Biodiastase 2000 24mg
Lipase AP12 15mg
Sodium bicarbonate 700mg
Precipitated calcium carbonate 1200mg
Magnesium carbonate 250mg
Hydroxypropylcellulose 24mg
Hardened oil 206mg
Polyvinyl alcohol 106mg
Carmellose calcium 142.5mg
Corn starch 24mg
Crystalline cellulose 274mg
Low-substituted hydroxypropylcellulose 133mg
Hydrous silicon dioxide 29.5mg
10 mg glyceryl monostearate
Polyoxyl stearate 3mg
Purified shellac 4mg
Talc 26.5mg
l-Menthol 4mg
Magnesium stearate 14.5mg

[Production Example 3]
Fine granules containing the following components in 3 packets were produced by a conventional method.
L-glutamine 405mg
Soyo powder 200mg
Cinnamon 150mg
Cinnamon oil (Keihi oil) 6mg
Shredded sand 90mg
This medicine (Assembly) 3mg
Sodium bicarbonate 1950mg
Heavy magnesium carbonate 600mg
Precipitated calcium carbonate 300mg
Sanalmin 399mg
Rohto extract 30mg
Diasmen SS 240mg
Prozyme 51mg
l-Menthol 5mg
Crystalline cellulose 200mg
Silicate Al 50mg
Stearic acid Mg 50mg

[Production Example 4]
Tablets containing the following components in 6 tablets were produced by a conventional method.
Takadiastase T 150mg
Methylmethioninesulfonium chloride 150mg
Mokko dry extract 100mg (Drug equivalent)
Ursodeoxycholic acid 16mg
Rohto extract 30mg
Sodium bicarbonate 1500mg
Magnesium aluminate metasilicate 750mg
Tokyo 20mg
Keihi 20.5mg
Nutmeg 20mg
l-Menthol 3.5mg
Lactose hydrate 270mg
Corn starch 100mg
Crystalline cellulose 275mg
Hydroxypropylcellulose 24mg
Carmellose calcium 70mg
Magnesium carbonate 250mg
Methylcellulose 50mg
Talc 26mg
Macrogol 50mg
Magnesium stearate 5mg
Perfume

[Production Example 5]
Tablets containing the following components in 6 tablets were produced by a conventional method.
Methylmethioninesulfonium chloride 150mg
Mokko dry extract 300mg (Drug equivalent)
Rohto extract 90mg
Assembly powder 30mg
Keihi powder 20.5mg
Biodiastase 2000 24mg
Lipase AP12 15mg
Sodium bicarbonate 700mg
Precipitated calcium carbonate 1200mg
Magnesium carbonate 250mg
Hydroxypropylcellulose 24mg
Hardened oil 206mg
Polyvinyl alcohol 106mg
Carmellose calcium 142mg
Corn starch 24mg
Crystalline cellulose 274mg
Low-substituted hydroxypropylcellulose 133mg
Hydrous silicon dioxide 29.5mg
10 mg glyceryl monostearate
Polyoxyl stearate 3mg
Purified shellac 4mg
Talc 26.5mg
l-Menthol 4mg
Magnesium stearate 14.5mg

[Production Example 6]
Fine granules containing the following components in 3 packets were produced by a conventional method.
L-glutamine 405mg
Mockow powder 80mg
Soyo powder 200mg
Cinnamon 150mg
Cinnamon oil (Keihi oil) 6mg
Shredded sand 90mg
This medicine (Assembly) 3mg
Sodium bicarbonate 1950mg
Heavy magnesium carbonate 600mg
Precipitated calcium carbonate 300mg
Sanalmin 399mg
Rohto extract 30mg
Diasmen SS 240mg
Prozyme 51mg
l-Menthol 5mg
Crystalline cellulose 200mg
Silicate Al 50mg
Stearic acid Mg 50mg

[Production Example 7]
Tablets containing the following components in 6 tablets were produced by a conventional method.
Methylmethioninesulfonium chloride 150mg
Soyo Dry Extract 270mg (Drug equivalent)
Rohto extract 90mg
Assembly powder 30mg
Keihi powder 20.5mg
Biodiastase 2000 24mg
Prozyme 6 18mg
Lipase AP12 15mg
Sodium bicarbonate 700mg
Precipitated calcium carbonate 1200mg
Magnesium carbonate 250mg
Hydroxypropylcellulose 24mg
Hardened oil 206mg
Polyvinyl alcohol 106mg
Carmellose calcium 124.5mg
Corn starch 24mg
Crystalline cellulose 274mg
Low-substituted hydroxypropylcellulose 133mg
Hydrous silicon dioxide 29.5mg
10 mg glyceryl monostearate
Polyoxyl stearate 3mg
Purified shellac 4mg
Talc 26.5mg
l-Menthol 4mg
Magnesium stearate 14.5mg

  According to the present invention, the gastrointestinal motility activation effect is remarkably enhanced even if it does not contain sojutsu or its extract, and it is suitable for improving symptoms such as leaning, stomach / abdominal fullness and stomach weight. Gastrointestinal composition that can be used in the pharmaceutical industry and can be used in the pharmaceutical industry, quasi-drug industry, and the like.

Claims (6)

The following components (A) and (B):
(A) One or more selected from Soyou and Moko and their extracts;
(B) at least one selected from assembly and extract thereof, rotocon and extract thereof, and methylmethionine sulfonium chloride;
A gastrointestinal composition comprising:   The gastrointestinal medicinal composition according to claim 1, wherein the component (A) contains at least one selected from Soyo and its extract.   The gastrointestinal composition according to claim 1 or 2, wherein the component (B) contains at least one selected from the assembly and an extract thereof.   The component (B) is a combination of one or more selected from the assembly and the extract thereof, one or more selected from the rotocon and the extract thereof, and methylmethionine sulfonium chloride. 2. The gastrointestinal composition according to item 1.   The gastrointestinal composition according to any one of claims 1 to 4, which is used for activation of gastrointestinal motility.   The gastrointestinal drug composition according to any one of claims 1 to 5, which is used for leaning, stomach / abdominal bloating or gastric weight.