Compressed solid composition

Abstract

This invention provides a compressed solid composition that suppresses unpleasant tastes in the oral cavity and provides a refreshing sensation in the throat. This is the challenge. [Solution] In this invention, (A) an inorganic compound-based antacid, a starch digesting enzyme, and a protein Digestive enzymes, fat digestive enzymes, oyster shell, cinnamon, licorice, dried tangerine peel, magnolia bark, and red bean One or more selected from the group consisting of kisses; and (B-1) monoterpenes and / or (B -2) A compressed solid composition containing sugar alcohol, (C) with a maximum diameter of 1 to 4 mm, (D) A compressed solid composition is prepared in which the ratio of height to maximum diameter is 0.5 to 2. ru.

Description

Technical Field

[0001] The present invention relates to a compressed solid composition having an excellent taste during administration.

Background Art

[0002] In a compressed solid composition such as a tablet, there are problems of unpleasant tastes such as bitterness caused by a medicinal ingredient during administration and difficulty in swallowing. Particularly, general pharmaceuticals such as Kampo preparations containing crude drugs, gastrointestinal drugs, and cold remedies have a larger daily dosage than medical pharmaceuticals containing a medicinal ingredient alone. Therefore, the compressed solid composition tends to be larger in size, and the unpleasant taste and difficulty in swallowing become prominent.

[0003] As a tablet that is easy to take, the form of a nucleated tablet is known (for example, Patent Document 1).

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] An object of the present invention is to provide a compressed solid composition having an excellent taste during administration, although a component exhibiting a medicinal effect is blended in a certain amount or more.

Means for Solving the Problems

[0006] The present invention focuses on the fact that it is different from the physiological sensations in the oral cavity such as the tongue and the pharynx, and controls so that disintegration occurs in the pharynx during administration. As a result, the inventors have found that a compressed solid composition having an excellent taste during administration can be obtained, and have completed the present invention. ​​​​

[0007] In other words, the present invention provides the following compressed solid compositions. Section 1. (A) Inorganic compound antacids, starch digesting enzymes, protein digesting enzymes, fat digesting enzymes, Selected from the group consisting of Rei, Keihi, Kanzo, Shishipi, Kouboku, and Belladonna extract. One or more of the following; and (B-1) A compressed solid composition containing a monoterpene and / or (B-2) a sugar alcohol. There is, (C) Maximum diameter 1~4mm, (D) A compressed solid composition having a height-to-maximum diameter ratio of 0.5 to 2. Section 2. The aforementioned component (A) is at least an inorganic compound antacid, oyster shell, cinnamon, licorice, and It contains one or more selected from the group consisting of corn, magnolia, and belladonna extract, and (A The compressed solid composition described in item 1, wherein the total amount of the component is 40% by mass or more of the compressed solid composition. thing. Section 3. It contains a binder and / or a disintegrant, and the total amount of the binder and disintegrant is 3 in the compressed solid composition. A compressed solid composition according to item 1 or 2, wherein the mass is 0% or less. Section 4. (E) According to the disintegration test method of the Japanese Pharmacopoeia (17th edition) (without auxiliary disc, using purified water at 37°C) A compressed solid composition according to any one of items 1 to 3, wherein the disintegration time is 1 to 20 minutes. Section 5. (F-1) The number of doses per dose is 5 to 30, and / or (F-2) the mass per unit is 1 m A compressed solid composition according to any one of items 1 to 4, wherein the amount is g to 100 mg. Section 6. The unpleasant taste in the mouth is suppressed, and a refreshing sensation is felt in the throat, as described in any one of items 1 to 5. Compressed solid composition. Section 7. containing menthol as the (B-1) monoterpene and the (B-2) sugar alcohol The compressed solid composition according to any one of items 1 to 6, containing xylitol.

Effect of the Invention

[0008] The compressed solid composition of the present invention is easy to swallow, suppresses unpleasant taste, and has a refreshing feeling in the throat and has an excellent feeling of taking.

Brief Description of the Drawings

[0009] [Figure 1] Figure 1 is a side view of a tablet according to one embodiment of the present invention. [Figure 2] Figure 2 is a perspective view of a tablet according to one embodiment of the present invention. [Figure 3] Figure 3 is a diagram for explaining the maximum diameter (W) of the tablet of Figure 2.

Modes for Carrying Out the Invention

[0010] Next, modes for carrying out the present invention will be described.

[0011] [Compressed Solid Composition] The present invention is a compressed solid composition containing (A) an inorganic compound-based antacid, starch digestive enzyme, protein digestive enzyme, fat digestive enzyme, bupleurum, cinnamon, licorice, gardenia, cork tree, and peony extract, one or more selected from the group; and (B-1) monoterpene and / or (B-2) sugar alcohol, and (C) having a maximum diameter of 1 to 4 mm, (D) a compressed solid composition having a ratio of height to maximum diameter of 0.5 to 2. The compressed solid composition of the present invention is for oral use. Details will be described below.

[0012] The compressed solid composition of the present invention will be described below. ((A-1) Inorganic compound antacids, starch digesting enzymes, protein digesting enzymes, or fat digesting enzymes) (Enzymes) The compressed solid composition of the present invention contains, as an inorganic compound antacid, sodium bicarbonate, and carbonate. Magnesium, magnesium hydroxide, precipitated calcium carbonate, and / or aluminum metasilicate It is preferable that the product contains magnesium oxide. Alternatively, it may contain aldioxa or aluminum metasilicate. Magnesium silicate, magnesium aluminosilicate, magnesium silicate, synthetic silicate Aluminum, sucrose sulfate aluminum salt, dried aluminum hydroxide gel, hydroxide Alumina magnesium, aluminum hydroxide gel, sodium bicarbonate, magnesium carbonate M, precipitated calcium carbonate, calcium hydrogen phosphate, cuttlefish bone, oyster shell, oyster shell, synthetic hydro Talcite, aminobutyric acid, dihydroaluminum aminoacetate, aluminum hydroxide • Sodium bicarbonate co-precipitation product, aluminum hydroxide-magnesium carbonate mixed dry gel It may also contain a co-precipitation product of aluminum hydroxide, magnesium carbonate, and calcium carbonate. Yes, it is possible. One or more of these can be used as inorganic compound antacids in combination. It can also be used.

[0013] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, is carbonated water In the case of sodium, preferably 10 to 95% by mass, more preferably 20 to 90% by mass It contains %, more preferably 30-80% by mass, and particularly preferably 40-70% by mass. In the case of magnesium carbonate, preferably 10 to 95% by mass, more preferably 20% It contains 90% by mass, more preferably 30-80% by mass, and particularly preferably 40-70% by mass. It contains %, and in the case of magnesium hydroxide, preferably 10 to 95% by mass, more preferably It contains 20-90% by mass, more preferably 30-80% by mass, and particularly preferably 40% It contains ~70% by mass, and in the case of precipitated calcium carbonate, preferably 10~95% by mass, Preferably, it contains 20-90% by mass, more preferably 30-80% by mass, and especially preferably It contains 40-70% by mass, and in the case of magnesium aluminometasilicate, preferably This is 10-95% by mass, more preferably 20-90% by mass, and even more preferably 30-8% by mass. It contains 0% by mass, and is particularly preferably 40-70% by mass. Sodium bicarbonate, carbon Magnesium sulfate, magnesium hydroxide, precipitated calcium carbonate and magnesium aluminometasilicate The total amount of magnesium is preferably 10 to 80% by mass, more preferably 15 to 75% by mass. It contains %, more preferably 20 to 70% by mass.

[0014] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, can be used for 1 day. The dosage per dose is preferably 1 to 5000 mg of sodium bicarbonate, more preferably More preferably, it can be 10 to 4000 mg, and more preferably 100 to 3000 mg. Magnesium carbonate, preferably 1 to 5000 mg, more preferably 10 to 400 mg The amount can be 0 mg, more preferably 100 to 3000 mg, and magnesium hydroxide. Preferably, 1 to 5000 mg, more preferably 10 to 4000 mg, even more preferably The amount can be 100 to 3000 mg, and precipitated calcium carbonate is preferably 1 ~5000mg, more preferably 10~4000mg, even more preferably 100~30 It can be 00 mg, and magnesium aluminometasilicate is preferably 1 to 5 000 mg, more preferably 10 to 4000 mg, even more preferably 100 to 3000 It can be expressed in mg. Sodium bicarbonate, magnesium carbonate, magnesium hydroxide , as the total amount of precipitated calcium carbonate and magnesium aluminometasilicate, per day The dosage is preferably 10 to 5000 mg, more preferably 100 to 3000 mg The amount can be mg, more preferably 800 to 2500 mg.

[0015] The compressed solid composition of the present invention may also contain starch digesting enzymes. Enzymes include, but are not limited to, α-amylase, β-amylase, glucoamylase, etc. It can be done. Commercially available products can also be used, such as diastase ( (Pharmacopoeia product), Biodiastase 2000 (complex enzyme preparation, manufactured by Amano Enzyme Co., Ltd.), Diasmen , Kleistase (manufactured by Yamato Kasei Co., Ltd.), Biotamylase (complex enzyme preparation, Nagase ChemteX) Examples include products manufactured by the company. The proportion of the mixture is not particularly limited, but preferably per day The minimum dose should be 100 units or more.

[0016] The compressed solid composition of the present invention may also contain protein digestive enzymes. Digestive enzymes include, but are not limited to, endopeptidases and exopeptidases. It is possible to use commercially available products, such as Biodiastase 2. 000, Prozyme 6, Neurase (manufactured by Amano Enzyme Co., Ltd.), Sumizyme P (Shin Nippon Chemical Co., Ltd.) Examples include Gakusha's product, Biotamilase (Nagase ChemteX Corporation), etc. The proportion of each is While not particularly limited, preferably the minimum daily dose is 750 units or more. good.

[0017] The compressed solid composition of the present invention may also contain a fat-digesting enzyme. However, it is not limited to any fat-digesting enzyme preparation of animal, plant, or microbial origin. It can also be used. Commercially available products can also be used, such as lipase A Examples include P12, etc. The proportion of the mixture is not particularly limited, but preferably, per day The minimum dose per person should be 50 units or more.

[0018] These digestive enzyme preparations may be used individually or in combination of two or more types. It is also possible to use a product that contains a pre-mixed blend of two or more enzymes as a complex enzyme preparation.

[0019] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, is made of starch. In the case of digestive enzymes, preferably 0.01 to 30% by mass, more preferably 0.05 to 2% by mass. It contains 5% by mass, more preferably 0.1 to 20% by mass, and in the case of protein digestive enzymes, More preferably 0.01 to 30 mass%, more preferably 0.05 to 25 mass%, even more preferably It contains 0.1 to 20% by mass, and in the case of fat digesting enzymes, preferably 0.01 to 30% by mass. Contains %, more preferably 0.05 to 25% by mass, and even more preferably 0.1 to 20% by mass. It contains. Preferably, the total amount of starch-digesting enzymes, protein-digesting enzymes, and fat-digesting enzymes is More preferably 0.01 to 30% by mass, more preferably 0.05 to 25% by mass, and even more preferably 0.01 to 30% by mass. It contains 0.1 to 20% by mass.

[0020] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, can be used for 1 day. The dosage per dose is preferably 10 to 1000 mg of starch digesting enzyme, more preferably More preferably, it can be 20-800 mg, and more preferably 30-500 mg. Protein digestive enzymes, preferably 10 to 1000 mg, more preferably 20 to 800 mg g, more preferably 30-500 mg, and a fat-digesting enzyme, preferably 10-1000 mg, more preferably 20-800 mg, even more preferably 30-5 It can be 00 mg. Starch digesting enzyme, protein digesting enzyme, and fat digesting enzyme The total amount of the active ingredient, and the daily dose, is preferably 10 to 1000 mg, more preferably The amount can be 20 to 800 mg, and more preferably 30 to 500 mg.

[0021] ((A-2) Consists of oyster shell, cinnamon, licorice, dried tangerine peel, magnolia bark, and belladonna extract) (One or more crude drugs selected from the group) The compressed solid composition of the present invention contains oyster shell (typically oyster shell powder), cinnamon, licorice, and citrus. It may also contain one or more crude drugs selected from the group consisting of Pi, Magnolia bark, and Belladonna extract. Crude drugs are those listed as "crude drugs" in the Japanese Pharmacopoeia and the Japanese Pharmacopoeia's Standards for Crude Drugs outside the Pharmacopoeia. It refers to something that is present.

[0022] These crude drugs can take the following forms, in addition to the crude drug itself (primitive drug). This is the gist of it. In other words, the crude drugs of this invention include "crude drug powder" which is made by putting the raw crude drug into a powder, and the raw crude drug or This is an "extract" obtained by extracting crude drug powder using water, ethanol, oil, or other organic solvents or mixtures thereof. This includes "extract powder," which is the dried and powdered extract, and "concentrated extract," which is the concentrated extract. This typically includes all forms used in traditional Chinese medicine preparations.

[0023] In this specification, "equivalent to crude drug" means the amount of crude drug extract, and the preparation of the extract. This refers to the amount of crude drugs (or herbal mixtures) needed for a particular purpose.

[0024] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, is a crude drug In terms of conversion, for volcanic ash, preferably 0.001 to 90% by mass, more preferably 0.0 It contains 1 to 70% by mass, more preferably 0.1 to 50% by mass, and in the case of cinnamon, preferably This is 0.001 to 90% by mass, more preferably 0.01 to 70% by mass, and even more preferably 0.01 to 70% by mass. It contains 0.1 to 50% by mass, and in the case of licorice, preferably 0.001 to 90% by mass. More preferably, it contains 0.01 to 70% by mass, and even more preferably, 0.1 to 50% by mass. In the case of dried tangerine peel, preferably 0.001 to 90% by mass, more preferably 0.01 to 70% by mass. It contains mass%, more preferably 0.1 to 50 mass%, and in the case of Magnolia bark, preferably 0 0.001 to 90% by mass, more preferably 0.01 to 70% by mass, even more preferably 0. It contains 1 to 50% by mass, and in the case of belladonna extract, preferably 0.001 to 90% by mass. Preferably, it contains 0.01 to 70% by mass, and more preferably, 0.1 to 50% by mass. Oyster shell, cinnamon, licorice, dried tangerine peel, magnolia bark, and belladonna extract and total belladonna extract In terms of quantity, preferably 0.001 to 90% by mass, more preferably 0. It contains 0.1 to 70% by mass, more preferably 0.1 to 50% by mass.

[0025] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, can be used for 1 day. The dosage per serving is preferably 1 to 3000 mg of oyster shell in terms of crude drug equivalent, more preferably It can be 10 to 2000 mg, and more preferably 100 to 1000 mg. In addition, cinnamon is added, preferably 1 to 5000 mg, more preferably 10 to 4000 mg. More preferably, the amount can be 100 to 3000 mg, and licorice is preferably 1 ~5000mg, more preferably 10~4000mg, even more preferably 100~30 It can be 00 mg, and preferably 1 to 5000 mg of dried tangerine peel, comfortably It can be 10 to 4000 mg, more preferably 100 to 3000 mg, and Kou I prefer 1 to 1500 mg, more preferably 5 to 750 mg, even more preferably The amount can be 10 to 350 mg, and the belladonna extract is preferably 1 to 500 mg 0 mg, more preferably 10 to 4000 mg, even more preferably 100 to 3000 mg This can be done. Oyster shell, cinnamon, licorice, dried tangerine peel, magnolia bark, and belladonna extract. The total amount, as a daily dose, is preferably 1 to 5000 ml in terms of crude drug equivalent. g, more preferably 10 to 4000 mg, even more preferably 100 to 3000 mg It is possible.

[0026] The compressed solid composition of the present invention preferably comprises at least one of the above components (A), which is inorganic. A compound antacid, made from oyster shell, cinnamon, licorice, citrus peel, magnolia bark, and belladonna extract. It contains one or more selected from the group, and the content of component (A) is 40% by mass or more. .

[0027] The compressed solid composition of the present invention contains, in total amount, component (A) above, preferably 8% by mass. The above is included, more preferably 15 to 98% by mass, even more preferably 20 to 95% by mass, even more preferably The amount is preferably 30-95% by mass, more preferably 40-95% by mass, and even more preferably 50-9% by mass. 2% by mass, more preferably 60-92% by mass, even more preferably 70-92% by mass, most Preferably, it contains 80-90% by mass.

[0028] ((B-1) Monoterpene) In the compressed solid composition of the present invention, (B-1) monoterpene is composed of two isoprene units or This is a known compound having the following structure. The present invention may include pharmaceutically or physiologically acceptable compounds. Any monoterpene can be used. The monoterpene may be a d-isomer, l-isomer, or dl-isomer. Either is fine.

[0029] Specifically, as monoterpenes, geraniol, nerol, myrcenol, and linalool. Acyclic monoterpenes such as linalool acetate and lavandulol; menthol, limonol Monocyclic monoterpenes such as ne, anethole, eugenol, and hinokitiol; camphor Bicyclic monoterpenes such as oleu, borneol, isoborneol, cineole, and pinene. Examples include, but are not limited to, those that can reliably produce a higher effect. From this viewpoint, preferably, it is a monocyclic monoterpene or a bicyclic monoterpene, Preferably, menthol, camphor, eugenol, geraniol, borneol, or is hinokitiol, more preferably menthol or camphor, and even more preferably Or menthol. These monoterpenes may be used individually, You may use two or more types in any combination.

[0030] Furthermore, as monoterpenes, essential oils containing them may be used. It contains cool mint oil, peppermint oil, spearmint oil, eucalyptus oil, bergamot oil, and spearmint oil. Examples include mint oil, rose oil, and camphor oil. For example, essential oils containing menthol or camphor. Examples include cool mint oil, peppermint oil, spearmint oil, camphor oil, fennel oil, and cinnamon. Examples include oils, lemon oil, etc. These essential oils may be used individually. Furthermore, two or more types may be used in any combination. These essential oils are derived from plants, known It can be extracted by the following methods. Known methods for extracting essential oils include steam distillation and decongestant distillation. Oils made by adding plant materials to odorized animal fats to adsorb essential oils, and then extracting the essential oils with ethanol. Adsorption method: Extracts plants with organic solvents such as hexane or benzene or supercritical fluids. Solvent extraction method, in which the substance is dissolved in ethanol, and then the ethanol is evaporated to collect the residue; pressing. Laws and regulations are among the examples. Monoterpenes are recovered from essential oils by various chromatography methods. It is also possible.

[0031] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, is used in one step. As the dosage per unit, the total amount of (B-1) monoterpenes contained in the composition is the monoterpene Preferably, 0.2 to 60 mg, more preferably 1 to 36 mg, even more preferably The amount can be 2 to 20 mg. Regarding this, even if it is included as an essential oil in the composition, the amount when converted to monoterpenes or It refers to a ratio.

[0032] The compressed solid composition of the present invention, as a single dose, is, for example, as a monoterpene. If menthol is included, preferably 0.1 to 60 mg, more preferably 0.2 mg 60 mg, more preferably 1 to 36 mg, even more preferably 0.5 to 30 mg, further Preferably, the amount can be 1 to 20 mg, and particularly preferably, 2 to 20 mg.

[0033] The compressed solid composition of the present invention contains (B-1) monoterpene as a single dose. If essential oils are included, the daily dose should preferably be 0.1 to 100% of the essential oil. The amount is 50 mg, more preferably 0.5 to 40 mg, and even more preferably 1 to 30 mg. It is possible.

[0034] The total monoterpene content in the compressed solid composition of the present invention is preferably 0.0001 ~1% by mass, more preferably 0.0005~0.25% by mass, and even more preferably 0. It is between 0.01% and 0.1% by mass.

[0035] Herein, however limited, the compressed solid composition of the present invention exhibits the effects of the present invention more effectively. From this viewpoint, the total amount of component (B-1) is preferably 1 part by mass of component (A). , 0.00001 to 0.1 parts by mass, more preferably 0.0001 to 0.01 parts by mass, further Preferably 0.001 to 0.05 parts by mass, particularly preferably 0.001 to 0.01 parts by mass Contains in amounts.

[0036] ((B-2) Sugar alcohol) The (B-2) sugar alcohol in the compressed solid composition of the present invention is pharmaceutically or physiologically permissible. Any acceptable sugar alcohol can be used. Examples of sugar alcohols include xylose. Litol, sorbitol, erythritol, maltitol, lactitol, isomaltulo Examples include reduced corn syrup, mannitol, or reduced starch syrup. Either the d-isomer, l-isomer, or dl-isomer. These sugars may be used, but d-mannitol or d-sorbitol may also be used. Alcohol may be used alone or in any combination of two or more types. That's fine.

[0037] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, is used in one step. The dosage is preferably the total amount of (B-2) sugar alcohol contained in the composition. , 10-1000 mg, more preferably 50-800 mg, even more preferably 100- It can be set to 600 mg.

[0038] The total sugar alcohol content in the compressed solid composition of the present invention is preferably 0.01 to 8 0% by mass, more preferably 0.1 to 60% by mass, and even more preferably 1 to 50% by mass. be.

[0039] Herein, however limited, the compressed solid composition of the present invention exhibits the effects of the present invention more effectively. From this viewpoint, the total amount of component (B-2) is preferably 1 part by mass of component (A). , 0.00001 to 10 parts by mass, more preferably 0.0001 to 5 parts by mass, even more preferably The amount is 0.001 to 3 parts by mass, and particularly preferably 0.01 to 2 parts by mass.

[0040] The compressed solid composition in embodiment 1 of the present invention is particularly useful as a gastrointestinal medicine. Specifically, It has effects such as protecting the gastric mucosa, increasing gastric mucus, and increasing gastric mucosal blood flow, thereby enhancing resistance to stomach acid. Furthermore, combined with its effect of regulating the amount of stomach acid, it is an excellent gastrointestinal medicine for gastritis, stomach ulcers, and stomach upset. It exerts the following effects. In particular, the pharmaceutical formulation of the present invention is effective against gastric ulcers, gastric mucosal lesions (erosions, bleeding, It is used to improve redness and edema, and to treat acute gastritis and acute exacerbations of chronic gastritis. In addition, Indigestion, overeating, excessive drinking, heartburn, loss of appetite. (Remission), gastric bloating (including that caused by indigestion), abdominal bloating (including that caused by indigestion) Nausea (upset stomach, nausea from hangover / alcohol intoxication, vomiting, sickness), vomiting Chest tightness, excessive stomach acid, feeling of heaviness in the stomach, weak stomach, stomach pain, stomach discomfort, promoting digestion, indigestion, abdominal pain, Colic (colic, epilepsy), belching, vomiting and diarrhea, loose stools Diarrhea (including diarrhea due to indigestion and diarrhea accompanied by abdominal pain), food poisoning, contaminated water, bowel regulation (stool). It can be used effectively for purposes such as regulating bowel movements, loose stools, and constipation. It is suitable for the elderly and those with weak physical condition (physiological function). It may be prescribed in a way that is suitable for use in individuals with reduced cognitive function or those with underlying medical conditions.

[0041] (active ingredient) The compressed solid composition of the present invention, insofar as the effects of the present invention are fully achieved, may otherwise be used as described above. It may contain further various components (pharmacologically active components or physiologically active components) as needed, or These can be used in combination. The types of such components are not particularly limited, for example, In product 1, stomachic agents, digestive agents, intestinal regulators, antidiarrheal agents, analgesics and antispasmodics, mucosal repair agents, antifoaming agents, etc. Examples include, but are not limited to, the following components in the present invention. This does not mean that the amount of these ingredients is added will vary depending on the type of formulation, the type of active ingredient, etc. Selected as appropriate.

[0042] Stomach remedies: Anise fruit, aloe, fennel, turmeric, rhizome, herbaceous herb, scutellaria, cinnamon Ku, Ouren, processed garlic, Gajutsu, Kakko, Karamu root, dried ginger, Kikka, Kijitsu, Gen Chiana, Koujin, Goshuyu, Pepper, Colombo, Conzurango, Sansho, Yamana, Shiso Shi, Shukuya, Shokyo, Shozuku, Aokawa, Ishishokon, Centaurum grass, Senburi , hibiscus, star anise, rhubarb, bamboo ginseng, clove, chili pepper, spruce, bitter Ki, nutmeg, ginseng, mint (including European mint), long pepper, and angelica tree. Ingredients: yuzu, hops, humicilla extract, water lily leaf, moonflower, yakuchi, gentian , crude drugs such as Ligusticum erythrorhizon or their extracts, ginger oil, cardamom oil, clove oil, Spruce oil, animal bile (including bear bile), betaine hydrochloride, glutamate, carnivorous chloride Chin, betanethol chloride, dried yeast, etc.

[0043] Digestive agents: Ursodeoxycholic acid, oxycoranates, cholic acid, bile powder, bile Extract (powder), dehydrocholic acid, animal bile (including bear bile), etc.

[0044] Intestinal regulators: Herbal medicines such as red oak, catechu, basil, cassia seed, geranium or similar Extracts, intestinal bacteria components, etc.

[0045] Antidiarrheal agents: Catechuan, Ubai, Oubaku, Ouren, Kujin, Geranium, Gallnut Crude drugs such as hawthorn, swertia japonica, and hibiscus, or their extracts, acrinol, beryl chloride Phosphorus, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, tannins Berberine acid, bismuth subsalicylate, bismuth subnitrate, bismuth subcarbonate, bismuth subgallate Sumas, tannic acid, tannic acid albumin, methylenethimole tannin, kaolin, tannin Natural aluminum silicate, aluminum hydroxynaphthoate, pectin, medicinal charcoal, lactic acid Calcium, etc.

[0046] Analgesic and antispasmodic agents: Herbal medicines such as Corydalis, Peony, Belladonna, etc. or their extracts, oxalic acid Cyphencycline, dicyclomine hydrochloride, methixene hydrochloride, scopolamine hydrobromide methylatropine bromide, methylanisotropine bromide, methylscopolamine bromide, bromide Chil-l-hyoscyamine, methylbenactidium bromide, isopropamide iodide, iodide Diphenylpiperidinomethyldioxolane, belladonna root total alkaloid citrate, hydrochloride Pavelin, ethyl aminobenzoate, etc.

[0047] Mucosal repair agents: Herbal medicines such as red oak and Corydalis or their extracts, sodium azulene sulfonate Um, aldioxa, glycyrrhizic acid and its salts, L-glutamine, copper chlorophyllin Potassium, copper chlorophyllin sodium, histidine hydrochloride, porcine stomach wall pepsin hydrolysate, Porcine stomach acid hydrolysate, methylmethionine sulfonium chloride, gefarnate, se Traxate hydrochloride, sucralfate hydrate (sucrose sulfate aluminum salt), Sofa arcon, etc.

[0048] Antifoaming agent: Dimethylpolysimethane, etc.

[0049] (Additives) The compressed solid composition of the present invention may contain appropriate additives depending on its dosage form. The compressed solid composition of the present invention particularly preferably contains a binder and / or a disintegrant.

[0050] A binder can effectively bind together the powder particles of the raw materials. Examples of binders include: Methylcellulose, ethylcellulose, hydroxypropylcellulose, hydroxypropyl Cellulose derivatives such as pyrumethylcellulose, polyvinylpyrrolidone, polyvinyl alcohol Acrylic acid polymer, lactose, sugar alcohol (mannitol, xylitol, sucrose) (e.g., loin), agar, tragacanth, sodium alginate, propylene glycol alginate Luester, gelatin, acacia gum, pullulan, pregelatinized starch, starch, etc. It can be used.

[0051] The disintegrant has the effect of appropriately promoting the disintegration of the compressed solid composition of the present invention. This includes low-substituted hydroxypropyl cellulose, carboxymethylcellulose calcium, Croscarmellose sodium, carmellose sodium, hydroxypropyl starch Partially pregelatinized starch, etc., can be used.

[0052] In the compressed solid composition of the present invention, it is also preferable to use a binder and a disintegrant in combination. The effects of the present invention become more pronounced with use, making it preferable.

[0053] The compressed solid composition of the present invention is, but is not limited to, the total amount of the binder and / or disintegrant as It is preferable that the content be 30% by mass or less, and more preferably 5 to 28% by mass. It is even more preferable that it contains 10 to 25% by mass.

[0054] (Dosage form, etc.) The compressed solid composition of the present invention can be used, for example, in pharmaceuticals, quasi-drugs, foods, or as raw materials for these. For example, pharmaceutical preparations, quasi-drug preparations, foods for specified health uses, nutritional functional foods, foods for the elderly, special Foods for specific uses, functional foods, health supplements, food preparations (e.g., confectionery tablets) It can be used as such.

[0055] In the present invention, a compressed solid composition means a pharmaceutical product molded into a specific shape. While not particularly limited, examples of dosage forms that are compressed include tablets, granules, and lozenges. It is particularly suitable for molded tablets and granules. The compressed solid composition is in the form of oral Any shape that can be swallowed is acceptable, such as a cylindrical shape, triangular prism shape, rectangular prism shape, or polygonal prism shape. Examples include disc-shaped, cylindrical, football-shaped, oval-shaped, petal-shaped, and animal-patterned designs. However, due to the ease of molding, tablets in the shape of a rice bale, disc, cylinder, or triangular prism are preferred. They are commonly used. This includes round corner locks and rounded corner locks. Round corner locks are used on both ends of a cylinder. These are tablets with a straight, chamfered edge. Circular, rounded-corner tablets have a cylindrical shape with the edges of both ends chamfered. The tablets have a chamfered shape with an R-shaped surface. As long as the essence of the present invention is not impaired, the Pharmaceutical Affairs Law and It can also be used for products classified as granules in the Japanese Pharmacopoeia.

[0056] ((C) Maximum diameter) The size of one unit (one piece) of the compressed solid composition of the present invention is in the range of 1 to 4.5 mm in maximum diameter. The area should be within a certain range, and may be between 1.5 and 4.5 mm, or between 2 and 4.5 mm, and 2. It may be 4-4.5mm, 2.8-4.5mm, or 3-4.5mm. It is fine if it is 3.2-4mm, fine if it is 3.4-4mm, and especially fine if it is 3.6- 4 mm, particularly 3.8 to 4 mm, is preferred. The maximum diameter of the compressed solid composition is within this range. If this is done, the effects of the present invention can be realized.

[0057] The maximum diameter of the compressed solid composition in this invention is as shown by W in Figures 1 and 3, and the curved surface The shape encompasses all the planar shapes when the object is placed in the most stable position relative to the floor surface. For the smallest possible diameter, in the case of a shape without curved surfaces, when the cross-section is made from the ground surface upwards, The smallest possible size that can encompass the entire shape of the plane when it is placed stationary in a way that minimizes the change in the area of ​​the surface drawing. It refers to the diameter.

[0058] ((D) Height) The height of each compressed solid composition of the present invention is 0.5 m, depending on the maximum diameter. It varies between m and 8 mm, and the ratio of height to maximum diameter (height / maximum diameter) is within the range of 0.5 to 2. It will be set to be as follows.

[0059] The height of the compressed solid composition in this invention is as shown by H in Figures 1 and 3, and has a curved surface. In terms of shape, the lowest and highest points in a side view when the device is placed most stably on the floor surface. For short distances and shapes without curves, when a cross-section is created above the contact surface, the area of ​​the cross-sectional diagram changes. This refers to the shortest distance between the bottom and top of the object in a side view when it is placed in a stationary position that minimizes distortion. .

[0060] Furthermore, the maximum diameter (the smallest diameter that can encompass the entire formulation) can be set to approximately 8 mm or less. Cut.

[0061] ((E) Disintegrative) The compressed solid composition in the present invention, although not limited to, has a disintegration time determined by a disintegration test method, It is preferable that the range is 1 to 20 minutes. It may be in the range of 2.0 to 10 minutes, and 2.5 It may be in the range of ~9.5 minutes, or in the range of 3.0 to 9.0 minutes, or 3.2 to 8.5 minutes. It may be in the range of minutes, more preferably in the range of 3.5 to 8.0 minutes, and even more preferably in the range of minutes. This ranges from 3.8 to 7.5 minutes.

[0062] The compressed solid composition of the present invention is a compressed solid composition prepared to have the same maximum diameter, When sieving is performed using a sieve 1.2 times the maximum diameter, more than 90% of the material passes through the sieve. It is preferable that 92% or more pass through the sieve, and especially preferable that 94% or more pass through. It is preferable that the material passes through the sieve. Furthermore, a sieve with a size 0.8 times the maximum diameter is used for sieving. When the sieving is performed, it is preferable that more than 90% remain on the sieve, and of those, more than 92% remain on the sieve. It is preferable that the material be retained, and in particular, that 94% or more remain on the sieve. Because the condensed solid composition has little variation in shape and size, it is possible to accurately ingest the specified ingredients. This can be done. For example, a cylindrical compressed solid assembly prepared using a mold with a maximum diameter of 4.0 mm. In the finished product, the maximum diameter of each of the multiple compressed solid compositions taken in a single dose was measured, and the average was taken. If the value is 4.0 mm, 1 g of the compressed solid composition is sieved using a 4.8 mm sieve. When this is done, 0.9g or more passes through the sieve, and then 1g of the compressed solid composition is sieved using a 3.2mm sieve. When sieved, 0.9g or more remained on the sieve, and the maximum diameter of the prepared compressed solid composition was... This will be 4.0 ± 0.80 mm.

[0063] (hardness) The hardness of the compressed solid composition of the present invention is not limited, but is preferably 0.5 to 10.0. The range is kp, more preferably 1.0 to 10.0 kp, and 1.6 to 9.5 kp. It is more preferably p, and particularly preferably 1.3 to 8.5 kp. In this context, hardness is determined by measuring the fracture strength of 10 randomly selected samples using a hardness tester. This refers to the average of the obtained values.

[0064] (mass) The mass per unit of the compressed solid composition of the present invention is not limited, but is preferably 1 to The range is 100 mg, more preferably 2-80 mg, and 5-60 mg. It would be even more preferable.

[0065] (feeling when taking) The compressed solid composition of the present invention suppresses disintegration in the oral cavity and dissolves in the pharynx, thus preventing... The pleasant taste is suppressed, and a refreshing sensation (clean feeling) may be present in the throat. Therefore, it has a superior taste and feel.

[0066] [Method for producing compressed solid composition] The compressed solid composition of the present invention can be obtained, for example, as follows: First, components (A) and (B), which will be the materials for the compressed solid composition, and any additives are mixed using a conventional method. The mixture is then mixed to produce a drug or herbal medicine-containing mixture. This mixture is then molded into a predetermined shape. By doing so, the compressed solid composition of the present invention can be obtained. The herbal medicine-containing mixture is usually The powder is used for molding as a particle size of 850 μm or less. Prepare the powder to have a diameter of 850 μm or less, and mix them to produce a crude drug powder with a particle size of 850 μm or less. It may also be a compound containing the herbal medicine. During molding, the herbal medicine-containing compound is compressed and molded using a molding machine. Before being subjected to the molding machine, the herbal mixture is granulated using a wet granulation method or a dry crushing and granulation method. You may do so.

[0067] The above wet granulation method involves adding a liquid such as water, ethanol, or oil to a powdered mixture containing crude drugs. This method involves adding a mixture containing crude drugs in a single batch or by spraying to form granules. Examples of the wet granulation methods mentioned above include kneading granulation, extrusion granulation, agitation granulation, and fluidized bed granulation. One example is a method called spray drying.

[0068] The above dry crushing and granulation method compresses a powdered herbal medicine mixture and forms it into dense lumps or plates. This method involves obtaining a material, crushing and pulverizing the molded product, and then sizing it to obtain granular material of a predetermined size. The above dry crushing and granulation method uses equipment such as a roller compactor or a slug tablet press. This can be done by [method].

[0069] When using a molding machine, for example, the crude drug-containing mixture obtained by the above method may be treated as needed. Then, after adding binders, disintegrants, etc. and mixing, the desired size of the compressed solid composition is determined. By using a molding machine equipped with a pestle and mortar (mold) that can compress tablets, the tablets are formed by compression molding. This allows us to obtain the compressed solid composition of the present invention, for example, with a maximum diameter of 4.0 mm. The cylindrical compressed solid composition is processed using a mortar and pestle designed for a diameter of 4.0 mm, with the mortar and pestle used to grind the powder. It can be obtained by pressing. Here, the shape of the pestle is not limited, but for example, R It may be a flat surface, a rounded corner surface, a rounded corner surface, a corner surface, etc., and the compressed solid composition corresponds to the punch. It has outer surface shapes such as rounded surfaces, corner rounded surfaces, rounded corner surfaces, and corner surface surfaces. Peripheral edge of compressed solid composition The part is called the land portion (for example, the part from the side of the tablet to the raised edge of the chamfered portion). It may have a strip-like shape.

[0070] The molding process using the above molding machine can be carried out, for example, under conditions of a temperature of 10 to 50°C. Normally, the process is carried out at room temperature (a temperature that is neither heated nor cooled). Also, molding with the above molding machine is usually The molding pressure is 1 to 30 kN, but it is preferable to use a molding pressure of 3 to 20 kN. It is even more preferable to use a molding pressure of ~12kN, and more preferably a molding pressure of 3~8kN. Furthermore, it is even more preferable to perform the molding with a molding pressure of 4 to 6 kN.

[0071] [Dosage of compressed solid composition] The compressed solid composition of the present invention allows for the intake of more units to be taken in order to absorb the active ingredients. It is preferable that the number of tablets to be taken at one time be individually packaged. Here, The number of tablets to take at one time is, for example, 5 to 30, preferably 6 to 28, more preferably 8. The number is approximately 26. The amount to be taken at one time is, for example, 1 to 3000 mg, preferably. The amount is 10-2000 mg, more preferably 10-1500 mg.

[0072] The number of compressed solid compositions to be taken per day is, for example, 1 to 200, preferably. The number is 5 to 159, more preferably 10 to 100. Also, the amount to be taken per day is For example, 1 to 8000 mg, preferably 10 to 7000 mg, more preferably 100 to 6 It is 000mg.

[0073] The above individual packaging is a sealable packaging material, SP (Strip Package) packaging material. Examples include stick-shaped packaging materials. Examples of such SP packaging materials and stick-shaped packaging materials include For example, the aluminum sheet material is sealed at its ends and at the top and bottom ends of the cylinder so that it forms a cylinder, and inside Examples include those with a sealed storage compartment. In particular, those that are taken in one dose It is preferable that the compressed solid composition is packaged in one SP package or stick-shaped package. For example, the packaging material for the above-mentioned SP packaging material and stick-shaped packaging material is Japanese Patent Publication No. 2006-1432. 76. Packaging materials etc. described in Japanese Patent Publication No. 2003-192023, with moisture permeability and ease of opening (pull Taking into consideration factors such as tearability, known materials may be used as appropriate, and the product may be manufactured using known methods. This is possible. And, the inclusion of compressed solid compositions in SP packaging or stick-shaped packaging is usually done on top A predetermined number of compressed solid compositions are placed in the container section of a cylindrical packaging material, with only the end seal remaining. Then, the upper end is sealed to create an airtight seal. Note that SP packaging material and stick To remove the compressed solid composition contained within the encapsulated packaging, the seal at the top of the packaging is usually removed. By cutting the section that extends inward in the longitudinal direction from the point, the upper end is opened, and this opening The process is carried out. The compressed solid composition of the present invention is particularly suitable for packaging in stick-shaped packaging due to its ease of administration. It is preferable that this be done. The compressed solid composition enclosed in SP packaging or stick-shaped packaging is packaged It is preferable that the material be inserted into the mouth through the opening of the material, thereby being removed from the packaging's containment section. stomach.

[0074] In the above-mentioned SP packaging materials and stick-shaped packaging materials, the width (short side) is 10 to 40 mm. It is preferable that it be 12 to 35 mm, more preferably 14 to 32 mm. It is even more preferable that it be 16-30 mm, and particularly preferable that it be 18-28 mm. This is especially preferable. If the width of the SP packaging or stick-shaped packaging is within this range, when taking the medication, When removing compressed solid compositions from SP packaging or stick-shaped packaging, the entire opening can be removed without force. This makes it easier to place the device in the mouth, allowing the effects of the present invention to be more pronounced. Furthermore, Its length (long side) is preferably 60-150 mm, and more preferably 50-130 mm. It is more preferable that it be 45-110 mm, and even more preferable that it be 40-100 mm. It is particularly preferable that there be a certain width, and it is particularly preferable that it be 35 to 90 mm. The above width (short side) and The length (long side) refers to the length of the sealed top, bottom, or both sides of the packaging, not the outer dimensions of the packaging material. This refers to the dimensions of the sealed space containing the compressed solid composition. The short and long sides are curved. When lines intersect, draw extensions of each side and use the intersection point as the endpoints of the shorter and longer sides to determine the above dimensions. Measure.

[0075] Furthermore, the ratio of width (short side) to length (long side) in the above-mentioned SP packaging material and stick-shaped packaging material is: A ratio of 1:1 to 1:10 is preferred, 1:1.2 to 1:9 is more preferred, and 1:1.5 to 1:8 More preferably, 1:1.8 to 1:7 is particularly preferred, and 1:2.0 to 1:6 is particularly preferred. It seems so. When the ratio of the two is within this range, the effects of the present invention can be more pronounced, and The convenience of the device will improve dramatically. [Examples]

[0076] Next, examples will be described together with comparative examples. However, the present invention is not limited thereto. It is not. Furthermore, unless otherwise specified, all component compositions shown below are based on mass (1 (Dose per day)

[0077] [Examples, Comparative Examples] The mixture prepared according to the compositions shown in Tables 1-4 below is used in a mortar and pestle of the desired diameter (R-shaped surface). The desired compressed solid material is formed by applying pressure using a compression molding machine equipped with (having) and then compressing it. The finished product was obtained. The crude drugs used were oyster shell, licorice, cinnamon bark, dried tangerine peel, and magnolia bark, all in powder form. We used [a specific product / method], and the additives used were those listed in the Japanese Pharmacopoeia.

[0078] [Table 1]

[0079] [Table 2]

[0080] [Table 3]

[0081] [Table 4]

[0082] The resulting compressed solid composition was cylindrical. Maximum diameter (W), height (H), maximum diameter Tables 1-4 show the ratio of height to maximum diameter (H / W) and the mass per unit.

[0083] Similarly, the mixture prepared as shown in Table 5 below is pressed using a press with a mortar and pestle of the desired diameter. The material was compressed and molded using a compression molding machine to obtain a compressed solid composition. The additives were from the Japanese Pharmacopoeia. The listed materials were used.

[0084] [Table 5]

[0085] For each example and each comparative example of the compressed solid composition, (1) disintegration time (minutes), (2) oral cavity The following four items were evaluated: (1) unpleasant taste, (2) refreshing feeling in the throat, and (3) overall feeling when taking the medication. The results are shown in the table. Note that all examples and comparative examples were prepared by compression tableting using a mold. did. The evaluation method for each item is as follows:

[0086] (1) Collapse time (minutes) The disintegration test method is the disintegration test method of the Japanese Pharmacopoeia (17th edition) (without auxiliary disc, using purified water at 37°C). ) is equivalent to the above. More specifically, without an auxiliary disc, using purified water at 37°C, i.e., the compressed solid composition The particle size of the formulation is sieved using a No. 30 sieve (500 μm) in accordance with the method for testing particle size of the formulation <6.03>. Next, take the 0.10g remaining in the No. 30 sieve into an auxiliary tube, and then place the auxiliary tube into the glass tube of the test apparatus. Fix it in place. Pour 1200 mL of purified water into the glass tube and operate the test apparatus at 37±2°C. The collapse of the compressed solid composition inside the auxiliary cylinder was observed, and no residue of the compressed solid composition was found. If there is no structure, or if it is a soft substance that clearly does not retain its original form, it is judged to have disintegrated. Then, the time from the start of operation of the test device to disintegration is measured. This is done three times, and the average is used as the disintegration time. It was calculated as follows.

[0087] (2) unpleasant taste in the mouth and (3) refreshing feeling in the throat Ten compressed solid compositions are filled into a stick-type packaging (7cm long, 1.5cm wide, made of aluminum). Packaged. Open by cutting horizontally 1 cm below the top vertical edge, and insert 10 compressed solid compositions. The medication was taken orally in one go and swallowed with 100 mL of water.

[0088] (Criteria for evaluating unpleasant tastes in the mouth) If you experience a strong unpleasant taste in your mouth while taking a compressed solid composition orally and before swallowing it. A score of 1 was assigned to indicate a pleasant taste, and 5 was assigned to indicate no unpleasant taste, with scores ranging from 1 to 5. If the average score of the 5 people is 1.0 or higher but less than 2.0, it is marked as ×. If the average score is 2.0 or higher but less than 3.0, △ indicates a score between 3.0 and 4.0, ○ indicates a score between 4.0 and 5.0, and ◎ indicates a score between 4.0 and 5.0. did.

[0089] (Evaluation criteria for throat refreshment) Regarding the refreshing sensation in the throat area immediately after swallowing the compressed solid composition, one point is awarded for not feeling any refreshing sensation at all. A score was given from 1 to 5, with 5 being the highest score for a strong feeling of refreshment. If the average value is 1.0 or higher but less than 2.0, it's marked with ×; if it's 2.0 or higher but less than 3.0, it's marked with △; if it's 3.0 or higher, it's marked with ×. A score of less than 4.0 is indicated by ○, and a score of 4.0 or higher but less than 5.0 is indicated by ◎, as shown in the table.

[0090] (4) Overall Impression The overall impression of taking the medication was evaluated using the following evaluation procedure. The results are shown in the table. (Procedure for evaluating overall patient experience) (1) If the evaluation result for unpleasant taste in the mouth and / or refreshing feeling in the throat is ×, rate it as ×. (2) If (1) is not applicable, the evaluation result for unpleasant taste in the mouth and / or refreshing feeling in the throat is △. If this is the case, it will be evaluated as △. (3) If (2) is not applicable, the evaluation result for unpleasant taste in the mouth and / or refreshing feeling in the throat is ○ If so, it will be evaluated as ○. If (4)(3) does not apply, evaluate with ◎.

[0091] As is clear from the evaluation results, the examples showed superior overall patient comfort. Examples 26 and 27 were It has a great feel, and users find that the nausea and discomfort in their throat caused by indigestion are relieved, leaving them feeling refreshed. When the composition passes down the throat, the heavy, blocked feeling from the throat to the stomach caused by a hangover is relieved and the medication is taken. The general consensus was that he had good intuition.

[0092] [Examples of formulations] Compressed solid compositions (Formulation Examples 1-10) were prepared using the components shown in the table below. Manufacturing Example Examples 1-8 are uncoated tablets, and manufacturing examples 9 and 10 can be taken without water. It is a chewable tablet, and the raw materials for formulation examples 1-10 are listed in the Japanese Pharmacopoeia. Used.

[0093] [Table 6] [Explanation of symbols]

[0094] W Maximum diameter H Height

Claims

[Claim 1] The invention described in the specification.

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