Granules

Abstract

To provide granules containing a superabsorbent component that exhibits resistance to powdering.SOLUTION: The present invention provides granules containing the following component (A) and component (B): (A) a superabsorbent component and (B) an alkyl cellulose.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to granules and the like. [Background technology]

[0002] Synthetic hydrotalcite is used as an antacid (for example, Patent Document 1). Synthetic hydrotalcite is also used as an additive for pharmaceuticals (Non-Patent Document 1).

[0003] Granulation is a unit operation that is relevant to all solid preparations, including powders, and the granules obtained by this process must have properties appropriate to the purpose. For example, for powders and granules, it is necessary to consider flowability, dispersibility, adhesion, mixability, etc. (Non-patent document 2). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP 2010-30963 A [Non-patent literature]

[0005] [Non-Patent Document 1] Pharmaceutical Additives Encyclopedia 2021, Yakuji Nipposha Co., Ltd., January 25, 2021, 1st edition, p.230-231 [Non-Patent Document 2] Latest Pharmaceutical Science, Hirokawa Publishing Co., Ltd., February 25, 2006, 7th printing, p.266-271 Summary of the Invention [Problem to be solved by the invention]

[0006] The present inventors have discovered that when granules containing synthetic hydrotalcite are produced, powdering occurs during production. In addition, since synthetic hydrotalcite is a highly water-absorbent component, it is expected that the same phenomenon will occur when a highly water-absorbent component other than synthetic hydrotalcite is used. When powdering of granules occurs, the operability is reduced due to fine powder during filling, packaging, etc. If the fine powder is removed to avoid the decrease in operability, the yield will decrease. Therefore, an object of the present invention is to provide granules containing a highly water-absorbent component that are inhibited from powdering. [Means for solving the problem]

[0007] Therefore, the present inventors conducted intensive research to solve the above problems and surprisingly discovered that powdering of granules can be suppressed by adding alkylcelluloses to the granules, thereby completing the present invention.

[0008] That is, the present invention provides granules containing the following components (A) and (B): (A) Highly absorbent component (B) Alkyl cellulose Effect of the Invention

[0009] According to the present invention, it is possible to provide granules containing a highly water-absorbent component that are inhibited from powdering. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0010] <(A) Highly absorbent component> In the present invention, the granules contain a "highly water-absorbent component." Without being bound by theory, the present inventors believe that the inclusion of a highly water-absorbent component inhibits granulation and makes the granules more likely to be powdered.

[0011] The highly water-absorbent component is not particularly limited, but may be, for example, one or more of various metal compounds, silicon compounds, polymer compounds, herbal medicine components, and the like. Examples of highly water-absorbent metal compounds include highly water-absorbent organic metal compounds and highly water-absorbent inorganic metal compounds such as synthetic hydrotalcite, dried aluminum hydroxide gel, magnesium aluminosilicate, magnesium silicate, natural aluminum silicate, synthetic aluminum silicate, magnesium oxide, magnesium alumina hydroxide, aluminum hydroxide gel, aluminum hydroxide-sodium hydrogen carbonate coprecipitate, aluminum hydroxide-magnesium carbonate mixed dried gel, aluminum hydroxide-magnesium carbonate-calcium carbonate coprecipitate, sodium hydrogen carbonate, magnesium carbonate, magnesium aluminometasilicate, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate hydrate, and calcium silicate. Examples of highly water-absorbent silicon compounds include silicon dioxide, hydrous silicon dioxide, silicic acid anhydride, light anhydrous silicon, and anhydrous silicic acid hydrate. Examples of highly water-absorbent polymeric compounds include dextrin, cellulose (crystalline cellulose, etc.), starch (potato starch, corn starch, etc.), carmellose or its salts (carmellose, carmellose calcium, carmellose sodium, etc.), modified starch (hydroxypropyl starch, starch sodium octenyl succinate, starch partial hydrolysates, partially pregelatinized starch, etc.), pullulan, polysaccharides such as sodium alginate, gelatin, polysorbate, macrogol, polyoxyethylene polyoxypropylene glycol, polyvinylpyrrolidone, polyvinyl alcohol, sucrose fatty acid esters, etc.

[0012] The highly water-absorbent herbal ingredients include Mallotus japonicus (red bud oak), Asarum oleifera (asenyaku), aniseed, arnica, aloe, Ubai (fennel), Coix seed, fennel, turmeric, Uyaku, Eleutherococcus senticosus (eleutherococcus, sclerotium), Corydalis chinense (corbiculatus), Scutellaria baicalensis (scutellaria), Coptis chinensis (cherry bark), Phellodendron bark, Coptis japonica (Coptis chinensis), Onji (apricot), processed garlic, oxoamide, Zedoary (gajus), Cuckoo Root, Valerian (valerian), Chamomile, Calonin, guarana, calamus root, and kalanchoe. Licorice, liquorice, bellflower, kijitsu, bellflower, apricot kernel, lycium bark, lycium bark leaf, sophora rhizome, keigai, cinnamon bark, cassia berry, gentiana, gennoshoko, kouka, safflower, koujin, kobushi, koubo, goo, gomi berry, goshuyu, kosho, gobaishi, kobaishi, kombo, saishin, hawthorn, gardenia berry, Japanese pepper, Sanna, saffron, sansou, sanyaku, shion, shigoka, jikoppi, Lithospermum root, Perilla serrata, Chinese peony, Shakusha, Musk, Shajin, Shazenshi, Shazensou, Ginger, Cardamomum serrata, Joteishi, Jiryu, Shini, Hawthorn, Horse chestnut, Seihi, Aster buckthorn, Aster buckthorn root, Senega, Cnidium officinalis, Zenko, Centaurium grass, Swertia britannica, Atractylodes macrocarpa, Soujutsu, Souhakuhi, Soyou, Illicium officinalis, Taiso U, Rhubarb, Daisan (garlic), Chikusetsu ginseng (bamboo joint ginseng), Clove, Chinpi (citrus peel), Chili pepper, Spruce, Touki (Angelica), Ipecac (Ipecac), Toshishi, Eucommia, Nantenjitsu (Nandina fruit), Bitter melon, Cistanche, Myrrh, Carrot, Garlic, Fritillaria, Bakumondou (Oryza sativa), Mint (including peppermint), Common mentha, Pinus communis, Scutellaria, Long pepper, Angelica serrata (White radish), Atractylodes rhizome (White atractylodes), Poria cocos (Poria cocos), Belladonna, Bowie, Hops, Peony bark,Examples of herbal medicines include Nux Vomica, Suisaiyo (sleeping cabbage leaf), Ephedra, Muira Puama, Saussurea, Yakuchi, Coix Seed, Youbaihi (plum bark), Longan Niku, Rhutan, Ryokyo, Rokujo (deer antler), Scolytem, ​​Scolytem root, Ajitzu, Cascara Sagrada, Kengoshi, Plandaco Obata seed coat (ispaghula seed coat), Kengoshi, Senna, Senna fruit (senna fruit), Frangula skin, and Yarappa, as well as their extracts (extracts, tinctures, dried extracts, etc.), etc.

[0013] Of the above-mentioned components, it is preferable to use an inorganic metal compound as the highly water-absorbent component, and it is more preferable to use one or more selected from synthetic hydrotalcite, magnesium aluminometasilicate, anhydrous calcium hydrogen phosphate, and calcium silicate. The above-mentioned components are all known components and may be produced by known methods, or commercially available products may be used. Furthermore, the highly water-absorbent component is preferably a substance that is solid at room temperature and normal pressure (25° C. and 1 atm).

[0014] In addition, as the highly water-absorbent component, it is preferable to use a component having a water absorption amount of, for example, 70mL / 100g or more. The lower limit of the water absorption amount can be 80mL / 100g, 90mL / 100g, 100mL / 100g, 110mL / 100g, 120mL / 100g, or 130mL / 100g. Among them, the water absorption amount is 70mL / 100g or more, preferably 100mL / 100g or more, and particularly preferably 130mL / 100g or more. In addition, the upper limit of the water absorption amount is not particularly limited, but can be 1000mL / 100g, 500mL / 100g, 400mL / 100g, 350mL / 100g, 300mL / 100g, 250mL / 100g, 200mL / 100g, or 180mL / 100g. In particular, the water absorption is preferably 500 mL / 100 g or less, and particularly preferably 400 mL / 100 g or less.

[0015] The water absorption amount of the highly water-absorbent component in this specification is measured by the following method. Weigh 1g of this product onto a dry watch glass. Pour water into the burette. Add water while mixing with a spatula. The end point is when the entire piece becomes a glue-like lump and peels off from the glass surface. Expressed in mL / 100g. Water absorption amount (mL / 100g) = titration value (mL) x 100

[0016] In the present invention, the content of the highly absorbent component is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of the granules, the type of highly absorbent component to be blended, the type and amount of other blended components, and the use of the granules, etc. For example, the upper limit of the total highly absorbent component relative to the total mass of the granules can be 80 mass%, 75 mass%, 70 mass%, 65 mass%, 60 mass%, 55 mass%, 50 mass%, 45 mass%, 40 mass%, 35 mass%, 30 mass%, 25 mass%, or 20 mass%, and the lower limit can be 1 mass%, 5 mass%, 10 mass%, 15 mass%, 20 mass%, 25 mass%, 30 mass%, 35 mass%, 40 mass%, 45 mass%, or 50 mass%. Among them, 1 to 75 mass% is preferable, 15 to 60 mass% is more preferable, and 20 to 50 mass% is particularly preferable. It can also be 25 to 60% by mass. In addition, even when the granules are provided as a composition described later, the content of the highly absorbent component is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of the granules, the type of highly absorbent component to be blended, the type and amount of other blended components, and the use of the granules, etc. For example, the upper limit of the total highly absorbent component relative to the total mass of the composition can be 75 mass%, 70 mass%, 65 mass%, 60 mass%, 55 mass%, 50 mass%, 45 mass%, 40 mass%, 35 mass%, 30 mass%, 25 mass%, 20 mass%, or 15 mass%, and the lower limit can be 1 mass%, 5 mass%, 10 mass%, 15 mass%, 20 mass%, 25 mass%, 30 mass%, 35 mass%, or 40 mass%. Among them, it is preferably 1 to 75 mass%, more preferably 5 to 50 mass%, and particularly preferably 10 to 40 mass%. It can also be 20 to 60 mass%.

[0017] In the present invention, the content of inorganic metal compounds used as the highly water-absorbent component is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of granules, the type of inorganic metal compounds to be blended, the type and amount of other blended components, and the use of the granules. For example, the upper limit of the total inorganic metal compounds relative to the total mass of the granules can be 80 mass%, 75 mass%, 70 mass%, 65 mass%, 60 mass%, 55 mass%, 50 mass%, 45 mass%, 40 mass%, 35 mass%, 30 mass%, or 25 mass%, and the lower limit can be 0.5 mass%, 0.75 mass%, 1 mass%, 5 mass%, 10 mass%, 15 mass%, 20 mass%, or 25 mass%. Among them, 1 to 75 mass% is preferable, 5 to 50 mass% is more preferable, and 10 to 40 mass% is particularly preferable. It can also be 20 to 50 mass%. In addition, even when the granules are provided as a composition described later, the content of the inorganic metal compound is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of the granules, the type of inorganic metal compound to be blended, the type and amount of other blended components, and the use of the granules, etc. For example, the upper limit of the total inorganic metal compound relative to the total mass of the composition can be 75 mass%, 70 mass%, 65 mass%, 60 mass%, 55 mass%, 50 mass%, 45 mass%, 40 mass%, 35 mass%, 30 mass%, 25 mass%, 20 mass%, or 15 mass%, and the lower limit can be 1 mass%, 5 mass%, 10 mass%, 15 mass%, 20 mass%, or 25 mass%. Among them, it is preferably 1 to 75 mass%, more preferably 5 to 50 mass%, and particularly preferably 10 to 40 mass%. It can also be 15 to 45 mass%.

[0018] In the present invention, the content of synthetic hydrotalcite as a highly water-absorbent component is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of granules, the type and amount of other blended components, and the use of granules. For example, the upper limit can be 80 mass%, 75 mass%, 70 mass%, 65 mass%, 60 mass%, 55 mass%, 50 mass%, 45 mass%, 40 mass%, 35 mass%, 30 mass%, or 25 mass%, and the lower limit can be 1 mass%, 5 mass%, 10 mass%, 15 mass%, 20 mass%, or 25 mass%, based on the total mass of the granules. Among them, 1 to 75 mass% is preferable, 5 to 50 mass% is more preferable, and 10 to 40 mass% is particularly preferable. It can also be 20 to 50 mass%. In addition, even when the granules are provided as a composition described later, the content of synthetic hydrotalcite is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of the granules, the type and amount of other blended components, and the use of the granules, etc. For example, the upper limit can be 75 mass%, 70 mass%, 65 mass%, 60 mass%, 55 mass%, 50 mass%, 45 mass%, 40 mass%, 35 mass%, 30 mass%, 25 mass%, 20 mass%, or 15 mass%, and the lower limit can be 1 mass%, 5 mass%, 10 mass%, 15 mass%, 20 mass%, or 25 mass%. Among them, it is preferably 1 to 75 mass%, more preferably 5 to 50 mass%, and particularly preferably 10 to 40 mass%. It can also be 15 to 45 mass%.

[0019] <(B) Alkyl cellulose> In this specification, the term "alkylcelluloses" refers to one or more compounds selected from the group consisting of cellulose compounds in which all or part of the hydroxyl groups are substituted with alkoxy groups. The alkoxy groups are preferably linear or branched alkoxy groups having 1 to 6 carbon atoms (more preferably 1 to 3 carbon atoms) (e.g., methoxy, ethoxy, etc.). In addition, the substitution rate of the alkoxy group of the alkyl cellulose is not particularly limited, but from the viewpoint of suppressing powdering of the granules, the upper limit can be 50 mass%, 45 mass%, 40 mass%, 36 mass%, or 34 mass% based on the converted dry matter, and the lower limit can be 10 mass%, 15 mass%, 20 mass%, 22 mass%, or 25 mass% based on the converted dry matter. Among them, the range of 10 to 50 mass% based on the converted dry matter is preferable, and the range of 25 to 34 mass% is more preferable. The quantification of the substitution rate of the alkoxy group of alkylcelluloses is carried out in accordance with the method for quantifying the methoxy group of methylcellulose described in the Japanese Pharmacopoeia, 18th Edition. The viscosity of the alkylcelluloses is not particularly limited, but from the viewpoint of suppressing powdering of the granules, the upper limit can be 800 mP·s, 500 mP·s, 300 mP·s, 100 mP·s, 50 mP·s, 30 mP·s, 25 mP·s, 20 mP·s, or 18 mP·s, and the lower limit can be 0.05 mP·s, 0.1 mP·s, 1 mP·s, 3 mP·s, 5 mP·s, 8 mP·s, or 10 mP·s. Among these, 1 to 50 mPa·s is preferable, and 10 to 20 mPa·s is more preferable. The viscosity of the alkylcelluloses is measured by measuring the viscosity of a 2% aqueous solution at 20°C in accordance with the viscosity measurement method for methylcellulose described in the 18th revised Japanese Pharmacopoeia. The alkyl celluloses may be used alone or in combination of two or more kinds.

[0020] Specific examples of such alkyl celluloses include methyl cellulose, ethyl cellulose, etc., and one of these may be used alone or two or more of them may be used in combination. As the alkyl cellulose, methyl cellulose is preferred from the viewpoint of preventing powdering. These alkylcelluloses are all known components, and may be produced by known methods or may be commercially available products.

[0021] The content of alkylcelluloses in the granules of the present invention is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of the granules, the type and amount of other blended components, and the use of the granules, etc., and the upper limit of the total amount of alkylcelluloses relative to the total mass of the granules can be 50 mass%, 35 mass%, 20 mass%, 15 mass%, 12 mass%, 9 mass%, 6 mass%, or 4 mass%, and the lower limit can be 0.01 mass%, 0.05 mass%, 0.3 mass%, 0.1 mass%, 0.5 mass%, 0.8 mass%, 1 mass%, or 1.5 mass%. Among them, 0.01 to 50 mass% is preferable, 0.05 to 12 mass% is more preferable, and 0.05 to 9 mass% is particularly preferable. In addition, even when the granules are provided as a composition described later, the content of alkyl celluloses is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the suppression of powdering of the granules, the type and amount of other blended components, and the use of the granules, and the upper limit of the total amount of alkyl celluloses relative to the total mass of the granules can be 50 mass%, 35 mass%, 20 mass%, 15 mass%, 12 mass%, 9 mass%, 6 mass%, 5 mass%, 4 mass%, or 3 mass%, and the lower limit can be 0.01 mass%, 0.05 mass%, 0.3 mass%, 0.1 mass%, 0.5 mass%, 0.8 mass%, 1 mass%, or 1.5 mass%. Among them, 0.01 to 50 mass% is preferable, 0.05 to 12 mass% is more preferable, and 0.05 to 9 mass% is particularly preferable.

[0022] In the present invention, the mass ratio of the (A) highly absorbent component and the (B) alkyl celluloses in the granules is not particularly limited, but the upper and lower limits can be appropriately set taking into consideration the prevention of powdering of the granules, the type of highly absorbent component to be blended, the types and amounts of other blended components, and the use of the granules. For example, the upper limit can be 10 parts by mass, 5 parts by mass, 3 parts by mass, 1.5 parts by mass, 1 part by mass, 0.8 parts by mass, 0.5 parts by mass, 0.3 parts by mass, 0.25 parts by mass, 0.18 parts by mass, or 0.15 parts by mass of alkyl celluloses per 1 part by mass of the highly absorbent components in total, and the lower limit can be 0.0001 parts by mass, 0.001 parts by mass, 0.005 parts by mass, 0.008 parts by mass, 0.01 parts by mass, 0.03 parts by mass, 0.05 parts by mass, 0.08 parts by mass, or 0.1 parts by mass. In particular, the alkylcelluloses are preferably contained in an amount of 0.001 to 3 parts by mass, more preferably 0.005 to 1 part by mass, and particularly preferably 0.01 to 0.5 part by mass, per 1 part by mass of the total highly water-absorbent components.

[0023] In addition, when an inorganic metal compound is used as the highly water-absorbent component, the upper and lower limits can be set appropriately taking into consideration the prevention of powdering of the granules, the type of inorganic metal compound to be blended, the types and amounts of other blended components, and the use of the granules, etc. For example, the upper limit can be 10 parts by mass, 5 parts by mass, 3 parts by mass, 1.5 parts by mass, 1 part by mass, 0.8 parts by mass, 0.5 parts by mass, 0.3 parts by mass, 0.25 parts by mass, 0.18 parts by mass, or 0.15 parts by mass of alkyl celluloses per 1 part by mass of inorganic metal compounds in total, and the lower limit can be 0.0001 parts by mass, 0.001 parts by mass, 0.005 parts by mass, 0.008 parts by mass, 0.01 parts by mass, 0.03 parts by mass, 0.05 parts by mass, 0.08 parts by mass, or 0.1 parts by mass. Among them, the alkylcelluloses are preferably contained in an amount of 0.001 to 3 parts by mass, more preferably 0.01 to 1 part by mass, and particularly preferably 0.05 to 0.5 parts by mass, per 1 part by mass of the total inorganic metal compounds.

[0024] In addition, when synthetic hydrotalcite is used as the highly water-absorbent component, the mass ratio of the synthetic hydrotalcite to the alkyl celluloses in the granules is not particularly limited, but the upper and lower limits can be appropriately set in consideration of the prevention of powdering of the granules, the type and amount of other blended components, and the use of the granules. For example, the upper limit can be 10 parts by mass, 5 parts by mass, 3 parts by mass, 1.5 parts by mass, 1 part by mass, 0.8 parts by mass, 0.5 parts by mass, 0.3 parts by mass, 0.25 parts by mass, 0.18 parts by mass, or 0.15 parts by mass of alkyl celluloses per 1 part by mass of synthetic hydrotalcite, and the lower limit can be 0.0001 parts by mass, 0.001 parts by mass, 0.005 parts by mass, 0.008 parts by mass, 0.01 parts by mass, 0.03 parts by mass, 0.05 parts by mass, 0.08 parts by mass, or 0.1 parts by mass. In particular, the alkylcelluloses are preferably contained in an amount of 0.001 to 3 parts by mass, more preferably 0.01 to 1 part by mass, and particularly preferably 0.05 to 0.5 parts by mass, per part by mass of synthetic hydrotalcite.

[0025] In the present invention, "granules" refers to those granulated into a granular form, and includes those provided as "powders" if they are granulated. The "granules" can be produced by, for example, mixing component (A), component (B), water and other additives added as necessary, and the active ingredient, by any known method. The order in which the components are mixed is not particularly limited, and they can be mixed in any order. Among them, production by a wet granulation method is preferred.

[0026] In the present invention, the "granules" may be directly used as granules (including effervescent granules and fine granules) or powders as defined in the General Provisions of Preparations of the Japanese Pharmacopoeia, 18th Edition. In addition, the granules may be made into compositions in the form usually used in medicines, quasi-drugs, cosmetics, foods, etc., depending on the intended use. For example, the granules of the present invention may be mixed with other granules, additives, and active ingredients to form granules or powders as defined in the General Provisions of Preparations of the Japanese Pharmacopoeia, 18th Edition. In addition, the granules of the present invention may be compressed to obtain tablets (including orally disintegrating tablets, chewable tablets, effervescent tablets, dispersible tablets, dissolving tablets, and oral tablets (including lozenges, sublingual tablets, buccal tablets, adhesive tablets, and gums)), or may be mixed with other granules, additives, and active ingredients, and filled into a capsule base to form capsules (hard capsules and soft capsules). Furthermore, the obtained granules can be used to prepare compositions in the dosage forms described in the General Provisions for Preparations of the Japanese Pharmacopoeia, 18th Edition, such as syrups and pills. In the present invention, since powdering of granules can be suppressed, it is more preferable to make the composition in a dosage form selected from the group consisting of tablets, capsules, granules, powders, and pills, and it is particularly preferable to make the composition in a dosage form selected from the group consisting of granules and powders.

[0027] The above composition can be manufactured according to the above-mentioned shape and dosage form, according to a method known in the fields of pharmaceuticals, quasi-drugs, cosmetics, food, etc., such as the method described in the General Provisions for Preparations of the Japanese Pharmacopoeia, 18th Edition.

[0028] In addition to the above-mentioned components, the granules of the present invention and the above-mentioned composition may contain one or more active ingredients and additives (such as excipients, binders, lubricants, colorants, flavorings, coating agents, etc.) used in the fields of pharmaceuticals, quasi-drugs, cosmetics, food, etc.

[0029] Examples of excipients include lactose, sucrose, mannitol, and the like. Examples of binders include gum arabic, powdered gum arabic, tragacanth, powdered tragacanth, and the like. Lubricants include, for example, magnesium stearate, talc, and the like. Examples of colorants include tar dyes and ferric oxide. Examples of flavoring agents include stevia and aspartame. Examples of the coating agent include film-forming polymers such as methacrylic acid copolymer S, methacrylic acid copolymer L, and methacrylic acid copolymer LD. When forming the film, it is also possible to mix plasticizers such as triethyl citrate and triacetin, and powders such as talc, titanium oxide, yellow ferric oxide, ferric oxide, and legal colorants.

[0030] The use of the composition is not particularly limited, and it can be used as a medicine, a quasi-drug, a food (particularly a food for specified health uses, a food with nutrient function claims, a food with functional claims, a supplement, etc.). For example, when used as a medicine, a quasi-drug, etc., it can be used as, specifically, for example, a cold medicine, an antipyretic analgesic, a cough suppressant expectorant, a gastrointestinal medicine, a laxative, an antiasthmatic, a vitamin-based drug preparation, a vitamin-containing health agent, a medicine for rhinitis, a medicine for allergies, a hypnotic sedative, an antidiarrheal drug, etc., depending on the type of the (A) component and the type of other blended components. In the present invention, it is preferable to use it as a gastrointestinal medicine.

[0031] In addition to the above-mentioned components, the composition may contain one or more other medicinal ingredients depending on the above-mentioned medicinal applications.

[0032] Hereinafter, medicinal ingredients that can be blended for each purpose will be described, however, the ingredients and purposes are not limited to those listed here, and medicinal ingredients may be blended appropriately according to the purpose. When used as a cold medicine, for example, aspirin, aluminum aspirin, acetaminophen, ethenzamide, sazapirine, salicylamide, lactylphenetidine, sodium loxoprofen, ibuprofen, isopropylantipyrine, isothipendyl hydrochloride, diphenylpyraline hydrochloride, diphenhydramine hydrochloride, difeterol hydrochloride, triprolidine hydrochloride, tripelennamine hydrochloride, thonzylamine hydrochloride, fenethazine hydrochloride, methdilazine hydrochloride, diphenhydramine salicylate, carbinoxamine diphenyldisulfonate, , alimemazine tartrate, diphenhydramine tannate, diphenylpyraline teoclate, mebhydroline napadisilate, promethazine methylenedisalicylate, carbinoxamine maleate, chlorpheniramine maleate, d-chlorpheniramine maleate, diphenterol phosphate, clemastine fumarate, mequitazine, azelastine hydrochloride, ebastine, epinastine hydrochloride, olopatadine hydrochloride, cetirizine hydrochloride, bepotastine besilate, fexofenadine, homochlorcyclizine hydrochloride, loratadine, allocramine hydrochloride , cloperastine hydrochloride, pentoxifylline citrate (carbetapentane citrate), tipepidine citrate, dibunate sodium, dextromethorphan hydrobromide, dextromethorphan phenolphthaline salt, tipepidine hibenzate, cloperastine fendizoate, pentoxyverine citrate, codeine phosphate, dihydrocodeine phosphate, dimemorphan phosphate, noscapine hydrochloride, noscapine, dl-methylephedrine hydrochloride, dl-methylephedrine saccharin salt, pseudoephedrine hydrochloride, guaiacolsulfone potassium caffeine, guaifenesin, potassium cresol sulfonate, bromhexine hydrochloride, L-carbocysteine, L-ethylcysteine ​​hydrochloride, ambroxol hydrochloride, isopropamide iodide, glycyrrhizic acid and its salts, tranexamic acid, sodium benzoate, caffeine, anhydrous caffeine, vitamin B1 and its derivatives and their salts, vitamin B2 and its derivatives and their salts, vitamin C and its derivatives and their salts, hesperidin and its derivatives and their salts, glycine, aminoacetic acid,Dihydroxyaluminum aminoacetate (aluminum glycinate) and other ingredients may be appropriately combined.

[0033] When used as an antipyretic analgesic, for example, acetaminophen, ibuprofen, loxoprofen sodium, lactylphenetidine, aspirin, aluminum aspirin, ethenzamide, sasapirin, salicylamide, sodium salicylate, isopropylantipyrine, allylisopropylacetylurea, bromvalerylurea, tranexamic acid, sodium benzoate, caffeine, anhydrous caffeine, vitamin B1 and its derivatives and salts thereof, vitamin B2 and its derivatives and salts thereof, vitamin C and its derivatives and salts thereof, hesperidin and its derivatives and salts thereof, aminoacetic acid, glycine, aminoacetic acid, dihydroxyaluminum aminoacetate (aluminum glycinate), etc. may be blended in appropriate combination.

[0034] When used as an antitussive and expectorant, for example, alloclamide hydrochloride, cloperastine hydrochloride, pentoxyverine citrate (carbetapentane citrate), tipepidine citrate, sodium dibunate, dextromethorphan hydrobromide, dextromethorphan phenolphthaline salt, tipepidine hibenzate, cloperastine phendizoate, codeine phosphate, dihydrocodeine phosphate, dimemorphan phosphate, trimetoquinol hydrochloride, methoxyphenamine hydrochloride, dl-methylephedrine hydrochloride, l-methyl hydrochloride Ephedrine, pseudoephedrine hydrochloride, noscapine hydrochloride, noscapine, tranexamic acid, aminophylline, diprophylline, theophylline, proxyphylline, ammonium chloride, l-menthol, potassium guaiacolsulfonate, guaifenesin, potassium cresolsulfonate, bromhexine hydrochloride, ambroxol hydrochloride, L-carbocysteine, lysozyme chloride, L-ethylcysteine ​​hydrochloride, L-methylcysteine ​​hydrochloride, isothipendyl hydrochloride, iproheptine hydrochloride, difeterol hydrochloride, hydrochloric acid Diphenylpyraline, diphenhydramine hydrochloride, triprolidine hydrochloride, tripelennamine hydrochloride, thonzylamine hydrochloride, fenethazine hydrochloride, promethazine hydrochloride, diphenhydramine salicylate, carbinoxamine diphenyldisulfonate, alimemazine tartrate, diphenhydramine tannate, fenethazine tannate, diphenylpyraline theoclate, promethazine methylenedisalicylate, carbinoxamine maleate, chlorpheniramine maleate, d-chlorpheniramine maleate, difeterol phosphate , clemastine fumarate, mequitazine, azelastine hydrochloride, ebastine, epinastine hydrochloride, olopatadine hydrochloride, cetirizine hydrochloride, bepotastine besilate, fexofenadine, homochlorcyclizine hydrochloride, loratadine, sodium caffeine benzoate, caffeine, caffeine anhydrous, cetylpyridinium chloride, dequalinium chloride, chlorhexidine hydrochloride, glycine, aminoacetic acid, dihydroxyaluminum aminoacetate (aluminum glycinate), etc. may be formulated in appropriate combination.

[0035] In the case of use as a gastrointestinal drug, for example, oxethazaine, magnesium hydroxide, precipitated calcium carbonate, abalone shell, tallow, glycine, dihydroxyaluminum aminoacetate, aminoacetic acid, l-menthol, dl-menthol, betaine hydrochloride, glutamic acid hydrochloride, carnitine chloride, bethanechol chloride, dry yeast, serrapeptase, starch digestive enzyme, protein digestive enzyme, fat digestive enzyme, cellulose digestive enzyme, ursodeoxycholine, etc. Acid, oxycholanates, cholic acid, bile powder, bile extract (powder), dehydrocholic acid, animal bile (including yutan), intestinal regulation probiotics, acrinol, berberine chloride, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, berberine tannate, bismuth subsalicylate, bismuth subnitrate, bismuth subcarbonate, bismuth subgallate, tannic acid, albumin tannate, methylene thimol tannin, kaolin, aluminum hydroxynaphthoate, bec Chin, medicinal charcoal, calcium lactate, loperamide hydrochloride, sucralfate, cetraxate hydrochloride, pirenzepine hydrochloride, famotidine, ranitidine, ranitidine hydrochloride, loxazine acetate hydrochloride, cimetidine, itopride hydrochloride, oxyphencyclimine hydrochloride, dicyclomine hydrochloride, methixene hydrochloride, scopolamine hydrobromide, atropine methyl bromide, anisotropine methyl bromide, scopolamine methyl bromide, l-hyoscyamine methyl bromide, benatidine methyl bromide Cthidium, isopropamide iodide, diphenylpiperidinomethyldioxolane iodide, papaverine hydrochloride, ethyl aminobenzoate, sodium azulene sulfonate, aldioxa, glycyrrhizinic acid and its salts, L-glutamine, potassium copper chlorophyllin, sodium copper chlorophyllin, histidine hydrochloride, pepsin hydrolysate of porcine stomach wall, acid hydrolysate of porcine stomach wall, methylmethionine sulfonium chloride, dimethylpolysiloxane, and the like may be blended in appropriate combination.

[0036] When used as a laxative, for example, dioctyl sodium sulfosuccinate, aloin, sulfur, casanthranol, sennosides A and B, bisacodyl, malt extract, flavored castor oil, castor oil, ursodeoxycholic acid, oxycholanic acid salts, dry yeast, cholic acid, dimethylpolysiloxane, intestinal regulating probiotic components, dehydrocholic acid, dl-menthol, l-menthol, vitamin B1 and its derivatives and their salts, vitamin B6 and its derivatives and their salts, nicotinamide, calcium pantothenate, etc. may be combined in an appropriate manner.

[0037] When used as an antidote, for example, diphenidol hydrochloride, diphenylpyraline hydrochloride, diphenhydramine hydrochloride, promethazine hydrochloride, meclizine hydrochloride, diphenhydramine salicylate, dimenhydrinate, diphenhydramine tannate, fenethazine tannate, diphenylpyraline teoclate, diphenhydramine fumarate, promethazine methylenedisalicylate, chlorpheniramine maleate, d-chlorpheniramine maleate, pheniramine maleate, scopolamine hydrobromide, oxyphencyclimine hydrochloride, dicyclomine hydrochloride, metixene hydrochloride, atropine methyl bromide, anisotropine methyl bromide, scopolamine methyl bromide, -l-hyoscyamine, methylbenactidium bromide, isopropamide iodide, diphenylpiperidinomethyldioxolane iodide, papaverine hydrochloride, ethyl aminobenzoate, cerium oxalate, ethyl piperidylacetylaminobenzoate, allylisopropylacetylurea, bromvalerylurea, caffeine, caffeine citrate, caffeine anhydrous, aminophylline, diprophylline, theophylline, dl-menthol, l-menthol, vitamin B1 and its derivatives and salts thereof, vitamin B2 and its derivatives and salts thereof, vitamin B6 and its derivatives and salts thereof, nicotinamide, calcium pantothenate, and the like may be blended in appropriate combination.

[0038] When used as a vitamin-based drug preparation or a vitamin-containing health supplement, for example, vitamin A, vitamin B1, vitamin B2, vitamin B5, vitamin B6, vitamin B12, vitamin C, vitamin D, vitamin E and their derivatives and their salts (retinol acetate, retinol palmitate, vitamin A oil, liver oil, liver oil, ergocalciferol, cholecalciferol, d-α-tocopherol succinate, dl-α-tocopherol succinate, dl-α-tocopherol succinate, Calcium ferrol, d-α-tocopherol acetate, dl-α-tocopherol acetate, d-α-tocopherol, dl-α-tocopherol, thiamine chloride hydrochloride, thiamine nitrate, bis-thiamine nitrate, thiamine disulfide, thiamine sulfide nitrate, thiamine dicetyl sulfate, dicethiamine hydrochloride, fursultiamine hydrochloride, octotiamine, sicotiamine, bis-ibuthiamine, bis-bentiamine, fursultiamine, prosultiamine, benfotiamine, flavin adenine Sodium dinucleotide, riboflavin, riboflavin sodium phosphate, riboflavin butyrate, pyridoxine hydrochloride, pyridoxal phosphate, hydroxocobalamin hydrochloride, hydroxocobalamin acetate, cyanocobalamin, hydroxocobalamin, mecobalamin, ascorbic acid, calcium ascorbate, sodium ascorbate, nicotinic acid, nicotinamide, panthenol, calcium pantothenate, sodium pantothenate, biotin, potassium aspartate, magnesium An appropriate combination of an equal amount of calcium carbonate, inositol hexanicotinate, hepronicate, dehydrocholic acid, ursodeoxycholic acid, L-cysteine ​​hydrochloride, L-cysteine, orotic acid, gamma oryzanol, calcium glycerophosphate, calcium gluconate, precipitated calcium carbonate, calcium lactate, glucuronolactone, glucuronic acid amide, sodium chondroitin sulfate, thioctic acid, thioctic acid amide, pantethine, rutin, royal jelly, etc. may be used.

[0039] The method of administration of the composition is not particularly limited and may be appropriately selected depending on the intended use of the composition, but oral administration is preferred. The method of use and dosage of the composition are not particularly limited and may be appropriately selected and determined depending on the intended use of the composition, the method of administration, the dosage form of the composition, etc.

[0040] Furthermore, the container in which the composition is packaged is not particularly limited, and the composition can be packaged in, for example, a bottle package, a strip package (SP), a press through package (PTP), a pillow package, a stick package, or the like.

[0041] The present invention also relates to a method for suppressing dusting of granules by blending (B) alkylcelluloses with granules containing (A) a highly water-absorbent component. In this embodiment of the invention, the meanings of the various terms, the amounts of the various components, etc. are all the same as those explained for the granules above.

[0042] In addition, the present specification discloses the following embodiments, for example, but is not limited to these. [Aspect 1] Granules comprising the following components (A) and (B): (A) Highly absorbent component (B) Alkyl cellulose [Aspect 2] 2. The granule according to claim 1, wherein the component (A) has a water absorption capacity of 70 mL / 100 g or more. [Aspect 3] The granule according to embodiment 1 or 2, wherein the component (A) is an inorganic metal compound. [Aspect 4] The granules of embodiment 3, wherein the (A) component is a synthetic hydrotalcite. [Aspect 5] A granule according to any one of aspects 1-4, wherein the (B) component is methylcellulose. [Aspect 6] A composition comprising a granule according to any one of aspects 1-5. [Aspect 7] A method for producing granules, comprising mixing and granulating the following components (A) and (B): (A) Highly absorbent component (B) Alkyl cellulose [Aspect 8] The method according to embodiment 7, wherein the component (A) has a water absorption capacity of 70 mL / 100 g or more. [Aspect 9] A method of suppressing powdering of granules by blending (B) alkylcelluloses with (A) granules containing a highly water-absorbent component. [Aspect 10] The method according to claim 9, wherein the component (A) has a water absorption capacity of 70 mL / 100 g or more. EXAMPLES

[0043] The present invention will be described in more detail below with reference to examples, but the present invention is not limited thereto. In the following test examples, the amount of each component used is the amount of the indicated component itself, unless otherwise specified as a converted amount.

[0044] [Example 1] Particle size distribution test Granules were produced by wet granulation using the components shown in Table 1 below (unless otherwise specified, the units of numbers indicate parts by mass).

[0045] The synthetic hydrotalcite used in this case was procured and used, which had a water absorption of 133 mL / 100 g as determined by the following water absorption test. Weigh 1g of this product onto a dry watch glass. Pour water into the burette. Add water while mixing with a spatula. The end point is when the entire piece becomes a glue-like lump and peels off from the glass surface. Expressed in mL / 100g. Water absorption amount (mL / 100g) = titration value (mL) x 100

[0046] [Table 1]

[0047] Regarding Formulation 1-3, when the obtained granules were classified after drying and sieving, the particle size distribution was confirmed using a 200 mesh (75 μm) sieve. The results are shown below.

[0048] [Table 2]

[0049] In Formulations 1 and 2, powdering occurred, and more than 10% of the granules passed through a 200-mesh sieve during classification. However, in Formulation 3, which further contains methylcellulose, the number of fine particles passing through the 200-mesh sieve was significantly reduced, making it difficult for powdering to occur. Therefore, it was found that the incorporation of alkylcelluloses such as methylcellulose can suppress powdering of granules. The increase in the percentage of granules passing through the 200-mesh sieve in Formulation 2 is thought to be due to the addition of ginger powder, a water-absorbing component.

[0050] [Manufacturing Examples 1 to 5] Granules containing the following ingredients are prepared in a conventional manner and packaged in strip-packaging aluminum foil (manufactured by Nissan Chemical Industries, Ltd.) (numbers are in parts by weight).

[0051] [Table 3]

[0052] [Manufacturing Examples 6-13] Granules containing the following ingredients are prepared in the usual way. The amounts of ingredients are listed based on the daily dose of 3 packets (3900 mg).

[0053] Production Example 6 Sodium bicarbonate 240mg Precipitated calcium carbonate 710mg Magnesium aluminometasilicate 900mg Magnesium hydroxide 550mg Pirenzepine hydrochloride hydrate 46.9mg Methylmethionine sulfonium chloride 75mg Perilla Root Dry Extract 30mg (Equivalent of Raw Herbal Medicine 270mg) Cinnamon powder 100mg D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0054] Production Example 7 Precipitated calcium carbonate 1000mg Synthetic hydrotalcite 780mg Magnesium hydroxide 300mg Pirenzepine hydrochloride hydrate 46.9mg Methylmethionine sulfonium chloride 75mg Aldioxa 150mg Itopride hydrochloride 150mg Carrot dry extract 20mg (equivalent to 290mg of raw drug) Ginger powder 100mg D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0055] Production Example 8 Precipitated calcium carbonate 1000mg Synthetic hydrotalcite 780mg Magnesium hydroxide 300mg Pirenzepine hydrochloride hydrate 46.9mg Methylmethionine sulfonium chloride 75mg Aldioxa 150mg Cinnamon powder 100mg Ginger powder 100mg D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0056] Production Example 9 Sodium bicarbonate 240mg Precipitated calcium carbonate 710mg Magnesium aluminometasilicate 900mg Magnesium hydroxide 550mg Pirenzepine hydrochloride hydrate 46.9mg Methylmethionine sulfonium chloride 75mg Itopride hydrochloride 150mg Chinpi powder 300mg Clove powder 50mg D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0057] Manufacturing Example 10 Sodium bicarbonate 240mg Precipitated calcium carbonate 710mg Magnesium aluminometasilicate 900mg Magnesium hydroxide 550mg Pirenzepine hydrochloride hydrate 46.9mg Methylmethionine sulfonium chloride 75mg Licorice extract powder 75mg (equivalent to 525mg of raw drug) Itopride hydrochloride 150mg Perilla Root Dry Extract 30mg (Equivalent of Raw Herbal Medicine 270mg) Carrot dry extract 20mg (equivalent to 290mg of raw drug) D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0058] Manufacturing Example 11 Precipitated calcium carbonate 1000mg Synthetic hydrotalcite 780mg Magnesium hydroxide 300mg Pirenzepine hydrochloride hydrate 46.9mg Aldioxa 150mg Itopride hydrochloride 150mg Carrot dry extract 20mg (equivalent to 290mg of raw drug) Ginger powder 100mg D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0059] Manufacturing Example 12 Sodium bicarbonate 240mg Precipitated calcium carbonate 710mg Magnesium aluminometasilicate 900mg Magnesium hydroxide 550mg Pirenzepine hydrochloride hydrate 46.9mg Itopride hydrochloride 150mg Chinpi powder 300mg Clove powder 50mg D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring

[0060] Manufacturing Example 13 Sodium bicarbonate 240mg Precipitated calcium carbonate 710mg Magnesium aluminometasilicate 900mg Magnesium hydroxide 550mg Pirenzepine hydrochloride hydrate 46.9mg Licorice extract powder 75mg (equivalent to 525mg of raw drug) Itopride hydrochloride 150mg Perilla Root Dry Extract 30mg (Equivalent of Raw Herbal Medicine 270mg) Carrot dry extract 20mg (equivalent to 290mg of raw drug) D-mannitol, methylcellulose, carmellose calcium, hardened oil, sucralose, hydroxypropyl cellulose, corn starch, l-menthol, hydrated silicon dioxide, flavoring [Industrial Applicability]

[0061] According to the present invention, it is possible to provide granules containing highly water-absorbent components that are inhibited from powdering and are used in the fields of pharmaceuticals, quasi-drugs, cosmetics, food, etc., and therefore the granules can be used, for example, in the pharmaceutical industry, quasi-drugs industry, cosmetics industry, food industry, etc.

Claims

1. Granules comprising the following components (A) and (B): (A) Highly absorbent component (B) Alkyl celluloses

2. 2. The granule according to claim 1, wherein the component (A) has a water absorption capacity of 70 mL / 100 g or more.

3. 3. Granules according to claim 1 or 2, wherein component (A) is an inorganic metal compound.

4. The granule according to claim 3, wherein component (A) is a synthetic hydrotalcite.

5. 3. A granule according to claim 1 or 2, wherein component (B) is methylcellulose.

6. A composition comprising the granules according to claim 1 or 2.

7. A method for producing granules, comprising mixing and granulating the following components (A) and (B): (A) Highly absorbent component (B) Alkyl celluloses

8. The method according to claim 7, wherein the component (A) has a water absorption capacity of 70 mL / 100 g or more.

9. A method for suppressing powdering of granules by blending (B) alkylcelluloses with (A) granules containing a highly water-absorbent component.

10. The method according to claim 9, wherein the component (A) has a water absorption of 70 mL / 100 g or more.

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