JP2022037173A - Solid pharmaceutical - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a solid pharmaceutical that contains at least a certain amount of herbal medicine but prevents the occurrence of a molding failure, has no variation in quality, and can be taken with a good feeling.

SOLUTION: A solid pharmaceutical 1 containing herbal medicine has a maximum diameter W of 2.5-9.0 mm.

SELECTED DRAWING: Figure 1

COPYRIGHT: (C)2022,JPO&INPIT

Description

The present invention relates to a solid drug in which a certain amount or more of a crude drug is blended, yet molding failure is unlikely to occur and the quality thereof is guaranteed.

When a solid drug containing a certain amount or more of a crude drug is produced, the crude drug generally has a high hygroscopicity, so that there is a problem that a molding disorder is likely to occur. In particular, over-the-counter drugs such as Chinese herbal preparations, gastrointestinal drugs, and common treatment drugs, which can contain multiple active ingredients in the form of crude drugs, require a higher daily dose than ethical drugs containing medicinal ingredients alone. Therefore, the size of the solid drug is large and it is easy to absorb moisture, so that there is a tendency for more molding problems to occur.

However, in pharmaceutical products, it is most important to manufacture accurately based on a fixed prescription, and manufacturing under conditions where molding failures occur frequently may cause variations in quality. , Not desirable.

On the other hand, it is generally known that it is difficult to mold a solid drug into a small size (Patent Document 1). Therefore, it was a common general skill of those skilled in the art to think that a solid drug containing a certain amount of crude drug would have the same tendency or be more difficult.

Japanese Unexamined Patent Publication No. 2011-126857

The present invention has been made by breaking through such conventional conventional wisdom, and is an excellent solid drug that is less likely to cause molding failure and has no variation in quality even though a certain amount or more of crude drug is blended. The purpose is to provide.

In order to achieve the above object, the first gist of the present invention is a solid drug having a crude drug and having a maximum diameter of 2.5 to 9.0 mm.

Then, among the solid drugs of the above first gist, those containing 1% by mass or more of crude drugs as a total amount with respect to the whole solid drug are taken as the second gist, and among the solid drugs of the above first and second gist. Of the solid medicines in the above 1st to 3rd gist, the crude drugs are plant roots, bark, leaves, rhizomes, above-ground stems, flowers, whole plants, fruits, and fruit skins. At least one selected from the group consisting of, seeds and resins is used, and those blended in at least one form of crude drug powder and extract powder are the fourth gist, and the gist of the above 1 to 4 is The fifth gist is a solid drug having a hardness of 1.0 to 10.0 kp.

Further, among the solid medicines of the above 1st to 5th gist, those containing 0.001 to 20 parts by mass of the additive as a total amount with respect to 1 part by mass of the total amount of the crude drug are referred to as the 6th gist, and the above 1st gist. The seventh gist is a package containing 2 to 80 solid medicines of the gist of ~ 6.

That is, the present inventors have repeated various studies on solid medicines containing a certain amount or more of crude drugs in order to suppress the occurrence of molding disorders in the manufacturing process. As a result, they have found that when the maximum diameter of a solid drug is set within a specific range, the occurrence of molding disorders can be suppressed and the quality of the solid drug can be guaranteed, and the present invention has been reached.

As described above, in the solid drug of the present invention, the occurrence of molding disorders is effectively suppressed in the manufacturing process, even though the crude drug is blended in a certain amount or more. Therefore, a solid drug having a desired prescription can be stably produced, and the quality of the solid drug can be guaranteed at a high level. In addition, since the maximum diameter of the solid drug is specified and the size is reduced, the feeling of taking the drug is improved, such as being easily swallowed.

(A) to (d) are explanatory views showing an example of the shape of the solid medicine of the present invention.

Next, a mode for carrying out the present invention will be described.

The present invention is a solid drug having a crude drug, the maximum diameter of which is 2.5 to 9.0 mm. Details will be described below.

The crude drug in the present invention includes, but is not limited to, all those listed as "herbal medicine" in the Japanese Pharmacopoeia and outside the Japanese Pharmacopoeia. It includes all dried or simply processed natural products such as plants, animals and minerals that have a medicinal purpose. Among them, the crude drug used in the present invention is preferably a plant crude drug. It is preferable to use plant crude drugs derived from plant roots, bark, leaves, rhizomes, rhizomes, flowers, whole plants, fruits, pericarps, seeds and resins. Among them, those derived from plant roots, bark, leaves, rhizomes, above-ground stems, whole plants, fruits and pericarps are more preferable, and those derived from plant roots, bark, leaves, rhizomes, above-ground stems, whole plants and pericarps are further preferable. More preferred. Further, the crude drug tends to have high hygroscopicity when it is in the form of crude drug powder or extract powder, and the present invention particularly relates to a crude drug containing such a highly hygroscopic drug. , Can exert an excellent effect.

Herbal medicines derived from the roots of plants include, for example, licorice, ipecac, valeriana, valeriana, valeriana, gentian, kojin, psycho, saishin, jiou, shakuyaku, senega, sohakuhi, touki, ipecac, carapichea, valeriana, Examples include gentiana, mokko, and ryutan. Examples of crude drugs derived from the bark of plants include cinnamon, Mallotus japonicus, Phellodendron amur, Magnolia officinalis, Marsdenia cundrum, and Eucommia ulmoides. Examples of crude drugs derived from the leaves of plants include aloe, senna, perilla, perilla, amacha, and manzanitas. Examples of crude drugs derived from the rhizome of a plant include turmeric, Coptis chinensis, zedoary, ginger, sankirai, senkyu, sojutsu, rhubarb, zedoary, bowie, and rotocon. Examples of crude drugs derived from the above-ground stems of plants include Ephedra, Geranium thunbergii, and Mokutsu. Examples of crude drugs derived from the flowers of plants include chamomile, kouka, saffron, faith, clove, inchinko, kagosou, kikuka, and schizonepeta. Examples of crude drugs derived from whole plants include Swertia japonica, Houttuynia cordata, Houttuynia cordata, and Mentha. Examples of crude drugs derived from the fruits of plants include fennel, catalpa ovata, foxtail, fennel, and capsicum. Examples of crude drugs derived from the pericarp of plants include Japanese pepper, chimpi, and spruce. Examples of crude drugs derived from plant seeds include apricot kernel, ketsumeishi, hedychium, tounin, and apricot kernel. Examples of crude drugs derived from plant resins include gum arabic and tragant.

Specific examples of the crude drug in the present invention include Keihi, Kanzo, Onji, Akamega wrinkle, Asenyaku, Amacha, Arabian gum, Aloe, Ansokko, Ireisen, Inchinkou, Inyoukaku, Uikyo, Ukon, Uyaku, Uwaurushi, Agetsu, and Engosaku. , Ougi, Ogon, Ousei, Oubaku, Ouren, Shazensou, Kagosou, Kashu, Gajutsu, Kakkon, Kanokosou, Karokon, Kankyo, Kikyo, Kikuka, Kisage, Kijitsu, Kyokatsu, Kyounin, Kukoshi, Kujin , Geranium thunbergii, Kouka, Kojin, Kobushi, Koboku, Goou, Gositsu, Goshuyu, Goboushi, Gomishi, Colombo, Konzlango, Psycho, Saishin, Saffron, Sankirai, Sanshishi, Sanshuyu, Sansho, Sansounin, Sanyaku, Jikou, Shigoka Shikon, Shitsurin, Shakuyaku, Jashoushi, Shazenshi, Juyaku, Shuksha, Shokyo, Shozuku, Shouma, Shini, Sekkoku, Senega, Senkyu, Senkotsu, Senso, Senna, Senburi, Sojutsu, Souhakuhi, Soboku, Soyou, Daio , Chikusetsu carrot, Chimo, Chouji, Geranium thunbergii, Chorei, Chinpi, Tenma, Tenmondou, Tougashi, Togarashi, Touki, Tounin, Tohi, Tokon, Tochu, Tragant, Nigaki, Carrot, Nindou, Baimo, Bakumondou Hange, Byakushi, Byakujutsu, Biwayou, Binrouji, Bukuryo, Bushi, Belladonna, Hens, Bowie, Bowcon, Bowfu, Buttonpi, Himika, Maou, Makuri, Mashinin, Mokutsu, Mokko, Yakuchi, Yutan, Yokuinin, Ryukotsu , Geranium thunbergii, gentian, rosin, rotocon and the like. In particular, from the point of being widely used for general-purpose medicines, Keihi, Kanzo, Onji, Akamega wrinkle, Amacha, Arabian gum, Aloe, Inchinkou, Uikyo, Turmeric, Uwaurushi, Ougi, Ogon, Oubaku, Ouren, Geranium thunbergii, Gajutsu, Kakkon, Kagosou , Kanokosou, Kikuka, Kyoko, Kijitsu, Kyonin, Keigai, Gentiana, Geranium, Kouka, Kojin, Koboku, Psycho, Saffron, Sansho, Juyaku, Jio, Shakuyaku, Shuksha, Ginger, Shini, Senega, Senkyu , Sojutsu, Soyo, Daiou, Taiso, Chouji, Chimpi, Togarashi, Tohi, Tochu, Touki, Tounin, Tokon, Tragant, Carrot, Hacka, Byakujutsu, Biwayou, Veradonna, Bowie, Bowfu, Maou, Mokko, Rotokon Turmeric, turmeric, licorice, licorice, licorice, geranium, geranium, gentian, geranium thunbergii, geranium thunbergii, ginger, ginger, ginger, ginger, licorice, swertia japonica, swertia japonica, swertia japonica, swertia japonica Is more preferably used, and in particular, Swertia japonica, Geranium thunbergii, and Onji can be preferably used. These can be used alone or in combination of two or more.

When these crude drugs are classified by taste, they can be roughly divided into six categories: "sweet", "spicy", "bitter", "egui", "astringent", and "no characteristic". Some crude drugs have a complex taste, such as cinnamon, and belong to a plurality of categories. Examples of herbal medicines classified as "sweet" include keihi, angelica acutiloba, licorice, gentiana, pearl oyster, cucumber, licorice, ginger, carrot, siler, rotocon, amacha, taiso, senega, peony, and yokuinin. Examples of crude drugs classified as "spicy" include keihi, touki, choy sum, ginger, ipecac, zedoary, capsicum, sansho, shukusha, shinii, clove, and inchinko. Herbal medicines classified as "bitter" include, for example, tokon, zedoary, shinii, gentiana, kakkon, kojin, marsdenia cundrum, ginger, carrot, rotokon, red mega wrinkle, atractylodes lanceolata, magnolia, veradonna, kanokosou, psycho, mokko, turmeric, and atractylodes lanceolata. , Senkyu, Sojutsu, Byakujutsu, Bowie, Swertia japonica, Uwaurushi, Senna, Soyo, Aloe, Kijitsu, Chimpi, Tohi, Kyonin, Tounin, Kouka, Saffron, Kikuka, Kikyo, Shakuyaku, Daiou, Maou, Ryutan, Byakushi Be done. Examples of crude drugs classified as "Egui" include Kikyo, Onji, Senega, and Mokutsu. Examples of crude drugs classified as "astringent" include peony, rhubarb, ephedra, geranium thunbergii, and catalpa ovata. Examples of crude drugs classified as "characterless" include Smilax glabra, Smilax glabra, Ketsumeishi, Sankirai, and Smilax glabra.

In addition, when these crude drugs are classified by the amount of ash described in the Japanese Pharmacopoeia and the Japanese Pharmacopoeia non-Japanese Pharmacopoeia standards, the upper limit is "less than 5%", "5% or more and less than 7%", and "7% or more and less than 10%". , "10% or more", and "not described" can be roughly divided into five categories. Examples of crude drugs classified as "less than 5%" include aloe, taiso, saussurea, coptis, platycodon grandiflorum, manzanitas, chimpi, arabic gum, tragant, carrot, kojin, and yokunin. Crude drugs classified as "5% or more and less than 7%" include, for example, ipecac, senega, ipecac, spruce, shinii, keihi, koboku, onji, belladonna, gentiana, kakkon, senkyu, psycho, jio, shakuyaku, and swertia japonica. Examples include catalpa and ketsumeishi. Crude drugs classified as "7% or more and less than 10%" include, for example, licorice, eucommia, zedoary, zedoary, sojutsu, biakujutsu, rotokon, bowi, phellodendron, chouji, atractylodes turmeric, saffron, tochu, ginger, and ginger. , Sansho, Kikuka, Shuksha, Inchinkou, Ryutan, Byakushi. Crude drugs classified as "10% or more" include, for example, valeriana, geranium thunbergii, biwayo, fennel, maou, schizonepeta, mallotus japonicus, hakka, senna, amacha, daiou, kagosou, juyaku, shazensou, soyo, kouka, marsdenia cundrum, and sohakuhi. , Mokutsu, Saishin, and Kamitsure. Examples of crude drugs classified as "not described" include apricot kernel and tounin.

The form of the crude drug includes not only the crude drug itself (herbal medicine) but also the following forms. That is, the crude drug of the present invention includes "herbal powder" in which the crude drug is powdered, "extract" obtained by extracting the crude drug or crude drug powder with an organic solvent such as water, ethanol, oil or a mixture thereof, and extraction. It includes all forms usually used for Chinese herbal preparations, such as "extract powder" obtained by drying the solution into powder and "concentrated extract" obtained by concentrating the extract.

In addition, the solid drug of the present invention may contain medicinal ingredients other than crude drugs. The medicinal ingredient other than the raw medicine is not particularly limited, but for example, an analgesic ingredient, an antihistamine ingredient, an antitussive ingredient, a bronchial dilator ingredient, an expectorant ingredient, a mucosal protective ingredient, an acid suppressant ingredient, a stomachic ingredient, an intestinal regulating ingredient, and an antidiarrheal ingredient. Ingredients, sympathetic nerve excitatory components, parasympathetic nerve blocking components, caffeine, vitamins, anti-inflammatory enzymes and the like can be mentioned.

The solid drug of the present invention can contain a large amount of crude drug, and specifically, it contains 1% by mass or more of the total amount of crude drug with respect to the whole solid drug. In particular, the total amount of crude drugs is 3 to 99% by mass, further 5 to 98% by mass, further 10 to 95% by mass, further 20 to 90% by mass, and further 30 to 80% by mass, based on the total amount of solid medicine. Further, it is preferably contained in an amount of 40 to 75% by mass, particularly 50 to 70% by mass. If the herbal medicine content is too low, a large amount of solid medicine must be taken in order to obtain the required amount of the active ingredient, which is complicated. Is. The total amount of the above-mentioned crude drugs means the total mass of the crude drugs when a plurality of kinds of crude drugs are used, and means the mass of the crude drugs alone when a single crude drug is used.

The solid medicine of the present invention can contain a large amount of crude drug, and the dose (dose) of the crude drug is the type and amount of the additive, the type and amount of other components, and the condition of the user (weight, age, It can be appropriately set according to gender, symptoms, physical condition, etc., and is not limited, but the following are exemplified from the viewpoint of exerting the effect of the present invention more remarkably. That is, usually, the oral dose per day can be 100 to 10000 mg as a cinnamon extract, more preferably 200 to 7500 mg, still more preferably 400 to 5000 mg, particularly preferably 600 to 4000 mg, and particularly more. It can be preferably 800 to 3500 mg, most preferably 3000 mg. The daily oral dose of cinnamon extract can be 100 to 10000 mg in terms of crude drug, more preferably 200 to 7500 mg, still more preferably 400 to 5000 mg, and particularly preferably 600 to 4000 mg. In particular, it can be more preferably 800 to 3500 mg, and most preferably 3000 mg.

Usually, the oral dose per day can be 200 to 10000 mg as a licorice extract, more preferably 400 to 8000 mg, still more preferably 600 to 7000 mg, particularly preferably 800 to 6000 mg, and particularly more preferably. It can be 1000 to 5000 mg, most preferably 5000 mg. The daily oral dose of licorice extract can be 200 to 10000 mg in terms of crude drug, more preferably 400 to 8000 mg, still more preferably 600 to 7000 mg, and particularly preferably 800 to 6000 mg. In particular, it can be more preferably 1000 to 5000 mg, and most preferably 5000 mg.

Usually, the daily oral dose can be 100 to 10000 mg as an ondi extract, more preferably 150 to 7500 mg, still more preferably 200 to 5000 mg, particularly preferably 250 to 3000 mg, and particularly more preferably. It can be 300 to 1500 mg. The daily oral dose of the ondi extract can be 800 to 5500 mg in terms of crude drug, more preferably 1000 to 5000 mg, still more preferably 1500 to 4500 mg, and particularly preferably 2000 to 4000 mg. Particularly more preferably, it can be 2500 to 3500 mg.

Usually, the oral dose per day can be 10 to 10000 mg as ginger extract, more preferably 20 to 7500 mg, still more preferably 50 to 6000 mg, particularly preferably 75 to 4000 mg, and particularly more preferably. Can be 100-2500 mg. The daily oral dose of ginger extract can be 30 to 30,000 mg in terms of crude drug, more preferably 60 to 22,500 mg, still more preferably 100 to 18,000 mg, and particularly preferably 200 to 12,000 mg. , Especially more preferably 300 to 7500 mg.

Usually, the oral dose per day can be 50 to 10000 mg as the geranium thunbergii extract, more preferably 500 to 7500 mg, still more preferably 1000 to 5000 mg, particularly preferably 2000 to 4000 mg, and particularly more preferably. It can be 2500 to 3500 mg. The daily oral dose of Geranium thunbergii extract can be 2000 to 25000 mg in terms of crude drug, more preferably 4000 to 20000 mg, still more preferably 6000 to 18000 mg, and particularly preferably 8000 to 15000 mg. Particularly more preferably, it can be 8500 to 12500 mg.

Usually, the oral dose per day can be 10 to 3500 mg as a Swertia japonica extract, more preferably 25 to 2500 mg, still more preferably 50 to 2000 mg, particularly preferably 75 to 1000 mg, and particularly more preferably. It can be 100 to 700 mg. The daily oral dose of Swertia japonica extract can be 250 to 5000 mg in terms of crude drug, more preferably 500 to 3000 mg, still more preferably 750 to 2500 mg, and particularly preferably 1000 to 2000 mg. In particular, it can be 1250 to 1750 mg, and most preferably 1500 mg.

Usually, the oral dose per day can be 100 to 20000 mg as a Houttuynia cordata extract, more preferably 500 to 18000 mg, still more preferably 1000 to 15000 mg, particularly preferably 1250 to 10000 mg, and particularly more preferably. It can be 1500 to 7000 mg. The daily oral dose of Houttuynia cordata extract can be 6000 to 20000 mg in terms of crude drug, more preferably 7000 to 18000 mg, further preferably 8000 to 17000 mg, and particularly preferably 9000 to 16000 mg. In particular, it can be 10,000 to 15,000 mg.

Usually, the oral dose per day can be 100 to 12000 mg as a manzanita extract, more preferably 150 to 10000 mg, still more preferably 300 to 8000 mg, particularly preferably 500 to 5000 mg, and particularly more preferably. It can be 750 to 2500 mg. The daily oral dose of the manzanita extract can be 6000 to 25000 mg in terms of crude drug, more preferably 7000 to 20000 mg, further preferably 8000 to 18000 mg, and particularly preferably 9000 to 16000 mg. In particular, it can be 9500 to 15500 mg, and most preferably 10000 to 15000 mg.

Usually, the oral dose per day can be 0.05 to 100 mg as a belladonna extract, more preferably 0.125 to 40 mg, still more preferably 0.25 to 20 mg, and particularly preferably 0. It can be 5 to 10 mg, more preferably 1 to 5 mg. The daily oral dose of belladonna extract can be 0.1 to 200 mg in terms of crude drug, more preferably 1 to 140 mg, still more preferably 10 to 120 mg, and particularly preferably 12 to. It can be 100 mg, more preferably 15-80 mg, most preferably 20-60 mg.

Usually, the oral dose per day can be 25 to 2000 mg as the gentiana extract, more preferably 50 to 1500 mg, still more preferably 100 to 1000 mg, particularly preferably 200 to 750 mg, and particularly more preferably. It can be 250 to 550 mg. The daily oral dose of the gentiana extract can be 25 to 2000 mg in terms of crude drug, more preferably 50 to 1500 mg, still more preferably 100 to 1000 mg, and particularly preferably 200 to 750 mg. In particular, it can be more preferably 250 to 550 mg, and most preferably 300 to 500 mg.

In addition, in this specification, "herbal medicine conversion" means the amount of the crude drug extract expressed as the amount of the crude drug (herbal medicine mixture) necessary for preparing the extract. The daily dose may be divided into 1 to 3 divided doses.

Next, the additive in the present invention includes all of the additives generally available pharmaceutically. Examples of such additives include stabilizers, stabilizers, surfactants, lubricants, lubricants, solubilizers, buffers, sweeteners, bases, adsorbents, and flavoring agents. Agents, Binders, Suspension Agents, Hardeners, Antioxidants, Brighteners, Fragrances, Coatings, Skins, Wetting Agents, Wetting Regulators, Fillers, Antifoaming Agents, Cooling Agents , Chewing agents, antistatic agents, flavoring agents / fragrances, coloring agents, sugar coating agents, tonicity agents, softening agents, emulsifiers, pressure-sensitive agents, pressure-sensitive adhesives, viscosity-adjusting agents, foaming agents, pH adjustment Examples include agents, pH regulators, excipients, dispersants, disintegrants, disintegrant aids, fragrances, moisture barriers, preservatives, preservatives, solubilizers, solubilizers, solvents and fluidizers. These can be used alone or in combination of two or more.

Specific examples of the additive include purified sucrose, glucose, trehalose, lactose, maltose, mannitol, sorbitol, xylitol, erythritol, granutol, sodium saccharin, aspartame, acesulfam potassium, sucralose, kanzo extract, stevia extract, lacanca. Extracts, corn starch, potato starch, wheat starch, sodium hydrogencarbonate, potassium hydrogencarbonate, sodium carbonate, magnesium aluminometasilicate, magnesium aluminometylate, magnesium oxide, magnesium hydroxide, alumina magnesium hydroxide, magnesium carbonate, Calcium carbonate, anhydrous calcium hydrogen phosphate, sodium chloride, crystalline cellulose, methyl cellulose, ethyl cellulose, hypromellose, hydroxypropyl cellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, carboxymethyl cellulose calcium, carmellose calcium, croscarmellose sodium, hypromellose phthalic acid Estel, Cellulose Acetate Phthrate, Dextrin, Pregelatinized Steel, Rubber Arabia, Gelatin, Sodium Arginate, Polyvinylpyrrolidone, Crospovidone, Polyvinyl Alcohol, Polyethylene Glycol, Casein, Sodium Casein, Carboxyvinyl Polymer, Tartrate Acid, Light Anhydrous Silicic Acid, Hydrous Dioxide Silicic acid, magnesium stearate, calcium stearate, sodium stearate, sodium lauryl sulfate, talc, hydrogenated vegetable oil, macrogol, silicone oil, agar, celac, glycerin, aromatic essential oils, water-soluble edible pigments, iron yellow oxide, Yellow iron sesquioxide, iron sesquioxide, brown iron oxide, black iron oxide, titanium dioxide, lake pigment, benzoic acid, sodium benzoate, paraoxybenzoic acid, cyclodextrin, polysorbate 80, glycerin fatty acid ester, propylene glycol fatty acid ester, lecithin , Sarashimitsuro, medium-chain fatty acid triglyceride, ascorbic acid, tocopherol, sodium thiosulfate, sodium edetate, plant-derived fragrances (fruit-based fragrances such as orange and lemon, coffee-based fragrances, tea-based fragrances), chocolate-based fragrances, yogurt-based fragrances Examples thereof include fragrances, milk-based fragrances, menthol, peppermint oil, lemon oil, peppermint oil, spare mint oil, and vegetable essential oils such as spice oil. These can be used alone or in combination of two or more.

Particularly preferred additives for molding the solid drug of the present invention are binders, fluidizers and lubricants. Among them, the lubricant is most preferable from the viewpoint of efficiently performing molding (molding).

Among the above additives, the binder can effectively bind the powder particles of the raw material to each other. Therefore, the use of a binder can improve the mechanical strength, that is, the hardness of the solid medicine. Examples of the binder include crystalline cellulose, cellulose derivatives (methyl cellulose, ethyl cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, carboxymethyl cellulose, croscarmellose, etc.), hydroxypropylmethyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol, acrylic acid. Cellulosic polymers, gelatin, gum arabic, purulan, pregelatinized starch (corn starch, potato starch, etc.), lactose, sugar alcohol (mannitol, xylitol, sucralose, etc.), agar, tragant, sodium alginate, propylene glycol alginate, etc. , Preferred are crystalline cellulose, cellulose derivatives, pregelatinized starch, lactose, sugar alcohol, and particularly preferred are crystalline cellulose, pregelatinized starch (corn starch, potato starch, etc.) and lactose.

The binder is preferably contained in an amount of 0.01 to 15 parts by mass, more preferably 0.05 to 10 parts by mass, and more preferably 0.1 to 1 part by mass of the total amount of the crude drug. It is more preferably contained in an amount of about 5 parts by mass, and particularly preferably 0.2 to 3 parts by mass.

By adding a fluidizing agent to the solid drug of the present invention, it is possible to suppress the aggregation of the materials when the materials are mixed. In addition, the fluidity of the mixed powder and granules, which are a mixture of materials, can be improved. Examples of the fluidizing agent include silicic acid, calcium silicate, hydrous silicon dioxide, light anhydrous silicic acid, anhydrous silicic acid, aluminum silicate, calcium silicate, magnesium aluminometasilicate, aluminum oxide, and aluminum hydroxide. Examples thereof include magnesium oxide, magnesium hydroxide, and alumina magnesium hydroxide, preferably calcium silicate, hydrous silicon dioxide, light anhydrous silicic acid, magnesium aluminometasilicate, and alumina magnesium hydroxide, and particularly preferably hydrous silicon dioxide. , Light anhydrous silicic acid, magnesium aluminometasilicate.

The fluidizing agent is preferably contained in an amount of 0.005 to 5 parts by mass, more preferably 0.01 to 3 parts by mass, and 0, based on 1 part by mass of the total amount of the crude drug. . It is particularly preferable to contain 1 to 1 part by mass.

By adding a lubricant to the solid drug of the present invention, it is possible to weaken the adhesive force between powders and prevent the powders from adhering to a molding machine, particularly a pestle or a mortar. Therefore, the solid medicine can be smoothly produced. If the powder is molded with the powder attached to the pestle or mortar, the surface of the finished tablet may become dull or the molding itself may become difficult. Examples of the lubricant include stearic acid, magnesium stearate, calcium stearate, polyoxyl stearate, sodium lauryl sulfate, cetanol, talc, hardened oil, sucrose fatty acid ester, dimethylpolysiloxane, beeswax, and salashimitsuro. Of these, magnesium stearate, calcium stearate, sodium lauryl sulfate, talc, honeydew, and honeydew syrup are preferable, and magnesium stearate is most preferable.

The lubricant is preferably contained in an amount of 0.001 to 2 parts by mass, more preferably 0.005 to 1 part by mass, and 0, based on 1 part by mass of the crude drug. It is more preferably contained in an amount of .007 to 0.5 parts by mass, and particularly preferably contained in an amount of 0.01 to 0.2 parts by mass.

The solid drug of the present invention can be efficiently molded by adding an appropriate amount of additives to the crude drug. Of these, the combined use of the three components of crystalline cellulose, light anhydrous silicic acid and magnesium stearate is preferable because the effects of the present invention appear more prominently. The amount of the additive is adjusted according to the type of crude drug or the like, but at least one selected from the group consisting of a binder, a fluidizing agent and a lubricant with respect to 1 part by mass of the total amount of the crude drug. Is preferably contained in an amount of 0.001 to 20 parts by mass, more preferably 0.01 to 15 parts by mass, and particularly preferably 0.1 to 5 parts by mass.

In the present invention, the solid pharmaceutical product means a pharmaceutical product molded into a certain shape, and is not particularly limited, and examples thereof include dosage forms such as tablets, granules, powders, pills, and troches, and in particular, compression. It is suitable for the dosage form molded by the above, that is, the mold-molded preparation. When the solid drug of the present invention is a mold-molded preparation, it becomes easy to design its hardness within a predetermined range, it is possible to improve swallowing ease and ingestion feeling, and it is also excellent in long-term storage stability. Suitable. The shape of the solid drug may be any shape that can be swallowed by a person, and examples thereof include a bale shape, a triangular columnar shape, a square columnar shape, a disk shape, a columnar shape, a football shape, and a spherical shape. Of these, bale-shaped, disc-shaped, and columnar tablets are preferably used because they are easy to mold, but they are classified as granules under the Pharmaceutical Affairs Law or the Japanese Pharmacopoeia as long as the essence of the present invention is not impaired. It can also be used for things.

The size of the solid drug of the present invention may be as long as the maximum diameter is in the range of 2.5 to 9.0 mm, particularly 2.5 to 8.5 mm, particularly 2.5 to 8.0 mm, and further 2. 5.5 to 7.5 mm, more particularly 2.5 to 7.0 mm, more 2.5 to 6.5 mm, even more 2.5 to 6.0 mm, more preferably 2.5 to 5.5 mm, even more preferably. Is preferably 2.5 to 5.0 mm, particularly 2.5 to 4.5 mm, more particularly 2.5 to 4.0 mm, and most preferably 3.0 to 4.0 mm. This is because if the maximum diameter of a solid drug is too large, molding problems are likely to occur, and if it is too small, molding itself becomes difficult. The maximum diameter in the present invention means the diameter of a circle in a plan view when it is allowed to stand on a floor surface as shown by W in FIGS. 1 (a) to 1 (c) in the case of a solid drug having a columnar shape. Further, in the case of a solid drug having a non-cylindrical shape, as shown by W in FIG. 1 (d), it means a long diameter or a side length in a plan view when the drug is allowed to stand on the floor surface. In FIGS. 1 (a) to 1 (d), reference numeral 1 indicates a solid drug.

Since the solid drug of the present invention is molded into a size that is easy to swallow, the feeling of ingestion is improved. From the viewpoint of facilitating swallowing, the size of the solid drug in the present invention is preferably in the range of 2.5 to 8.5 mm in maximum diameter, particularly preferably in the range of 2.5 to 8.0 mm, and in particular 2. The range of 5 to 7.5 mm is preferable, the range of 2.5 to 7.0 mm is preferable, the range of 3.0 to 6.5 mm is more preferable, and the range of 3.5 to 6.0 mm is particularly preferable. The ease of swallowing in this range can be verified by measuring the throat myoelectric potential when a human takes the solid drug of the present invention using a myoelectric electrometer.

The hardness of the solid drug of the present invention is usually in the range of 1.0 to 10.0 kp, preferably 1.6 to 10.0 kp, and is particularly 1.6 to 8.5 kp, particularly 1. 6 to 8.0 kp, particularly 2.0 to 7.8 kp, more preferably 2.5 to 7.6 kp, and more preferably 3.0 to 7.5 kp. This is because if the hardness of the solid drug is too high, it is difficult to disintegrate in the body, and if it is too low, it is easily damaged in the manufacturing process and distribution channel after molding, and the quality cannot be maintained. The hardness in the present invention means the average of the values obtained by measuring the breaking strength of 10 randomly selected pieces using a hardness tester.

In the solid drug of the present invention, when solid drugs prepared to have the same maximum diameter are sieved using a sieve having a size 1.2 times the maximum diameter, 90% or more pass through the sieve. It is preferable that 92% or more pass through the sieve, and 94% or more is particularly preferable to pass through the sieve. Further, when sieving is performed using a sieve having a size of 0.8 times the maximum diameter, 90% or more is preferably left on the sieve, and 92% or more is preferably left on the sieve. In particular, it is preferable that 94% or more remains on the sieve. Since such solid medicines have a small variation in shape and size, it is possible to accurately take a predetermined amount of the active ingredient. For example, in a columnar solid drug prepared using a mold having a maximum diameter of 4.0 mm, the maximum diameters of a plurality of solid drugs to be taken at one time were measured, and the average value was 4.0 mm. In this case, when 1 g of solid drug is sieved using a 4.8 mm sieve, 0.9 g or more passes through the sieve, and 1 g of solid drug is further sieved using a 3.2 mm sieve. 0.9 g or more remains on the sieve, and the maximum diameter of the prepared solid drug is 4.0 ± 0.80 mm.

According to the configuration of the present invention, it is possible to prepare a solid drug having a high content ratio of crude drugs, so that the amount of additives used can be reduced. The total amount of the additive to the solid medicine is usually less than 90% by mass, but it is preferable that it is less than 75% by mass, and more preferably less than 50% by mass. In addition, since molding disorders are effectively suppressed, solid medicines can be efficiently produced and the quality of solid medicines is stabilized. In addition, despite increasing the content ratio of crude drugs,
It has the hardness required for solid medicines and has excellent storage stability. Further, since the solid drug is small, it can be taken by a person who has difficulty swallowing the solid drug, such as an elderly person. In addition, the degree to which the unpleasant odor peculiar to crude drugs is felt when taken is remarkably suppressed. Therefore, it can be provided to a wide range of users.

The solid drug of the present invention can be obtained, for example, as follows. That is, first, a crude drug as a material for a solid drug and an additive thereof are mixed by a conventional method to prepare a crude drug-containing mixture. Then, by molding this crude drug-containing mixture into a predetermined shape, the solid drug of the present invention can be obtained. The crude drug-containing mixture in which the above crude drug and the additive are mixed is usually subjected to molding as a powder having a particle size of 850 μm or less. The crude drug and the additive may be prepared in advance into a powder having a particle diameter of 850 μm or less, and the mixture may be mixed to obtain a crude drug-containing mixture of the powder having a particle diameter of 850 μm or less. Further, it is preferable to compression-mold the crude drug-containing mixture with a molding machine at the time of molding. Then, the crude drug-containing mixture may be granulated by a wet granulation method, a dry crushing granulation method, or the like before being subjected to a molding machine. When the granular crude drug-containing mixture is subjected to a molding machine, molding obstacles can be further suppressed.

The wet granulation method is a method of granulating a crude drug-containing mixture by adding a liquid such as water, ethanol, or oil to the powdered crude drug-containing mixture in a batch or by spraying. Examples of the wet granulation method include a method called a kneading granulation method, an extrusion granulation method, a stirring granulation method, a fluidized bed granulation method, and a spray drying method.

As the liquid to be added to the crude drug-containing mixture, a liquid obtained by dissolving the binder or fluidizing agent in water, ethanol, oil or the like may be used. The binder and fluidizing agent can be added to the crude drug-containing mixture as they are, instead of being added by dissolving them in a solvent such as water, ethanol, or oil. The binder and the fluidizing agent do not necessarily have to be added to the crude drug-containing mixture.

In the above-mentioned dry crushing and granulation method, a crude drug-containing mixture of powders is compressed to obtain a dense lumpy or plate-shaped molded product, and the molded product is crushed, crushed, and granulated to be granulated to a predetermined size. It's a way to get things. The dry crushing and granulating method can be performed by using a device such as a roller compactor or a slug locking machine.

The solid drug of the present invention can also be molded without using a molding machine. For example, the solid drug of the present invention can be obtained by molding a crude drug-containing mixture into a predetermined size by the above-mentioned wet granulation method or dry crushing granulation method.

When using a molding machine, for example, after adding a lubricant to the crude drug-containing mixture obtained by the above method and mixing the mixture, a punch and a mortar corresponding to the size of the target solid drug are used. The solid drug of the present invention can be obtained by compression molding using a molding machine equipped with a (mold). That is, for example, a columnar solid drug having a maximum diameter of 4.0 mm can be obtained by using a pestle and a mortar designed for a diameter of 4.0 mm.

Molding with the above molding machine can be performed, for example, under the condition of a temperature of 10 to 50 ° C., but is usually performed at room temperature (a temperature that is neither heated nor cooled). Further, molding with the above molding machine is usually performed at a molding pressure of 1 to 30 kN, preferably performed at a molding pressure of 3 to 20 kN, more preferably performed at a molding pressure of 3 to 12 kN, and 3 to 3 to. It is more preferably performed at a molding pressure of 8 kN, and further preferably performed at a molding pressure of 4 to 6 kN. This is because if the molding pressure is too high, the solid drug tends to have molding problems such as cracking and chipping, and if it is too low, the molding itself tends to be difficult.

The molded solid drug may be used as it is as a product, or the surface may be surface-treated such as sugar coating or coating. As described above, the maximum diameter of the surface-treated solid drug can be measured in a plan view depending on the shape of the solid drug.

The solid drug of the present invention is not particularly limited, but may be a ethical drug, an over-the-counter drug, or a food product. Here, ethical drugs (medical drugs) mean those obtained by prescription issued by a medical institution, and over-the-counter drugs are marketed through retail stores or the Internet and are obtained by the user at his / her own discretion. .. Since the solid drug of the present invention is easy to take, it can be suitably used for over-the-counter drugs that the user takes without the guidance of a doctor. Over-the-counter drugs often contain a complex of highly hygroscopic crude drugs, and are molded with a certain degree of hardness and strength, considering that distribution and management are carried out under harsh conditions. It is desirable that the present invention is used.

Since the solid drug of the present invention has a maximum diameter of 2.5 to 9.0 mm and a smaller volume than the conventional product, it may not be possible to add the same amount of active ingredient as the conventional product. Therefore, in order to ingest the same amount of the active ingredient as the conventional product, it is preferable to take a larger number. Therefore, it is preferable that the number of doses to be taken at one time is individually packaged. The number of doses to be taken at one time is, for example, 2 to 80, especially 3 to 75, especially 4 to 70, 5 to 65, 6 to 60, and 7 to 55, 8. ~ 50 pieces are preferable, 10 to 40 pieces are more preferable, and 10 to 30 pieces are particularly preferable. The number of doses to be taken daily is, for example, usually 4 to 200, particularly 6 to 180, particularly 8 to 160, further 10 to 150, and further 10 to 120. The number is preferably 10 to 100, more preferably 10 to 90, and particularly preferably 20 to 75.

The individual wrapping is a sealable wrapping material, and examples thereof include SP (Strip Package) wrapping material and stick-shaped wrapping material. As such an SP packaging material or a stick-shaped packaging material, for example, the end portion and the upper and lower end portions of the tubular shape are sealed so that the aluminum sheet material has a cylindrical shape, and an accommodating portion serving as a closed space is provided inside. I can give you what you are doing. In particular, it is preferable that the number of solid medicines to be taken at one time is packaged in one SP packaging material or one stick-shaped packaging material. As the packaging material for the SP packaging material and the stick-shaped packaging material, for example, the packaging materials described in JP-A-2006-143276 and JP-A-2003-192023 are considered in consideration of moisture permeability and openability (tearability). A known material can be used as appropriate, and it can be produced by a known method. Then, in the storage of the solid medicine in the SP packaging material or the stick-shaped packaging material, a predetermined number of solid medicines are usually stored in the storage portion of the tubular packaging material in a state where only the seal at the upper end is left, and then the solid medicine is stored. This is done by sealing and sealing the top edge. In order to take out the solid medicine contained in the SP packaging material or the stick-shaped packaging material, usually, the upper end portion is opened by cutting the portion inside from the sealed portion at the upper end portion in the length direction. It is done from this opening. The solid drug of the present invention is particularly preferably packaged in a stick-shaped packaging material because of its ease of administration. It is preferable that the solid drug contained in the SP packaging material or the stick-shaped packaging material is taken out from the container of the packaging material by throwing it into the mouth through the opening of the packaging material.

In the SP packaging material and the stick-shaped packaging material, the width (short side) thereof is preferably 10 to 40 mm, more preferably 12 to 35 mm, further preferably 14 to 32 mm, and 16 to 16 to. It is particularly preferably 30 mm, and more preferably 18 to 28 mm. When the width of the SP packaging material or the stick-shaped packaging material is within this range, it becomes easy to comfortably fit the entire opening in the mouth when taking out the solid medicine from the SP packaging material or the stick-shaped packaging material. , The effect of the present invention can be more prominently exhibited. The length (long side) thereof is preferably 60 to 150 mm, more preferably 50 to 130 mm, further preferably 45 to 110 mm, and particularly preferably 40 to 100 mm. It is particularly preferably 35 to 90 mm. The width (short side) and length (long side) are not the outer dimensions of the packaging material, but the lengths of the sealed upper end, lower end, or both sides, that is, the closed space where solid medicines are stored. Means dimensions. When the short side and the long side intersect in a curve, an extension line of each side is drawn, and the above dimension is measured with the intersecting point as the end point of the short side and the long side.

The ratio of the width (short side) to the length (long side) in the SP packaging material or the stick-shaped packaging material is preferably 1: 1 to 1:10, more preferably 1: 1.2 to 1: 9. , 1: 1.5 to 1: 8, more preferably 1: 1.8 to 1: 7, and particularly preferably 1: 2.0 to 1: 6. When the ratio of the two is within this range, the effect of the present invention can be more remarkably exhibited, and the convenience of the user is remarkably improved.

Next, Examples will be described together with Comparative Examples. However, the present invention is not limited to this. Unless otherwise specified, all the component compositions shown below are shown on a mass basis (parts by mass).

[Examples 1 to 14, Comparative Examples 1 to 10] A crude drug-containing mixture prepared according to the compositions shown in Tables 1 to 6 below was prepared by using a compression molding machine equipped with a mortar and a pestle having a target diameter. The target solid drug was obtained by compression molding at a molding pressure of 3 kN to 20 kN. The crude drug used was cinnamon, licorice, and onji in the form of crude drug powder or extract powder, and the additive used was a product listed in the Japanese Pharmacopoeia. In addition, in Tables 1 to 6, as each crude drug, those using crude drug powder are described as "-end", and those using extract powder are described as "-extract powder" (the same applies to the following table). The obtained solid drug was columnar.

The solid medicines of each example and each comparative example were evaluated for three items of (1) molding failure, (2) hardness (kp), and (3) abrasion degree (%), and the results were evaluated in Tables 1 to 1 below. It is also shown in Table 6. The evaluation method for each item is as shown below.

(1) Molding failure In the solid medicines of each example and comparative example, 50 randomly selected states were visually observed, and even one of them was cracked or chipped. Those without any missing solid medicines were evaluated as "none" for molding disorders.

(2) Hardness (kp) For the hardness (kp), the breaking strength was measured for each of 10 randomly selected tablets using a tablet hardness tester (PTB-311E, PHARMA TEST), and the average of the obtained values was the hardness. And said.

(3) Abrasion degree (%) The abrasion degree (%) was measured as follows according to the "tablet abrasion degree test method" described in the Japanese Pharmacopoeia. That is, using a tablet abrasion degree tester (TFT-1200, manufactured by Toyama Sangyo Co., Ltd.), a minimum number having a mass exceeding 6.5 g was placed in the testing machine, and the mixture was rotated 100 times at 25 rpm with respect to the total mass of the solid drug before rotation. The amount of decrease in the total mass of the solid drug after rotation was calculated as the degree of wear. Abrasion degree (%) = (total mass before rotation-total mass after rotation) / total mass before rotation x 100

As shown in Table 1 above, Comparative Example 1, which is a solid drug having a maximum diameter of 10.0 mm and containing a certain amount or more of cinnamon powder as a crude drug, is obtained when molded at any molding pressure of 3 kN to 20 kN. It was also found that molding failure occurred, and that the hardness and wearability of solid medicines were also inferior. On the other hand, in Example 1, although the contained components are the same as in Comparative Example 1, the maximum diameter is 4.0 mm, so that even when molding is performed at any molding pressure of 3 kN to 20 kN. Not only did it not cause molding problems, but it also had suitable hardness and abrasion.

As shown in Table 2 above, Examples 2 to 5, which are solid pharmaceutical products having a maximum diameter of 3.0 to 8.5 mm and containing a certain amount or more of cinnamon powder, were molded at a molding pressure of 5 kN. Even in this case, molding failure did not occur, and the hardness and the degree of abrasion were suitable. Among them, in Example 2 having a maximum diameter of 3.0 mm and Example 3 having a maximum diameter of 5.0 mm, the hardness and the degree of abrasion were particularly suitable.

As shown in Table 3 above, Comparative Examples 2 and 3, which are solid drugs having a maximum diameter of 10.0 mm and containing cinnamon powder as a crude drug, had a molding failure when molded at a molding pressure of 5 kN. .. On the other hand, Examples 6 and 7 are suitable because the maximum diameter is 4.0 mm even though the contained components are the same as those of Comparative Examples 2 and 3, so that molding failure does not occur. It had hardness and a degree of wear.

As shown in Table 4 above, Comparative Examples 4 and 5, which are solid medicines having a maximum diameter of 10.0 mm and containing a certain amount or more of licorice powder or ondi extract powder which are crude drugs, were molded at a molding pressure of 5 kN. In some cases, molding failure occurred, and it was found that the hardness and the degree of abrasion of the solid drug were also inferior. On the other hand, in Examples 8 and 9, although the contained components are the same as those of Comparative Examples 4 and 5, the maximum diameter is 4.0 mm, so that even when molded with a molding pressure of 5 kN. , No molding failure occurred, and had suitable hardness and abrasion degree.

As shown in Table 5 above, the solid medicines of Examples 10 to 12 have a maximum diameter of a certain amount or more of any of belladonna extract powder, gentiana powder and geranium thunbergii powder as crude drugs. Since the particle size was as small as 4.0 mm, molding failure did not occur, and the hardness and the degree of abrasion were suitable. On the other hand, Comparative Examples 6 and 7 having a maximum diameter of 10.0 mm had a molding failure even though they had the same components as in Example 10 or 11. Further, Comparative Example 8 was inferior in hardness and abrasion degree to Example 12 having the same components, although molding failure did not occur. Since veradonna, gentiana lutea and gentian lutea use their roots or rhizomes as crude drugs, the present invention relates not only to kanzo and rhizomes that also use their roots and rhizomes, but also to crude drugs that widely use their roots, rhizomes and rhizomes. It can be seen that the effect of is obtained.

As shown in Table 6 above, the solid medicines of Examples 13 and 14 have a maximum diameter of 4.0 mm and a particle size, even though they contain a certain amount or more of Swertia japonica powder or Bearberry extract powder as crude drugs. However, molding failure did not occur, and the hardness and the degree of abrasion were suitable. On the other hand, in Comparative Example 9 having the same components as in Example 13, since the maximum diameter was 10.0 mm, a molding failure occurred. Further, Comparative Example 10 not only caused a molding failure, but was also inferior in hardness and abrasion degree to Example 14 having the same component. Since Swertia japonica is a crude drug using whole plants on the ground and bearberry is a crude drug using leaves, it can be seen that the effects of the present invention can be obtained also for crude drugs using whole plants and leaves.

[Examples 15 to 22, Comparative Examples 11 to 18] Solid medicines having the compositions shown in Tables 7 and 8 below were prepared. Using a compression molding machine equipped with a mortar and a pestle having a target diameter, compression molding was performed at a molding pressure of 3 kN to 20 kN to obtain the desired solid drug. The obtained solid drug is columnar. Next, these solid medicines were enclosed in a stick-shaped aluminum laminated packaging material having a housing portion of 20 mm in width and 70 mm in length. The number of encapsulated solid medicines is as shown in Tables 7 and 8.

In Examples 15 to 22 and Comparative Examples 11 to 18, the crude drugs used were herbal powders or extract powders of gentian, onji, licorice, gentiana, geranium thunbergii, swertia japonica, sardine, and geranium thunbergii, and the additives were Japanese Pharmacopoeia. The listed products of were used.

For each example and each comparative example, there are four items: (4) ease of taking out from the packaging material, (5) ease of putting in the mouth, (6) ease of swallowing, and (7) feeling of taking. Evaluation was performed. These evaluations were carried out by four subjects opening the stick-shaped aluminum laminated packaging material and taking all of the contained solid medicines directly into the mouth from the aluminum laminated packaging material. In addition, the opened portion of the aluminum laminated packaging material was set at a position 5 mm inside from the short side in the length direction, and all the subjects opened at the same position. The evaluation method for each item is as shown below.

(4) Ease of removal from the packaging material For the solid medicines of each Example and Comparative Example, I feel that the ease of movement from the aluminum laminated packaging material to the mouth is the easiest to move into the mouth (easy to remove from the packaging material). Each subject scored a maximum of 8 points, with 8 points for cases and 0 points for cases that were not felt at all, and the average score was x from 0 points to 2.0 points or less, and greater than 2.0 points. A score of 0 or less was evaluated as Δ, a score of 6.0 or less was evaluated as ◯, and a score of greater than 6.0 or 8.0 was evaluated as ⊚.

(5) Ease of putting into the mouth It is easiest to reach the solid drug of each example and comparative example that entered the mouth from the aluminum laminated packaging material whether or not it is easy to reach the position where it is easy to swallow (to the mouth). Each subject scores a maximum of 8 points, with 8 points if they feel it is easy to put in) and 0 points if they do not feel it at all, and the average score is 0 to 2.0 points or less x, 2.0. A score greater than a score of 4.0 or less was evaluated as Δ, a score greater than 4.0 and a score of 6.0 or less was evaluated as ◯, and a score greater than 6.0 and a score of 8.0 or less was evaluated as ⊚.

(6) Ease of swallowing Whether or not the solid medicines of each example and comparative example easily pass through the esophagus is 8 points when it feels most easy to pass (easy to swallow), and 0 points when it does not feel at all. Each subject scores a maximum of 8 points, and the average score is x for 0 to 2.0 points or less, Δ for 4.0 points or less that is larger than 2.0 points, and 6 that is larger than 4.0 points. A score of 0.0 or less was evaluated as ◯, and a score of 8.0 or less was evaluated as ⊚.

(7) Feeling of taking The solid medicines of each example and comparative example are comprehensive evaluations of a series of actions from the aluminum laminated packaging material to the mouth and swallowing, and the above three items (easiness to take out from the packaging material). The average score of (easy to put in the mouth, easy to swallow) is x from 0 points to 2.0 points or less, greater than 2.0 points and 4.0 points or less is Δ, and greater than 4.0 points. A score of 0 or less was evaluated as ◯, and a score of 8.0 or less was evaluated as ⊚.

As shown in Tables 7 and 8 above, Examples 15 to 22 have a maximum diameter of 4.0 mm and contain a crude drug of any one of Keihi, Onji, Kanzo, Gentiana, Geranium thunbergii, Swertia japonica, Manzanitas, and Geranium thunbergii. It can be seen that the solid medicine is easier to take out from the packaging material, easier to put into the mouth, easier to swallow, and more comfortable to take than the solid medicine having the maximum diameter of 10.0 mm. Here, since cinnamon is a crude drug using bark, it can be seen that the effect of the present invention can be obtained also with the crude drug using bark.

[Examples 23 to 30] Solid medicines having the compositions shown in Table 9 below were prepared. Using a compression molding machine equipped with a mortar and a pestle with a desired diameter, compression molding was performed at a molding pressure of 3 kN to 20 kN to obtain solid medicines having a maximum diameter of 4.0 mm and 10.0 mm. Each of the obtained solid medicines is columnar. Among the above-mentioned solid medicines, a solid medicine having a maximum diameter of 4.0 mm was used as an example, and a solid medicine having a maximum diameter of 10.0 mm was used as a corresponding comparative example. Next, these solid medicines were enclosed in a stick-shaped aluminum laminated packaging material having a housing portion of 20 mm in width and 70 mm in length. The number of encapsulated solid medicines is as shown in Table 9, and there is only one comparative example in each case. The number of examples was set so as to have the same mass as the mass of one corresponding comparative example. In addition, the crude drug used was a crude drug powder or extract powder of Keihi, Onji, Kanzo, Gentiana, Geranium thunbergii, Swertia japonica, Uwaurushi, and Geranium thunbergii, and the additive used was a product listed in the Japanese Pharmacopoeia.

The taste of each example and the corresponding comparative solid drug was evaluated. At this time, four subjects opened the stick-shaped aluminum laminated packaging material, and all of the contained solid medicines were directly injected into the mouth from the aluminum laminated packaging material and taken. The opened part of the aluminum laminated packaging material was set to a position 5 mm inside from the short side in the length direction, and all the subjects opened at the same position. After taking the drug, the average score was calculated by scoring a maximum of 8 points, 8 points when the taste was most felt and 0 points when the taste was not felt at all. Then, the taste improvement rate (%) was determined based on the following [Equation 1]. The obtained results are also shown in Table 9. [Equation 1] Taste improvement rate (%) = {1- (mean value of examples / average value of corresponding comparative examples)} × 100

As shown in Table 9 above, a solid drug having a maximum diameter of 4.0 mm and containing a crude drug of any one of cinnamon, onji, licorice, gentiana, geranium thunbergii, swertia japonica, manzanitas, and geranium thunbergii (Examples 23 to 30). ), It can be seen that the taste is significantly improved as compared with the solid drug having the same component and having a maximum diameter of 10.0 mm (comparative example corresponding to each example). This is recognized to be an excellent effect, especially in solid medicines using crude drugs that have a spicy, bitter, harsh, and astringent taste. In addition, the upper limit of ash content is classified as less than 5%, Manzanitas, 5% or more and less than 7%, Keihi, Gentiana, Swertia japonica, 7% or more and less than 10%, Licorice, Geranium, 10% or more. Since the taste of all of the geranium thunbergii classified into the above is significantly improved, it can be seen that the crude drug having the upper limit of the ash content classified into any of the categories has the effect of the present invention.

[Test Examples 1 to 3] Solid medicines having the compositions shown in Table 10 below were prepared. Using a compression molding machine equipped with a mortar and a pestle having a target diameter, compression molding was performed at a molding pressure of 3 kN to 20 kN to obtain a solid drug having a maximum diameter of 4.0 mm or 10.0 mm. The obtained solid drug is columnar. Next, these solid medicines were enclosed in a stick-shaped aluminum laminated packaging material having a housing portion of 20 mm in width and 70 mm in length. The number of encapsulated solid medicines was 1 for Test Example 1, 1 for Test Example 2, and 2 for Test Example 3.

In Test Examples 1 to 3, the crude drug used was an extract powder of Onji, and the additive used was a product listed in the Japanese Pharmacopoeia.

For each test example, the feeling of taking the drug was evaluated for the items of (8) ease of movement in the oral cavity. In these evaluations, three subjects opened the stick-shaped aluminum laminated packaging material, and the total number of solid medicines contained (1 in Test Examples 1 and 2 and 2 in Test Example 3) was taken from the aluminum laminated packaging material. It was done by putting it directly into the mouth and taking it. In addition, the opened portion of the aluminum laminated packaging material was set at a position 5 mm inside from the short side in the length direction, and all the subjects opened at the same position. The evaluation method for each item is as shown below.

(8) Ease of movement in the oral cavity For the solid drug of each test example, it is most likely to move in the throat direction on the tongue after being put into the mouth from the aluminum laminated packaging material. Each subject scored a maximum of 8 points, with 8 points for cases and 0 points for cases that were not felt at all, and the average score was x from 0 points to 2.0 points or less, and greater than 2.0 points. A score of 0 or less was evaluated as Δ, a score of 6.0 or less was evaluated as ◯, and a score of greater than 6.0 or 8.0 was evaluated as ⊚.

As shown in Table 10 above, when one solid drug having a maximum diameter of 4.0 mm and containing ondi is taken, one solid drug having the same component and having a maximum diameter of 10.0 mm is taken. In comparison, the ease of movement in the oral cavity is improved, indicating that the feeling of taking the drug is better. Furthermore, when two solid medicines with a maximum diameter of 4.0 mm and containing onji are taken, the ease of movement in the oral cavity is improved as compared with the case of taking one solid medicine with the same maximum diameter. The ease of movement in the oral cavity was significantly improved as compared with the case of taking one solid drug having a diameter of 10.0 mm. That is, it can be seen that the feeling of taking a plurality of solid medicines having a maximum diameter smaller than 10.0 mm is further enhanced. The same applies to solid medicines containing crude drug powder or extract powder of geranium, licorice, gentiana, geranium thunbergii, swertia japonica, and ginger instead of onji as the crude drugs contained in the solid medicine. Results were obtained.

[Pharmaceutical Examples 1 to 18] The solid pharmaceutical products of the present invention (Pharmaceutical Examples 1 to 18) were prepared using the materials shown in Tables 11 to 13 below. As the materials of Pharmaceutical Examples 1 to 18, the products listed in the Japanese Pharmacopoeia were used. The hardness is a value when molded with a molding pressure of 5 kN.

With respect to the pharmaceutical examples 1 to 18 shown in Tables 11 to 13, the three items of molding failure, hardness (kp), and abrasion degree (%) were evaluated by the same method as in the examples. As a result, no molding failure occurred in all of Pharmaceutical Examples 1 to 18. In addition, all of Pharmaceutical Examples 1 to 18 had suitable hardness and degree of wear, and there was no problem with the feeling of ingestion.

The present invention is a solid drug containing a certain amount or more of crude drug and has no variation in quality. It is molded into a size that is easy to swallow and has an excellent feeling of ingestion, so that it can be taken by users of a wide range of ages. ..

1 Solid drug W maximum diameter

Claims (1)

The invention described in the specification of the present application.

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