Tablet

Abstract

To provide a new tablet or the like.SOLUTION: In tablets for taking high doses of active ingredient per day (e.g., above 5000mg, above 6000mg), Bofutsushosan Extract is selected as the active ingredient. In such tablets, the content of Bofutsushosan Extract may be 45% by mass or more.SELECTED DRAWING: None

Description

[Technical Field]

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

[0002] Active ingredients (active pharmaceutical ingredients) such as herbal extracts are ingested in various forms. Tablets are one form of such a formulation. For example, Patent Document 1 discloses a tablet containing (A) a herbal extract and (B) magnesium aluminometasilicate and / or magnesium aluminosilicate, the tablet having a herbal extract content of 87% by weight or more. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Japanese Patent Application Laid-Open No. 2012-224581 Summary of the Invention [Problem to be solved by the invention]

[0004] An object of the present invention is to provide novel tablets and the like. [Means for solving the problem]

[0005] As mentioned above, it is sometimes desirable to increase the content of the active ingredient in tablets. However, tablets usually contain other ingredients such as excipients because they cannot be molded (tableted), or even if they can be molded, they do not have sufficient strength. As a result, tablets containing a predetermined low content of the active ingredient are distributed.

[0006] On the other hand, since there is an effective amount (effective intake amount) of active ingredients for the desired symptoms or disease, in order to ingest the active ingredient through tablets, it is necessary to ingest the size and number of tablets corresponding to that effective amount.

[0007] Therefore, the larger the intake amount, the larger the size of the tablets and the greater the number of tablets. However, in either case, the total amount (volume) of tablets to be taken increases, and as a result, oral administration becomes more cumbersome. For example, larger size makes it difficult to take tablets, and increasing the number of tablets makes it similarly difficult to take, or requires ingenuity in administration, such as reducing the number of tablets taken at one time. In particular, putting large tablets or many tablets in the mouth can lead to aspiration.

[0008] In order to reduce the total tablet amount, it would be thought that the proportion of the active ingredient in the tablet could be increased. However, as mentioned above, in reality, there are naturally restrictions on the amount of active ingredient that can be contained in a tablet in order for it to be viable as a tablet, and it can be said that it is virtually impossible to increase the effective intake amount while reducing the total tablet amount.

[0009] Therefore, based on a completely different idea, the inventor investigated various active ingredients to see if it would be possible to increase the effective intake amount and physical properties (hardness, etc.) while reducing the total tablet weight, which is a trade-off relationship that was originally thought to be impossible.However, of course, this would go against common technical knowledge, and it was extremely difficult to achieve.

[0010] In this situation, the inventors have found, quite surprisingly, that when, among various active ingredients, Bofutsushosan extract is used as the active ingredient, even if the proportion of the active ingredient in the tablet is relatively high, the tablet's moldability and / or physical properties are not impaired, and in some cases the tablet's moldability and / or physical properties (hardness, etc.) may even be improved; therefore, the effective intake amount can be made relatively high without excessively increasing the total tablet weight, and after further investigations, the present invention has been completed.

[0011] That is, the present invention relates to the following inventions. [1] A tablet for taking more than 6000 mg of Bofutsushosan extract per day, containing 45% or more by mass of Bofutsushosan extract. [2] A tablet for taking more than 6000 mg of Bofutsushosan extract per day, containing 45% or more by mass of Bofutsushosan extract and having a mass of 200 to 800 mg. [3] A tablet for taking more than 6000 mg of Bofutsushosan extract per day, containing 45% or more by mass and 90 mg or more of Bofutsushosan extract, and having a mass of 200 to 800 mg. [4] A tablet for taking more than 5000 mg of Bofutsushosan extract per day, which does not contain aluminum metasilicate or magnesium aluminosilicate, and contains 45% by mass or more (e.g., 45 to 88% by mass) of Bofutsushosan extract. [5] A tablet for taking more than 5000 mg of Bofutsushosan extract per day, which does not contain aluminum metasilicate or magnesium aluminosilicate, contains 45% by mass or more (e.g., 45 to 88% by mass) and 90 mg or more of Bofutsushosan extract, and has a mass of 200 to 800 mg. [6] The tablet according to any one of [1] to [5], which contains 50% by mass or more and 100 mg or more of Bofutsushosan extract and has a mass of 250 to 700 mg. [7] The tablet according to any one of [1] to [6], which contains 60% by mass or more and 150 mg or more of Bofutsushosan extract and has a mass of 300 to 600 mg. [8] Tablets described in any of [1] to [7], to be taken three times a day, 15 tablets or less per dose. [9] Daily intake of Bofutsushosan extract: 13,000 mg or less, total volume 15,000 mm 3 A tablet described in any of [1] to [8] to be taken in the following amounts.

[10] 12 tablets or less per dose, 3 times a day, 12,000 mg or less of Bofutsushosan extract per day, total volume 15,000 mm3 The tablet according to any one of [1] to [9], which is to be taken in the following amount, contains 60% by mass or more and 200 mg or more of Bofutsushosan extract, and has a mass of 300 to 600 mg.

[11] A method for manufacturing tablets for taking more than 6000 mg of an active ingredient per day, in which bofutsushosan extract is selected as the active ingredient and the tablets are molded (tablet-molded) to contain 45% or more of the bofutsushosan extract by mass.

[12] A method for manufacturing tablets for taking more than 6000 mg of active ingredient per day, in which bofutsushosan extract is selected as the active ingredient, the bofutsushosan extract is contained in an amount of 45% by mass or more, and the tablet is molded (tablet-molded) to have a mass of 200 to 800 mg.

[13] A method for manufacturing tablets for taking more than 6000 mg of active ingredient per day, in which bofutsushosan extract is selected as the active ingredient, the bofutsushosan extract is contained in an amount of 45% by mass or more and 90 mg or more, and the tablet is molded (tablet-molded) to have a mass of 200 to 800 mg.

[14] The method according to any one of

[11] to

[13] , which is a method for obtaining a tablet for taking more than 6000 mg of an active ingredient per day by improving or improving the moldability and / or hardness of a tablet for taking 6000 mg or less of an active ingredient per day.

[15] A method for producing tablets for taking more than 5000 mg of an active ingredient per day, in which bofutsushosan extract is selected as the active ingredient, and the extract is molded (tableted) to contain 45% by mass or more (e.g., 45 to 88% by mass) of the bofutsushosan extract without containing aluminum metasilicate or magnesium aluminosilicate.

[16] The method according to

[15] , which is a method for obtaining tablets for taking more than 5000 mg of an active ingredient per day by improving or improving the moldability and / or hardness of tablets for taking 5000 mg or less of an active ingredient per day.

[17] A method for enhancing or improving the moldability of tablets containing an active ingredient, which method selects (uses) Bofutsushosan extract as the active ingredient.

[18] A method for increasing or improving the hardness of tablets containing an active ingredient, in which Bofutsushosan extract is selected (used) as the active ingredient.

[19] A method for improving or enhancing the moldability and hardness of tablets containing an active ingredient, in which Bofutsushosan extract is selected (used) as the active ingredient.

[20] A method for improving or enhancing the moldability of tablets containing less than 45% by mass of an active ingredient, which comprises selecting (using) bofutsushosan extract as the active ingredient and increasing the content of the active ingredient (bofutsushosan extract) to 45% by mass or more (increasing it to 45% by mass or more). [twenty one] A method for improving or enhancing the hardness of a tablet containing less than 45% by mass of an active ingredient, which comprises selecting (using) bofutsushosan extract as the active ingredient and increasing the content of the active ingredient (bofutsushosan extract) to 45% by mass or more (increasing it to 45% by mass or more). [twenty two] A method for improving or enhancing the moldability and hardness of tablets containing less than 45% by mass of an active ingredient, which comprises selecting (using) bofutsushosan extract as the active ingredient and increasing the content of the active ingredient (bofutsushosan extract) to 45% by mass or more (increasing it to 45% by mass or more). [twenty three] The method according to any one of

[17] to

[22] , wherein the tablet has a mass of 200 to 800 mg. [twenty four] The method according to any one of

[17] to

[23] , wherein the content of the active ingredient (Bofutsushosan extract) is 90 mg or more. [twenty five] The method according to any one of

[17] to

[24] , wherein aluminum metasilicate and magnesium aluminosilicate are not contained.

[26] A tablet (multiple tablets, combination tablets) comprising a combination of multiple tablets according to any one of [1] to [3] and [6] to

[10] , wherein the multiple tablets are combined to provide more than 6000 mg of Bofutsushosan extract (multiple tablets to be taken so that more than 6000 mg of Bofutsushosan extract is taken per day).

[27] A tablet (multiple tablets, combination tablets) comprising a combination of multiple tablets according to any one of [4] to

[10] , wherein the multiple tablets are combined to provide more than 5000 mg of Bofutsushosan extract (multiple tablets to be taken so that more than 5000 mg of Bofutsushosan extract is taken per day). [Effects of the Invention]

[0012] The present invention can provide novel tablets and the like.

[0013] In one embodiment of such a tablet, a specific active ingredient (ie, bofutsushosan extract) may be contained in a relatively high content (for example, 45% by mass or more). Such tablets are suitable as tablets containing a relatively high daily dose (for example, more than 5000 mg, more than 6000 mg, etc.) of a specific active ingredient (ie, bofutsushosan extract).

[0014] According to the present invention, by selecting Bofutoujiosan extract from among the wide variety of active ingredients (such as herbal extracts), it is surprisingly often the case that the high moldability and / or physical properties of the tablet are not impaired even if the amount of active ingredient in the tablet is high. In particular, in the case of the tablet of the present invention, it is quite surprising that, far from impairing the compactibility and physical properties, increasing the content of Bofutsushosan extract can sometimes improve (or improve) the compactibility and / or physical properties (e.g., hardness). Furthermore, such tablets can achieve both compactibility and physical properties (especially in a well-balanced manner). Therefore, the present invention can also provide a method for improving (or enhancing) the moldability and / or physical properties [for example, hardness] of tablets containing an active ingredient. DETAILED DESCRIPTION OF THE INVENTION

[0015] [1. Tablets] The tablet of the present invention contains Bofutsushosan extract.

[0016] Examples of Bofutsushosan extract (Bofutsushosan, Bofutsushosan ingredients) include extracts of a mixture (mixed raw materials) containing Bofu, Scutellaria Root, Rhubarb, Glauber's salt, Ephedra, Gypsum, Atractylodes macrocarpa, Forsythia Fruit, Platycodon grandiflorum, Gardenia Fruit, Peony, Angelica Root, Szechuan Gum, Mint, talc, ginger and licorice.

[0017] In the mixture, the ratio of each component is not limited, and examples include a mixture containing 1.2 parts by mass of scutellaria root, 2 parts by mass of Scutellaria root, 1.5 parts by mass of rhubarb, 1.5 parts by mass of Glauber's salt, 1.2 to 1.5 parts by mass of ephedra, 2 parts by mass of gypsum, 2 parts by mass of Atractylodes root, 1.2 to 1.5 parts by mass of Jingjiang root, 1.2 to 1.5 parts by mass of Forsythia fruit, 2 parts by mass of Platycodon root, 1.2 to 1.5 parts by mass of Gardenia fruit, 1.2 to 1.5 parts by mass of Peony root, 1.2 to 1.5 parts by mass of Angelica root, 1.2 to 1.5 parts by mass of Szechuan ginseng, 1.2 to 1.5 parts by mass of Mint, 3 parts by mass of talc, 0.3 to 0.5 parts by mass of ginger (1.2 to 1.5 parts by mass if ginger is used), and 2 parts by mass of licorice.

[0018] Such a mixture is one example, and the mixture also includes, for example, a mixture that does not contain other herbal medicines (for example, Atractylodes macrocarpa), a mixture in which the blending ratio is appropriately changed, and the like.

[0019] The extractant for the extract is not particularly limited, but is preferably water or alcohol (e.g., ethanol), and more preferably water. The extractant may be used alone or in combination of two or more.

[0020] The Bofutsushosan extract may be used alone or in combination of two or more kinds.

[0021] As long as the tablet contains bofutsushosan extract, it may contain other active ingredients (e.g., herbal extracts), but preferably it may contain substantially only bofutsushosan extract as the active ingredient. When the tablet contains other active ingredients other than bofutsushosan extract, the ratio of the other active ingredients to the total active ingredients may be 30% by mass or less, 20% by mass or less, 10% by mass or less, 5% by mass or less, 3% by mass or less, 1% by mass or less, etc.

[0022] The tablet may contain other ingredients (inactive ingredients) besides the active ingredient, as needed. Examples of such ingredients (additives) include excipients, binders, disintegrants, lubricants, sweeteners, flavoring agents, preservatives, chelating agents, antioxidants, cooling agents, coating agents, stabilizers, fluidizing agents, thickening agents, solubilizing agents, thickeners, buffers, flavorings, colorants, adsorbents, wetting agents, moisture-proofing agents, antistatic agents, plasticizers, antifoaming agents, surfactants, etc.

[0023] Specific examples of additives include sugars (e.g., lactose, sucrose, etc.), sugar alcohols (e.g., mannitol, sorbitol, etc.), celluloses [e.g., crystalline cellulose, cellulose derivatives (e.g., cellulose ethers such as hydroxypropyl cellulose), etc.], inorganic substances [e.g., stearates (magnesium stearate, etc.), talc, titanium oxide, silicon dioxide, silicic acid anhydride, silicates (e.g., magnesium aluminometasilicate, magnesium aluminosilicate), hydrates thereof (e.g., hydrated silicon dioxide), etc.].

[0024] The other components (additives) may be used alone or in combination of two or more.

[0025] Among these, sugar alcohols, celluloses, inorganic substances, etc. may be preferably used.

[0026] The tablet may be substantially free of magnesium aluminometasilicate and magnesium aluminosilicate. As mentioned above, Patent Document 1 requires magnesium aluminometasilicate and / or magnesium aluminosilicate as essential components, but the present invention makes it possible to efficiently obtain tablets containing Bofu-tsushosan extract at a relatively high content without using these.

[0027] In the tablet of the present invention, the content ratio of Bofutsushosan extract (or active ingredient) (ratio to the entire tablet) is relatively high, and may be selected from a range of, for example, about 30% by mass or more (e.g., 40% by mass or more), 45% by mass or more (e.g., 48% by mass or more), preferably 50% by mass or more (e.g., 53% by mass or more), more preferably 55% by mass or more (e.g., 58% by mass or more), particularly about 60% by mass or more (e.g., 63% by mass or more), and may also be 65% by mass or more (e.g., 68% by mass or more), 70% by mass or more (e.g., 73% by mass or more), 75% by mass or more (e.g., 78% by mass or more), 80% by mass or more (e.g., 83% by mass or more), 85% by mass or more (e.g., 88% by mass or more), 90% by mass or more (e.g., 93% by mass or more), etc.

[0028] The upper limit of the content of Bofutsushosan extract (or active ingredient) is not particularly limited, and may be 100% by mass, or less than 100% by mass, for example, 99% by mass, 98% by mass, 97% by mass, 96% by mass, 95% by mass, 94% by mass, 93% by mass, 92% by mass, 91% by mass, 90% by mass, 89% by mass, 88% by mass, 87% by mass, 86% by mass, 85% by mass, 84% by mass, 83% by mass, 82% by mass, 81% by mass, 80% by mass, 79% by mass, 78% by mass, 77% by mass, 76% by mass, 75% by mass, 74% by mass, 73% by mass, 72% by mass, 71% by mass, 70% by mass, etc.

[0029] The upper limit of the content of the bofutsushosan extract may be appropriately selected from the viewpoints of moldability, the type and intended use of other ingredients to be contained, other physical properties and performance (e.g., disintegrability, etc.), etc. For example, in a tablet or the like that is substantially free of magnesium aluminometasilicate and magnesium aluminosilicate, the upper limit of the content of the bofutsushosan extract (or active ingredient) may be 88% by mass or less (e.g., 87% by mass or less, less than 87% by mass, etc.).

[0030] In addition, when the tablet contains ingredients other than Bofutsushosan extract (active ingredient), the content ratio of the other ingredients may be 70% by mass or less, 60% by mass or less, 50% by mass or less, 40% by mass or less, 30% by mass or less, 25% by mass or less, 20% by mass or less, 15% by mass or less, 10% by mass or less, etc., relative to the total amount of Bofutsushosan extract and other ingredients, or may be 1% by mass or more, 3% by mass or more, 5% by mass or more, 7% by mass or more, 10% by mass or more, 15% by mass or more, 20% by mass or more, 25% by mass or more, 30% by mass or more, etc.

[0031] For example, when a tablet contains a lubricant, the proportion of the lubricant may be, for example, 0.01% by mass or more, 0.05% by mass or more, 0.1% by mass or more, etc., or 10% by mass or less, 5% by mass or less, 3% by mass or less, etc.

[0032] Tablets (1 tablet, single tablet, hereinafter, not dosage, mass (mg) or size (volume, mm 3) etc.) can be selected depending on the content ratio of Bofutsushosan extract and the desired dosage (effective intake amount), but it is preferable that it is not too large, and may be, for example, 1200 mg or less (e.g., 1100 mg or less), preferably 1000 mg or less (e.g., 900 mg or less), more preferably 800 mg or less (e.g., 750 mg or less), particularly 700 mg or less (e.g., 650 mg or less), particularly preferably 600 mg or less (e.g., 550 mg or less), or may be 500 mg or less, 490 mg or less, 480 mg or less, 470 mg or less, 460 mg or less, 450 mg or less, 440 mg or less, 430 mg or less, 420 mg or less, 410 mg or less, 400 mg or less, 390 mg or less, 380 mg or less, 370 mg or less, 360 mg or less, 350 mg or less, etc.

[0033] The lower limit of the tablet mass is not particularly limited, and may be, for example, 50 mg, 100 mg, 120 mg, 150 mg, 160 mg, 170 mg, 180 mg, 190 mg, preferably 200 mg or more (e.g., 200 mg, 210 mg, 220 mg, 230 mg, 240 mg, 250 mg, 260 mg, 270 mg, 280 mg, 290 mg), and more preferably 300 mg or more (e.g., 300 mg, 310 mg, 320 mg, 330 mg, 340 mg, 350 mg, 360 mg, 370 mg, 380 mg, 390 mg, 400 mg, 410 mg, 420 mg, 430 mg, 440 mg, 450 mg).

[0034] The size of the tablet can be selected depending on the content of the Bofutsushosan extract, the desired dosage (effective intake amount), etc., but it is preferable that the size is not too large, for example, 1000 mm. 3 Less than (e.g., 950 mm 3 or less), preferably 900 mm 3 Less than (e.g., 850 mm 3 or less), more preferably 800 mm 3 Less than (e.g., 750 mm 3 below), especially 700mm 3 Less than (e.g., 650 mm 3 less than 600 mm), particularly preferably3 Less than (e.g., 550 mm 3 (less than 500mm) 3 Less than (e.g., 450 mm 3 below), 400mm 3 Less than (e.g., 350 mm 3 below), 300mm 3 Less than (e.g., 250 mm 3 (See below) etc.

[0035] The lower limit of the size of the tablet is not particularly limited, but is, for example, 200 mm 3 , 250mm 3 , 300mm 3 etc., and preferably 350 mm 3 or more (e.g., 360 mm 3 , 370mm 3 , 380mm 3 , 390mm 3 , ), more preferably 400 mm 3 or more (e.g., 410 mm 3 , 420mm 3 , 430mm 3 , 440mm 3 , 450mm 3 , 460mm 3 , 470mm 3 , 480mm 3 , 490mm 3 , 500mm 3 ) etc.

[0036] In the tablet, the content of the bofutsushosan extract (or active ingredient) can be selected depending on the mass of the tablet, etc., and may be selected from a range of, for example, about 50 mg or more (e.g., 60 mg or more), 70 mg or more (e.g., 80 mg or more), preferably 90 mg or more (e.g., 95 mg or more), more preferably 100 mg or more (e.g., 105 mg or more), particularly 110 mg or more (e.g., 115 mg or more), particularly preferably 120 mg or more (e.g., 125 mg or more), 130 mg or more, 140 mg or more, 150 mg or more, 160 mg or more, 170 mg or more, 180 mg or more, 190 mg or more, 200 mg or more, 210 mg or more, 220 mg or more, 230 mg or more, 240 mg or more, 250 mg or more, 260 mg or more, 270 mg or more, 280 mg or more, 290 mg or more, 300 mg or more, 310 mg or more, 320 mg or more, 330 mg or more, 340 mg or more, 350 mg or more, 360 mg or more, 370 mg or more, 380 mg or more, 390 mg or more, 400 mg or more, 410 mg or more, 420 mg or more, 430 mg or more, 440 mg or more, 450 mg or more, 460 mg or more, 470 mg or more, 480 mg or more, 490 mg or more, 500 mg or more, 510 mg or more, 520 mg or more, 530 mg or more, 540 mg or more, 55 It may be 90 mg or more, 200 mg or more, 210 mg or more, 220 mg or more, 230 mg or more, 240 mg or more, 250 mg or more, 260 mg or more, 270 mg or more, 280 mg or more, 290 mg or more, 300 mg or more, 310 mg or more, 320 mg or more, 330 mg or more, 340 mg or more, 350 mg or more, 360 mg or more, 370 mg or more, 380 mg or more, 390 mg or more, 400 mg or more, 410 mg or more, 420 mg or more, 430 mg or more, 440 mg or more, 450 mg or more, 510 mg or more, 520 mg or more, 530 mg or more, 540 mg or more, 550 mg or more, etc.

[0037] In addition, the upper limit of the content of Bofutsushosan extract (or active ingredient) in tablets can be selected depending on the mass of the tablet, etc., and may be, for example, 1000mg, 950mg, 900mg, 850mg, 800mg, 750mg, 700mg, 650mg, 600mg, 550mg, 500mg, 490mg, 480mg, 470mg, 460mg, 450mg, 440mg, 430mg, 420mg, 410mg, 400mg, 390mg, 380mg, 370mg, 360mg, 350mg, 340mg, 330mg, 320mg, 310mg, 300mg, 250mg, 200mg, 150mg, etc.

[0038] The tablet may be a disintegrating tablet.

[0039] The tablet (tablet shape) is not particularly limited, and may be, for example, a round tablet (so-called ordinary tablet), an irregularly shaped tablet (caplet, ring tablet, flower-shaped, star-shaped, heart-shaped, etc.), or the like.

[0040] The tablets may be coated (for example, sugar coated, film coated, etc.).

[0041] The tablet of the present invention is particularly suitable as a tablet for use in a relatively high dose, although not limited thereto.

[0042] The dosage of such tablets (amount of active ingredient, oral dosage, intake amount, effective intake amount) may be selected from the range of, for example, 3000 mg or more per day of Bofutsushosan extract (active ingredient), preferably 4000 mg or more, more preferably 5000 mg or more (e.g., more than 5000 mg, 5050 mg or more), 5100 mg or more, 5200 mg or more, 5300 mg or more, 5400 mg or more, 5500 mg or more, 5600 mg or more, 5700 mg or more, 5800 mg or more, 5900 mg or more, particularly 6000 mg or more (e.g., more than 6000 mg, 6030 mg or more, 6050 mg or more, 6080 mg or more, 6100 mg or more, 6150 mg or more, 6200 mg or more, 6250 mg or more, 6300 mg or more, etc.).

[0043] The upper limit of the tablet dose is not particularly limited, but for example, the following dosages are available: 20,000 mg, 19,000 mg, 18,000 mg, 17,000 mg, 16,000 mg, 15,000 mg, 14,000 mg, 13,000 mg, 12,000 mg, 11,000 mg, 10,000 mg, 9,500 mg, 9,000 mg, 8,500 mg g, 8400 mg, 8300 mg, 8200 mg, 8100 mg, 8000 mg, 7900 mg, 7800 mg, 7700 mg, 7600 mg, 7500 mg, 7400 mg, 7300 mg, 7200 mg, 7100 mg, 7000 mg, 6900 mg, 6800 mg, 6700 mg, 6600 mg, 6500 mg, 6400 mg, etc.

[0044] The dosage (dosage, oral dosage, intake amount) of the tablet (tablet itself) depends on the effective intake amount of the active ingredient and the content ratio in the tablet, but may be selected from the range of, for example, 30,000 mg or less (e.g., 25,000 mg or less) per day, preferably 20,000 mg or less (e.g., 18,000 mg or less), more preferably 15,000 mg or less (e.g., 13,000 mg or less), and particularly preferably 12,000 mg or less. It may be 0 mg or less (for example, 11,000 mg or less), 10,000 mg or less, 9,500 mg or less, 9,000 mg or less, 8,500 mg or less, 8,200 mg or less, 8,000 mg or less, 7,900 mg or less, 7,800 mg or less, 7,700 mg or less, 7,600 mg or less, 7,500 mg or less, 7,400 mg or less, 7,300 mg or less, 7,200 mg or less, 7,100 mg or less, 7,000 mg or less, etc.

[0045] The lower limit of the dose of the tablet (the tablet itself) is not particularly limited, but may be, for example, 300 mg, 3500 mg, 4000 mg, 4500 mg, 4800 mg, 5000 mg, 5100 mg, 5200 mg, 5300 mg, 5400 mg, 5500 mg, 5600 mg, 5700 mg, 5800 mg, 5900 mg, 6000 mg, 6100 mg, 6200 mg, 6300 mg, 6400 mg, 6500 mg, 6600 mg, 6700 mg, 6800 mg, 6900 mg, 7000 mg, 7100 mg, 7200 mg, 7300 mg, etc. per day.

[0046] The dosage (dosage, oral administration, intake) of the tablet (the tablet itself) depends on the effective intake amount of the active ingredient and the content ratio in the tablet, but for example, per day (as the total volume of the tablet taken per day), 20,000 mm 3 Less than (e.g., 17500 mm 3 The thickness may be selected from the range of 15,000 mm or less, preferably 15,000 mm 3 Less than (e.g., 12500 mm 3 or less), more preferably 10,000 mm 3 Less than (e.g., 9500 mm 3 (less than 9000 mm) 3 Less than (e.g., 8500 mm 3(or less) may be 8000mm 3 Below, 7500mm 3 Below, 7000mm 3 Below, 6500mm 3 Below, 6000mm 3 Below, 5500mm 3 Below, 5000mm 3 The following may also be used:

[0047] The lower limit of the dose of the tablet (the tablet itself) is not particularly limited, but for example, 2000 mm per day 3 , 2500mm 3 , 3000mm 3 , 3500mm 3 , 4000mm 3 , 4500mm 3 , 5000mm 3 , 5500mm 3 , 6000mm 3 , 6500mm 3 , 7000mm 3 , 7500mm 3 etc. may also be used.

[0048] The tablet may be taken, for example, once or more times per day (for example, 1 to 10 times), but may also be taken, for example, twice or more times (for example, 2 to 6 times), and particularly 3 times.

[0049] The number of tablets per day (number taken, number administered, number ingested) depends on the effective intake amount, the content ratio in the tablets, etc., but may be selected from a range of about 60 tablets or less (e.g., 55 tablets or less), for example, 50 tablets or less (e.g., 48 tablets or less), preferably 45 tablets or less (e.g., 42 tablets or less), more preferably 39 tablets or less (e.g., 36 tablets or less), particularly 33 tablets or less (e.g., 30 tablets or less), particularly preferably 27 tablets or less (e.g., 24 tablets or less), or may be 21 tablets or less, 18 tablets or less, 15 tablets or less, etc.

[0050] The lower limit of the number of tablets per day may be, for example, 3 tablets, 6 tablets, 9 tablets, 12 tablets, 15 tablets, etc.

[0051] The number of tablets per dose (number of doses, number of administrations, number of ingestions) may be selected from a range of about 20 tablets or less (e.g., 19 tablets or less), depending on the method of use, etc., and may be, for example, 18 tablets or less (e.g., 17 tablets or less), preferably 16 tablets or less (e.g., 15 tablets or less), more preferably 14 tablets or less (e.g., 13 tablets or less), particularly 12 tablets or less (e.g., 11 tablets or less), particularly preferably 10 tablets or less (e.g., 9 tablets or less), and most preferably 8 tablets or less (e.g., 7 tablets or less, 6 tablets or less, 5 tablets or less, 4 tablets or less, etc.). The lower limit of the number of tablets per dose may be, for example, 1 tablet, 2 tablets, 3 tablets, 4 tablets, 5 tablets, etc.

[0052] The present invention also includes multiple tablets (multiple tablets, combination tablets) corresponding to such dosage regimens.

[0053] For example, if the daily dose of tablet X is A mg, the multiple tablets would be tablets combining multiple tablets X to provide A mg of Bofutsushosan extract (multiple tablets for taking a daily dose of A mg). The specific number of tablets (number of tablets per day) of multiple tablets can be selected, for example, from the range exemplified above.

[0054] Furthermore, if the dose of tablet X per administration is B mg, the multiple tablets will be tablets obtained by combining multiple tablets X to provide B mg of Bofutsushosan extract (multiple tablets for taking a dose of B mg per administration). The specific number of tablets (number of tablets per dose) of multiple tablets can be selected, for example, from the range exemplified above.

[0055] The tablets are not particularly limited as long as they are composed of the active ingredient (bofutsushosan extract), and can be produced by a conventional method (molding method). Examples of such a molding method (tablet molding method) include, but are not limited to, direct powder compression method (direct compression method) and granule compression method (indirect tablet compression method).

[0056] In the molding method, the constituent components of the tablet and their ratios may be selected to be the same as those described above (or to be the same as those described above).

[0057] [2. Improvement of moldability and physical properties] In the present invention, by selecting Bofutsushosan extract as the active ingredient, the moldability and physical properties of the tablets can be improved or enhanced.

[0058] Thus, as one embodiment of the present invention, the following method is provided.

[0059] A method for improving or enhancing the moldability and / or physical properties [e.g., hardness (hardness, strength)] of tablets containing an active ingredient, which method selects (uses) Bofutsushosan extract as the active ingredient.

[0060] A method for improving or enhancing the moldability and / or physical properties [e.g., hardness] of a tablet containing less than A% by mass (e.g., less than 45% by mass) of an active ingredient, which comprises selecting (using) bofutsushosan extract as the active ingredient and increasing the content of the active ingredient (bofutsushosan extract) to A% by mass or more (e.g., 45% by mass or more) [increasing the content to A% by mass or more (e.g., 45% by mass or more)].

[0061] In such methods, the enhanced or improved moldability may be evidenced, for example, by the prevention (or reduction) of the occurrence of capping.

[0062] In this method, various properties of the tablet (mass, content of Bofutsushosan extract, etc.) may be selected in the same manner as described above. [Example]

[0063] The present invention will be explained in more detail below by way of examples, but the present invention is not limited to these examples, and many modifications can be made by those skilled in the art within the technical spirit of the present invention.

[0064] [Test Example 1] Various tablets were prepared as follows:

[0065] <Tablets (A1)> Based on the formulation shown in Table 1, 630 g of Bofutsushosan extract, 762.8 g of D-mannitol, and 40 g of crystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 7.2 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed to 600 mg tablets under the following tableting conditions: final pressure 13 kN, preload 5 kN, turntable rotation speed 30 rpm, and stirring blade rotation speed 50 rpm.

[0066] <Tablets (A2)> Based on the formulation shown in Table 1, 630 g of Bofutsushosan extract, 415 g of D-mannitol, and 30 g of crystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 5.4 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed under the following tableting conditions: a final pressure of 13 kN, a preload of 5 kN, a rotating disk rotation speed of 30 rpm, and a stirring blade rotation speed of 50 rpm, so that each tablet weighed 600 mg, to obtain tablets.

[0067] <Tablets (A3)> Based on the formulation shown in Table 1, 630 g of Bofutsushosan extract, 241 g of D-mannitol, and 25 g of microcrystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 4.5 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed to 600 mg tablets under the following tableting conditions: final pressure 13 kN, preload 5 kN, turntable rotation speed 30 rpm, and stirring blade rotation speed 50 rpm.

[0068] <Tablets (A4)> Based on the formulation shown in Table 1, 1260 g of Bofutsushosan extract, 133 g of D-mannitol, and 40 g of microcrystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 7.2 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed to 600 mg tablets under the following tableting conditions: a final pressure of 13 kN, a preload of 5 kN, a turntable rotation speed of 30 rpm, and a stirring blade rotation speed of 50 rpm.

[0069] <Tablets (B1)> Based on the formulation shown in Table 1, 630 g of Bofutsushosan extract, 762.8 g of D-mannitol, and 40 g of crystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 7.2 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed to 300 mg tablets under the following tableting conditions: a final pressure of 13 kN, a preload of 5 kN, a turntable rotation speed of 30 rpm, and a stirring blade rotation speed of 50 rpm.

[0070] <Tablets (B2)> Based on the formulation shown in Table 1, 630 g of Bofutsushosan extract, 241 g of D-mannitol, and 25 g of microcrystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 4.5 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed to 300 mg tablets under the following tableting conditions: a main pressure of 13 kN, a preload of 4 kN, a turntable rotation speed of 30 rpm, and a stirring blade rotation speed of 50 rpm.

[0071] <Tablets (B3)> Based on the formulation shown in Table 1, 1260 g of Bofutsushosan extract, 133 g of D-mannitol, and 40 g of crystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 7.2 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed to 300 mg tablets under the following tableting conditions: a final pressure of 13 kN, a preload of 5 kN, a turntable rotation speed of 30 rpm, and a stirring blade rotation speed of 50 rpm.

[0072] <Tablets (C1)> Based on the formulation shown in Table 1, 315 g of yokukansan extract, 381 g of D-mannitol, and 20 g of microcrystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 3.6 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed under the following conditions: a main pressure of 15 kN, a preload of 7 kN, a rotating disk rotation speed of 15 rpm, and a stirring blade rotation speed of 50 rpm, so that each tablet weighed 600 mg, to obtain tablets.

[0073] <Tablets (C2)> Based on the formulation shown in Table 1, 630 g of yokukansan extract, 6.4 g of D-mannitol, and 20 g of microcrystalline cellulose were mixed in a vinyl tube. The mixture was then crushed in a crusher and mixed with 3.6 g of magnesium stearate to prepare powder for tableting. This powder for tableting was compressed under the following tableting conditions: a main pressure of 15 kN, a preload of 7 kN, a rotating disk rotation speed of 15 rpm, and a stirring blade rotation speed of 50 rpm, so that each tablet was 600 mg, to obtain tablets.

[0074] The Bofu-tsushosan extract used contained, by mass, 1.2 parts of Bofu, 2 parts of Scutellaria Root, 1.5 parts of Rhubarb, 1.5 parts of Glauber's salt, 1.2 parts of Ephedra, 2 parts of Gypsum, 2 parts of Atractylodes Root, 1.2 parts of Scutellaria Root, 1.2 parts of Forsythia Fruit, 2 parts of Platycodon Root, 1.2 parts of Gardenia Fruit, 1.2 parts of Peony Root, 1.2 parts of Angelica Root, 1.2 parts of Rhizome, 1.2 parts of Mint, 3 parts of talc, 0.4 parts of ginger, and 2 parts of licorice, and was prepared by conventional methods.

[0075] The hardness H1 of the obtained tablets was measured (n=5) using a hardness tester (PHARMA TEST, PTTB311E), and the ratio (H1 / H2) of the hardness H1 to the hardness H2 of the tablet with the smallest amount of active ingredient (A1, B1, or C1 in this example, when the amount was 43.8% by mass), which differed only in the amount of active ingredient and mannitol, was calculated.

[0076] In addition, the uncapping rate [1-(number of tablets on which capping occurred / number of tablets)] X1 at the end of tableting was examined, and the ratio (X1 / X2) of the uncapping rate X2 for the tablet with the smallest amount of active ingredient (A1, B1, or C1 in this example), which differed only in the amount of active ingredient and the amount of mannitol, was calculated.

[0077] [Table 1]

[0078] [Test Example 2] The tablets obtained in Test Example 1 were administered three times a day at the doses shown in Tables 2 and 3 below (daily dose as Bofutsushosan extract), and the number of tablets, etc., was determined. The tablets were taken according to the dosage and administration method, and the administration characteristics were investigated as follows. The ease of administration was evaluated using the following criteria, in comparison with the same tablet containing the smallest amount of active ingredient per day (A1 or B1 in this example).

[0079] 3 points: It became much easier to take 2 points: It became easier to take 1 point: Slightly easier to take 0 points: No change in ease of administration -1 point: It became a little difficult to take -2 points: Difficult to take -3 points: It became very difficult to take the medicine

[0080] The ease of taking the tablets was evaluated comprehensively by each panelist, taking into account the ease of taking each tablet and the number of tablets taken at one time and per day.

[0081] The results are shown in Tables 2 and 3 below. In the table, the ease of administration (points) is the average of the points given by each panelist (average point).

[0082] In addition, in the table, the number and volume of tablets per day or per serving are average values ​​(calculated values). If the number of tablets to be taken per day contained a decimal point, the number was adjusted by rounding off to the nearest whole number so that the number of tablets taken per dose was an integer and there was no variation. For example, tablet type B2, dose 4000 mg / day (second row in Table 2), is calculated as "19.0 tablets / day" and "6.3 tablets / time," but the actual dosage was "6 tablets," "6 tablets," and "7 tablets," a total of three times per day. Additionally, for tablet type B1, the dose was 5000 mg / day (fourth row in Table 2), which was calculated as "38.1 tablets / day" and "12.7 tablets / time," but the actual dosage was "13 tablets," "13 tablets," and "12 tablets," a total of three times per day.

[0083] [Table 2]

[0084] [Table 3] [Industrial Applicability]

[0085] The present invention can provide novel tablets and the like.

Claims

[Claim 1] The invention described herein.

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