Tablet

The combination of Garcinia cambogia with excipients and lubricants in tablet formulation addresses the challenges of poor tableting properties and hardness, resulting in tablets with improved hardness and disintegration.

JP2026002686APending Publication Date: 2026-01-08TOYO SHINYAKU KK
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Patent Information

Application Number
JP2024100847
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-06-21
Publication Date
2026-01-08

AI Technical Summary

Technical Problem

Garcinia cambogia is unsuitable for tablet formulation due to poor tableting properties and difficulty in increasing tablet hardness, leading to issues like poor punch release and delayed disintegration.

Method used

A tablet formulation comprising Garcinia cambogia, an excipient, and a lubricant, such as cellulose, sugar alcohols, and metal stearates, to enhance hardness and tableting properties.

Benefits of technology

The formulation achieves tablets with high hardness and good tableting properties, ensuring effective punch release and appropriate disintegration times.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a tablet containing garcinia and having both of hardness and tableting property.SOLUTION: The tablet of the present invention contains (A) garcinia, (B) an excipient and (C) a lubricant. The (A) garcinia is preferably garcinia indica. The (B) excipient also preferably contains one or more selected from cellulose, reduced maltose, and hydroxypropyl cellulose. It is also preferable that the content of (A) garcinia in the tablet is 1 to 40% by mass.SELECTED DRAWING: None
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Description

[Technical Field]

[0001] The present invention relates to tablets containing Garcinia cambogia. [Background technology]

[0002] In recent years, growing interest in health has led to the development of various ingredients for use in health foods. Garcinia is one such ingredient. Garcinia is a general term for plants in the genus Garcinia (also known as Garcinia) of the family Hypericaceae, specifically including plants such as Garcinia indica and Garcinia cambogia. Garcinia is known to have various beneficial effects, such as retinal protection, anti-aging of the eye, and inhibition of ocular angiogenesis (see, for example, Patent Document 1). Therefore, there is a demand for the development of health foods containing Garcinia. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] International Publication No. 2020 / 179747 Summary of the Invention [Problem to be solved by the invention]

[0004] Tablets are a common dosage form for health foods, but Garcinia cambogia has the problem of being unsuitable as an ingredient for tablet formulation. Specifically, Garcinia cambogia is not well suited for tableting, so when Garcinia cambogia is incorporated into tablets, it is prone to causing tableting problems such as poor punch release. In addition, the incorporation of Garcinia cambogia tends to make it difficult to increase the tablet hardness, but if an attempt is made to forcibly increase the hardness by increasing the tableting pressure, this could result in delayed disintegration. [Means for solving the problem]

[0005] The present inventors, while studying tablets containing Garcinia, discovered that by adding an excipient and a lubricant together with Garcinia, the hardness of the tablets can be increased and the tableting properties can be improved, leading to the completion of the present invention. That is, the present invention provides a tablet containing (A) Garcinia, (B) an excipient, and (C) a lubricant. [Effects of the Invention]

[0006] The present invention provides a tablet containing Garcinia, which has both high hardness and good tableting properties. DETAILED DESCRIPTION OF THE INVENTION

[0007] The present invention will be described below based on preferred embodiments thereof. As used herein, a tablet refers to a compressed solid dosage form containing (A) Garcinia cambogia together with (B) excipients and (C) a lubricant. The tablet can be prepared by compressing a mixture. In the present invention, "tablet" includes plain tablets, orally disintegrating tablets, and film-coated tablets.

[0008] The tablet of the present invention contains (A) Garcinia cambogia, (B) an excipient, and (C) a lubricant.

[0009] (A) Garcinia Garcinia is a plant (scientific name: Garcinia) of the family Hypericaceae, genus Garcinia (also known as the genus Mangosteen or Garcinia), and examples include Garcinia indica (scientific name: Garcinia indica) and Garcinia cambogia (scientific name: Garcinia Cambogia), with the use of Garcinia indica being particularly preferred due to its excellent tablet disintegration properties.

[0010] The parts of Garcinia used in the present invention are not particularly limited, and leaves, fruits, and other parts can be used in combination. However, from the viewpoint of fully demonstrating the health and beauty effects of Garcinia, fruits are preferred, and pulp and peel are particularly preferred.

[0011] The processing method of Garcinia used in the present invention is not particularly limited, and any suitable combination of extracts and pulverized products can be used. However, extracts are particularly preferred, as they are superior in terms of the technical significance of the present invention in terms of better demonstrating the health and beauty benefits inherent to Garcinia and achieving both hardness and tabletability.

[0012] Known methods for extracting Garcinia include adding an extraction solvent commonly used by those skilled in the art and heating the mixture as needed. The extraction solvent used in the extraction process can be water or an organic solvent. Polar solvents are often used, such as water, methanol, ethanol, isopropanol, acetone, 1,3-butylene glycol, ethylene glycol, propylene glycol, glycerin, acetic acid, ethyl acetate, ether, and hexane. Polar solvents are preferred as the extraction solvent, as they enhance the health and beauty benefits inherent to Garcinia and achieve the technical significance of the present invention, which is to achieve both hardness and tabletability. Water, ethanol, or a mixture of water and ethanol is more preferred, and ethanol is most preferred. When extracting using a mixture of water and an organic solvent, the proportion of the organic solvent in the mixture is preferably 50% by mass or more, more preferably 60% by mass or more, particularly preferably 70% by mass or more, and even more preferably 80% by mass or more.

[0013] When extraction is performed with a polar solvent, the extraction method is not particularly limited, and continuous extraction, immersion extraction, countercurrent extraction, etc. can be suitably selected, and any apparatus can be used at room temperature or under reflux heating. The extract can be concentrated and dried into a powder as needed.

[0014] The proportion of Garcinia in the tablet of the present invention is not particularly limited, but from the viewpoint of fully demonstrating the health and beauty effects of Garcinia, it is preferable to incorporate it in an amount of 1% by mass or more, converted to dry mass, more preferably 2% by mass or more, even more preferably 3% by mass or more, even more preferably 4% by mass or more, particularly preferably 5% by mass or more, particularly preferably 7% by mass or more, even more preferably 10% by mass or more, even more preferably 12% by mass or more, and most preferably 15% by mass or more.

[0015] The proportion of Garcinia in the tablet of the present invention is not particularly limited, but from the viewpoint of ensuring the amount of excipients and increasing hardness, the proportion of Garcinia in the tablet is preferably 35% by mass or less, more preferably 33% by mass or less, even more preferably 30% by mass or less, and even more preferably 27% by mass or less, and is preferably 40% by mass or less, converted into dry mass.

[0016] (B) excipients The tablet of the present invention contains (B) an excipient, such as cellulose, cellulose derivatives, sugars, starch and its derivatives, and dextrin.

[0017] Examples of cellulose include powdered cellulose and crystalline cellulose. Crystalline cellulose is obtained by partially depolymerizing α-cellulose obtained as pulp from fibrous plants with an acid and purifying it. For example, it corresponds to the crystalline cellulose described in the 15th Revised Japanese Pharmacopoeia Commentary (published by Hirokawa Shoten). Crystalline cellulose can be classified into crystalline cellulose powder and crystalline cellulose complex. Powdered cellulose is obtained by treating α-cellulose obtained as pulp from fibrous plants, purifying it, and mechanically pulverizing it. For example, it corresponds to the powdered cellulose described in the 15th Revised Japanese Pharmacopoeia Commentary (published by Hirokawa Shoten). It is particularly preferable to use crystalline cellulose as the cellulose from the viewpoint of achieving both tabletability and hardness.

[0018] Examples of the cellulose derivatives include carboxymethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, and methyl cellulose. Of these, from the viewpoint of achieving both tableting properties and hardness, nonionic cellulose derivatives such as hydroxypropyl cellulose, hydroxypropylmethyl cellulose, and methyl cellulose are preferred, with hydroxypropyl cellulose being particularly preferred.

[0019] The sugars include sugar alcohols, monosaccharides, disaccharides, and oligosaccharides.

[0020] Sugar alcohols include monosaccharide alcohols, disaccharide alcohols, and trisaccharide or higher saccharide alcohols. Examples of monosaccharide alcohols include tetritols such as erythritol, D-threitol, and L-threitol; pentitols such as D-arabinitol and xylitol; hexitols such as D-iditol, galactitol (dulcitol), and D-glucitol (sorbitol); cyclitols such as inositol; mannitol, volemitol, ribitol, perseitol, and D-erythro-D-galacto-octitol. Examples of disaccharide alcohols include reduced maltose (maltitol), lactitol, and reduced palatinose (isomalt). Examples of trisaccharide or higher saccharide alcohols include maltotriitol, isomaltotriitol, and panitol.

[0021] Monosaccharides include glucose, galactose, fructose, and mannose. Disaccharides include sucrose, maltose, lactose (milk sugar), trehalose, turanose, and cellobiose. Examples of oligosaccharides include those having from three to twenty sugars, preferably from three to ten sugars, and more preferably from three to six sugars.

[0022] Among the sugars, sugar alcohols are preferred, disaccharide alcohols are more preferred, and reduced maltose is particularly preferred.

[0023] When the tablet of the present invention contains reduced maltose, from the viewpoint of achieving both tableting properties and hardness, the proportion of reduced maltose in the sugars is preferably 35% by mass or more, more preferably 40% by mass or more, even more preferably 50% by mass or more, and even more preferably 60% by mass or more.

[0024] Examples of starch include natural starch, and starch sources include corn, potato, arrowroot, tapioca, sweet potato, rice, wheat, barley, yam, and taro.

[0025] Examples of starch derivatives include modified starch, oxidized starch, enzyme-treated starch, pregelatinized starch, starch phosphate, distarch phosphate, starch acetate, starch octenylsuccinate, glycerol distarch, carboxymethyl starch, hydroxypropyl starch, crosslinked starch, soluble starch, grafted starch, and sodium carboxymethyl starch.

[0026] From the viewpoint of the balance between hardness and tableting properties, it is preferable that the (B) excipient contains one or more selected from cellulose, sugar alcohols, and cellulose derivatives, and it is particularly preferable that it contains one or more selected from cellulose, reduced maltose, and cellulose derivatives, and it is particularly preferable that it contains at least one selected from cellulose, reduced maltose, and hydroxypropyl cellulose.

[0027] From the viewpoint of the balance between tablet hardness, disintegrability, and tableting properties, the content of (B) excipient in the tablet of the present invention is preferably 10% by mass or more, more preferably 20% by mass or more, preferably 30% by mass or more, more preferably 40% by mass or more, and particularly preferably 50% by mass or more.

[0028] From the viewpoint of the balance between tablet hardness, disintegrability, and tableting properties, the content of (B) excipient in the tablet of the present invention is preferably 95% by mass or less, more preferably 90% by mass or less, even more preferably 80% by mass or less, even more preferably 78% by mass or less, and particularly preferably 75% by mass or less.

[0029] Furthermore, from the viewpoint of the balance between tablet hardness, disintegrability, and tableting ability, the ratio of the mass of the excipient (B) to the mass of the Garcinia (A) in the tablet of the present invention ((B) / (A)) is preferably 0.01 or more, more preferably 1 or more, even more preferably 3 or more, even more preferably 8 or more, and particularly preferably 8.2 or more. Moreover, the ratio ((B) / (A)) is preferably 200 or less, more preferably 120 or less, more preferably 80 or less, and even more preferably 40 or less.

[0030] When the tablet of the present invention contains a sugar alcohol, from the viewpoint of the balance between disintegration property, hardness, and tableting property, the amount thereof in the tablet is preferably 30% by mass or more, more preferably 45% by mass or more, even more preferably 50% by mass or more, and particularly preferably 60% by mass or more. In particular, the amount of reduced maltose is preferably the lower limit mentioned above, that is, 30% by mass or more, more preferably 45% by mass or more, even more preferably 50% by mass or more, and particularly preferably 60% by mass or more in the tablet.

[0031] Furthermore, when the tablet of the present invention contains a sugar alcohol, from the viewpoint of the balance between hardness, disintegrability, and tableting, the amount thereof is preferably 90% by mass or less, more preferably 85% by mass or less, even more preferably 80% by mass or less, and particularly preferably 75% by mass or less. In particular, the amount of reduced maltose is preferably the above-mentioned upper limit or less, that is, 90% by mass or less, more preferably 85% by mass or less, even more preferably 80% by mass or less, and particularly preferably 75% by mass or less.

[0032] When the tablet of the present invention contains a cellulose derivative, the hardness of the tablet can be further increased. When the tablet of the present invention contains a cellulose derivative, the amount of the cellulose derivative in the tablet is preferably 0.1% by mass or more, more preferably 1% by mass or more, and even more preferably 2% by mass or more. In the tablet of the present invention, the content of the cellulose derivative may be 25% by mass or less, 20% by mass or less, 14% by mass or less, 12% by mass or less, 10% by mass or less, 8% by mass or less, 5% by mass or less, or 3% by mass or less.

[0033] When the tablet of the present invention contains cellulose, the hardness of the tablet can be further increased. When the tablet of the present invention contains cellulose, the amount of cellulose in the tablet is preferably 0.1% by mass or more, more preferably 1% by mass or more, and even more preferably 2% by mass or more. When the tablet of the present invention contains cellulose, from the viewpoint of the balance between hardness and tableting properties, the content thereof in the tablet is preferably 90% by mass or less, more preferably 85% by mass or less, and even more preferably 80% by mass or less.

[0034] The tablet of the present invention is preferably one in which the total proportion of cellulose and sugars in the excipient is high, as this has a high effect of improving disintegration property. From this viewpoint, the total proportion of cellulose and sugars in the excipient is preferably 70% by mass or more, more preferably 80% by mass or more, even more preferably 90% by mass or more, and particularly preferably 95% by mass or more.

[0035] (C) Lubricant The tablet of the present invention contains a (C) lubricant. A (C) lubricant refers to a substance added to a dosage form to reduce friction or wear and thereby allow tablets, granules, etc., to separate from a mold or die after compression. In the present invention, the use of a (C) lubricant not only improves tableting properties but also increases tablet hardness. Examples of the (C) lubricant include metal stearates; stearic acid; high-melting-point waxes; and water-soluble lubricants such as sodium oleate and polyethylene glycol. Examples of the metal stearates include alkali metal salts and alkaline earth metal salts of stearic acid, such as magnesium stearate, calcium stearate, and potassium stearate. In particular, metal stearates are preferred as the (C) lubricant due to their excellent effects, with magnesium stearate or calcium stearate being more preferred, and calcium stearate being particularly preferred.

[0036] In order to facilitate the exertion of the above-mentioned effects of (C) lubricant, the content of (C) lubricant in the tablet is preferably 0.1% by mass or more, more preferably 0.2% by mass or more, even more preferably 0.4% by mass or more, even more preferably 0.6% by mass or more, particularly preferably 0.8% by mass or more, particularly preferably 1.0% by mass or more, and most preferably 1.2% by mass or more. Furthermore, in order to facilitate the exertion of the above-mentioned effects, the content of (C) lubricant in the tablet is preferably 3% by mass or less, more preferably 2.9% by mass or less, even more preferably 2.8% by mass or less, even more preferably 2.7% by mass or less, particularly preferably 2.6% by mass or less, and especially preferably 2.5% by mass or less.

[0037] Furthermore, from the viewpoint of the balance between tablet hardness and tableting properties, the ratio of the mass of the lubricant (C) to the mass of the Garcinia (A) in the tablet of the present invention ((C) / (A)) is preferably 0.001 or more, more preferably 0.005 or more, more preferably 0.01 or more, and even more preferably 0.02 or more. Moreover, the ratio ((C) / (A)) is preferably 20 or less, more preferably 10 or less, more preferably 3 or less, and even more preferably 1 or less.

[0038] Other ingredients Furthermore, the tablet of the present invention preferably contains (D) a fluidizing agent. (D) A fluidizing agent is an agent added to prevent powder from caking during tableting and to improve fluidity. By containing (D) a fluidizing agent, the hardness of the tablet of the present invention can be further increased.

[0039] Examples of the (D) fluidizing agent include silicon dioxide, magnesium aluminometasilicate, etc. Examples of silicon dioxide include light anhydrous silicic acid, heavy anhydrous silicic acid, and hydrous silicon dioxide. In the tablet of the present invention, silicon dioxide is particularly preferred as the (D) fluidizing agent because it can more easily increase the hardness.

[0040] When (D) a fluidizing agent is contained, from the viewpoint of the balance between hardness and tableting properties, the amount of (D) a fluidizing agent in the tablet is preferably 0.1% by mass or more, more preferably 0.2% by mass or more, even more preferably 0.4% by mass or more, even more preferably 0.6% by mass or more, particularly preferably 1% by mass or more, particularly preferably 1.2% by mass or more, and most preferably 1.5% by mass or more.

[0041] From the viewpoint of the balance between hardness and tabletability, the amount of (D) fluidizer in the tablet is preferably 3% by mass or less, more preferably 2.9% by mass or less, even more preferably 2.8% by mass or less, even more preferably 2.7% by mass or less, particularly preferably 2.6% by mass or less, and especially preferably 2.5% by mass or less.

[0042] From the viewpoint of the balance between tablet hardness and tableting properties, the ratio of the mass of the fluidizing agent (D) to the mass of the Garcinia cambogia (A) in the tablet of the present invention ((D) / (A)) is preferably 0.001 or more, more preferably 0.005 or more, more preferably 0.01 or more, and even more preferably 0.02 or more. Moreover, the ratio ((D) / (A)) is preferably 20 or less, more preferably 10 or less, more preferably 3 or less, and even more preferably 1 or less.

[0043] The tablet of the present invention preferably contains (E) vitamins, which not only increase the hardness of the tablet but also improves disintegration properties. Furthermore, since vitamins are components necessary for the body, it is also preferable to add vitamins separately in addition to (A) Garcinia cambogia from the viewpoint of nutritional intake. For example, a vitamin preparation containing vitamins at high purity (e.g., 80% by mass or more) may be used as the added vitamin. Vitamins are a general term for organic compounds other than carbohydrates, proteins, and lipids that are necessary in small amounts for the survival and growth of living organisms, but cannot be synthesized in sufficient amounts within the body of the organism. Vitamins are classified into water-soluble vitamins and fat-soluble vitamins.

[0044] Water-soluble vitamins include vitamin B and vitamin C. Vitamins belonging to the vitamin B group include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (niacin), vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine, pyridoxal, pyridoximine), vitamin B7 (biotin), vitamin B9 (folic acid), and vitamin B12 (cyanocobalamin). These vitamins may be the components in parentheses, or may be salts or derivatives of the components in parentheses. These may be used alone or in combination of two or more.

[0045] Examples of fat-soluble vitamins include vitamin A, vitamin D, vitamin E, and salts and derivatives thereof. These may be used alone or in combination of two or more.

[0046] Derivatives include disulfide compounds and acylated compounds, and salts include nitrates and hydrochlorides.

[0047] Examples of thiamine derivatives include bisthiamine, thiamine disulfide (TDS), thiamine dicetyl sulfate, benfotiamine (BTMP), prosultiamine (TPD), fursultiamine (TTFD), bisbentiamine (BTDS), sicotiamine (CCT), octotiamine (TATD), allithiamine, thiamine propyl disulfide, thiamine tetrahydrofurfuryl disulfide (TPFD), dicethiamine (DCET), bisbutiamine, bisibutiamine (DBT), thiamine monophosphate disulfide, thiamine pyrophosphate, sicotiamine, thiamine ethyl disulfide, thiamine propyl disulfide, etc. Examples of salts of thiamine or derivatives include thiamine hydrochloride, thiamine nitrate, bisthiamine nitrate, dicethiamine hydrochloride, fursultiamine hydrochloride, etc.

[0048] Further, for example, pyridoxine hydrochloride is an example of a salt of pyridoxine.

[0049] When vitamins are used in the tablets of the present invention, it is preferable to use water-soluble vitamins from the viewpoint of the balance between hardness, tableting properties, and disintegration properties, and among these, at least one selected from vitamin B is preferred, and at least one selected from vitamin B1 and vitamin B6 is particularly preferred.

[0050] When a vitamin is used in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting properties, and disintegrability, the amount thereof in the tablet is preferably 0.1% by mass or more, more preferably 0.2% by mass or more, even more preferably 0.4% by mass or more, even more preferably 0.6% by mass or more, particularly preferably 0.8% by mass or more, particularly preferably 1.0% by mass or more, and most preferably 1.2% by mass or more.

[0051] Furthermore, when a vitamin is used in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting ability, and disintegrability, the amount thereof in the tablet is preferably 3% by mass or less, more preferably 2.9% by mass or less, even more preferably 2.8% by mass or less, even more preferably 2.7% by mass or less, particularly preferably 2.6% by mass or less, and especially preferably 2.5% by mass or less.

[0052] From the viewpoint of the balance between tablet hardness, disintegrability, and tableting properties, the ratio of the mass of vitamin (E) to the mass of Garcinia (A) in the tablet of the present invention ((E) / (A)) is preferably 0.001 or more, more preferably 0.005 or more, more preferably 0.01 or more, and even more preferably 0.05 or more. Moreover, the ratio ((E) / (A)) is preferably 15 or less, more preferably 8 or less, more preferably 2 or less, and even more preferably 0.5 or less.

[0053] When vitamin B1 is used in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting properties, and disintegration properties, the amount thereof in the tablet is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.2% by mass or more, even more preferably 0.3% by mass or more, particularly preferably 0.4% by mass or more, particularly preferably 0.5% by mass or more, especially preferably 1.0% by mass or more, and most preferably 1.1% by mass or more.

[0054] When vitamin B1 is used in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting properties, and disintegration properties, the amount thereof in the tablet is preferably 3% by mass or less, more preferably 2.9% by mass or less, even more preferably 2.8% by mass or less, even more preferably 2.7% by mass or less, particularly preferably 2.6% by mass or less, and especially preferably 2.5% by mass or less.

[0055] When vitamin B6 is used in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting ability, and disintegrability, the amount thereof in the tablet is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.2% by mass or more, even more preferably 0.3% by mass or more, particularly preferably 0.4% by mass or more, and particularly preferably 0.5% by mass or more.

[0056] When vitamin B6 is used in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting ability, and disintegrability, the amount thereof in the tablet is preferably 3% by mass or less, more preferably 2.9% by mass or less, even more preferably 2.8% by mass or less, even more preferably 2.7% by mass or less, particularly preferably 2.6% by mass or less, and especially preferably 2.5% by mass or less.

[0057] When vitamins B1 and B6 are used in combination in the tablet of the present invention, from the viewpoint of the balance between hardness, tableting ability, and disintegration ability, the ratio of vitamins B1:B6 is preferably 100:0.01 or more, more preferably 100:0.1 or more, even more preferably 100:1 or more, particularly preferably 100:5 or more, and most preferably 100:10 or more. Furthermore, when vitamins B1 and B6 are used in combination, from the viewpoint of the balance between hardness and tableting ability, the ratio of vitamins B1:B6 is preferably 100:1000 or less, more preferably 100:200 or less, even more preferably 100:150 or less, even more preferably 100:90 or less, and most preferably 100:70 or less.

[0058] The tablet of the present invention may contain components other than (A) Garcinia cambogia, (B) excipients, (C) lubricants, (D) fluidizing agents, and (E) vitamins in an amount of 40% by mass or less, It may be 20% by mass or less, 10% by mass or less, or 5% by mass or less.

[0059] Dimensions, physical properties The tablet of the present invention preferably has a weight of 200 mg or more, more preferably 210 mg or more, per tablet, from the viewpoint of easily achieving a balance between ease of swallowing, hardness, and tableting. Also, the tablet of the present invention preferably has a weight per tablet of 500 mg or less, more preferably 400 mg or more, even more preferably 300 mg or less, and most preferably 280 mg or less, from the viewpoint of easily achieving a balance between ease of swallowing, hardness, and tableting.

[0060] The tablet of the present invention preferably has a tablet diameter of 5 mm or more, more preferably 5.5 mm or more, and most preferably 6 mm or more, from the viewpoint of easily achieving a balance between ease of swallowing, hardness, and tableting. From the same viewpoint, the diameter is preferably 12 mm or less, more preferably 11 mm or less, and particularly preferably 10 mm or less, from the viewpoint of easily achieving a balance between ease of swallowing, hardness, and tableting. Here, if the lock is not circular, the diameter of the lock is the area-equivalent diameter based on the projected area when the lock is projected vertically from above when placed so that the contact area with the horizontal surface is maximized. The tablet may be in the shape of a round tablet, an oval tablet, a flower-shaped tablet, or the like.

[0061] The tablet of the present invention preferably has a hardness of 6.7 kgf or more, more preferably 7.0 kgf or more, particularly preferably 7.5 kgf or more, and most preferably 8 kgf or more, in order to easily achieve a balance between hardness and tableting properties.

[0062] The tablet of the present invention preferably has a hardness of 15 kgf or less, more preferably 12 kgf or less, particularly preferably 10 kgf or less, and most preferably 9.5 kgf or less, in order to easily achieve a balance between hardness and tableting properties. The hardness can be measured by the method described in the Examples.

[0063] Furthermore, the disintegration time of the plain tablet of this embodiment, when using water as a solvent, is preferably within 60 minutes, more preferably within 40 minutes, even more preferably within 35 minutes, and particularly preferably within 30 minutes. The lower limit of the disintegration time is, for example, 1 minute or more, which facilitates tablet production. The disintegration time refers to the time it takes for a sample in a solvent to disintegrate. The procedure for measuring the disintegration time follows the method described in "Disintegration Test Method" in Item "6.09" of the General Test Methods of the Japanese Pharmacopoeia, 17th Edition. When using tablets with a diameter of 3 to 15 mm, a thickness of 4 to 7 mm, and a weight of 150 to 500 mg, it is preferable to use a disintegration tester manufactured by Toyama Sangyo Co., Ltd., Model No. NT-400.

[0064] <Measuring procedure for disintegration time> One tablet is placed in each of six glass tubes in a disintegration tester. Each glass tube is open at the top and bottom, and a stainless steel mesh with a mesh size of 1.8 mm to 2.2 mm is attached to the bottom of the glass tube. The glass tube containing the tablets is placed in water at 37±2°C, and the disintegration tester is started. The glass tube in the disintegration tester is observed, and when it is confirmed that the tablets are about to disintegrate, the glass tube is pulled out and the disintegration state of the tablets is observed. This process is repeated until the tablets are completely disintegrated. The time from when the disintegration tester is started to when all six tablets have disintegrated is measured, and this measured time is taken as the disintegration time. The tablets are considered to have disintegrated when no tablet residue is found in the glass tube, or if any is found, it is a soft substance that clearly does not retain its original shape.

[0065] ·Manufacturing method A preferred method for producing the tablet of this embodiment will be further described below. The tablet manufacturing method of this embodiment preferably includes a step of mixing raw material powder containing (A) Garcinia, (B) an excipient, and (C) a lubricant, and a step of tableting the resulting mixed powder. The preferred mass ratios and preferred components of (A) Garcinia, (B) excipient, and (C) lubricant in the raw material powder, as well as the excipient, disintegrant, and lubricant, are the same as those in the tablets described above.

[0066] The tablets may be core-coated or core-less. In the case of core-coated tablets, raw powder containing any core is compressed into tablets.

[0067] The raw material powder may be a mixture of (A) Garcinia, (B) an excipient, (C) a lubricant, and other powdered ingredients that are included as needed, or it may be a granulated powder obtained by granulating a mixture of a powdered gelling agent, a powdered specific excipient, and other powdered ingredients that are included as needed. As the granulation method, any known granulation method used in producing oral tablets by granulation tableting can be used without any particular limitation.

[0068] The tablet of the present invention may be a chewable tablet, i.e., a tablet to be chewed in the mouth; a swallowable tablet, i.e., a tablet to be swallowed by simply pouring it down with water or the like; a gargle tablet; or a tablet to be licked in the mouth and gradually dissolved, specifically a troche tablet. From the viewpoint of excellent hardness, it is particularly preferable that the tablet of the present invention be used for swallowing. The tablet of this embodiment is for oral administration, i.e., taken internally. The tablet of this embodiment can be used as a food composition or a pharmaceutical composition (such as a drug or quasi-drug), and can be used as a supplement, health food, nutrient-functional food, functional food, food with specified health uses, and drug.

[0069] Preferred embodiments of the present invention Preferred embodiments of the present invention include, for example, the following. [1] A tablet containing (A) Garcinia cambogia, (B) an excipient, and (C) a lubricant. [2] (A) The tablet described in [1], wherein the Garcinia is Garcinia indica. [3] (B) The tablet according to [1] or [2], wherein the excipient comprises one or more selected from cellulose, reduced maltose, and hydroxypropyl cellulose. [4] (A) The tablet according to any one of [1] to [3], wherein the content of Garcinia is 1 to 40% by mass. [5] The tablet according to any one of [1] to [4], wherein the content of the excipient (B) is 10 to 80% by mass. [6] (C) The tablet according to any one of [1] to [5], wherein the lubricant contains calcium stearate. [7] The tablet according to any one of [1] to [6], wherein the content of (C) lubricant is 0.1 to 3% by mass. [8] The tablet according to any one of [1] to [7], further comprising (D) a fluidizing agent. [9] (D) The tablet according to [8], wherein the glidant comprises silicon dioxide.

[10] The tablet according to any one of [8] to [9], wherein the content of the fluidizing agent (D) is 0.1 to 3% by mass.

[11] The tablet according to any one of [1] to

[10] , further comprising (E) a vitamin.

[12] The tablet according to

[11] , wherein (E) vitamin includes either vitamin B1 or vitamin B6.

[13] The tablet according to any one of [1] to

[12] , wherein the content of vitamin (E) is 0.1 to 3% by mass.

[14] The tablet according to any one of [1] to

[13] , wherein the weight of each tablet is 200 to 500 mg.

[15] The tablet according to claim 1, wherein the tablet has a hardness of 6.7 to 12 kgf.

[16] The tablet according to claim 1, having a disintegration time of 60 minutes or less.

[17] The tablet according to claim 1, which has a disintegration time of 60 minutes or less according to the general test method / disintegration test method of the 17th edition of the Japanese Pharmacopoeia. [Example]

[0070] The present invention will be described in more detail below with reference to examples, but the scope of the present invention is not limited to these examples.

[0071] [Preparation of Garcinia indica extract] The seeds were removed from the fruit of Garcinia indica (pulp and peel), which were then dried and extracted with ethanol at 70°C or higher for over 6 hours. The resulting extract was filtered and concentrated to remove impurities. The concentrated extract was then processed into powder to obtain powdered Garcinia indica extract.

[0072] [Preparation of Garcinia Cambogia Extract] The seeds were removed from the fruit of Garcinia cambogia (pulp and skin), which were then dried and extracted with ethanol at 70°C or higher for over 6 hours. The resulting extract was filtered and concentrated to remove impurities. The concentrated extract was then processed into powder to obtain powdered Garcinia cambogia extract.

[0073] Other commercially available products were used as ingredients listed in Table 1. Crystalline cellulose was used as the cellulose. Fine silicon dioxide was used as the silicon dioxide. Thiamine hydrochloride was used as the vitamin B1. Pyridoxine hydrochloride was used as the vitamin B6.

[0074] (Test 1: Evaluation of hardness and punch release) (Comparative Example 1, Examples 1 to 13)

[0075] [Creating tablets] Mixed powders were obtained according to the formulations of the Comparative Examples and Examples shown in Tables 1 and 2. The obtained mixed powders were made into tablets (tablets for swallowing) weighing 250 mg each and having a diameter of 8 mm using a single punch tableting machine. The punching pressure was 3 kN.

[0076] <Hardness measurement> The hardness of the tablets obtained in the comparative examples and examples was measured using a hardness tester (Portable Checker PC-30 manufactured by Okada Seiko Co., Ltd.) and the average value of measurements of three tablets randomly selected for each example is shown in Tables 1 and 2.

[0077] <Evaluation of punch release (tablet compression)> The tablets obtained in the Comparative Examples and Examples were evaluated for punch release according to the following criteria. The results are shown in Tables 1 and 2.

[0078] (Evaluation criteria for punch release) ◯: After tableting, the compressed particles separate from the punch tip and there is no slight clouding of the punch. △: After tableting, the compressed granules separate from the punch tip, but there is slight clouding of the punch. ×: After tableting, the compressed granules adhere to the tip of the punch and do not fall off.

[0079] [Table 1] [Table 2]

[0080] As shown in Tables 1 and 2, each Example achieved both good hardness and tabletability.

[0081] (Evaluation of disintegration time and punch separation) (Examples 14 to 18) Mixed powders were obtained according to the formulations of the Comparative Examples and Examples shown in Table 3. The obtained mixed powders were made into tablets (tablets for swallowing) weighing 250 mg each and having a tablet diameter of 8 mm using a single punch tablet press. The punching pressure was 5 kN.

[0082] <Measurement of disintegration time> The disintegration time was measured using a disintegration tester (Toyama Sangyo Co., Ltd., model number: NT-40H) according to the method described in "Disintegration Test Method" in Section "6.09" of the Seventeenth Edition of the Japanese Pharmacopoeia, n=6. Water was used as the solution. The results are shown in Table 3.

[0083] <Evaluation of punch release> The results were evaluated according to the same criteria as above, and are shown in Table 3.

[0084] [Table 3]

[0085] As shown in Table 3, among the Garcinia species, Garcinia indica was preferable in terms of tablet disintegration. It was also found that the inclusion of vitamins improved disintegration.

[0086] (Test 2: Tablet production) (Examples 19 to 29)

[0087] [Creating tablets] Mixed powders were obtained using the formulations of the Comparative Examples and Examples shown in Tables 4 and 5. The obtained mixed powders were used in a single punch tablet press to produce tablets (tablets for swallowing) each weighing 250 mg and having a tablet diameter of 8 mm. The compression force was 3 kN. All of the obtained tablets were excellent in terms of compressibility and hardness. Among them, tablets in which the proportion of reduced maltose in the sugars was 50 mass % or more and tablets in which the weight ratio of vitamin B1 to vitamin B6 was 100:10-90 were particularly excellent in terms of compressibility and hardness.

[0088] [Table 4] [Table 5] [Industrial Applicability]

[0089] The tablets of the present invention contain Garcinia cambogia, which has excellent health and beauty benefits, and have both good hardness and tableting properties, making them highly industrially applicable.

Claims

1. A tablet comprising (A) Garcinia cambogia, (B) an excipient, and (C) a lubricant.

2. 2. The tablet of claim 1, wherein (A) Garcinia is Garcinia indica.

3. The tablet according to claim 1, wherein the excipient (B) comprises one or more selected from cellulose, reduced maltose, and hydroxypropyl cellulose.

Citation Information

Patent Citations

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