Oral composition
A charcoal-based oral composition with specific blending ratios of charcoal, fluidizing agent, and lubricant addresses moldability issues, providing a solid form with enhanced hardness and abrasion resistance for improved ingestion.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- TOYO SHINYAKU KK
- Filing Date
- 2020-01-24
- Publication Date
- 2026-05-15
AI Technical Summary
Compositions containing charcoal have poor moldability, particularly when the charcoal content is high, making it difficult to form solid compositions such as tablets.
An oral composition containing charcoal, a fluidizing agent, and a lubricant, with specific blending ratios of each component, to enhance hardness and abrasion resistance.
The composition achieves a solid oral composition with excellent hardness and reduced abrasion, facilitating ease of ingestion and effective utilization of charcoal.
Smart Images

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Abstract
Description
Technical Field
[0001] The present invention relates to an oral composition containing charcoal.
[0002] Charcoal is a porous substance composed of carbon, oxygen, hydrogen, calcium, etc., with the majority being carbon, and it has the property of adsorbing various substances in its fine pores.
[0003] Charcoal is industrially used as a decolorizing agent (Patent Document 1) that adsorbs coloring components and a deodorizing agent (Patent Document 2) that adsorbs odor substances, and is also used as an aid for filtration and purification. In recent years, supplements utilizing the effects of charcoal have attracted attention.
Prior Art Documents
Patent Documents
[0004]
Patent Document 1
Patent Document 2
Disclosure of the Invention
Problems to be Solved by the Invention
[0005] However, compositions containing charcoal have poor moldability, and particularly when the charcoal content is high, there is a problem that it is difficult to form solid compositions such as tablets.
[0006] An object of the present invention is to provide an oral composition in which the hardness and abrasion degree of a composition containing charcoal are improved and which is easy to ingest, for the purpose of effectively utilizing charcoal.
Means for Solving the Problems
[0007] As a result of diligent research, the inventors discovered that a solid oral composition with excellent hardness and abrasion resistance properties can be obtained using an oral composition containing charcoal, a fluidizing agent, and a lubricant, leading to the present invention. In particular, they discovered that a tablet-type oral composition with even better hardness and abrasion resistance can be obtained by using specific blending ratios of charcoal and fluidizing agent, specific blending ratios of fluidizing agent in the oral composition, and specific blending ratios of charcoal and lubricant, leading to the present invention.
[0008] The outline of this invention is as follows: [1] An oral composition characterized by containing (A) charcoal and (B) a fluidizing agent. [2] The oral composition according to [1], characterized in that the content of (B) is 5% by mass or more relative to the total amount of (A) and (B). An oral composition according to any one of [1] to [2], characterized in that the content of [3](B) is 10% by mass or less. [4] An oral composition characterized by containing (A) charcoal and (C) a lubricant, wherein the content of (C) is 70% by mass or less of the total amount of (A) and (C). [5] An oral composition characterized by containing (A) charcoal, (B) a fluidizing agent, and (C) a lubricant. [6] A solid oral composition characterized by containing (A) charcoal, (B) a fluidizing agent, and (C) a lubricant, and having a hardness of 2 kgf or more. [7] A solid oral composition characterized by containing (A) charcoal, (B) a fluidizing agent, and (C) a lubricant, and having a degree of abrasion of 3% or less at 300 revolutions. An oral composition according to any one of [1] to [7], characterized in that [8](A) is activated carbon. [9](A) is of plant origin, as described in any of [1] to [8]. [Effects of the Invention]
[0009] According to the present invention, a solid oral composition having excellent hardness and abrasion resistance can be provided. In particular, by using specific proportions of charcoal and fluidizer, using specific proportions of fluidizer in the oral composition, and using specific proportions of charcoal and lubricant, a solid oral composition with even better hardness can be provided. [Modes for carrying out the invention]
[0010] The oral compositions of the present invention will be described below. However, the present invention is not limited to the embodiments described below.
[0011] (A) charcoal Charcoal is produced by processing plants, organic compounds, and synthetic resins under high-temperature conditions, and is mainly used as fuel and as an aid in filtration and purification. There are no particular restrictions on the raw materials for charcoal that can be used in this invention as long as they are orally ingestible. Examples include woods such as Ubame oak, sawtooth oak, chestnut, larch, Japanese red pine, and cedar, which are used in Binchotan charcoal, as well as bamboo, coconut shells, walnut shells, and rice husks. Furthermore, it is preferable to use activated carbon obtained by dry distillation of the raw materials and further activating them through high-temperature treatment. There are no particular restrictions on the activated carbon as long as its adsorption capacity is activated, but for example, in the case of commercially available products, those that are labeled as activated carbon in the raw material specifications are preferred. There are no particular restrictions on the shape of the charcoal that can be used in this invention as long as it is suitable for consumption, but examples include powder, granules, fibers, and formed charcoal, with powder and granules being preferred. The raw materials for the charcoal of the present invention are preferably bamboo, Japanese red pine, coconut shell, and rice husk, with bamboo, coconut shell, and rice husk being particularly preferred. In particular, when the oral composition of the present invention is in tablet or chewable form, it is most preferable to use activated charcoal derived from coconut shell, as it exhibits hardness improvement and abrasion reduction effects when combined with certain other materials.
[0012] The content of (A) charcoal in the oral composition of the present invention is not particularly limited, but is preferably 0.0001 to 75% by mass, more preferably 0.001 to 50% by mass, and even more preferably 0.01 to 30% by mass.
[0013] (B) Fluidizing agent A fluidizer is used to improve the fluidity of mixed powders or granules. The fluidizer that can be used in this invention is not particularly limited as long as it is capable of achieving the above objective. Examples include talc, silicon dioxide (light anhydrous silicic acid, hydrated silicon dioxide), hydrophilic silica, hydrophobic silica, calcium silicate, alkyl phosphate (PAP), anhydrous calcium hydrogen phosphate, magnesium oxide, titanium dioxide, magnesium silicate, and calcium silicate. These may be used individually or in combination of two or more. Commercially available fluidizers can be used. In this invention, silicon dioxide, magnesium oxide, titanium dioxide, magnesium silicate, and calcium silicate are preferred because they yield an excellent solid oral composition, with silicon dioxide, magnesium oxide, and titanium dioxide being more preferred. Silicon dioxide is most preferred because it yields an oral composition with excellent hardness improvement and abrasion reduction effects.
[0014] The content of (B) fluidizer in the oral composition of the present invention is not particularly limited, but is preferably 30% by mass or less, more preferably 10% by mass or less, and even more preferably 5% by mass or less. Furthermore, it is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, and particularly preferably 0.01% by mass or more. By using the above blending ratio, an oral composition with high hardness and reduced abrasion can be obtained.
[0015] (C) Lubricant A lubricant is used to reduce friction between the tablet press die and the tablet when compressing powder for tablets, thereby preventing tableting defects such as sticking. The lubricant that can be used in this invention is not particularly limited as long as it is capable of achieving the above objective. Examples include stearic acid, calcium stearate, magnesium stearate, or other stearic acid or its salts, sodium stearyl fumarate, polyethylene glycol, fatty acid esters such as sucrose fatty acid esters, vegetable oils, and hydrogenated oils. These may be used individually or in combination of two or more. Commercially available lubricants can be used. In this invention, stearic acid or its salts, fatty acid esters, and hydrogenated rapeseed oil are preferred, and calcium stearate, magnesium stearate, and sucrose fatty acid esters are more preferred because they yield oral compositions with excellent hardness and abrasion resistance.
[0016] The content of (C) lubricant in the oral composition of the present invention is not particularly limited, but is preferably 0.01 to 30% by mass, more preferably 0.1 to 10% by mass, and even more preferably 1 to 5% by mass. By using the above blending ratio, an oral composition with high hardness and reduced abrasion can be obtained.
[0017] In the present invention, the content of (A) charcoal is preferably 0.1% by mass or more, more preferably 1% by mass or more, relative to the total amount of (A) charcoal and (B) fluidizer. Furthermore, it is preferably 99% by mass or less, and more preferably 70% by mass or less. Similarly, the content of (A) charcoal is preferably 1% by mass or more, more preferably 10% by mass or more, relative to the total amount of (A) charcoal and (C) lubricant. Furthermore, it is preferably 99% by mass or less, and more preferably 95% by mass or less. Moreover, the content of (A) charcoal is preferably 10% by mass or more, more preferably 20% by mass or more, and particularly preferably 30% by mass or more, relative to the total amount of (A) charcoal, (B) fluidizer and (C) lubricant. Furthermore, it is preferably 99% by mass or less, more preferably 95% by mass or less, and particularly preferably 90% by mass or less. By using the above blending ratios, an oral composition with high hardness and reduced abrasion can be obtained.
[0018] In the present invention, the content of the (B) fluidizing agent is preferably 0.1% by mass or more, more preferably 1% by mass or more, and particularly preferably 5% by mass or more, based on the total amount of the (A) charcoal and the (B) fluidizing agent. Also, it is preferably 50% by mass or less, more preferably 30% by mass or less. Similarly, the content of the (B) fluidizing agent is preferably 0.1% by mass or more, more preferably 1% by mass or more, based on the total amount of the (A) charcoal, the (B) fluidizing agent, and the (C) lubricant. Also, it is preferably 30% by mass or less, more preferably 20% by mass or less. By setting the above mixing ratio, an oral composition with high hardness and reduced abrasion can be obtained.
[0019] In the present invention, the content of the (C) lubricant is preferably 5% by mass or more, more preferably 10% by mass or more, based on the total amount of the (A) charcoal and the (C) lubricant. Also, it is preferably 90% by mass or less, more preferably 70% by mass or less. Similarly, the content of the (C) lubricant is preferably 1% by mass or more, more preferably 3% by mass or more, based on the total amount of the (A) charcoal, the (B) fluidizing agent, and the (C) lubricant. Also, it is preferably 60% by mass or less, more preferably 40% by mass or less. By setting the above mixing ratio, an oral composition with high hardness and reduced abrasion can be obtained.
[0020] In the present invention, in addition to the (A) charcoal, the (B) fluidizing agent, and the (C) lubricant, components that can be used in oral compositions can be used. For example, components derived from animals and plants, excipients, binders, disintegrants, various carriers, stabilizers, surfactants, plasticizers, solubilizers, reducing agents, buffers, sweeteners, bases, adsorbents, flavor correctors, antioxidants, brightening agents, coating agents, drug coatings, wetting agents, wetting regulators, fillers, cooling agents, coloring agents, flavoring agents, fragrances, sugar coating agents, isotonic agents, softening agents, emulsifiers, thickening agents, thickeners, foaming agents, pH adjusters, diluents, dispersants, disintegration aids, disintegration extenders, fragrances, moisture-proof agents, preservatives, storage agents, solvents, solubilization aids, solvents, antistatic agents, moisturizing agents, humidifying agents, etc. can be mentioned.
[0021] Examples of the oral composition of the present invention include powder, solid form (tablet, granule, fine granule, chewable, granular, rod, plate, block, round, caplet, stick), and capsule form such as soft capsules and hard capsules. Among these, powder or solid form is preferred, and powder, tablet, granule, fine granule, and chewable form are more preferred.
[0022] When the oral composition of the present invention is in solid form, its hardness is preferably 0.5 kgf or more, more preferably 1 kgf or more, and particularly preferably 2 kgf or more, from the viewpoint of ease of ingestion. Furthermore, it is preferably 30 kgf or less, more preferably 25 kgf or less, and particularly preferably 20 kgf or less. Hardness can be measured, for example, according to the method described in the Japanese Pharmacopoeia.
[0023] Furthermore, when the oral composition of the present invention is in solid form, the degree of abrasion is preferably 10% or less, more preferably 8% or less, particularly preferably 5% or less, and especially preferably 3% or less, from the viewpoint of ease of ingestion. The degree of abrasion refers to the degree of chipping, cracking, and abrasion that occurs in the solid oral composition, and the degree of abrasion can be measured, for example, in accordance with the method described in the Japanese Pharmacopoeia.
[0024] Furthermore, when the oral composition of the present invention is in solid form, the disintegration time is preferably 400 seconds or less, more preferably 300 seconds or less, and particularly preferably 250 seconds or less. The disintegration time can be measured, for example, according to the method described in the Japanese Pharmacopoeia.
[0025] The oral composition of the present invention is preferable to have a hardness of 2 kgf or more and an abrasion degree of 3% or less, as this is expected to result in excellent moldability and the early manifestation of its effects after ingestion.
[0026] The oral composition of the present invention is preferably used as a food, particularly as a food for specified health uses, a food with nutritional function claims, a food with functional claims, or a health food. [Examples]
[0027] The following are examples of the present invention, but the present invention is not limited thereto.
[0028] Manufacturing of charcoal-containing compositions (1) The raw materials were mixed in the proportions shown in Table 1 to produce 250 mg tablets. The compression pressure was 3.0 kN, and the tablet thickness was 5.8 mm.
[0029] [Table 1]
[0030] Tablet evaluation The physical properties of the obtained tablets were evaluated. Hardness was evaluated using a tablet hardness tester (manufactured by Okada Seikou Co., Ltd.). For abrasion resistance, the mass of the tablet to be measured (initial mass) was measured using an electronic balance, and the weighed tablet was placed in a tablet abrasion resistance tester and rotated at 300 revolutions per minute. After the test, the tablet was removed from the tester, any powder adhering to the tablet was lightly wiped off, and the mass was measured again (mass after test). The mass percentage of the mass reduction relative to the initial mass was calculated. The results are shown in Table 2.
[0031] [Table 2]
[0032] Table 2 shows that Comparative Example 1, which did not contain a fluidizing agent and a lubricant, could not be molded into a tablet. On the other hand, the composition of the present invention, which contains a fluidizing agent and a lubricant, could be molded into a tablet and had a hardness of 3 kgf or more. Furthermore, the abrasion rate was very low, less than 1.1%, indicating that excellent tablets that are resistant to chipping and breakage were obtained.
[0033] Manufacturing of charcoal-containing compositions (2) The raw materials were mixed in the proportions shown in Table 3 to produce 250 mg tablets. The pressure applied during tableting was 3.0 kN.
[0034] [Table 3]
[0035] The disintegration time of the obtained tablets was measured. The disintegration time was measured according to the method described in the Japanese Pharmacopoeia. All tablets had a disintegration time of 180 seconds or less, indicating excellent disintegration properties.
[0036] [Preparation of the oral composition of the present invention] (Tablet manufacturing) Tablets (300 mg) with the composition shown in Table 4 below were prepared. The resulting tablets were an oral composition with excellent hardness and abrasion resistance.
[0037] [Table 4]
[0038] Tablets (300 mg) with the composition shown in Table 5 below were prepared. The resulting tablets were an oral composition with excellent hardness and abrasion resistance.
[0039] [Table 5] [Industrial applicability]
[0040] According to the present invention, in an oral composition containing charcoal and a fluidizing agent, by adjusting the ratio of the amount of lubricant to the amount of charcoal and lubricant, an oral composition with increased hardness and reduced abrasion can be provided. Furthermore, according to the present invention, in an oral composition containing charcoal and at least one selected from a fluidizing agent and a lubricant, an oral composition with increased hardness and reduced abrasion can be provided. In particular, by setting the proportions of charcoal and fluidizing agent to specific proportions, setting the proportion of fluidizing agent in the oral composition to specific proportions, and setting the proportions of charcoal and lubricant to specific proportions, an oral composition with even better hardness and abrasion can be provided.
Claims
[Claim 1] A solid oral composition characterized by containing (A) charcoal, (B) a fluidizing agent, and (C) a lubricant, having a hardness of 2 kgf or more and an abrasion degree of 3% or less, (C) The amount of lubricant is 45.5% by mass or more of the total amount of (A) charcoal and (C) lubricant, or (C) The amount of lubricant is 40% by mass or more of the total amount of (A) charcoal, (B) fluidizer and (C) lubricant in the solid oral composition (excluding the tablets described in (1) to (5) below). (1) Tablets containing activated carbon (derived from bamboo), crystalline cellulose, calcium stearate, hydroxypropyl cellulose, silicon dioxide, reduced maltose, and at least one other material selected from the group consisting of calcium 3-hydroxy-3-methylbutyrate, creatine hydrate, L-isoleucine, collagen peptide, and soy protein. (2) Tablets consisting of the following ingredients Charcoal powder (activated charcoal made from rice husks) 10% HMBCa 50% Creatine monohydrate 1% Collagen peptide 0.01% Black garlic powder 3% Lactic acid bacteria 0.1% Calcium stearate 2% Silicon dioxide 2% Crystalline cellulose 10% Reduced maltose remainder (3) Tablets consisting of the following ingredients Charcoal powder (derived from Japanese red pine) 3% Blackcurrant extract powder 0.1% Korean ginseng juice powder 0.01% Barley grass powder 1% Reduced maltose 35% Calcium stearate 2% Silicon dioxide 1% Cellulose 57.89% (4) Tablets consisting of the following ingredients Medicinal charcoal 100 mg Safflower oil 50 mg Hydroxypropylcellulose 10 Crystalline cellulose 5 mg Sennoside 133 mg Aloe vera powder 200 mg Japanese Red Maple Extract 625 mg Rhubarb extract 200 mg Gen'oshoko extract 150 mg Light anhydrous silicic acid 77 mg Carmellose calcium 70 mg Lactose hydrate 30mg Magnesium stearate 5 mg (5) Tablets consisting of the following ingredients Medicinal charcoal 2000 mg Safflower oil 1000 mg Hydroxypropylcellulose 100 mg Crystalline cellulose 100 mg Methacrylic acid copolymer L 500 mg Sodium bicosulfate 10 mg Light anhydrous silicic acid 650 mg Carmellose calcium 720 mg Lactose hydrate 300mg Magnesium stearate 20 mg.