Oral composition

A solid oral composition with charcoal, a fluidizing agent, and a lubricant, using specific blending ratios, addresses the moldability issues of charcoal compositions, resulting in tablets with high hardness and low friability for easy ingestion.

JP2024170645AInactive Publication Date: 2024-12-10TOYO SHINYAKU KK
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Patent Information

Application Number
JP2024159895
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2019-01-25
Filing Date
2024-09-17
Publication Date
2024-12-10
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Compositions containing charcoal have poor moldability, particularly when the charcoal content is high, making it difficult to form solid compositions such as tablets.

Method used

A solid oral composition containing charcoal, a fluidizing agent, and a lubricant, with specific blending ratios of charcoal and superplasticizer, achieves improved hardness and friability.

Benefits of technology

The composition provides a tablet-shaped oral composition with high hardness and low friability, ensuring ease of ingestion and effective utilization of charcoal.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide an oral composition in which the hardness and wear of a charcoal-containing composition are improved and it is easy to take, for effective use of charcoal.SOLUTION: An oral composition contains (A) charcoal and (B) a fluidization agent.SELECTED DRAWING: None
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Description

[Technical field]

[0001] The present invention relates to oral compositions containing charcoal.

[0002] Charcoal is a porous substance composed mostly of carbon, but also of oxygen, hydrogen, calcium, etc., and has the ability to adsorb a variety of substances into its tiny holes.

[0003] Charcoal is used industrially as a decolorizing agent by adsorbing coloring components (Patent Document 1), as a deodorizing agent by adsorbing odorous substances (Patent Document 2), and as an auxiliary agent for filtration and purification. In recent years, supplements that utilize the effects of charcoal have been attracting attention. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Publication No. 6-65591 [Patent Document 2] JP 2013-81649 A DISCLOSURE OF THEINVENTION [Problem to be solved by the invention]

[0005] However, compositions containing charcoal have poor moldability, and there has been a problem that it is difficult to mold the composition into a solid form such as a tablet, particularly when the charcoal content is high.

[0006] An object of the present invention is to provide an oral composition which contains charcoal and has improved hardness and friability, and which is easy to ingest, with the aim of making effective use of charcoal. [Means for solving the problem]

[0007] As a result of intensive research, the present inventors have found that a solid oral composition containing charcoal, a fluidizing agent, and a lubricant can be obtained that has excellent hardness and friability characteristics, and have arrived at the present invention. In particular, the present inventors have found that a tablet-shaped oral composition having even better hardness and friability can be obtained by using a specific blend ratio of charcoal and a fluidizing agent, a specific blend ratio of the fluidizing agent in the oral composition, and a specific blend ratio of charcoal and a lubricant, and have arrived at the present invention.

[0008] The outline of the present invention is as follows. [1] An oral composition comprising (A) charcoal and (B) a fluidizing agent. [2] The oral composition according to [1], wherein the content of (B) is 5% by mass or more based on the total amount of (A) and (B). [3] The oral composition according to any one of [1] to [2], wherein the content of (B) is 10% by mass or less. [4] (A) charcoal; and (C) a lubricant; An oral composition, characterized in that the content of (C) is 70% by mass or less based on the total amount of (A) and (C). [5] An oral composition comprising (A) charcoal, (B) a flow agent, and (C) a lubricant. [6] A solid oral composition comprising (A) charcoal, (B) a flow agent, and (C) a lubricant, and having a hardness of 2kgf or more. [7] A solid oral composition comprising (A) charcoal, (B) a flow agent, and (C) a lubricant, the composition having a friability of 3% or less at 300 revolutions. [8] The oral composition according to any one of [1] to [7], wherein (A) is activated carbon. [9] The oral composition according to any one of [1] to [8], wherein (A) is derived from a plant. Effect of the Invention

[0009] According to the present invention, a solid oral composition having excellent hardness and friability can be provided. In particular, by using a specific blend ratio of charcoal and a fluidizing agent, a specific blend ratio of the fluidizing agent in the oral composition, and a specific blend ratio of charcoal and a lubricant, a solid oral composition having even better hardness can be provided. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0010] The oral composition of the present invention will be described below. Note that the present invention is not limited to the following embodiments.

[0011] (A) Charcoal Charcoal is a material obtained by treating plants, organic compounds, and synthetic resins under high temperature conditions, and is mainly used as fuel or as an auxiliary for filtration and purification. The raw material for charcoal that can be used in the present invention is not particularly limited as long as it can be orally ingested, and examples of such raw materials include ubamegashi, sawtooth oak, chestnut, larch, red pine, and cedar, which are used in binchotan charcoal, as well as bamboo, coconut shells, walnut shells, and rice husks. In addition, it is preferable to use activated charcoal obtained by dry distilling the raw material and further activating it by high-temperature treatment. There is no particular limit to the activated charcoal as long as its adsorption ability is activated, but for example, in the case of a commercially available product, there is a product that has the term "activated charcoal" written on the raw material specification. The shape of the charcoal that can be used in the present invention is not particularly limited as long as it is suitable for consumption, and examples of such shapes include powder, granule, fiber, and formed charcoal, and powder and granule shapes are preferable. As the raw material for the charcoal of the present invention, bamboo, red pine, coconut shell, and rice husk are preferably used, and bamboo, coconut shell, and rice husk are particularly preferred. In particular, when the oral composition of the present invention is in the form of a tablet or chewable tablet, it is most preferred to use activated carbon derived from coconut shell, since it exerts the effect of improving hardness and reducing abrasion when combined with other specific 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 mass %, more preferably 0.001 to 50 mass %, and even more preferably 0.01 to 30 mass %.

[0013] (B) Superplasticizer A fluidizing agent is used for the purpose of improving the fluidity of mixed powders or granules. The fluidizing agent that can be used in the present invention is not particularly limited as long as it is a component that can achieve the above-mentioned purpose, and examples thereof include talc, silicon dioxide (light anhydrous silicic acid, hydrous silicon dioxide), hydrophilic silica, hydrophobic silica, calcium silicate, alkyl phosphate (PAP), anhydrous calcium hydrogen phosphate, magnesium oxide, titanium oxide, magnesium silicate, calcium silicate, etc. These may be used alone or in combination of two or more. Commercially available fluidizing agents can be used. In the present invention, silicon dioxide, magnesium oxide, titanium oxide, magnesium silicate, and calcium silicate are preferred because an excellent solid oral composition can be obtained, silicon dioxide, magnesium oxide, and titanium oxide are more preferred, and silicon dioxide is most preferred because an oral composition that is particularly excellent in the effect of improving hardness and the effect of reducing abrasion can be obtained.

[0014] The content of the (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. Also, 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 having high hardness and low friability can be obtained.

[0015] (C) Lubricant A lubricant is used to reduce friction between the punch and die of a tablet press and the tablet when compressing powder for tablets, and to prevent tableting problems such as sticking. The lubricant that can be used in the present invention is not particularly limited as long as it is a component that can achieve the above-mentioned purpose, and examples thereof include stearic acid or its salts such as stearic acid, calcium stearate, and magnesium stearate, sodium stearyl fumarate, polyethylene glycol, fatty acid esters such as sucrose fatty acid esters, vegetable oils and fats, and hardened oils. These may be used alone or in combination of two or more. Commercially available products can be used as the lubricant. In the present invention, stearic acid or its salts, fatty acid esters, and rapeseed hardened oil are preferred, and calcium stearate, magnesium stearate, and sucrose fatty acid esters are more preferred because they can provide oral compositions with excellent hardness and friability.

[0016] The content of the lubricant (C) 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 having high hardness and low friability 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, based on the total amount of (A) charcoal and (B) fluidizing agent. Also, 99% by mass or less is preferable, and 70% by mass or less is more preferable. Similarly, the content of (A) charcoal is preferably 1% by mass or more, more preferably 10% by mass or more, based on the total amount of (A) charcoal and (C) lubricant. Also, 99% by mass or less is preferable, and 95% by mass or less is more preferable. Furthermore, 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, based on the total amount of (A) charcoal, (B) fluidizing agent, and (C) lubricant. Also, 99% by mass or less is preferable, and 95% by mass or less is more preferable, and 90% by mass or less is particularly preferable. By using the above blending ratio, an oral composition having high hardness and reduced friability 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, and 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, and more preferably 20% by mass or less. By using the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

[0019] In the present invention, the content of the lubricant (C) is preferably 5% by mass or more, more preferably 10% by mass or more, based on the total amount of the charcoal (A) and the lubricant (C). Also, it is preferably 90% by mass or less, more preferably 70% by mass or less. Similarly, the content of the lubricant (C) is preferably 1% by mass or more, more preferably 3% by mass or more, based on the total amount of the charcoal (A), the flow agent (B) and the lubricant (C). Also, it is preferably 60% by mass or less, more preferably 40% by mass or less. By using the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

[0020] In the present invention, in addition to (A) charcoal, (B) fluidizing agent, and (C) lubricant, ingredients that can be used in oral compositions can be used, such as animal and plant-derived ingredients, excipients, binders, disintegrants, various carriers, stabilizers, surfactants, plasticizers, solubilizers, reducing agents, buffers, sweeteners, bases, adsorbents, flavorings, antioxidants, glossing agents, coating agents, shells, wetting agents, wetting regulators, fillers, refreshing agents, colorants, flavorings, flavorings, sugar coating agents, isotonicity agents, softeners, emulsifiers, thickening agents, thickening agents, foaming agents, pH regulators, diluents, dispersants, disintegration aids, disintegration extension agents, fragrances, moisture-proofing agents, preservatives, preservatives, solubilizers, solubilization aids, solvents, antistatic agents, moisturizing agents, wetting agents, etc.

[0021] Examples of the form of the oral composition of the present invention include powder, solid (tablet, granule, fine granule, chewable, granular, rod, plate, block, round, caplet, stick), capsule such as soft capsule, hard capsule, etc. Among these, powder or solid is preferred, and powder, tablet, granule, fine granule, chewable form is more preferred.

[0022] When the oral composition of the present invention is in a solid form, the 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. Also, it is preferably 30 kgf or less, more preferably 25 kgf or less, and particularly preferably 20 kgf or less. The hardness can be measured, for example, according to the method described in the Japanese Pharmacopoeia.

[0023] When the oral composition of the present invention is in a solid form, the friability 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 friability refers to the degree of chipping, cracking, and scraping in a solid oral composition, and the friability can be measured, for example, according to the method described in the Japanese Pharmacopoeia.

[0024] When the oral composition of the present invention is in a 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 preferably has a hardness of 2 kgf or more and a friability of 3% or less, which is expected to provide excellent moldability and to quickly exert 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 nutrient function claims, a food with functional claims, or a health food. EXAMPLES

[0027] Examples of the present invention will be described below, but the present invention is not limited thereto.

[0028] Preparation of charcoal-containing composition (1) The raw materials were mixed in the proportions shown in Table 1 to produce 250 mg tablets. The tableting pressure was 3.0 kN, and the thickness of the tablets was 5.8 mm.

[0029] [Table 1]

[0030] Tablet evaluation The obtained tablets were evaluated for each physical property. Hardness was evaluated using a tablet hardness tester (Okada Seiko Co., Ltd.). Friability was evaluated by measuring the mass (initial mass) of the tablet to be measured using an electronic balance, and the measured tablet was placed in a tablet friability tester and rotated 300 times. After the test was completed, the tablet was removed from the tester, the powder adhering to the tablet was lightly wiped off, and the mass was measured (mass after test), and the mass percentage of the reduced mass relative to the initial mass was calculated. The results are shown in Table 2.

[0031] [Table 2]

[0032] From Table 2, Comparative Example 1, which does not contain a flow agent and a lubricant, could not be molded into a tablet. On the other hand, the composition of the present invention, which contains a flow agent and a lubricant, could be molded into a tablet composition and had a hardness of 3 kgf or more. In addition, the friability was very low at less than 1.1%, so it was found that excellent tablets that were not easily chipped or broken were obtained.

[0033] Preparation of charcoal-containing composition (2) The raw materials were mixed in the proportions shown in Table 3 to produce 250 mg tablets. The tableting pressure was 3.0 kN.

[0034] [Table 3]

[0035] The disintegration time of the obtained tablets was measured according to the method described in the Japanese Pharmacopoeia. The disintegration time was 180 seconds or less in all cases, indicating excellent disintegrability.

[0036] [Preparation of oral composition of the present invention] (Tablet manufacturing) Tablets (300 mg) having the composition shown in Table 4 below were produced. The obtained tablets were oral compositions excellent in hardness and friability.

[0037] [Table 4]

[0038] Tablets (300 mg) were produced having the composition shown in Table 5 below. The obtained tablets were oral compositions excellent in hardness and friability.

[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 the lubricant to the amount of the charcoal and the lubricant, an oral composition having increased hardness and reduced friability 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 lubricating agent, an oral composition having increased hardness and reduced friability can be provided. In particular, by setting the blending ratio of charcoal and the fluidizing agent to a specific blending ratio, by setting the blending ratio of the fluidizing agent in the oral composition to a specific blending ratio, and by setting the blending ratio of charcoal and the lubricating agent to a specific blending ratio, an oral composition having even better hardness and friability can be provided.

Claims

1. A solid oral composition comprising (A) charcoal, (B) a fluidizing agent, and (C) a lubricant, and having a hardness of 2 kgf or more and a friability of 3% or less (excluding the following (1) to (4)). (1) An oral composition comprising charcoal and at least one other ingredient selected from the group consisting of 3-hydroxy-3-methylbutyric acid, creatine, amino acids, and peptides. (2) A composition for food or drink, comprising charcoal and at least one selected from the group consisting of currant, black soybean, black vinegar, ginseng, and young barley leaves. (3) An oral medication comprising a combination of an adsorbent, a room temperature liquid oil, a granulated material containing a water-soluble polymer, and a laxative.

2. An oral composition comprising (A) coconut shell-derived charcoal and (B) a fluidizing agent.

3. 1. An oral composition comprising (A) charcoal and (C) a lubricant, the content of (C) being 45% by mass or more and 70% by mass or less relative to the total amount of (A) and (C).

Citation Information

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