JP2020117503A - Oral composition - Google Patents

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

Description

The present invention relates to an oral composition containing charcoal.

Charcoal is a porous substance composed of oxygen, hydrogen, calcium, etc. in addition to the majority of carbon, and has the property of adsorbing various substances into its fine pores.

Charcoal is industrially used as a decolorizing agent by adsorbing a coloring component (Patent Document 1) and a deodorizing agent by adsorbing odorous substances (Patent Document 2), and is used as an auxiliary agent for filtration and purification. .. Further, in recent years, supplements utilizing the effect of charcoal have been receiving attention.

JP-A-6-65591 JP, 2013-81649, A

However, the composition containing charcoal has poor moldability, and particularly when the content of charcoal is high, there is a problem that it is difficult to mold into a solid composition such as a tablet.

An object of the present invention is to provide an oral composition in which the composition containing charcoal is improved in hardness and friability and is easy to ingest, for the purpose of effectively utilizing the charcoal.

As a result of diligent studies, the present inventors have found that in an oral composition containing charcoal, a fluidizing agent and a lubricant, a solid oral composition having excellent hardness characteristics and friability characteristics can be obtained. The present invention has been reached. In particular, it is more excellent to set the charcoal and the fluidizing agent in a specific blending ratio, the fluidizing agent in the oral composition to a specific blending ratio, and the charcoal and the lubricant in a specific blending ratio. It was found that a tablet-shaped oral composition having excellent hardness and friability can be obtained, and the present invention has been completed.

The outline of the present invention is as follows.
[1] An oral composition containing (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] Charcoal (A) and lubricant (C) are contained, and the content of (C) is 70% by mass or less based on the total amount of (A) and (C). Oral composition.
[5] An oral composition comprising (A) charcoal, (B) superplasticizer and (C) lubricant.
[6] A solid oral composition 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 comprising (A) charcoal, (B) superplasticizer and (C) lubricant, and 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.

According to the present invention, a solid oral composition having excellent hardness and friability can be provided. In particular, the charcoal and the fluidizing agent have a specific blending ratio, the fluidizing agent in the oral composition has a specific blending ratio, and the charcoal and the lubricant have a specific blending ratio, which are more excellent. A solid oral composition having hardness can be provided.

Hereinafter, the oral composition of the present invention will be described. The present invention is not limited to the embodiments described below.

(A) Charcoal Charcoal is obtained by treating plants, organic compounds and synthetic resin under high temperature conditions, and is mainly used as a fuel and an auxiliary agent for filtration and purification. The raw material of charcoal that can be used in the present invention is not particularly limited as long as it can be orally ingested, and examples thereof include Ubamegashi, Kunugi, chestnut, larch, red pine, and cedar trees used for Bincho charcoal, bamboo, coconut shell, walnut. Examples include shells and rice husks. As the charcoal, it is preferable to use activated carbon obtained by dry-distilling the raw material and further activating it by high-temperature treatment. The activated carbon is not particularly limited as long as the adsorption ability is activated, but when it is a commercial product, for example, those having the notation of activated carbon in the specifications of raw materials are mentioned. The shape of the charcoal that can be used in the present invention is not particularly limited as long as it is edible, but examples thereof include powder, granules, fibrous and formed charcoal, and powder and granules are preferable. .. As the raw material of the charcoal of the present invention, it is preferable to use bamboo, red pine, coconut shell, and rice husk, and bamboo, coconut shell, and rice husk are particularly preferable. In particular, when the oral composition of the present invention is in the form of a tablet or a chewable form, it exhibits an effect of improving hardness and an effect of reducing friability when combined with a specific other material, so that activated carbon derived from coconut shell is used. Most preferably used.

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 0.01 to 30% by mass. More preferable.

(B) Superplasticizer The superplasticizer is used for the purpose of improving the fluidity of the mixed powder and 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 object, and examples thereof include talc, silicon dioxide (light anhydrous silicic acid, hydrous silicon dioxide), hydrophilic silica, Examples thereof include hydrophobic silica, calcium silicate, alkyl phosphate (PAP), anhydrous calcium hydrogen phosphate, magnesium oxide, titanium oxide, magnesium silicate, calcium silicate and the like. These may be used alone or in combination of two or more. As the superplasticizer, a commercially available product can be used. In the present invention, since an excellent solid oral composition is obtained, silicon dioxide, magnesium oxide, titanium oxide, magnesium silicate, calcium silicate are preferable, and silicon dioxide, magnesium oxide, titanium oxide are more preferable, In particular, silicon dioxide is most preferable because an oral composition excellent in hardness improving effect and friability reducing effect can be obtained.

The content of the fluidizing agent (B) 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 further preferably 5% by mass or less. Moreover, 0.001 mass% or more is preferable, 0.005 mass% or more is more preferable, and 0.01 mass% or more is particularly preferable. With the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

(C) Lubricants Lubricants are used to alleviate friction between the tableting machine die and the tablet when compressing powder for tablets and prevent tableting failures such as sticking. Is. 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 objects, and examples thereof include stearic acid, calcium stearate, stearic acid such as magnesium stearate or a salt thereof, and fumaric acid. Examples thereof include fatty acid esters such as sodium stearyl, polyethylene glycol, and sucrose fatty acid esters, vegetable oils and fats, hydrogenated oils and the like. These may be used alone or in combination of two or more. As the lubricant, a commercially available product can be used. In the present invention, stearic acid or a salt thereof, fatty acid ester, and rapeseed hydrogenated oil are preferable, and calcium stearate, magnesium stearate, and sucrose fatty acid ester are more preferable because an oral composition excellent in hardness and friability can be obtained. ..

The content of the (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 1 to 5% by mass. Is more preferable. With the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

In the present invention, the content of (A) charcoal is preferably 0.1% by mass or more, and more preferably 1% by mass or more, based on the total amount of (A) charcoal and (B) superplasticizer. Further, it is preferably 99% by mass or less, and more preferably 70% by mass or less. Similarly, the content of the (A) charcoal is preferably 1% by mass or more, and more preferably 10% by mass or more, based on the total amount of the (A) charcoal and the (C) lubricant. Further, it is preferably 99% by mass or less, and more preferably 95% by mass or less. Further, the content of (A) charcoal is preferably 10% by mass or more, more preferably 20% by mass or more, based on the total amount of (A) charcoal, (B) superplasticizer and (C) lubricant. Yes, and particularly preferably 30% by mass or more. Further, it is preferably 99% by mass or less, more preferably 95% by mass or less, and particularly preferably 90% by mass or less. With the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

In the present invention, the content of the (B) superplasticizer is preferably 0.1% by mass or more, and more preferably 1% by mass or more, based on the total amount of the (A) charcoal and the (B) superplasticizer. , Particularly preferably 5 mass% or more. Moreover, 50 mass% or less is preferable, and 30 mass% or less is more preferable. Similarly, the content of the (B) superplasticizer is preferably 0.1% by mass or more, and more preferably based on the total amount of the (A) charcoal, the (B) superplasticizer, and the (C) lubricant. It is 1 mass% or more. Moreover, 30 mass% or less is preferable and 20 mass% or less is more preferable. With the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

In the present invention, the content of the (C) lubricant is preferably 5% by mass or more, and more preferably 10% by mass or more, based on the total amount of the (A) charcoal and the (C) lubricant. Further, it is preferably 90% by mass or less, and more preferably 70% by mass or less. Similarly, the content of the (C) lubricant is preferably 1% by mass or more, and more preferably 3% by mass based on the total amount of the (A) charcoal, the (B) superplasticizer and the (C) lubricant. % Or more. Moreover, 60 mass% or less is preferable, and 40 mass% or less is more preferable. With the above blending ratio, an oral composition having high hardness and reduced friability can be obtained.

In the present invention, in addition to (A) charcoal, (B) superplasticizer and (C) lubricant, components that can be used in an oral composition can be used. For example, components derived from animals and plants, excipients, binders, disintegrants, various carriers, stabilizing agents, surfactants, plasticizers, solubilizing agents, reducing agents, buffers, sweeteners, bases , Adsorbents, flavoring agents, antioxidants, brightening agents, coating agents, skins, wetting agents, wetting agents, fillers, cooling agents, coloring agents, flavoring agents, perfumes, sugar coating agents, isotonic agents. Agents, softeners, emulsifiers, thickeners, thickeners, foaming agents, pH adjusters, diluents, dispersants, disintegration aids, disintegration extenders, fragrances, moisturizers, preservatives, preservatives, solubilizers Examples include agents, solubilizing agents, solvents, antistatic agents, moisturizers, moisturizers, and the like.

The form of the oral composition of the present invention is, for example, powder, solid (tablet, granule, fine granule, chewable, granule, rod, plate, block, round, caplet, stick) Examples thereof include capsules such as soft capsules and hard capsules. Among these, powdery or solid form is preferable, and powdery form, tablet form, granular form, fine granular form, and chewable form are more preferred.

The hardness of the oral composition of the present invention when it is solid 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. Further, 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.

When the oral composition of the present invention is in a solid state, the friability is preferably 10% or less, more preferably 8% or less, particularly preferably 5% or less, particularly preferably 3% or less, from the viewpoint of ease of ingestion. preferable. Friability refers to the degree of occurrence of chipping, cracking and scraping in a solid oral composition, and as a method for measuring the friability, for example, it may be measured according to the method described in the Japanese Pharmacopoeia. it can.

When the oral composition of the present invention is solid, the disintegration time is preferably 400 seconds or shorter, more preferably 300 seconds or shorter, and particularly preferably 250 seconds or shorter. The disintegration time can be measured, for example, according to the method described in the Japanese Pharmacopoeia.

The oral composition of the present invention preferably has a hardness of 2 kgf or more and a friability of 3% or less, because it is expected that the moldability is excellent and the effect after ingestion is exhibited at an early stage.

The oral composition of the present invention is preferably used as a food, particularly a food for specified health use, a food with nutritional function, a food with functional claims, and a health food.

Examples of the present invention will be shown below, but the present invention is not limited thereto.

Production of charcoal-containing composition (1)
The raw materials were mixed in the ratios shown in Table 1 to produce 250 mg tablets. The pressure during tableting was 3.0 kN, and the tablet thickness was 5.8 mm.

Evaluation of tablet Each physical property of the obtained tablet was evaluated. The hardness was evaluated using a tablet hardness meter (Okada Seiko Co., Ltd.). The friability was obtained by measuring the mass (initial mass) of the tablet to be measured with an electronic balance, placing the measured tablet in the tablet friability tester, and rotating the tablet 300 times. After the test was completed, the tablet was taken out of the tester, the powder adhering to the tablet was lightly wiped off, the mass was measured (post-test mass), and the mass percentage of the reduced mass relative to the initial mass was calculated. The results are shown in Table 2.

From Table 2, Comparative Example 1 containing no fluidizing agent and lubricant could not be formed into tablets. On the other hand, the composition of the present invention containing a fluidizing agent and a lubricant could be molded into a tablet-like composition and had a hardness of 3 kgf or more. In addition, since the friability was very low at less than 1.1%, it was found that an excellent tablet that was not easily chipped or broken was obtained.

Production of charcoal-containing composition (2)
The raw materials were mixed in the ratios shown in Table 3 to produce 250 mg tablets. The pressure during tableting was 3.0 kN.

The disintegration time of the obtained tablets was measured. The disintegration time was measured according to the method described in the Japanese Pharmacopoeia. The disintegration time was 180 seconds or less in all cases, showing excellent disintegration property.

[Production of Oral Composition of the Present Invention]
(Production of tablets)
A tablet (300 mg) having the composition shown in Table 4 below was produced. The obtained tablets were oral compositions excellent in hardness and friability.

A tablet (300 mg) having the composition shown in Table 5 below was produced. The obtained tablets were oral compositions excellent in hardness and friability.

According to the present invention, in an oral composition containing charcoal and a superplasticizer, the hardness is increased and the friability is increased by adjusting the ratio of the amount of the lubricant to the amount of the charcoal and the lubricant. A reduced oral composition 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 having high hardness and reduced friability is provided. can do. In particular, it is more excellent to set the charcoal and the fluidizing agent in a specific blending ratio, the fluidizing agent in the oral composition to a specific blending ratio, and the charcoal and the lubricant in a specific blending ratio. Oral compositions having different hardness and friability can be provided.

Claims (5)

A solid oral composition containing (A) charcoal (B) a fluidizing agent and (C) a lubricant, having a hardness of 2 kgf or more and a friability of 3% or less. An oral composition comprising (A) charcoal and (B) a fluidizing agent. An oral composition comprising (A) charcoal and (B) a fluidizing agent, wherein the content of (B) is 5% by mass or more based on the total amount of (A) and (B). Content of (B) contained in a composition is 10 mass% or less, The oral composition in any one of Claim 3 characterized by the above-mentioned. An oral composition comprising (A) charcoal and (C) a lubricant, wherein the content of (C) is 70% by mass or less based on the total amount of (A) and (C). ..