JP2023066089A - Tablet and method for improving disintegratability of tablet - Google Patents

Abstract

To provide a tablet comprising plant extract, the tablet having improved disintegratability while retaining its hardness.SOLUTION: In order to solve the foregoing problem, there is provided a tablet comprising (A) plant extract and (B) carrageenan, with the content of the component (A) being 10 mass% or more and 60 mass% or less and the content of the component (B) being 1 mass% or more and 15 mass% or less. This can provide a tablet comprising plant extract, the tablet having improved disintegratability while retaining its hardness.SELECTED DRAWING: None

Description

The present invention relates to tablets containing plant extracts. More specifically, it relates to tablets containing plant extracts and carrageenan.

Plant extracts such as herbal medicines are blended in pharmaceuticals and supplements in order to exert their medicinal effects. However, tablets containing more than a certain amount of plant extract tend to disintegrate for a long time, and there is a problem that the plant extract is not sufficiently absorbed in the body.

In order to improve the disintegration properties of tablets containing such plant extracts, it is conceivable to add a large amount of disintegrant. However, in that case, there is a problem that the hardness of the tablet is lowered and the tablet is broken during filling or distribution. In addition, when a large amount of disintegrant is blended, there arises a problem that the fluidity of the tableting powder is deteriorated.

In response to such problems, Patent Document 1 discloses tablets containing ginkgo biloba extract, starch, and sugar alcohol, and Patent Document 2 discloses fibrous fibers having an average fiber length of 20 to 1000 μm per particle. A tablet base material is disclosed in which 5 parts by mass or more and less than 100 parts by mass of water are absorbed into 100 parts by mass and then dried.

Japanese Unexamined Patent Application Publication No. 2021-90358 Japanese Patent Application Laid-Open No. 2020-152712

However, even in the method of the patent document shown above, although the effect of improving disintegration and improving tablet hardness is observed for specific ingredients, tablets containing more than a certain amount of many other plant extracts On the other hand, when used, it was difficult to achieve both disintegration and tablet hardness.

An object of the present invention is to provide a plant extract-containing tablet having improved disintegration properties and maintaining tablet hardness.

As a result of intensive studies on the above-mentioned problems, the inventors of the present invention found that, in a tablet containing a certain amount or more of a plant extract, the disintegration property of the tablet can be improved by incorporating carrageenan, and furthermore, the appropriate hardness of the tablet can be maintained. The findings were found and the present invention was completed.

That is, the present invention provides the following [1] to [6].
[1] (A) contains a plant extract and (B) carrageenan,
A tablet, wherein the content of component (A) is 10% by mass or more and 60% by mass or less, and the content of component (B) is 1% by mass or more and 15% by mass or less.
According to the present invention, it is possible to provide a plant extract-containing tablet with improved disintegration properties and maintained tablet hardness.
[2] The A component is (A) one or more selected from bacopa extract, artichoke extract, ginkgo biloba extract, bilberry extract, milk thistle extract, agrimony extract, and African mango extract [1] Tablets described in.
As a result, it is possible to provide a plant extract-containing tablet with improved disintegration and better tablet hardness.
[3] In [1] or [2], wherein the mass ratio (A/B) of the content of the component (A) to the content of the component (B) is 2 or more and 60 or less. Tablets as described.
This makes it possible to provide a plant extract-containing tablet with improved disintegration properties and maintained tablet hardness.
[4] The tablet according to any one of [1] to [3], characterized in that the disintegration time in water at 37° C. of the tablet according to the disintegration test method described in the Japanese Pharmacopoeia is within 60 minutes. .
As a result, it is possible to provide a plant extract-containing tablet with improved disintegration properties and further maintained tablet hardness.
[5] (A) A method for improving disintegration properties of a tablet containing 10% by mass or more and 60% by mass or less of a plant extract,
(B) A method for improving disintegration properties of tablets, characterized by containing 1% by mass or more and 15% by mass or less of carrageenan.
ADVANTAGE OF THE INVENTION According to this invention, it is a tablet containing a plant extract. WHEREIN: Disintegratability can be improved and tablet hardness can be maintained.
[6] In [5], wherein the A component is (A) one or more selected from bacopa extract, artichoke extract, ginkgo biloba extract, bilberry extract, milk thistle extract, agrimony extract, and African mango extract. A method for improving the disintegration properties of the described tablets.
As a result, the plant extract-containing tablet can be more improved in disintegration properties and more maintainable in tablet hardness.

ADVANTAGE OF THE INVENTION According to this invention, it is possible to provide a plant extract-containing tablet having improved disintegration properties and maintaining tablet hardness.

[tablet]
The tablet of the present invention contains (A) a plant extract and (B) carrageenan,
The content of component (A) is 10% by mass or more and 60% by mass or less, and the content of component (B) is 1% by mass or more to 15% by mass.

Tablets containing a certain amount or more of a plant extract tend to disintegrate for a long time, and there is a problem that the plant extract is not sufficiently absorbed in the body. Although it has been difficult to improve the disintegration properties of tablets containing plant extracts with conventionally used disintegrants, the present inventors have found that the disintegration properties of tablets can be improved by adding a predetermined amount of carrageenan as a disintegrant. I have found that it can be improved. Further, in the tablet of the present invention, the tablet hardness is maintained, and the occurrence of the problem of breakage during filling and distribution is suppressed.

<(A) plant extract>
The tablet of the invention contains a plant extract. Plant extracts are not particularly limited, and for example, plant extracts used in pharmaceuticals, quasi-drugs, OTC drugs, herbal medicines, herbal medicines, cosmetics, health foods, supplements, veterinary drugs, etc. are used. The plant extract is preferably one or more selected from bacopa extract, artichoke extract, ginkgo biloba extract, bilberry extract, milk thistle extract, Agrimony extract, and African mango extract. These plant extracts may be blended alone or in combination of two or more.

The plant extract in the tablet of the present invention is not particularly limited, and is an extract with a polar solvent such as water, various organic solvents or mixtures thereof, a distillate obtained by steam distillation, an extract or a distillate and a powder extract obtained by drying the Among these, a powder extract obtained by drying an extract or a distillate is preferable from the viewpoint of tablet production.
Powdered extracts are, for example, pulverized fruits, seeds, leaves, etc., or extracts extracted from fruits, seeds, leaves, etc. with ethanol aqueous solution, etc. are separated and concentrated, and if necessary, additives such as excipients are added. A commercially available product can be used regardless of the production method.

The content of the plant extract in the tablet of the present invention is, for example, 10% by mass or more and 60% by mass or less. The lower limit is preferably 20% by mass or more, more preferably 30% by mass or more, from the viewpoint of exhibiting the efficacy of the plant extract.

<Carrageenan>
The tablet of the present invention contains carrageenan. Carrageenan is a polysaccharide naturally extracted mainly from red algae. Carrageenan is a galactan having a linear structure in which α (1→3) and β (1→4) bonds are alternately repeated. Part or all of it exists as 3,6-anhydro-D-galactose and its sulfate ester. Carrageenan is classified into three types, kappa, iota and lambda, depending on the amount of sulfate group and anhydro group contained in the molecule. can. Among these, a mixture containing kappa-carrageenan or kappa-carrageenan is preferred, and kappa-carrageenan is more preferred, from the viewpoint of disintegration and tablet hardness.

The content of carrageenan in the tablet of the present invention is 1% by mass or more and 15% by mass or less. The lower limit is preferably 3% by mass or more from the viewpoint of disintegration. The upper limit is preferably 15% by mass or less from the viewpoint of maintaining tablet hardness.

In addition, the mass ratio (A/B) of the content of component (A) to the content of component (B) in the tablet of the present invention (hereinafter also referred to as "A/B ratio") is not particularly limited, but for example, It is 1 or more and 100 or less. The lower limit is preferably 2 or more, more preferably 3 or more. The upper limit is preferably 60 or less, more preferably 12 or less.

<Other ingredients>
Additives such as excipients, binders, lubricants, stabilizers, preservatives, fluidizing agents, and coloring agents may be added to the tablet of the present invention, if necessary. In addition, other disintegrants than carrageenan may be blended.

Excipients are not particularly limited, and examples thereof include microcrystalline cellulose, lactose, sucrose, mannitol, glucose, starch, calcium phosphate, calcium sulfate and the like. In addition, these excipients may be blended alone or in combination of two or more. By adding excipients, the volume of useful substances can be adjusted.

The binder is not particularly limited, and examples thereof include carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid, polymethacrylic acid, glucose, sucrose, lactose, maltose, Dextrin, sorbitol, mannitol, macrogol, paraffin, gum arabic, gelatin, agar, starch, pullulan and the like. Moreover, these binders may be blended alone or in combination of two or more. By adding a binder, a binding force can be imparted to the powder components and a stable tablet can be produced.

Lubricants are not particularly limited, and examples include talc, colloidal silica, magnesium stearate, calcium stearate, magnesium carbonate, sodium benzoate, palmitic acid, sodium stearyl fumarate, waxes, hydrogenated vegetable oils, fats, Examples include polyethylene glycol. Moreover, these lubricants may be blended alone, or two or more of them may be blended together. By adding a lubricant, it is possible to suppress the occurrence of tableting problems such as sticking during tablet production.

Other disintegrants may be added to further improve the disintegration properties of the tablet of the present invention. Other disintegrants are not particularly limited, and examples include corn starch, low-substituted hydroxypropylcellulose, carboxymethylcellulose calcium, microcrystalline cellulose, croscarmellose sodium, carboxymethylstarch sodium, crospolyvinylpyrrolidone, and alginate. etc. Moreover, these disintegrants may be blended alone, or two or more of them may be blended together.

Examples of the present invention will be described below, but the present invention is not limited to only these examples, and various modifications are possible within the technical concept of the present invention.

(1) Test 1 Effect of carrageenan in tablets containing plant extract Regarding the effect of carrageenan in tablets containing plant extracts, tablets of Examples and Comparative Examples shown in Table 1 were produced, and tablet hardness and disintegration were tested. . In Test 1, an artichoke extract was used as the plant extract. The raw materials used in the examples are shown in Table 1 below.

(Manufacturing of tablets)
Tablets of Examples and Comparative Examples were produced by the following procedure.
Each raw material was mixed at the raw material compounding ratio (% by mass) of the composition shown in Table 2 and sieved to obtain a powder for tableting. The powder for tableting was tableted with a single punch tableting machine N-30E (manufactured by Okada Seiko Co., Ltd.) with a punch size of φ9 mm, R12, and a tableting pressure of 1000 kgf to obtain tablets with a diameter of about 9 mm and a weight of 300 mg.

(Measurement of tablet hardness)
The hardness of the tablets produced in the production of the above tablets was measured using New Speed Checker TS-75N (manufactured by Okada Seiko Co., Ltd.). A hardness of 10 kgf or more was evaluated as a hardness capable of withstanding actual use. Table 1 shows the hardness measurement results.

(Tablet disintegration test)
The disintegration time of the manufactured tablets was measured according to "6.09 disintegration test method" described in the general test method of "Japanese Pharmacopoeia 17th Edition". Ion-exchanged water was used as the test liquid. As a disintegration tester, a disintegration tester NT-610 (manufactured by Toyama Sangyo Co., Ltd.) was used.
The test liquid (purified water) was tested with a liquid volume of 900 mL, and the disintegration time was measured in water according to the method described in the Japanese Pharmacopoeia "Disintegration Test Method", and the disintegration time was measured according to the following criteria. evaluated.
<Evaluation Criteria for Disintegration Time>
◎: 40 minutes or less ○: Over 40 minutes and 50 minutes or less △: Over 50 minutes and 60 minutes or less ×: Over 60 minutes

As a result of the test, the tablets containing the plant extract had insufficient disintegration properties when tablets containing no disintegrant (Comparative Examples 1 to 3) and tablets prepared with a general disintegrant (Comparative Example 6 7, 8), good disintegration properties were obtained by adding carrageenan as a disintegrant in the range of 1 to 15%. However, tablets containing 20% or more of carrageenan did not exhibit sufficient disintegration (Comparative Examples 4 and 5). In addition, the tablets to which carrageenan was added had good tablet hardness.

(2) Test 2 Confirmation of the effect of carrageenan in tablets containing other plant extracts Regarding the effect of carrageenan in tablets containing plant extracts other than artichoke extract, tablets of Examples and Comparative Examples shown in Tables 3 to 5 were manufactured. Then, tablet hardness and disintegration were tested in the same manner as Test 1. In Test 2, bacopa extract, ginkgo biloba extract, bilberry extract, marian thistle extract, artichoke extract, agrimony extract and African mango extract were used as plant extracts.

As a result of the test, it was confirmed that adding a predetermined amount of carrageenan to tablets containing plant extracts other than artichoke extract also improved disintegration and maintained tablet hardness. In addition, it was shown that the A/B ratio is preferably 2 or more and 60 or less, more preferably 2 or more and 12 or less, from the viewpoint of disintegration and tablet hardness.

(3) Formulation Examples Chewable tablets were produced according to a conventional method with the formulations of the production examples described below.

INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a plant extract-containing tablet having improved disintegration and maintaining tablet hardness. INDUSTRIAL APPLICABILITY The present invention can be utilized in various fields such as pharmaceuticals, quasi-drugs, veterinary products, foods, and supplements.

Claims (6)

(A) a plant extract, and (B) containing carrageenan,
A tablet, wherein the content of component (A) is 10% by mass or more and 60% by mass or less, and the content of component (B) is 1% by mass or more and 15% by mass or less. 2. The method according to claim 1, wherein the component A is (A) one or more selected from bacopa extract, artichoke extract, ginkgo biloba extract, bilberry extract, milk thistle extract, agrimony extract, and African mango extract. tablets. The tablet according to claim 1 or 2, wherein the mass ratio (A/B) of the content of component (A) to the content of component (B) is 2 or more and 60 or less. The tablet according to any one of claims 1 to 3, characterized in that the disintegration time of the tablet in water at 37°C according to the disintegration test method described in the Japanese Pharmacopoeia is 60 minutes or less. (A) A method for improving disintegration properties of a tablet containing 10% by mass or more and 60% by mass or less of a plant extract,
(B) A method for improving tablet disintegration, characterized by containing 1% by mass or more and 15% by mass or less of carrageenan. 6. The method according to claim 5, wherein the component A is (A) one or more selected from bacopa extract, artichoke extract, ginkgo biloba extract, bilberry extract, milk thistle extract, agrimony extract, and African mango extract. A method for improving tablet disintegration.