CN111671732B

CN111671732B - Tablet containing astaxanthin and calcium

Info

Publication number: CN111671732B
Application number: CN202010775620.8A
Authority: CN
Inventors: 胡文波
Original assignee: Jiangsu Yangxin Biomedical Co ltd
Current assignee: Jiangsu Yangxin Biomedical Co ltd
Priority date: 2020-08-05
Filing date: 2020-08-05
Publication date: 2022-03-22
Anticipated expiration: 2040-08-05
Also published as: CN111671732A

Abstract

The invention provides a tablet containing astaxanthin and calcium, which comprises 220 parts of astaxanthin, 60-80 parts of calcium citrate, 60-70 parts of microcrystalline cellulose, 3-5 parts of magnesium stearate, 3-15 parts of polyvinylpyrrolidone K3012 and 3-5 parts of a disintegrating agent, wherein the astaxanthin is astaxanthin microcapsule powder; the tablet has relatively low tablet weight and is convenient for administration.

Description

Tablet containing astaxanthin and calcium

Technical Field

The invention relates to a tablet composition, belongs to the field of medicine/food preparations, and particularly relates to a tablet composition containing astaxanthin and calcium in contents.

Background

Astaxanthin (astaxanthin), also known as astaxanthin and lobster shell pigment, is a carotenoid, is dark pink, insoluble in water, unstable under acid, oxygen, high temperature and ultraviolet conditions, and is easily oxidized and degraded. The stability and the antioxidant activity of the artificially synthesized astaxanthin are lower than those of natural astaxanthin. The astaxanthin raw material of natural source mainly has two forms of oil form and powder form. The astaxanthin oil has higher astaxanthin content, but is easily damaged and lost due to direct exposure to the environment, and the oily raw materials have limited applicable dosage forms, mainly soft capsules. The astaxanthin powder is microcapsule powder of astaxanthin oil subjected to inclusion treatment, has obviously improved stability compared with the astaxanthin oil, can be used for various solid preparations or foods, and is widely applied.

However, the astaxanthin has large particle size, can not be crushed, has low viscosity, can not resist high temperature and the like, and is not beneficial to the preparation of tablets. Although haematococcus pluvialis powder with small and uniform particle size (the stability is weaker than that of astaxanthin contained in microcapsule powder) exists, the performance of the haematococcus pluvialis powder in the aspect of preparing tablets is better than that of astaxanthin microcapsule powder, a large amount of auxiliary materials are still required to be added if qualified astaxanthin tablets are obtained, and the weight of the astaxanthin tablet is usually larger and reaches 700 mg/tablet or even higher due to the fact that the content of astaxanthin in the astaxanthin powder is low under the condition that the intake of astaxanthin is guaranteed, so that people can difficultly swallow the tablet, or foreign body sensation is obvious after the tablet is swallowed, and the comfort level is poor.

Astaxanthin has multiple biological functions of antioxidation, retina protection, immunity enhancement, cancer resistance, anti-inflammation and the like, but is limited by the properties of astaxanthin, and the current products containing astaxanthin cannot meet the health requirements of people.

Disclosure of Invention

The invention aims to provide an astaxanthin-containing tablet, in particular an astaxanthin tablet which takes astaxanthin microcapsule powder as a raw material and has lower tablet weight of less than 400 mg.

The invention provides a tablet containing astaxanthin and calcium, which comprises the following raw materials, by weight, 220 parts of astaxanthin, 60-80 parts of calcium citrate, 60-70 parts of microcrystalline cellulose, 3-5 parts of magnesium stearate, 3-15 parts of polyvinylpyrrolidone K3012 and 3-5 parts of a disintegrating agent, wherein the astaxanthin is astaxanthin microcapsule powder, but not astaxanthin powder or haematococcus pluvialis powder with the particle size of more than 60 meshes.

The astaxanthin microcapsule powder is prepared by the inclusion process of astaxanthin oil, the capsule shell effectively avoids the damage of oxygen and light to astaxanthin, so that the stability of the astaxanthin is obviously improved, but the astaxanthin microcapsule powder still can not resist high temperature, such as the drying temperature (50-60 ℃) of wet granulation. The particle size of the astaxanthin microcapsule powder is larger due to the existence of the capsule shell, the particle size can only reach the degree that the astaxanthin microcapsule powder can completely pass through a 20-mesh sieve, and the microcapsules are regular or irregular round and have good fluidity. Therefore, compared with other raw and auxiliary materials in the formula, the astaxanthin is heavier, more easily flowable, and easily sinks during mixing, is difficult to be uniformly mixed with other raw and auxiliary materials, and cannot be pressed into tablets by a process of directly tabletting powder.

The inventor tried to wet granulate the raw and auxiliary materials except astaxanthin and then mix the granulated raw and auxiliary materials with astaxanthin and tabletting, but the consumption of astaxanthin is large, the astaxanthin accounts for more than 55% of the total weight of the tablet, the compressibility is poor, and the hardness of the obtained tablet is only 10-20N (Newton), which is far from the requirement. After the astaxanthin tablet is prepared by a dry granulation method, the compressibility is improved, but the requirement cannot be met. In addition, various binders and different dosage are considered, the hardness of the tablet is not qualified, and the phenomenon of disintegration overtime is caused. However, the inventors have unexpectedly discovered when adjusting the calcium source in the formulation: the hardness of the tablet is obviously improved after calcium carbonate is replaced by calcium citrate, and the technical scheme of the invention is obtained by further optimizing the formula on the basis. The astaxanthin sheet prepared by the scheme has smooth surface, hardness, friability, disintegration and other performances meeting the requirements.

The recommended dose of natural astaxanthin as antioxidant is 3mg per day; when the food is eaten for a long time to play an anti-fatigue role, 8-10 mg needs to be supplemented every day, and when the blood fat reducing effect is played, 10-12 mg (calculated by the amount of pure astaxanthin) needs to be supplemented every day. The content of the astaxanthin in the astaxanthin microcapsule powder is not less than (not less than) 1.4%. The dosage of 3mg of pure astaxanthin in each tablet is met, so that the edible amount of the tablet is convenient for an eater to determine according to the requirement of the eater, and the compliance of the eater cannot be reduced due to large dosage (more tablets).

The disintegrant is croscarmellose sodium and/or crospovidone, and in a preferred embodiment, the disintegrant is: croscarmellose sodium.

In another embodiment, the tablet containing astaxanthin and calcium is prepared from the following raw materials, by weight, 220 parts of astaxanthin, 70 parts of calcium citrate, 65 parts of microcrystalline cellulose, 3 parts of magnesium stearate, 3 parts of polyvinylpyrrolidone K3015, and 4 parts of croscarmellose sodium.

In order to fully supplement nutrients required by human body, the tablet of the invention also contains one or the combination of amino acid, vitamin and trace element. Wherein the amino acids include tryptophan, methionine, and arginine; vitamins such as vitamin B, folic acid, etc.; trace elements such as iron and zinc.

Furthermore, the tablet of the invention contains 0.5 to 1.5 parts of vitamin B, in particular vitamin B6 and/or B12.

The tablet containing the astaxanthin and the calcium is prepared by dry granulation and tabletting. The specific process is as follows: mixing astaxanthin, calcium citrate, microcrystalline cellulose, polyvinylpyrrolidone K30 and disintegrating agent, granulating with a dry granulating machine, sieving with 18 mesh sieve, adding magnesium stearate, mixing, and tabletting. Wherein, the roller pressure of the dry granulator is preferably 40-50 bar.

To further preserve the efficacy of astaxanthin, the preparation of the tablets may also include a coating process, such as film coating the tablets containing astaxanthin and calcium.

The tablet containing astaxanthin not only enriches the market of astaxanthin products, but also contains not less than 3mg of pure astaxanthin per tablet, and meets the daily basic intake. More importantly, the tablet weight of each tablet is less than 400mg, which is reduced by more than 40% compared with the existing astaxanthin tablet, thereby greatly facilitating the taking and eliminating the discomfort after the large tablet is taken. Is beneficial for eaters to insist on supplementing nutrients and achieve the purpose of building up body.

The inventors further verified the technical effects of the present invention through experiments.

Restated again: the following experiments are merely illustrative of the many experiments performed during the development of the present invention and do not cover and exhaust all of the experiments performed by the inventors for the purpose of describing the effect of different formulations on tablet performance using only those data.

And (3) testing: effect of different calcium sources and Binders on tablets

Weighing astaxanthin, calcium, microcrystalline cellulose, polyvinylpyrrolidone K30 and croscarmellose sodium 100 tablets according to the formula shown in the following table, mixing, granulating by dry method, adding magnesium stearate, and mixing

The tablets were compressed with a round punch and the hardness, friability and disintegration time of the resulting tablets were examined (all three are routinely checked and the specific methods and standards are not described in detail) and the results are detailed in the following table.

From the experimental results, the hardness of the tablet is obviously improved after calcium carbonate is replaced by calcium citrate, but the dosage of the adhesive and the disintegrant directly influences whether the disintegration time limit and the friability are qualified or not, wherein in the formula 5, although all three indexes are qualified, the friability result is close to the upper limit, and the product is easily influenced by other factors to cause disqualification, so the formula is not suitable for selection.

Detailed Description

Example 1

Astaxanthin tablet (1000 tablets)

220g of astaxanthin, 70g of calcium citrate, 65g of microcrystalline cellulose, 3g of magnesium stearate, polyvinylpyrrolidone K3012g and 4g of croscarmellose sodium.

The process comprises the following steps: 1. mixing the raw and auxiliary materials except magnesium stearate, granulating by a dry method, and sieving by a 18-mesh sieve;

2. adding magnesium stearate, mixing, and tabletting.

Example 2

Astaxanthin tablet (1000 tablets)

220g of astaxanthin, 60g of calcium citrate, 65g of microcrystalline cellulose, 3g of magnesium stearate, K3012g of polyvinylpyrrolidone and 5g of crospovidone.

The process comprises the following steps: the same as in example 1.

Example 3

Astaxanthin tablet (1000 tablets)

220g of astaxanthin, 80g of calcium citrate, 60g of microcrystalline cellulose, 4g of magnesium stearate, K3014g of polyvinylpyrrolidone and 5g of crospovidone.

The process comprises the following steps: the same as in example 1.

Example 4

Astaxanthin tablet (1000 tablets)

220g of astaxanthin, 75g of calcium citrate, 70g of microcrystalline cellulose, 3g of magnesium stearate, polyvinylpyrrolidone K3015g and 3g of croscarmellose sodium.

The process comprises the following steps: the same as in example 1.

Example 5

Astaxanthin tablet (1000 tablets)

220g of astaxanthin, 65g of calcium citrate, 65g of microcrystalline cellulose, 5g of magnesium stearate, polyvinylpyrrolidone K3013g and 5g of croscarmellose sodium.

The process comprises the following steps: the same as in example 1.

Example 6

Astaxanthin tablet (1000 tablets)

220g of astaxanthin, 70g of calcium citrate, 121 g of vitamin B121 g, 70g of microcrystalline cellulose, 3g of magnesium stearate, K3013g of polyvinylpyrrolidone and 4g of crospovidone.

The process comprises the following steps: the difference from example 1 is that the compressed tablets are film coated.

The above are only some examples of the present invention, which are further intended to illustrate the present invention and not to limit the scope of the present invention. Modifications and variations of the above-described embodiments may be made by anyone without departing from the scope and spirit of the invention, and are intended to be covered by the appended claims.

Claims

1. The tablet is characterized by comprising the following raw materials, by weight, 220 parts of astaxanthin, 60-80 parts of calcium citrate, 60-70 parts of microcrystalline cellulose, 3-5 parts of magnesium stearate, 2-15 parts of polyvinylpyrrolidone K3012 and 3-5 parts of a disintegrating agent, wherein the astaxanthin is astaxanthin microcapsule powder.

2. The tablet according to claim 1, wherein the astaxanthin content in the astaxanthin microcapsule powder is not less than 1.4%.

3. The tablet of claim 1, wherein the disintegrant is croscarmellose sodium and/or crospovidone.

4. The tablet of claim 1, further comprising one or a combination of amino acids, vitamins and trace elements.

5. The tablet of claim 4, wherein the vitamin is 0.5 to 1.5 parts vitamin B.

6. The tablet according to claim 1, which is prepared from 220 parts by weight of astaxanthin, 70 parts by weight of calcium citrate, 65 parts by weight of microcrystalline cellulose, 3 parts by weight of magnesium stearate, 3 parts by weight of polyvinylpyrrolidone K3015 and 4 parts by weight of croscarmellose sodium.

7. The tablet of claim 1, wherein the tablet is formed by dry granulation tableting.

8. The tablet of claim 7, wherein the preparation further comprises a coating process.