JP2001348333A - Riboflavin formulated composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a riboflavin formulated composition masking a bitter taste of riboflavin and giving a fine feeling on taking the medicine. SOLUTION: This riboflavin formulated composition features being obtained by formulating a sweetner, a mucopolysaccharide and a clathrate.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a composition containing riboflavin. More specifically, the present invention relates to a riboflavin-containing composition which masks the bitterness unique to riboflavin and has an improved taste.

[0002]

2. Description of the Related Art Riboflavin is involved in carbohydrate, lipid and protein metabolism, and it is known that deficiency lowers each metabolic system and affects cell growth and division.
It is used for the treatment of stomatitis, glossitis, chinitis, conjunctivitis, keratitis and seborrheic dermatitis.

However, riboflavin has a strong bitter taste, and it is difficult to mask bitterness by ordinary methods such as increasing the amount of a sweetener, especially when the riboflavin is added at a high concentration, which significantly reduces the commerciality and makes the riboflavin-containing composition having a good taste. It was difficult to get things.

[0004]

An object of the present invention is to provide a riboflavin-containing composition which masks the bitterness of riboflavin and has a good taste.

[0005]

As a method of masking bitterness, a method using sodium chondroitin sulfate (Japanese Patent Laid-Open No. 146253/1993: Vitamin B1) has been proposed.
Bitterness of derivatives, JP-A-5-163154: Vitamin B2
Bitterness), a method using cyclodextrin (Japanese Unexamined Patent Publication No.
6-48849: Citrus bitterness, JP-A-59-3167
9: tannin bitterness) and the like.

[0006] The inventors of the present invention examined the bitterness masking effect of riboflavin blended in a liquid preparation using these methods, and found that the masking effect of bitterness was insufficient. Particularly, riboflavin was blended at a high concentration (0.3 mg / mL). In some cases, the masking effect was significantly lower.

Therefore, the present inventors have further studied diligently. As a result, by adding a sweetener, a mucopolysaccharide and an inclusion compound to the liquid formulation containing riboflavin,
It has been found that the bitterness of riboflavin is masked and a riboflavin-containing composition having a good taste can be obtained, and the present invention has been completed.

[0008] That is, the present invention is a composition containing riboflavin, which comprises a sweetener, a mucopolysaccharide and an inclusion compound.

[0009] As described above, the riboflavin of the present invention has a strong bitter taste, and the sweetener, mucopolysaccharide and clathrate can be increased in proportion to the amount thereof to mask the bitter taste. There is no particular limitation.

The sweeteners of the present invention include sugar, glucose, trehalose, fructose and sugar alcohols or polyhydric alcohols such as sorbitol, xylitol, erythritol, maltitol and glycerin, and high sweetness such as stevia, aspartame and sucralose. Sweeteners and the like. As for the sweetener, not only one but also one
You may mix and combine 2 or more types.

[0011] In the case of sugar, the amount of the sweetener of the present invention is
It is usually at least 30 parts by mass, preferably 300 to 7,500, per 1 part by mass of riboflavin. However, there is no upper limit as a critical significance for the amount of the sweetener to be compounded.
Even if it is added in an amount of not less than 00 parts by mass, there is no change in that the bitter taste masking action of riboflavin is exhibited.

Since the amount of the sweetener varies depending on the sweetness, the sweetness is generally represented by the degree of sweetness. The method of measuring the sweetness is defined as follows.

[0013] 10 g of sugar is dissolved in water at room temperature to give a total amount of 10 g.
The concentration of the sweetener corresponding to the sweetness of the 0 mL solution is determined by sensory evaluation by a specialized panel. For example, erythritol has a sweetness of about 0.8 because it is equivalent to the sweetness of an aqueous solution in which about 12.5 g is dissolved. The sweetness is determined by this method.

When the degree of sweetness is determined as described above, glucose is 0.7 and trehalose is 0.1 with respect to 1 for sugar.
4, fructose 1.5, sorbitol 0.7, xylitol 1, erythritol 0.8, maltitol 0.1.
8, glycerin is 0.7, stevia is 180, aspartame is 180 and sucralose is 600. Therefore, the compounding amount of the sweetener other than sugar is a value obtained by dividing the compounding amount of the above-mentioned sugar by the respective sweetness degrees.

The mucopolysaccharid of the present invention (mucopolysaccharid)
e) is a complex polysaccharide containing an amino sugar that is widely distributed in connective tissues, substrates and body fluids of animals, and it is known that it contains and does not contain a sulfate group. Such mucopolysaccharides include chondroitin, chondroitin sulfate, collagen, hyaluronic acid, heparin, mucin, casein, keratosulfate, heparan sulfate, dermatan sulfate, and the like, but these may be salts.

The amount of the mucopolysaccharide is usually 0.05 parts by mass or more, preferably 1.5 to 2500 parts by mass, per 1 part by mass of riboflavin. However, 2500
There is no change in the fact that riboflavin has a bitter taste masking action even if it is added in an amount of at least one part by mass.

As the clathrate compound of the present invention, a compound in which some compounds gather to form an clathrate lattice, or a compound having an inner hole such as cyclodextrin that can contain another substance is known. . Cyclodextrin is a cyclic dextrin formed by the degradation of starch by amylase.
Type, β type, and γ type are known. The cyclodextrin referred to in the present invention may be any of the above types, and may have a ring modified with a compound.

The compounding amount of the clathrate compound is usually at least 0.05 part by mass, preferably 1.5 to 500 parts by mass, per 1 part by mass of riboflavin. However, the addition of 500 parts by mass or more does not change the fact that riboflavin has a bitter taste masking action.

The riboflavin-combined composition of the present invention is suitable for use in oral liquid preparations, nutritional drinks, functional drinks, and soft drinks in which the pharmacological effects of riboflavin are expected. It can also be used as an agent.

The riboflavin-combined composition of the present invention may be formulated, if necessary, by blending one or more other vitamins, one or more medicinal or crude drug components that are allowed to be blended. It is possible.

Further, additives such as a preservative, a solubilizing agent, a fragrance, a coloring agent and the like can be appropriately added to the composition of the present invention.

[0022]

The following examples, comparative examples and test examples are given below.
The present invention will be described in more detail, but the present invention is not limited thereto.

Example 1 Riboflavin (30 mg) was dissolved in heated purified water, cooled, and 15 g of sugar, 900 mg of sodium chondroitin sulfate, 200 mg of α-cyclodextrin and 240 mg of citric acid were added. After adjusting the pH to 3.5 with a 5N sodium hydroxide solution, purified water was added to bring the total volume to 100 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

(Example 2) Riboflavin (30 mg) was dissolved in heated purified water, cooled, and 15 g of sugar, 900 mg of sodium chondroitin sulfate, 200 mg of β-cyclodextrin, and 240 mg of citric acid were added. After adjusting the pH to 3.5 with a 5N sodium hydroxide solution, purified water was added to bring the total volume to 100 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

(Example 3) Riboflavin (30 mg) was dissolved in heated purified water, cooled and cooled, and sugar (15 g), chondroitin sodium (900 mg), α-cyclodextrin (200 mg), β-cyclodextrin (600 mg), and
240 mg of citric acid were added. After adjusting the pH to 3.5 with a 5N sodium hydroxide solution, purified water was added to bring the total volume to 100 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

Comparative Example 1 Riboflavin (30 mg) was dissolved in warm purified water, cooled, and sugar (30 g) and citric acid (240 mg) were added. After adjusting the pH to 3.5 with a 5N sodium hydroxide solution, purified water was added to adjust the total amount to 1.
00 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

(Comparative Example 2) 30 mg of riboflavin was dissolved in heated purified water, cooled, and 1800 mg of sodium chondroitin sulfate and 240 mg of citric acid were added.
After adjusting the pH to 3.5 with a 5N sodium hydroxide solution, purified water was added to bring the total volume to 100 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

(Comparative Example 3) 30 mg of riboflavin was dissolved in warm purified water, cooled, 400 mg of α-cyclodextrin and 240 mg of citric acid were added, and the pH was adjusted to 3.5 with a 5N sodium hydroxide solution. Then, purified water was added to adjust the total volume to 100 mL. This aqueous solution was filtered through filter paper, filled in a brown glass bottle, capped,
The solution was sterilized at 0 ° C. for 25 minutes to give an oral solution.

(Comparative Example 4) 30 mg of riboflavin was dissolved in heated purified water, and then cooled, followed by 15 g of sugar, 900 mg of sodium chondroitin sulfate, and 240 mg of citric acid.
And adjust the pH to 3 with 5N sodium hydroxide solution.
After adjusting to 5, purified water was added to bring the total volume to 100 mL. After filtering this aqueous solution through a filter paper, filling in a brown glass bottle,
The solution was capped and sterilized at 80 ° C. for 25 minutes to give an oral solution.

Comparative Example 5 30 mg of riboflavin was dissolved in warm purified water, cooled, 15 g of sugar, 200 mg of α-cyclodextrin and 240 mg of citric acid were added, and the pH was adjusted with a 5N sodium hydroxide solution. After adjusting to 3.5, purified water was added to bring the total volume to 100 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

(Comparative Example 6) 30 mg of riboflavin was dissolved in heated purified water, cooled, and 900 mg of sodium chondroitin sulfate and 200 m of α-cyclodextrin were dissolved.
g, 240 mg of citric acid. After adjusting the pH to 3.5 with a 5N sodium hydroxide solution, purified water was added to bring the total volume to 100 mL. This aqueous solution was filtered through a filter paper, filled in a brown glass bottle, capped, sterilized at 80 ° C. for 25 minutes to give an oral solution.

Test Example 1 The oral liquid preparations prepared in Examples 1 and 2 and Comparative Examples 1 to 6 were stored at 5 ° C. Carried out. After taking 10 mL of the sample, the sample was evaluated for bitterness, and after evaluating one sample solution, the mouth was rinsed with warm water, and after the lapse of 30 minutes or more, the next sample solution was taken. I went in that way.
The evaluation of the ingestibility was based on the following criteria, and the average value of the evaluation scores is shown in Table 1 together with the components. Evaluation of ingestibility Very strong bitterness 5 points Strong bitterness 4 points Bitterness 3 points Slightly bitterness 2 points Slightly bitterness 1 point No bitterness 0 points

[0033]

[Table 1]

As is clear from Table 1, Examples 1 and 2
In the oral liquid preparations of the above, almost no bitterness was felt, whereas in the oral liquid preparations of Comparative Examples 1 to 6, bitterness was felt.

[0035]

Industrial Applicability According to the present invention, it has become possible to provide a riboflavin-containing composition in which the bitter taste of riboflavin is masked and the riboflavin is easily taken.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 47/40 A61K 47/40 A61P 1/02 A61P 1/02 3/00 3/00 17/08 17 / 08 27/02 27/02 // A23L 2/52 A23L 2/00 FF term (reference) 4B017 LC02 LC03 LK11 LK13 LK16 LL02 4B018 MD23 MD33 MD36 ME14 4C076 AA12 BB01 CC24 DD30 DD33 DD67 EE37 EE39 FF52 4C086 CB09 MA03 MA05 MA05 MA52 NA09 ZA33 ZA67 ZC26 ZC33 ZC35

Claims (4)

[Claims] 1. A riboflavin-containing composition comprising a sweetener, a mucopolysaccharide and an inclusion compound. 2. The riboflavin-containing composition according to claim 1, wherein the mucopolysaccharide is sodium chondroitin sulfate. 3. The riboflavin-containing composition according to claim 1, wherein the clathrate compound is α-type cyclodextrin, β-type cyclodextrin, or γ-type cyclodextrin. 4. The composition containing riboflavin according to any one of claims 1 to 3, which is an oral liquid preparation.