JPS6322782B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a method for producing effervescent tablets containing dipeptide sweeteners. Dipeptide sweeteners are low-calorie sweeteners that have a refreshing sweetness similar to sucrose, but their low solubility and dispersibility pose problems when considering practical use as sweeteners. . In order to improve the solubility and dispersibility of such dipeptide sweeteners, it has been proposed to form dipeptide sweeteners into effervescent tablets. Effervescent tablets are manufactured by blending carbonate or bicarbonate and acidic substances with base ingredients and additives (excipients, binders, disintegrants, lubricants, etc.). When the manufactured tablets are placed in water, both are neutralized and gases such as carbon dioxide are released, causing them to dissolve quickly. Conventionally, sodium hydrogen carbonate has been widely used as a blowing agent, and fumaric acid has been used as a neutralizing agent. However, when such effervescent ingredients are blended, tablets with high hardness cannot be obtained or
Alternatively, even if highly hard tablets are obtained, there are drawbacks such as extremely poor solubility, and improvements have been desired, particularly when dipeptide sweeteners are used as the main ingredient. In other words, tablets containing sweeteners as the main ingredient have a certain degree of high tablet hardness from the standpoint of abrasion resistance, etc.
In addition, it is required to be quickly soluble during use. An object of the present invention is to provide an effervescent tablet containing a dipeptide sweetener that satisfies such requirements. The present invention relates to a method for producing effervescent tablets containing a dipeptide sweetener, characterized in that tartaric acid is added as a neutralizing agent during the production of effervescent tablets containing a dipeptide sweetener. In the present invention, the main ingredient is a dipeptide sweetener, and the additives include starches such as wheat starch, potato starch, and corn starch, sugars such as glucose, sucrose, lactose, and sorbitol, and inorganic substances such as calcium phosphate and calcium sulfate. Excipients (or diluents) such as;
There are binders such as starch, sucrose, gelatin, gum arabic, and methylcellulose; blowing agents such as sodium bicarbonate; and lubricants such as leucine, isoleucine, and L-valine. It is sufficient to take this into consideration and select it appropriately. In the present invention, tartaric acid is further blended as a neutralizing agent for the foaming agent. Conventionally, acidic substances, particularly fumaric acid, have been used as neutralizing agents, but when tablets were manufactured using other organic acids and the tablet hardness and dissolution rate were investigated, it was found that tablets were placed in hot water at 60°C. In order to dissolve within 30 seconds, if fumaric acid is added, the tablet hardness must be kept to around 1 kg, whereas if tartaric acid is added, the tablet dissolves quickly even if the tablet hardness is 2.5 to 4.0 kg. I found out what to do. Here, d-type tartaric acid is preferred, but dl-type tartaric acid can also be used. When producing effervescent tablets containing dipeptide sweeteners, known production methods can be applied; for example, the above tablet components may be mixed and produced by direct powder compression, wet granule compression, dry granule compression, or the like. The amount of tartaric acid added as a neutralizing agent is determined by considering the type of dipeptide sweetener, the amount of disintegrant added, etc. For example, α-L-aspartyl-L-phenylalanine methyl as a dipeptide sweetener When using an ester (hereinafter abbreviated as AP), tartaric acid should be added in a range of 5 to 35%, with a preferred range of 15 to 25%, since it is desired that it dissolves quickly during use. In addition, the amount of tartaric acid added is the molar equivalent of the disintegrant used,
That is, the amount that causes the neutralization reaction quickly is preferable. According to the present invention, a tablet with excellent rapid dissolution properties can be obtained even if the tablet hardness is 2 kg or more (breaking hardness). Next, examples of the present invention will be shown. Example 1 Effervescent tablets containing a dipeptide sweetener were manufactured from a tablet composition having the composition shown in the table below by a dry granule compression method.

[Table] The measurement results for the various properties of each sample above are shown in the second table.
Shown in the table.

【table】

[Table] As is clear from Table 2, Sample 3 has an excellent appearance, good abrasion resistance, and quick dissolution, and d-tartaric acid has an excellent effect on effervescent tablets containing dipeptide sweeteners. It was found that it has. Example 2 A dipeptide sweetener-containing effervescent tablet was manufactured from a tablet composition having the composition shown in Table 3 by a dry granule compression method.

[Table] The measurement results for the various properties of each sample above are shown in the 4th table.
Shown in the table.

[Table] As is clear from the above results, satisfactory dipeptide sweetener-containing effervescent tablets can be obtained when the amount of tartaric acid added is 5 to 35%, preferably 15 to 25%.

Claims (1)

[Scope of Claims] 1. A method for producing an effervescent tablet containing a dipeptide sweetener, which comprises adding tartaric acid as a neutralizing agent in producing the effervescent tablet containing a dipeptide sweetener. 2 The dipeptide sweetener is α-L-aspartyl-
The manufacturing method according to claim 1, which is L-phenylalanine methyl ester. 3. The manufacturing method according to claim 1, wherein the amount of tartaric acid added is 5 to 35%. 4. The manufacturing method according to claim 1, wherein the amount of tartaric acid added is 15 to 25%.