JPH035364B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to an oral preparation containing a dipeptide sweetener, and more specifically, by adding lecithin,
The present invention relates to an oral preparation that stably retains a dipeptide sweetener. Oral preparations such as toothpastes contain sweeteners such as saccharin for the purpose of masking odors and tastes derived from the various ingredients contained therein and enhancing the feeling of use. Sweeteners added to these oral preparations include:
In general, characteristics such as anti-cariogenic properties, good sweetness and no unpleasant aftertaste, and high safety are required. It has been pointed out that women are not necessarily satisfied with their sexuality. On the other hand, dipeptide sweeteners represented by aspartame (α-L-aspartyl-L-phenylalanine methyl ester) are highly suitable for use in oral preparations as sweeteners with all of the above properties; In toothpastes and the like, the stability of dipeptide sweeteners during storage is an issue. In other words, when dipeptide sweeteners are kept in the presence of water, their stability decreases due to the effects of pH and temperature; however, in toothpastes, etc., the pH is neutral due to the abrasives and other ingredients blended. ~ Because it is in the alkaline region, the dipeptide sweetener decomposes during the manufacturing process or storage and distribution stage, turning into diketopiperazine, which is non-toxic and completely safe but has no sweet taste, and the odor and taste masking function in oral preparations is lost. Also,
Regardless of the pH, holding dipeptide sweeteners at relatively high temperatures also reduces their storage stability. Efforts to improve the stability of dipeptide sweeteners in such oral preparations include a method of dispersing dipeptide sweeteners in a non-aqueous paste and storing the paste in a container separated from an aqueous composition (Japanese Patent Laid-Open No. 56 -3610) or a method of encapsulating and blending a dipeptide sweetener with an acid (US Pat. No. 3,929,988), but the manufacturing process,
The actual situation is that it is still not satisfactory due to the complexity of packaging materials, etc. Against this background, the present inventors have conducted extensive research to stabilize dipeptide sweeteners in oral preparations. As a result, lecithin has been found to be particularly effective in stabilizing dipeptide sweeteners under weakly acidic to alkaline conditions. We obtained the knowledge that this significantly improves the The present invention was completed based on this knowledge, that is, it contains a dipeptide sweetener as all or a part of the sweetener, and contains 50% of the weight of the dipeptide sweetener in terms of the weight of phosphatidylcholine.
A dipeptide sweetener-containing oral preparation characterized by containing lecithin in an amount of % by weight or more. The lecithin used in the present invention is composed of (1) phospholipids such as phosphatidylcholine (PC), phosphatidylethanolamine (PE), and phosphatidylinositol (PI) and triglycerides, and is industrially known as lecithin. and (2) the above-mentioned PC, PE, and PI, particularly the phospholipids represented by PC. Lecithin has an emulsifying effect because its main components, such as PC, PE, and PI, have both hydrophilic and lipophilic functional groups in one molecule, and it is used for many purposes as an emulsifier. However, there is no knowledge regarding the stabilization of heat- and alkali-labile substances such as dipeptide sweeteners. not exist. As lecithin, soybean lecithin, rapeseed lecithin, corn lecithin, egg yolk lecithin, cottonseed lecithin, and others can be used without particular limitation, and these lecithins may be used alone or in combination. Since lecithin is separated and purified from the various oil seeds, egg yolks, etc., it often contains impurities other than phospholipids, particularly triglycerides. As mentioned above, lecithin in the present invention can be used even if it contains these impurities and has a low degree of purification, but lecithin with a high phospholipid ratio that has been sufficiently purified by deodorization, deacidification, decolorization, etc. should be used. This further improves the stability of the dipeptide sweetener. It goes without saying that acetylated lecithin, partially hydrolyzed lecithin, hydroxylated lecithin, and various other modified lecithins can be substituted for all or part of lecithin. The above lecithin can be used in any form such as powder, granules, liquid, etc. The amount of lecithin added is calculated based on the weight of phosphatidylcholine contained in the dipeptide sweetener.
Set it so that it is 50% by weight or more. In other words, if lecithin already exists in the raw material, a stabilizing effect can be obtained by adding the insufficient amount, but preferably purified lecithin is added in an equivalent amount or more to aspartame in terms of PC. Add so that If the lecithin content is too high, the taste, flavor, texture, etc. may be impaired;
PC content is 50% by weight compared to aspartame
Below this, the stabilizing effect is lacking. The oral preparation of the present invention contains a dipeptide sweetener alone or in combination with other sweeteners as a sweetener. The type of other sweeteners is not limited, but the combination with one or more types selected from acesulfum K, saccharin sodium, and stevia extract sweeteners,
preferable. In other words, these sweeteners cannot satisfy the sweetness quality by themselves, but when used in combination with dipeptide sweeteners, the sweetness quality, especially the aftertaste, is improved and the sweetness intensity is synergistically enhanced, so the overall sweetness is improved. A product can be provided that suppresses loss of sweet taste and loss of odor/taste masking effect after storage, and is advantageous in terms of cost. Aspartame is a preferred representative example of the dipeptide sweetener, but other α-L-aspartyl-L-phenylalanine lower alkyl esters can of course be used. The concentration of the dipeptide sweetener may be appropriately set depending on the desired degree of sweetness of the oral preparation, and is not particularly limited. The same applies to the concentration of other sweeteners when they are used together. Oral preparations targeted by the present invention include toothpaste,
water toothpaste, gargle, gum pine surge cream,
Mouth fresheners, mouth cleansers, etc., which include all drugs that are applied to the oral cavity, have a pH of 4.5.
In the above oral preparations, the stabilizing effect of the dipeptide sweetener of the present invention is particularly high. There are no particular limitations on the method and timing of adding lecithin as long as it is uniformly dispersed in the aqueous compartment of the final product. If the stability of the dipeptide sweetener decreases due to heating under low temperature, it is effective to add lecithin at least before or simultaneously with the addition of the dipeptide sweetener. Furthermore, if a dipeptide sweetener and lecithin are mixed and dissolved in advance and added, the effect will be even higher. In addition, when dipeptide sweeteners such as cyclodextrin (Japanese Patent Application No. 111304/1982) and sucrose fatty acid ester (Japanese Patent Application No. 58/23459) that have a water stability effect are used in combination, or when the pH is high, The pH of the dipeptide sweetener is adjusted to a value as close to the stable range of the dipeptide sweetener as possible without affecting its efficacy as an oral preparation, and the dipeptide sweetener is coated with an appropriate encapsulating agent. However, methods such as coexisting with lecithin are also effective. Next, the present invention will be further explained using experimental examples and examples. Experimental example 1 Add and mix 0.1% by weight of purified lecithin to an aqueous solution containing 50mg/dl of aspartame, and adjust the pH to 3.0 (experimental group 1)
and 6.5 (experimental group 2) as samples, and aspartame 50 whose pH was adjusted to 3.0 (control group 1) and 6.5 (control group 2) without the addition of purified lecithin.
Samples and controls were each bottled using an aqueous solution containing mg/dl as a control, and then heat treated at 80°C for 15 minutes and placed in a constant temperature bath at 44°C to measure the storage stability of aspartame. The results are shown in Table 1. In the case of pH 3.0, the lecithin-added area (experimental area 1) and the non-additive area (control area 1)
No difference was observed in the residual amount of aspartame between
Even after 20 days, more than 70% of aspartame remained in each sample, and the remaining amount of aspartame increased by about 1.5 times compared to the additive-free control (control group 2).

[Table] Purified lecithin Soybean lecithin is treated with acetone to remove neutral oil, and then the P and C categories are fractionated with a 95% ethanol aqueous solution, containing 83% PC and 7% neutral oil. there was. Experimental example 2 Purified lecithin (containing 83% PC) and acetylated lecithin ^* in an aqueous solution containing 50 mg/dl of aspartame
(Contains 20% PC) and adjusted the pH to 6.5 as a sample. Heat treated at 80℃ for 15 minutes together with the control in the same manner as in Experimental Example 1, then placed in a constant temperature bath at 44℃, and aspartame. The storage stability was measured. The results are shown in Table 2, and the results for purified lecithin and acetylated lecithin

[Experimental area]

The above experimental composition was added at once and thoroughly kneaded, then filled into a tube and sealed in a cap to prepare a toothpaste. [Experimental Group 2] First, the entire amount of aspartame and soy lecithin of the above experimental group composition was dissolved in 1/6 volume of water to prepare a sweetening solution, and then the entire composition except aspartame and soy lecithin was dissolved in water. After kneading with the remaining amount (5/6), the previously prepared sweetening solution was added and thoroughly kneaded, and the toothpaste was prepared as a prototype by filling a tube and sealing the cap. [Control Group] The above control group composition was added at once and thoroughly kneaded with a trowel, then filled into a tube and sealed with a cap to prepare a toothpaste. These prototype toothpastes were stored at 34℃ for 4 months.
The storage stability of aspartame was measured. The results are shown in Table 1.

[Experimental area]

Of the above experimental compositions, first dissolve all of aspartame, stevia extract sweetener, and acetylated lecithin in 1/5 volume of water to prepare a sweetening solution, then dissolve the entire composition except these in water. Remaining amount (4/
After kneading in step 5), the previously prepared sweetening solution was added and thoroughly kneaded, packed into a tube and sealed in a cap to produce a prototype toothpaste. [Control Group] The above-mentioned control group composition was added at once and thoroughly kneaded, then filled into a tube and sealed in a cap to prepare a toothpaste. These prototype toothpastes were stored at 34℃ for 6 months.
The storage stability of aspartame was measured, and the sweetness level was sensory evaluated. The results are shown in Table 2.

[Table] Compared to the control plot, where most of the aspartame was decomposed, the experimental plot had a residual rate of over 70%, and the taste was sufficiently sweet with almost no bitterness. This can be considered to be due to the fact that the addition of lecithin significantly improves the stability of aspartame, thereby suppressing the bitterness of stevia-extracted sweeteners and foaming agents. Furthermore, since the sweetness significantly decreased in the control group, it can be considered that the addition of lecithin also improves the stability of the stevia-extracted sweet product.

Claims (1)

[Claims] 1. Contains a dipeptide sweetener as all or a part of the sweetener, and contains lecithin in an amount of 50% or more by weight of the dipeptide sweetener in terms of phosphatidylcholine weight. An oral preparation containing a characteristic dipeptide sweetener. 2. Claim 1, characterized in that aspartame is used in combination with one or more sweeteners selected from acesulfum K., saccharin, saccalin sodium, and stevia extract sweeteners as sweeteners.
Oral preparation containing a dipeptide sweetener as described in 2. 3. The dipeptide sweetener-containing oral preparation according to claim 1, wherein the oral preparation is a toothpaste.