JP6008116B2 - Oral solution - Google Patents

Description

  The present invention relates to an internal liquid preparation containing an unsaturated fatty acid-containing polyglycerin fatty acid ester and vitamin B2, which can be used in the fields of pharmaceuticals, quasi drugs, health functional foods and foods.

  Polyglycerin fatty acid esters are widely used when dissolving fat-soluble ingredients in beverages and the like, and are highly versatile surfactants that are recognized not only for pharmaceuticals but also for foods.

  Vitamin B2 is known to have various medicinal effects and is widely incorporated in pharmaceuticals, quasi drugs, foods and the like. Depending on the purpose, it is blended with fat-soluble active ingredients.

  When using polyglycerin fatty acid ester as an internal solution, the physical properties such as hydrophilicity differ depending on the type of fatty acid that is a hydrophobic group and the degree of polymerization of polyglycerin that is a hydrophilic group. In general, a specific polyglycerin fatty acid ester is selected and used in accordance with physical properties.

  When the polyglycerin fatty acid ester whose hydrophobic group is an unsaturated fatty acid is used, the present inventors have suppressed the occurrence of suspended matters compared to the case where a polyglycerin fatty acid ester whose hydrophobic group is a saturated fatty acid is used. It was found that the long-term storage stability was excellent. Therefore, when an internal solution was prepared using a polyglycerin fatty acid ester whose hydrophobic group is an unsaturated fatty acid, when the hydrophobic group of the polyglycerin fatty acid ester is an unsaturated fatty acid, it gives off a unique odor and taste, I found that there was a problem in terms of points. Furthermore, when vitamin B2 was mix | blended simultaneously with the internal use liquid agent, it discovered that the increase in an unpleasant taste and an unpleasant odor was remarkable.

  Until now, the method of suppressing the unpleasant flavor which arises from the fats and oils containing an unsaturated fatty acid using a gallic acid etc. is disclosed. However, it is not known how the flavor is affected when polyglycerin fatty acid ester containing vitamin B2 and unsaturated fatty acid is blended simultaneously in the liquid preparation.

JP-A-8-23939

  This invention makes it a subject to suppress the unpleasant flavor which arises in the internal use liquid agent which mix | blended polyglyceryl fatty acid ester and vitamin B2 containing an unsaturated fatty acid simultaneously.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors have formulated propyl gallate in an oral solution containing polyglycerin fatty acid ester containing unsaturated fatty acid and vitamin B2 at the same time, By blending propyl gallate and a citrus fragrance, it was found that the unpleasant taste and unpleasant odor that occur over time are suppressed, and the unpleasant flavor is suppressed, and the present invention has been completed.

That is, the present invention
(1) An oral liquid preparation comprising a polyglycerin fatty acid ester containing an unsaturated fatty acid, vitamin B2, and propyl gallate,
(2) The internal liquid preparation according to (1), wherein the polyglycerol fatty acid ester containing an unsaturated fatty acid is a polyglycerol oleate ester,
(3) The internal liquid preparation according to (1), further comprising a citrus fragrance,
(4) A method for suppressing an unpleasant flavor of an oral liquid containing a polyglycerin fatty acid ester containing vitamin B2 and an unsaturated fatty acid, characterized by containing propyl gallate
(5) The method for suppressing unpleasant flavor according to (4), further comprising a citrus flavor.
It is.

  According to the present invention, it was possible to suppress the unpleasant taste and unpleasant odor that occurred over time in the internal liquid preparation containing polyglycerin fatty acid ester containing an unsaturated fatty acid and vitamin B2 at the same time, and to suppress the unpleasant flavor.

It is the figure which showed the sensory evaluation result of the unpleasant odor of the comparative examples 1-4 of the test example 1, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. It is the figure which showed the sensory evaluation result of the unpleasant taste of the comparative examples 1-4 of the test example 1, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. It is the figure which showed the sensory evaluation result of the unpleasant odor of the comparative example 2 of the test example 2, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. It is the figure which showed the sensory evaluation result of the unpleasant taste of the comparative example 2 of the test example 2, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. It is the figure which showed the sensory evaluation result of the unpleasant odor of the comparative example 5 of the test example 3, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. It is the figure which showed the sensory evaluation result of the unpleasant taste of the comparative example 5 of the test example 3, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. FIG. It is the figure which showed the sensory evaluation result of the unpleasant taste of Comparative Examples 6-8 of Test Example 4, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 4. It is the figure which showed the sensory evaluation result of the unpleasant odor of the comparative examples 6-8 of the test example 4, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 4. It is the figure which showed the sensory evaluation result of the unpleasant odor of Examples 1-3 of Test Example 5 and Comparative Examples 6 and 9, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. FIG. It is the figure which showed the sensory evaluation result of the unpleasant taste of Examples 1-3 of Test Example 5 and Comparative Examples 6 and 9, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 3. FIG. It is the figure which showed the sensory evaluation result of the unpleasant odor of Examples 4-9 of Test Example 6, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 4. It is the figure which showed the sensory evaluation result of the unpleasant taste of Examples 4-9 of Test Example 6, and a vertical axis | shaft is the sensory evaluation criteria shown in Table 4.

  The polyglycerol fatty acid ester containing an unsaturated fatty acid in the present invention is a polyglycerol obtained by polymerizing 4 to 20 glycerol and 8 to 20 carbon atoms, and one to three carbon-carbon double bonds. This ester is a condensed fatty acid. Specific examples include polyglycerin oleate, polyglycerin linoleic acid ester, polyglycerin linolenic acid ester, and the like. Examples of polyglycerin oleate include dodecaglycerin oleate, decaglycerin oleate, hexaglycerin oleate, etc., and polyglycerin linoleate as dodecaglycerin linoleate, decaglycerin linoleate. And hexaglycerin monolinoleic acid ester. Examples of the polyglycerin linolenic acid ester include dodecaglycerin linolenic acid ester, decaglycerin linolenic acid ester, and hexaglycerin monolinolenic acid ester. Among these, polyglycerin oleate is particularly preferable.

  In the internal use liquid preparation of the present invention, the blending amount of the polyglycerin fatty acid ester containing an unsaturated fatty acid is preferably 0.0001% by mass to 10% by mass, more preferably 0.001% by mass to 1% with respect to the total internal use liquid preparation. % By mass.

  Vitamin B2 used in the present invention is usually edible. Specific examples include riboflavin, riboflavin phosphate, riboflavin butyrate, and salts thereof. The compounding quantity of vitamin B2 in this internal use liquid preparation is 0.00005 mass% (W / V%)-5 mass% (W / V%) of the whole internal use liquid preparation, 0.0001 mass%-1 mass%. More preferably, 0.0005% by mass to 0.5% by mass is most preferable.

  In the internal use liquid preparation according to the present invention, the amount of propyl gallate is usually 0.0001 parts by mass to 10,000 parts by mass, preferably 0.001 parts by mass to 5000 parts by mass with respect to 1 part by mass of vitamin B2. More preferably, it is 0.01 mass part-1000 mass parts.

  The citrus fragrance used in the present invention is not particularly limited as long as it has a fragrance equivalent to a processed product of the citrus genus, kumquat genus, and karatachi genus of the citrus family. Specific examples include orange flavor, lime flavor, grapefruit flavor, and mandarin flavor. As these fragrances, any of natural fragrances, synthetic fragrances, and blended fragrances can be used, and they can be obtained industrially. The compounding quantity of these fragrance | flavors in the drink of this invention is 0.001-1 mass% with respect to the whole internal use liquid agent, Preferably it is 0.01-0.5 mass%.

  The preferred pH of the internal solution of the present invention is 2.5 to 7.0. This is because a pH of less than 2.5 is not preferable in terms of commercial properties. For adjusting the pH, for example, citric acid, malic acid, fumaric acid, tartaric acid, lactic acid, salts of organic acids such as succinic acid, inorganic acids such as phosphoric acid, hydrochloric acid, sodium hydroxide, potassium hydroxide, etc. Inorganic bases can be used.

Moreover, you may mix | blend a fat-soluble component with the internal use liquid agent of this invention. As fat-soluble components, vitamins such as vitamin A, vitamin D, vitamin E, vitamin K, riboflavin acetate and γ-oryzanol and their derivatives, medium chain fatty acid triglycerides such as caprylic acid triglyceride and tri (caprylic / capric acid) glyceryl And herbal medicine extracts such as triglycerin fatty acid esters such as γ-linolenic acid, herbal medicine dry powder, extract extract, flow extract, and the like.
Herbal medicines include Ikarisou, Ogi, Ousei, Onji, Kaikujin, Kaiba, Kashiwa, Kanzo, Kukoshi, Keihi, Gooh, Garbage, Psycho, Sanyaku, Sanshuyu, Giou, Peonies, Jashoushi, Shukusha, Shokyo, Jyoshi, Senkyu, Examples include Taisou, Chinpi, Toki, Tochukaso, Toshishi, Tochu, Tochu, Nikujuyo, Carrot, Bakumondo, Vulture, Hampi, Byakutsu, Bukkyou, Muirapuama, Yokuinin, Ryuganiku, Rokujo and the like.

  Vitamins, minerals, herbal medicines, herbal extracts and the like can be appropriately added to the internal liquid preparation of the present invention as long as the effects of the present invention are not impaired. In addition, additives such as sweeteners, colorants, fragrances, surfactants, solubilizing agents, preservatives and the like can be appropriately blended as necessary so long as the effects of the present invention are not impaired. These additives and the like may be blended singly or in combination of two or more.

  The method for preparing the internal liquid preparation of the present invention is not particularly limited as long as the effects of the present invention are exhibited. Usually, after dissolving each component with an appropriate amount of purified water, the pH and volume are adjusted to the remaining purified water. It is the method of adding and adjusting, and filtering and sterilizing as needed. The method of blending vitamin B2 and propyl gallate is not particularly limited and is the same as other components.

  Moreover, when mix | blending a fat-soluble component with the internal use liquid agent of this invention, it manufactures as follows, for example. Water is mixed with the polyglycerin fatty acid ester containing the fat-soluble component and the unsaturated fatty acid, and the mixture is heated and stirred until the entire stirring tank becomes uniform. Regarding the heating temperature, it is sufficient that the entire stirring tank is uniform, but depending on the type of polyglycerin fatty acid ester containing unsaturated fatty acid, there are solid and semi-solid states at room temperature, which increases fluidity during stirring and mixing. Therefore, 70 degreeC or more is preferable if possible.

  The internal liquid preparation of the present invention can be provided as, for example, pharmaceutical products such as syrups and drinks, designated quasi-drugs, health functional foods and foods.

Hereinafter, the present invention will be described in more detail with reference to Examples, Comparative Examples, and Test Examples, but the present invention is not limited to these Examples.
In Tables 1 and 2 below, Examples 1 to 9 and Comparative Examples 1 to 9 are shown. Each component of the formulation described in Tables 1 and 2 was weighed and dissolved in purified water, and the pH was adjusted to 3.0, and the total amount of internal solution was adjusted to 100 mL. After that, it filled into the glass bottle, the cap was given, and the internal use liquid agent of Examples 1-9 and Comparative Examples 1-9 was obtained.

Test example 1
Evaluation of the intensity of unpleasant odor and unpleasant taste immediately after the preparation of the internal liquid preparations having the compositions shown in Comparative Examples 1 to 4 shown in Table 2 was performed by 6 specialist panels. Sensory evaluation was performed according to the criteria in Table 3, and the average value was obtained. The results are shown in FIGS.

  As is apparent from the experimental results shown in FIG. 1 and FIG. 2, Comparative Example 2 in which a surfactant containing oleic acid, which is an unsaturated fatty acid, was blended, Comparative Example 1 in which no surfactant was blended, and unsaturated It was found that the unpleasant flavor and unpleasant odor were specifically strong as compared with Comparative Examples 3 and 4 containing a polyglycerin fatty acid ester not containing a fatty acid.

Test example 2
Evaluation of strength of unpleasant odor and unpleasant taste of preparations for internal liquids having the composition shown in Comparative Example 2 shown in Table 2 after heating at 65 ° C. for 3 days and storage without adjustment at 5 ° C. It was conducted by 6 specialist panels. Sensory evaluation was performed according to the criteria in Table 3, and the average value was obtained. The results are shown in FIGS.
As is apparent from the experimental results shown in FIGS. 3 and 4, in Comparative Example 2 in which a surfactant containing oleic acid, which is an unsaturated fatty acid, was blended, the unpleasant odor may increase over time due to heat. I understood.

Test example 3
Unpleasant odors of preparations of internal liquids having the composition shown in Comparative Example 5 shown in Table 2 that were stored at 5 ° C. without being irradiated with light and those that were irradiated with 600,000 lx · hr of light after preparation with a white fluorescent lamp And the evaluation of the intensity of unpleasant taste was performed by 6 specialist panels. Sensory evaluation was performed according to the criteria in Table 3, and the average value was obtained. The results are shown in FIGS.
As is apparent from the experimental results shown in FIGS. 5 and 6, Comparative Example 5 containing a surfactant containing oleic acid, which is an unsaturated fatty acid, has an unpleasant odor and unpleasant taste due to light irradiation over time. It turned out to increase.

Test example 4
After preparing the oral solution of the composition shown in Table 2 in Comparative Examples 6 to 7 and stored at 65 ° C. for 1 day, the unpleasant odor and unpleasant taste of the composition shown in Comparative Example 5 after preparation of the internal solution of 65 ° C. for 1 day Comparative Example 5 shows the unpleasant odor and unpleasant taste of the results of relative evaluation with the stored ones and those irradiated with 600,000 lx · hr of light with a white fluorescent lamp after preparing the internal liquid preparations of the compositions shown in Comparative Examples 6-8. 7 and FIG. 8 show the results of a relative evaluation of the internal liquid preparation having the composition shown in FIG. 7 that was irradiated with 600,000 lx · hr of light with a white fluorescent lamp. The evaluation was performed according to the criteria shown in Table 4 by 6 expert panels, and the average value was obtained.

  As is apparent from the experimental results shown in FIGS. 7 and 8, Comparative Examples 6 to 8 in which vitamin B2 was added in addition to the surfactant containing oleic acid, which is an unsaturated fatty acid, were not compared with vitamin B2. It was found that the unpleasant odor and unpleasant taste were stronger than Example 5.

Test Example 5
The evaluation results of the intensity of unpleasant odor and unpleasant taste of preparations of internal liquid preparations of the compositions shown in Examples 1 to 3 shown in Table 1 and Comparative Examples 6 and 9 shown in Table 2 were stored at 65 ° C. for 1 day. It was done by a specialized panel of names. Sensory evaluation was performed according to the criteria in Table 3, and the average value was obtained. The results are shown in FIGS.
As apparent from the experimental results shown in FIGS. 9 and 10, in addition to the surfactant containing oleic acid, which is an unsaturated fatty acid, propyl gallate is added as an unpleasant flavor that occurs when vitamin B2 is added. (Examples 1 to 3), and the effect was found to be remarkable compared with cyclodextrin (Comparative Example 9) generally used for masking of unpleasant flavors.

Test Example 6
After preparing the internal liquid preparations having the compositions shown in Examples 1 and 4 to 9 shown in Table 1, 600,000 lx · hr of light was irradiated with a white fluorescent lamp. The result of relatively evaluating Examples 4 to 9 and the intensity of unpleasant odor and unpleasant taste were evaluated by Example 6 with respect to Example 1. Sensory evaluation was performed based on the criteria in Table 4, and the average value was obtained. The results are shown in FIGS.
As is apparent from the experimental results shown in FIGS. 11 and 12, Examples 4 to 9 to which fragrance was added in addition to propyl gallate further suppressed unpleasant flavor as compared to Example 1 to which fragrance was not added. Although it was able to be done, it turned out that especially when a citrus fragrance | flavor (Examples 7-9) is added, the inhibitory effect of an unpleasant flavor is remarkable.

Examples 10 and 11
Table 5 below shows the formulations of Examples 10 and 11. Each component described in Table 5 was weighed, and vitamin E and carrot extract, which are fat-soluble components, were mixed with polyglycerin oleate and heated and stirred until the entire stirring tank was uniform. Then, it was made to melt | dissolve in purified water with other components, and it adjusted so that pH might be set to 3.0 and the total amount of internal use liquid agent might be 100 mL. Thereafter, it was filled into a glass bottle and a cap was applied to obtain an internal solution.

  According to the present invention, it is possible to produce an internal liquid preparation containing an unsaturated fatty acid-containing polyglycerin fatty acid ester and vitamin B2 at the same time. Therefore, in the fields of pharmaceuticals, designated quasi drugs, foods, etc. It is expected to provide a liquid composition containing a polyglycerin fatty acid ester and a vitamin B2 containing an unsaturated fatty acid.

Claims (5)

  An oral liquid preparation comprising a polyglycerin fatty acid ester containing an unsaturated fatty acid, vitamin B2, and propyl gallate.   The internal liquid preparation according to claim 1, wherein the polyglycerol fatty acid ester containing an unsaturated fatty acid is a polyglycerol oleate.   Furthermore, citrus fragrance | flavor was mix | blended, The internal use liquid agent of Claim 1 characterized by the above-mentioned.   A method for suppressing an unpleasant flavor of an oral solution containing a polyglycerin fatty acid ester containing vitamin B2 and an unsaturated fatty acid, characterized by containing propyl gallate.   Furthermore, the unpleasant flavor suppression method of Claim 4 which mix | blended the citrus fragrance | flavor.

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