JP6769052B2 - Taurine-containing composition - Google Patents

Description

The present invention relates to a composition containing taurine or a derivative thereof and an α-amino acid or a salt thereof and being basic.

Many biological and chemical substances are sensitive to pH, and it is necessary to control the pH when handling them. In the preparation of pharmaceuticals, quasi-drugs, and cosmetics, the pH greatly contributes to the stability of the active ingredient and the base ingredient, so it is important to maintain the preparation at the target pH.

However, the pH of pure water easily fluctuates due to external factors such as carbon dioxide in the atmosphere and internal factors such as metabolites of microorganisms themselves, so long-term use in an environment where contamination is likely to occur. Is unsuitable. In such cases, a buffer is often used as a method of keeping the pH of the solution constant. The buffer solution is generally an aqueous solution in which a weak acid and its salt coexist, and has the effect that the pH hardly changes even if a small amount of acid or base is added or the concentration changes due to evaporation or dilution. ..

Generally, organic acids such as succinic acid, tartaric acid, citric acid, and acetic acid are widely used as substances having a buffering ability, but all of these are substances having a buffering ability in a weakly acidic region and are in a weakly basic region. There are few substances that have a buffering capacity. It is known that boric acid, triethanolamine, sodium carbonate, etc. have a buffering capacity in the weakly basic region, but boric acid is irritating to the skin, and triethanolamine produces coloring and a unique amine odor. Since sodium carbonate may generate carbon dioxide gas, it has been difficult to prepare a stable preparation having a weakly basic buffering capacity.

Taurine is known to be effective in improving rough skin, moisturizing, hair growth, etc., and is also used as an active ingredient in external compositions targeting skin and hair. Since the aqueous solution in which taurine is dissolved exhibits weakly acidic properties, the taurine-containing composition is usually used in a weakly acidic region having a pH of about 5 to 6 (Patent Document 1). On the other hand, in external compositions such as cosmetics, there is a need to use them in the basic region for the purpose of skin-beautifying effect and the like.

Japanese Unexamined Patent Publication No. 2012-20994

When the taurine-containing composition was produced in the basic region, a problem was found that the pH decreased over time. The present invention is to provide a stable basic composition containing taurine or a derivative thereof while suppressing a decrease in pH over time.

As a result of intensive studies to solve the above problems, the present inventors have found that by blending taurine or a derivative thereof with α-amino acid or a salt thereof under basic conditions, the pH decrease of the preparation is suppressed. , The present invention has been completed.

That is, the present invention comprises (1) taurine or a derivative thereof, and an α-amino acid or a salt thereof, which is a basic composition.
(2) The composition according to (1), wherein the α-amino acid or a salt thereof contains at least one selected from those contained in a living body.
(3) The description according to (1) or (2), wherein the α-amino acid contains at least one selected from glycine, alanine, arginine, lysine, proline, isoleucine, histidine, serine, valine and glutamic acid. Composition,
(4) The composition according to any one of (1) to (3), wherein the α-amino acid contains at least one selected from alanine, arginine, lysine, isoleucine, valine and glutamic acid.
(5) The composition according to any one of (1) to (4), which has a pH of 8 to 11.

INDUSTRIAL APPLICABILITY According to the present invention, it has become possible to provide a stable basic composition containing taurine or a derivative thereof, which suppresses a decrease in pH over time.

One aspect of the present invention is a composition containing taurine or a derivative thereof, and α-amino acid or a salt thereof, which is basic.

The taurine used in the present invention is conventionally used in pharmaceuticals, quasi-drugs, and cosmetics, and is not particularly limited, and includes any of synthetic products and extracts from natural products. In addition, the taurine derivative of the present invention also includes hypotaurine, thiotaurine, and salts thereof. The blending amount of taurine or a derivative thereof is preferably 0.01% by mass to 10% by mass, more preferably 0.1% by mass to 5% by mass, and further preferably 0.5% by mass to 3% by mass in the composition. .. This is because if it is 0.01% by mass or less, the effect may not be expected, and if it is 10% by mass or more, it may be difficult to formulate from the viewpoint of solubility.

The α-amino acid or a salt thereof used in the present invention is conventionally used in pharmaceuticals, non-pharmaceutical products, and cosmetics, and is not particularly limited, but glycine, aspartic acid, alanine, glutamic acid, valine, glutamine, Includes leucine, arginine, isoleucine, lysine, serine, histidine, threonine, phenylalanine, cysteine, tyrosine, methionine, tryptophan, aspartic acid, proline. Glycine, alanine, arginine, lysine, proline, isoleucine, histidine, serine, valine or glutamic acid, or salts thereof are more preferable, and glycine or alanine is further preferable, from the viewpoint of suppressing the pH decrease with time. A basic composition containing taurine or a derivative thereof causes a problem that the composition is colored as the pH decreases with time. However, suppression of pH decrease with time and suppression of coloration of the preparation with time 2 From the viewpoint of simultaneously exerting the two effects, alanine, arginine, lysine, isoleucine, valine or glutamic acid are particularly preferable. One or more kinds of α-amino acid or a salt thereof can be blended, and the blending amount is preferably 0.001% by mass to 10% by mass, more preferably 0.01% by mass to 5% by mass in the composition. , More preferably 0.1% by mass to 3% by mass. This is because if it is 0.001% by mass or less, the effect may not be expected, and if it is 10% by mass or more, it may be difficult to formulate from the viewpoint of solubility.

The storage container for the composition of the present invention is generally used for pharmaceuticals, quasi-drugs, and cosmetics, and is not particularly limited. Materials such as PET, glass, polyethylene, polypropylene, aluminum, and aluminum laminates are used. Is particularly preferable.

The pH of the composition of the present invention is basic, greater than 7, preferably 7.5-11, more preferably 8-11, and even more preferably 9-10.5. This is because there is a concern of skin irritation at pH 11 or higher.

The composition of the present invention can be used mainly as an external composition for cosmetics and the like. The dosage form of the composition of the present invention is not particularly limited, and examples thereof include liquids, lotions, emulsions, creams, aqueous gels, ointments, and aerosols. These preparations can be prepared by a conventional method. In addition, the composition of the present invention can be used as a pack, a sunscreen lotion, a sunscreen lotion, a sunscreen cream, a sunscreen cream, and the like.

Liquids and lotions can be prepared by dissolving and dispersing taurine or a derivative thereof, and α-amino acid or a salt thereof in water, ethanol, polyhydric alcohol or a mixture thereof. Further, it is also possible to prepare an aerosol agent by putting such a liquid agent and an appropriate liquefied gas (liquefied petroleum gas, dimethyl ether, etc.) in an aluminum pressure-resistant container. It is also possible to prepare an aqueous gel preparation by blending an appropriate gelling agent with such a liquid preparation.
For creams and emulsions, taurine or its derivatives, α-amino acids or salts thereof, surfactants, and water-soluble components are dissolved in water and heated to form an aqueous phase, and oily components and surfactants are separately heated. To be the oil phase. The oil phase and the aqueous phase can be combined, emulsified and cooled to obtain a preparation. O / W creams and emulsions can be prepared by using a surfactant having a high HLB, and W / O creams and emulsions can be prepared by using a surfactant having a low HLB.

The ointment is prepared by heating oily components such as petrolatum, beeswax and stearyl alcohol to form an oil phase, and separately dissolving or dispersing taurine or a derivative thereof and α-amino acid or a salt thereof in a liquid component to form a main drug phase. .. An oily ointment can be prepared by adding the main drug phase to the oil phase, mixing and cooling. Further, macrogol 4000 is heated to make a solution, and taurine or a derivative thereof, and α-amino acid or a salt thereof are separately dissolved or dispersed in liquid macrogol 400 to serve as the main drug phase. The main drug phase can be added to the solution of Macrogol 4000 and mixed and cooled to obtain a water-soluble ointment.

In addition to the above, the composition of the present invention includes tar pigments, coloring pigments such as iron oxide, preservatives, silicone oils, vegetable oils, lower alcohols, higher fatty acids, terpenes, anionic surfactants, and nonionic surfactants. Agents, cationic surfactants, amphoteric surfactants, natural surfactants, pigments, antioxidants, inorganic salts, organic acids and their salts, organic amines and their salts, chelating agents, thickeners, neutralizing Agents, UV absorbers, polyhydric alcohols, various amino acids, vitamin derivatives and the like can be appropriately blended within the range of achieving the object of the present invention.

Further, one aspect of the present invention is a method of suppressing a decrease in pH of the composition over time by adding an α-amino acid or a salt thereof to a basic composition containing taurine or a derivative thereof.

In addition, one aspect of the present invention is a pH regulator under basic conditions containing α-amino acid or a salt thereof, more preferably taurine or a derivative thereof, and basicity containing α-amino acid or a salt thereof. A pH regulator under conditions.

Hereinafter, the present invention will be described in detail with reference to Examples, Comparative Examples and Test Examples, but the present invention is not limited to the following examples. In the examples and comparative examples, the unit of the numerical values in the table is "g".

The composition of the present invention was prepared by weighing each component according to the formulation shown in Table 1, adding purified water to a total volume of 100 g, and stirring and dissolving the mixture. Each composition was adjusted to the desired pH by adding an appropriate amount of sodium hydroxide.

(Test Example 1)
After storing the compositions of Examples 1 to 17 and Comparative Examples 1 and 2 at 65 ° C. for 1 week, the pH at 25 ° C. and the absorbance at 400 nm were measured, and the difference from the pH at the start of the test was calculated.
The results are shown in Tables 2 and 3.

As shown in Tables 2 and 3, the formulations containing taurine and α-amino acids (Examples 1 to 17) suppress the decrease in pH over time as compared with the formulations of taurine alone (Comparative Examples 1 and 2). I was able to.
In addition, from the viewpoint of simultaneously exerting the two effects of suppressing the decrease in pH over time and suppressing the coloring of the preparation over time, in a formulation containing alanine, arginine, lysine, isoleucine, valine or glutamic acid together with taurine. An excellent effect was observed.

The composition of the present invention was prepared by weighing each component according to the formulation shown in Table 4, adding purified water to a total volume of 100 g, and stirring and dissolving the mixture. Each composition was prepared so that the amino acid concentration was 0.02 mol / 100 g.

(Test Example 2)
0.5N hydrochloric acid was added dropwise to the compositions of Examples 18 and 19 and Comparative Examples 3 to 5, the amount of hydrochloric acid required to lower the pH of the composition from 10 to 8 was calculated, and 1 mol of amino acids in the preparation was calculated. Converted as the amount for. The results are shown in Table 5.

As shown in Table 5, the formulations containing taurine and α-amino acids (Examples 18 and 19) adjusted the pH of the formulations from 10 to 8 as compared with the formulations of taurine and α-amino acids alone (Comparative Examples 3 to 5). Since a large amount of hydrochloric acid was required to reduce the pH, it was found that the pH decrease when hydrochloric acid was added dropwise was suppressed.

INDUSTRIAL APPLICABILITY According to the present invention, it has become possible to provide a stable basic composition containing taurine or a derivative thereof while suppressing a decrease in pH over time. Therefore, the development of the pharmaceutical and cosmetics industries is expected through the marketing of basic preparations with higher commercial value.

Claims (2)

A basic external composition containing taurine , hypotaurine or thiotaurine or salts thereof, and at least one α-amino acid selected from alanine, arginine, lysine, isoleucine, valine and glutamic acid or a salt thereof. The composition according to claim 1 , which has a pH of 8 to 11.