TW201919591A - Alopecia relaxation composition including an apigenin with improved solubility - Google Patents

Abstract

The present invention relates to an alopecia relaxation composition including an apigenin with improved solubility, wherein the solubility of the apigenin is increased to enhance the apigenin concentration in the composition. The alopecia relaxation composition includes an apigenin, a polar oil, polyhydric alcohol and monatomic alcohol as active ingredients, wherein the cLog P value of the polar oil is 1 to 5.

Description

Relaxation composition with improved stability and apigenin

The present invention relates to a hair loss alleviation composition including apigenin, and more specifically, it relates to a hair loss alleviation composition including apigenin which improves the solubility of apigenin to increase the concentration of apigenin in the composition. .

Apigenin, as a poorly soluble flavonoid, stimulates hair growth through various biological pathways to increase hair thickness, reduce the generation of white hair, and provides a rich appearance of hair. It is known as the main component to ease hair loss (see Paper Dermatol Res. (2009) 301: 381-385). However, apigenin does not dissolve when applied to a conventional cosmetic composition, and it is extremely difficult to prepare a composition in which an effective amount of apigenin is dissolved due to the problem of precipitation during long-term storage. On the other hand, a technique for dissolving apigenin by using a large amount of ethanol, a surfactant, and a polyhydric alcohol is known. However, when the composition as described above is used, there is a problem that it is not only difficult to express a light feeling, but also Excessive irritation of the scalp due to high levels of alcohol (ethanol). From this viewpoint, there is an urgent need to develop a hair care composition that can increase the concentration of an effective hair growth stimulant, namely apigenin, in order to improve the appearance of the hair, and also to get rid of excessive scalp irritation.

[Prior Art Literature] [Patent Literature] (Patent Literature) Japanese Patent Publication No. 2007-197328 [Non-Patent Literature] (Non-Patent Literature) Dermatological Research Literature (2009) 301: 381-385

[Problems to be Solved by the Invention]

An object of the present invention is to provide a hair loss alleviating composition comprising apigenin with improved solubility, using a polar oil to increase the solubility of apigenin, and preventing precipitation of apigenin.

Another object of the present invention is to provide a hair loss alleviating composition including apigenin with improved solubility, which can minimize scalp damage by reducing the content of the alcohol component as compared with the prior art.

[Means for solving problems]

In order to achieve the above object, the present invention provides a hair loss alleviating composition including apigenin with improved solubility, which includes apigenin, a polar oil, a polyhydric alcohol, and a monohydric alcohol as active ingredients, and the cLog P value of the polar oil is 1 to 5.

[Effect of the invention]

According to the present invention, a hair loss alleviating composition comprising apigenin with improved solubility, including polar oil in the composition, thereby improving the solubility of apigenin and preventing precipitation, and reducing the content of alcohol components to minimize scalp damage. In addition, the composition described above has a thin and light usability and can be prepared as a single-layer transparent dosage form.

Hereinafter, the present invention will be described in detail.

The hair loss alleviation composition comprising apigenin with improved solubility includes apigenin, a polar oil, a polyhydric alcohol, and a monohydric alcohol as active ingredients, and the cLog P value of the polar oil is 1 to 5.

The above-mentioned apigenin is known as a poorly soluble flavonoid and is contained in various plants and exhibits an antioxidant effect or a brain cell production and protection effect. Not only that, apigenin increases hair thickness by stimulating hair growth through various biological pathways, reduces the generation of white hair, and provides a rich appearance of hair. Apigenin is also used as a main ingredient to ease hair loss.

The content of the above-mentioned apigenin is 0.1 to 1% by weight, preferably 0.2 to 0.8% by weight, and more preferably 0.4 to 0.6% by weight based on the entire composition. When the content of apigenin is less than 0.1% by weight with respect to the overall composition, the hair loss alleviation effect (hair growth effect) achieved by apigenin is small, and when it exceeds 1% by weight, it is used in mass production. The solubility of apigenin may be lowered by other ingredients, the stability of the composition may be deteriorated, or scalp irritation may be caused by a high concentration of apigenin. Here, the reason for setting the lower limit of the apigenin content to 0.1% by weight is that the applicant of the present case tested the germinal efficacy of apigenin, and as a result, confirmed that the use of apigenin in an amount of 10 ppm to 20 ppm promoted Wnt Activity, when it is applied to the human body, it is analyzed that it needs to be used in an amount of 250 to 1,000 times. When it is applied to the present invention in the same way, at least 0.1% by weight of apigenin must be included to show the effect of birth hair. Therefore, the content is set to the lower limit as described above.

The polar oil not only improves the solubility of the apigenin to increase the concentration of apigenin in the composition, but also prevents precipitation of apigenin even if the composition is stored for a long period of time at normal temperature and low temperature. In order to perform the functions as described above, the cLog P value used for verifying the degree of hydrophilicity of the above-mentioned polar oil compound must satisfy 1 to 5, preferably converge to the cLog P value (2.90) of apigenin, in order to dissolve more easily Apigenin.

On the other hand, the above "cLog P" refers to a software calculation value of a general distribution coefficient (LogP). Here, the distribution coefficient is a degree indicating which solution the target substance is more soluble in octanol and water, and the LogP value. A higher value means more soluble in octanol (higher hydrophobicity), and a lower LogP value means more soluble in water (stronger hydrophilicity). In addition, c is an abbreviation for calculate, which means that it is obtained by calculation.

Examples of the polar oil having the above-mentioned properties include succinate-based oils. More specific examples include diethoxyethyl succinate and dioctyl succinate. Dicarpryl Succinate) and Diethyl Succinate. The content of the polar oil is 10 to 30% by weight, and preferably 15 to 30% by weight based on the entire composition. When the content of the polar oil is less than 10% by weight with respect to the overall composition, the solubility or stability of apigenin may decrease. When the content exceeds 30% by weight, it may be oily and uncomfortable when used. Used as a cosmetic.

The above-mentioned polyhydric alcohol is also a component used to dissolve the above-mentioned apigenin, and examples thereof include glycerol, 1,3-butylene Glycol, Propylene Glycol, and polyethylene glycol. Polyol Glycol, Dipropylene Glycol and Propanediol can be used alone or as a mixture of two or more of them. The content of the above-mentioned polyhydric alcohol is 5 to 20% by weight, and preferably 10 to 20% by weight based on the entire composition. When the content of the polyhydric alcohol is less than 5% by weight with respect to the entire composition, the solubility or stability of apigenin may decrease. When the content exceeds 20% by weight, it may be oily and uncomfortable to use. Used as a cosmetic.

The monohydric alcohol is the same component as the polar oil and the polyhydric alcohol used to dissolve the apigenin. A general monohydric alcohol compound can be used, but it is preferred to use ethanol, n-butanol, and isobutanol as examples. Lower alcohols having 2 to 5 carbons, the most preferred of which is ethanol. The content of the above-mentioned monohydric alcohol is 20 to 50% by weight, and preferably 30 to 50% by weight based on the entire composition. When the content of the monohydric alcohol is less than 20% by weight with respect to the overall composition, the solubility or stability of apigenin will decrease, and when it exceeds 50% by weight, the solubility or stability of apigenin will decrease. It may increase, but may cause irritation to the scalp and skin. On the other hand, the hair loss reducing composition of the present invention has the advantage of reducing the content of alcohol components compared with the conventional hair loss reducing agents, and also has the advantage of minimizing damage to the scalp.

On the other hand, the aforementioned hair loss alleviating composition may be generally used in the industry, including distilled water and purified water, if necessary (that is, when the total content of apigenin, polyol, monoalcohol, and polar oil is less than 100% by weight). Water. In addition, the hair loss alleviation composition of the present invention may include any one or more additives generally used in the industry, such as an appropriate amount of a pigment, a preservative, and a fragrance, within the range of maintaining the stability of the composition, if necessary.

On the other hand, the hair loss alleviating composition of the present invention exhibits a turbidity of 1 NTU to 5 NTU (Nepthelometric Turbidity Unit), preferably 1.10 NTU to 5 NTU. In addition, the hair loss alleviating composition of the present invention can be formulated into a hair nourishing agent or a hair nourishing lotion, etc., but it is most preferably a dosage form into a hair nourishing agent.

The hair loss alleviating composition including apigenin with improved solubility as described above includes polar oils having specific physical properties, thereby having the advantages of not only improving the solubility of apigenin and preventing precipitation, but also reducing the content of alcohol components as compared with before In addition, the scalp damage is minimized, and in addition, it has a thin and light use feeling, which can double the user's satisfaction, and can be prepared into a single-layer transparent dosage form.

In the following, preferred embodiments are provided to help understand the present invention. However, the following embodiments are merely examples of the present invention. Those skilled in the art should understand that various changes and modifications can be made within the scope of the present invention and the technical idea. Of course, such changes and amendments also fall within the scope of the accompanying invention application patent.

[ Examples 1] Preparation of hair loss relief composition

First, according to the composition of Table 1 below, 0.5% by weight of apigenin, 20% by weight of dipropylene glycol (polyol), 49.5% by weight of ethanol (monohydric alcohol), and 30% by weight of cLog P value of 1.42 Diethoxyethyl succinate (polar oil) is supplied to the container. At this time, each time the raw materials are charged, they are heated to 60 ° C and homogenously mixed at a speed of about 3,600 rpm (HOMOGENIZING MIXER). (Model) 2.5, Manufacturing company: PRIMIX, Country: United States) More than 1 minute. Next, after supplying water heated to 60 ° C., the mixture was mixed at a speed of about 3,600 rpm for 10 minutes to prepare a hair loss reducing composition.

[ Examples 2] Preparation of hair loss relief composition

The content of dipropylene glycol (polyol) was changed from 20% by weight to 10% by weight, the content of ethanol (monohydric alcohol) was changed from 49.5% by weight to 30% by weight, and diethyl succinate was changed, as in the composition of Table 1 below. The content of oxyethyl ester (polar oil) was changed from 30% by weight to 15% by weight, and the rest was performed using water. The same procedure as in Example 1 was performed to prepare a hair loss reducing composition.

[ Comparative example 1] Preparation of hair loss relief composition

Except that water was used instead of the monohydric alcohol and the polar oil like the composition in Table 1 below, it was performed in the same manner as in Example 1 to prepare a hair loss alleviating composition.

[ Comparative example 2] Preparation of hair loss relief composition

The water-reducing composition was prepared in the same manner as in Example 1 except that water was used instead of the polyol and the polar oil as in the composition of Table 1 below.

[ Comparative example 3] Preparation of hair loss relief composition

Except that water was used instead of the polyhydric alcohol and the monohydric alcohol as in the composition of Table 1 below, it was carried out in the same manner as in Example 1 to prepare a hair loss reducing composition.

[ Comparative example 4] Preparation of hair loss relief composition

A hair loss reducing composition was prepared in the same manner as in Example 1 except that water was used instead of the polar oil as in the composition of Table 1 below.

[ Comparative example 5] Preparation of hair loss relief composition

A hair loss reducing composition was prepared in the same manner as in Example 1 except that water was used instead of the polyol as in the composition of Table 1 below.

[ Comparative example 6] Preparation of hair loss relief composition

Except that water was used instead of the monohydric alcohol as in the composition of Table 1 below, it was carried out in the same manner as in Example 1 to prepare a hair loss reducing composition.

[ Comparative example 7] Preparation of hair loss relief composition

An ester oil (C12-15 alkyl benzoate) was used instead of diethoxyethyl succinate as a polar oil as in the composition of Table 2 below. Example 1 was performed in the same manner to prepare a hair loss alleviating composition.

[ Comparative example 8] Preparation of hair loss relief composition

An alcoholic oil (Oleyl alcohol) was used instead of diethoxyethyl succinate as the polar oil, as in the composition of Table 2 below. Except that, it was performed in the same manner as in Example 1 to prepare a hair loss alleviation.组合 物。 Composition.

[ Comparative example 9] Preparation of hair loss relief composition

A triglyceride oil (Caprylic / capric triglyceride) was used instead of diethoxyethyl succinate as a polar oil as in the composition of Table 2 below. Example 1 was performed in the same manner to prepare a hair loss alleviating composition.

[ Comparative example 10] Preparation of hair loss relief composition

Instead of diethoxyethyl succinate as a polar oil, a malic acid oil (alkyl malate C 12-13 alkyl ester) was used as in the composition of Table 2 below. The same procedure was performed to prepare a hair loss alleviating composition.

[Table 1] ※ Unit: Weight% (wt%)

[Table 2] ※ Unit: Weight% (wt%)

[ Test example 1] Solubility Evaluation of Apigenin

On the day of preparation (D + 0) and after 30 days (D + 30) from the day of preparation, the hair loss mitigating compositions prepared in Example 1, Example 2 and Comparative Examples 1 to 10 were observed with the naked eye, and The degree of dissolution was evaluated, and the results are shown in Tables 3 and 4 below. On the other hand, in the following Tables 3 and 4, the "○" mark means that apigenin is completely dissolved and the composition is transparent, the "△" mark means that apigenin is dissolved but precipitated, and the "×" mark means that apigenin is not dissolved. Dissolved and the composition was opaque.

[table 3]

[Table 4]

The solubility of apigenin in the composition was confirmed as described above, and the results are shown in Table 3. The apigenin was completely dissolved only in the compositions of Examples 1 and 2 including a polyhydric alcohol, a monohydric alcohol, and a polar oil. After 30 days, there was no phenomenon of apigenin precipitation or the composition became opaque. Conversely, in the case of the comparative example excluding one of a polyhydric alcohol, a monohydric alcohol, and a polar oil, both D + 0 and D + 30 precipitated apigenin or the composition became opaque.

On the other hand, as shown in Table 4, an ester oil (cLog P value: 7), an alcohol oil (cLog P value: 9), a triglyceride oil (cLog P value: 7), or a malic acid oil ( cLog P value: 8) The solubility of apigenin in Comparative Example 7 to Comparative Example 10 instead of diethoxyethyl succinate as a polar oil was significantly lower than that of Example 1 and Examples using diethoxyethyl succinate 2. It can be confirmed that the solubility of apigenin varies depending on the cLog P value even on the same polar oil (on the other hand, Cetyl ehtylhexanoate) is used as another ester oil. In the case of Dicaprylyl carbonate, 2-octyldodecanol as other alcohol oils, the solubility of apigenin is also similar to that of Comparative Examples 7 to 10 above. Lower than Example 1).

[ Test example 2] Turbidity Evaluation of Hair Loss Relief Composition

Using a portable turbidity meter (Turbidity Portable Meter (HI-98703, HANNA instruments, USA)), the turbidity of the hair loss alleviation composition of Example 1 whose transparency was confirmed in Test Example 1 was measured based on the number of days elapsed. The results are shown in Table 5 below. On the other hand, in Table 5 below, the turbidity unit is NTU (Nepthelometric Turbidity Unit).

[table 5]

The turbidity of the hair loss mitigating composition prepared in Example 1 was measured, and the results are shown in Table 5. Even if 30 days have passed since the preparation date of the composition, the turbidity has not changed significantly and is maintained. Even if time passes, the hair loss relaxation composition of this invention does not precipitate apigenin, and maintains initial solubility.

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Claims (15)

A hair loss alleviating composition includes apigenin, polar oil, a polyhydric alcohol, and a monohydric alcohol with improved solubility as active ingredients, and the cLog P value of the polar oil is 1 to 5. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the polar oil is a succinate oil. The hair loss alleviating composition according to item 1 of the scope of the patent application, wherein the polar oil is selected from the group consisting of Diethoxyethyl Succinate, Dicarpryl Succinate, and Diethyl Succinate (Diethyl Succinate). The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the cLog P value of the polar oil converges to the cLog P value of the apigenin of 2.90. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the polyhydric alcohol is selected from the group consisting of glycerin, 1,3-butanediol, 1,2-propylene glycol, polyethylene glycol, dipropylene glycol, and propylene glycol Ethnic group. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the monohydric alcohol is a lower alcohol having 2 to 5 carbon atoms. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the monohydric alcohol is selected from the group consisting of ethanol, n-butanol, and isobutanol. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the monohydric alcohol is ethanol. The hair loss alleviation composition according to item 1 of the scope of patent application, wherein the content of the apigenin is from 0.1% by weight to 1% by weight. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the content of the polar oil is 10% to 30% by weight. The hair loss alleviation composition according to item 1 of the scope of the patent application, wherein the content of the polyhydric alcohol is 5 to 20% by weight. The hair loss alleviating composition according to item 1 of the scope of patent application, wherein the content of the monohydric alcohol is 20% by weight to 50% by weight. The hair loss alleviation composition according to item 1 of the scope of the patent application, wherein the hair loss alleviation composition further includes any one or more selected from the group consisting of water, a pigment, a preservative, and a fragrance. The hair loss alleviation composition according to item 1 of the scope of the patent application, wherein the hair loss alleviation composition has a turbidity of 1 NTU to 5 NTU. The hair loss alleviation composition according to item 1 of the scope of the patent application, wherein the hair loss alleviation composition is formulated into a group selected from the group consisting of a hair nourishing agent, a shampoo, a conditioner, a conditioner, and a hair nourishing lotion. In the type.