JPH0258245B2 - - Google Patents

Description

[Detailed description of the invention]

[B] Purpose of the Invention The present invention provides a stable cosmetic product in which baicalin (hereinafter, for convenience, this is simply referred to as Ba.G) or baicalein (hereinafter, for convenience, this is simply referred to as Ba) is solubilized. The present invention relates to a food composition. [Industrial Application Field] The composition according to the present invention contains Ba, G, or
Stably contains Ba, and is used in external skin preparations such as ointments and bandages, as well as skin and hair cosmetics such as lotions and hair tonics (hereinafter, for convenience, both preparations are simply used externally). It can be applied to such things as agents (described as agents). [Prior Art] Ba.G or Ba has the structure shown below and is known as a substance that is insoluble in water. Ba・G or Ba
Both dissolve in alkaline solution (pH around 8.6). It also dissolves in hot acetic acid. In addition, ethanol and methanol dissolve in very small amounts, but for example, Ba・G dissolves in ethanol at 0.01
%, in ethanol, about half the amount dissolves, and in acetone, about half the amount that dissolves in methanol. Regarding its solubility and stability (soluble amount),
The results were as shown in the following table (Table 1).

[Problem that the invention seeks to solve]

In 1966, Eda et al.'s antihistamine and antiacetylcholine effects attracted attention when using Huang, its extract, or Ba/G or Ba for internal and external preparations, and research on its formulation was conducted. is being actively carried out. However, as mentioned at the beginning, Ba・G
and Ba must be insoluble in water. A drawback is that it is poorly soluble in ethanol, and as a result, when used in clear liquid products, where water or ethanol are often used in the formulation.
This often leads to precipitation of Ba, G, and Ba that occurs after blending, and it is often not possible to achieve a sufficient effect. Therefore, as a measure to prevent precipitation of Ba/G and Ba,
It is necessary to formulate formulations in the form of ointments, creams, emulsions, and milk lotions in the form of dispersions or emulsions using surfactants and the like. However, in an emulsified or dispersed state, unlike in a dissolved state, the expected effect is halved, and sufficient action is not exerted. It has disadvantages such as worsening hives and eczema in people who are prone to rashes. Therefore, when formulating Ba/G or Ba, one of the essential conditions is to do the formulation without using surfactants as much as possible. In addition, Ba, G or
It was necessary to create a stable aqueous solution containing 0.05% or more Ba, more preferably 0.1% or more. When Ba/G and Ba are in a stable water-soluble state, even if the content in external preparations is 0.01%, long-term application can prevent skin irritation, hives, itching, etc. effect will be obtained. However, when formulating using a dispersant,
Although Ba/G and Ba can be blended in large amounts, unfortunately, their effects are not sufficiently exhibited and their use is wasted. In other words, even though Ba/G and Ba have antihistamine effects, even if they are simply blended by dispersion or emulsification, if they are not in a dissolved state, sufficient effects will not be obtained. . On the other hand, Ba・G and Ba, as mentioned at the beginning,
As a known solubilization method, if an alkaline solution is used, it dissolves well, but for oral administration of external preparations and drinks, it is preferable to use both neutral or acidic solutions. Particularly in external preparations for people with allergies, alkaline solutions are inappropriate because they often worsen inflammation, eczema, and skin diseases. Based on the above drawbacks, the present inventors have developed Ba・G,
Research has begun to establish an advantageous formulation method for Ba. [B] Structure of the Invention [Means for Solving the Problems] The present inventors have high hopes for the therapeutic effects of Ba, G, and Ba, and have continued to experiment with the best way to use them as external preparations. As a result, we succeeded in producing a solution as shown in the following example. That is, it contains 0.1 to 0.6% Ba/G or Ba,
By using an amino acid and sugar together, or using an acid amide compound or urea as a solubilization stabilizer, Ba, G or Ba can be stably dissolved in the solution for a long period of time. . Example 1 Ba.
A mixture of (C) is prepared in advance, and 0.1 to 0.6% of Ba.G or Ba is added to either of the mixtures. The addition is carried out at a temperature of 60 to 80°C with gentle stirring. However, it still does not dissolve completely under heating.
Further, by cooling, Ba, G or Ba in the soluble portion precipitates. <Mixture> (A) Mixture of water and propylene glycol in a ratio of 1:1 (B) Mixture of water and butylene glycol in a ratio of 1:1 (C) Solution of water and ethanol in a ratio of 1:1 Above After adding Ba・G or Ba to the mixed solution,
As the solubilization stabilizer shown below, the amino acids (D) consisting of at least one type of proline are used, and the total amount of the amino acids added is the same as the content in the solution of Ba, G or Ba. Or add double the amount. After adding (D), use a saccharide (E) consisting of at least one type of sutucarose so that the total amount of the saccharide added is the same or twice the content in the mixture of Ba and G or Ba. Add quantity. When adding these (D) and (E), Ba・G or Ba
It may be continued after adding (D) and (E), but the order of addition of (D) and (E) may be reversed, with (E) being added first and then (D) being added. On the other hand, when (D) and (E) are not used, one of the acid amide compounds of (F) is added to the mixture.
Add the same amount or up to twice the amount of Ba.G or Ba content under heating at 60 to 80°C. <Solubilization stabilizer> (D) Amino acids Proline is an essential component, arginine, aspartic acid, serine, glycine, alanine, valine, methionine, tyrosine, lysine, histidine, glutamic acid, isoleucine, leucine, phenylalanine, threonine, Cysteine, cystine, tryptophan, hydroxyproline, ornithine. (E) Saccharide Satucarose is an essential component, glucose,
fructose, xylose, galactose, mannose. (F) Acid amide compounds, etc. Nicotinic acid amide, thioctic acid amide, glucuronic acid amide, urea. In other words, the solubilizing stabilizer used here may be the same or twice the amount of amino acids and saccharides relative to the content of Ba, G, or Ba, or a combination of amino acids and saccharides; Instead, one type of acid amide compound or urea may be used alone. The final result obtained by the above-mentioned operation method is
Both Ba.G and Ba-containing composition liquids are stable over a long period of time. In addition, as the above-mentioned solubilization stabilizer, amino acids
When using only (D) or only saccharide (E), Ba・
The stable dissolution amount of G or Ba is around 0.1 to 0.3. Further, if any component selected from (F) is further added after using (D) and (E) together, the upper limit of the amount dissolved will be a little less than 1%. But in this case,
Looking at the changes over time after long-term storage at a low temperature of -20℃, some precipitates were observed,
When the temperature returns to room temperature, the precipitate dissolves again. [C] Effects of the invention Obtained in the above embodiments according to the present invention,
Ba・G or Ba-containing composition liquid is shown in the following table (Table-2).
As shown in Table 3, no precipitation was observed not only at room temperature but also under conditions of heat treatment, 45°C constant temperature bath, and -20°C freezing for long periods of time. Furthermore, since this Ba/G or Ba-containing liquid composition is obtained as a yellow-brown transparent liquid, it can be used as an external preparation as it is, and it can also be used in known lotions, hair tonics, skin care products, hair care products, etc. It can be used in the formulation of clear liquid products for use. In this case, the amount to be added may be about 1 to 10%. Of course, it can also be added to ointments, bandages, creams, milky lotions, lotions, lip creams, and powder-type external preparations. In addition, the mixture shown in the example is (C), and the solubilization stabilizer is Ba・G obtained by using other than urea (F).
Or, if it is a Ba-containing composition liquid, it can be administered orally, and it can also be incorporated into, for example, a drink or a syrup form of an oral preparation for children. The composition liquid according to the present invention in which Ba/G contains Ba has the effect of alleviating the symptoms of various allergic diseases, and is aimed at improving people with weak constitutions, such as hives or Helps relieve irritation. In addition, for skin prone to roughness accompanied by allergic skin diseases, apply the Ba/G or Ba-containing composition solution obtained in the example locally, and when the local area dries, apply egg yolk oil or egg yolk. This method is used in conjunction with the application of Vaseline or a paste with a lecithin content of around 25-60%, and continued use over a long period of time will improve allergic tendencies. Similar effects can be expected even if both are taken. In particular, this effect is remarkable in children, and Ba/G and Ba-containing composition liquids can also be used together with egg yolk lecithin as ingredients for improving the constitution for health drinks or health foods. It is. (Table 4) shows the clinical trial results. On the other hand, according to the published patent publication No. 1973-73509, which was mentioned in the beginning, powder and extract of yellow baicalin (estimated to be crude baicalin) can be used to treat rough skin, age spots, freckles, acne, and itching. It is reported to be effective. Therefore, we conducted a clinical trial on external application using the Ba/G or Ba-containing composition liquid obtained in the examples. I tried applying it three times, but I couldn't get the desired effect. On the other hand, when compared with known antihistamine-containing ointments, it is effective against itching as almost the same effect can be obtained. In addition, it has a fast-acting effect on areas affected by mosquito bites and eliminates itching. For eczema, it is effective for chronic eczema, but it could not be expected to be as fast-acting as the adrenal skin hormone-containing ointment. Furthermore, with regard to acne, the initial swelling accompanied by flushing was shown to have an anti-inflammatory tendency to disappear. However, overall, in order to enhance the above-mentioned effects, it is better to add a small amount of menthol when using it as an external preparation than to apply Ba/G or Ba-containing composition liquid alone. is better.

[Table] (Commentary to Table 2) The results shown in Table 2 are based on the solvent compositions (mixed liquids: A to C) specified in Example 1, and C (the ratio of water and ethanol is 1: 1), 0.6% of Ba・G or Ba was added to the mixture of Example 1.
Regarding the stability of the solution when one of the solubilization stabilizers (F) identified in (Nicotinic acid amide) was added in the same amount as Ba and G,
Various temperatures (60-80℃, 45℃ thermostat, left at room temperature, 5
~10℃ in the refrigerator, -20℃ in the freezer),
Changes over time (presence or absence of precipitates such as lees) were determined over a period of 1 hour to 12 months. In addition, among the solubilization stabilizers specified in Example 1, amino acids (D) consisting of at least one type of proline, and saccharides (E) consisting of at least one type of sutucarose, or One of the solubilization stabilizers (F) (thioctic acid amide, glucuronic acid amide, urea) was
In each case, Ba・
I tried to find the stability of the composition liquid containing G or Ba, but
In both cases, almost the same good results were obtained. Furthermore, regarding the solvents used, mixture A (water: propylene glycol = 1:1) and mixture B
(Water: butylene glycol = 1:1) We tried various combinations of solubilizing stabilizers such as those mentioned above, and searched for such stabilizers, but the results were similar. It was found that the gender was preserved.

【table】

[Table] (Commentary to Table 3) The results shown in Table 3 are based on the results shown in Table 3.・When 0.6% G or Ba is added, and in addition, nothing is added as a solubilization stabilizer (no addition) When only proline is added from among the amino acids shown in (D) in various proportions When only sutucarose is added in various proportions from among the sugars shown in (E) When only one type of acid amide compound shown in (F) or only urea is added in various proportions Proline and When the same amount of sutucarose is added, and when the same amount of nicotinic acid amide selected from among proline, sutucarose, and the acid amide compound shown in (F) is added, using the recipe of ~. This figure shows changes over time of the composition solution obtained after two weeks. Incidentally, tests similar to those described above were also conducted for the solvents (A) and (B), and good results were obtained in almost the same manner in either case.

【table】

Claims (1)

[Claims] 1 The ratio of water and propylene glycol, water and butylene glycol, or water and ethanol is 1:1.
The mixture contains 0.1 to 0.6% of baicalin or baicalein as the main drug, and at least 1 proline from amino acids as a solubilization stabilizer.
Contains at least one type of sucarose from saccharides, 0.1 to 1.2% each, or contains nicotinamide, thioctic acid amide, glucuronic acid amide, or urea as a solubilizing stabilizer. 1. A cosmetic composition liquid characterized by being solubilized and stabilized and containing 0.1 to 1.2% of one of the following.