A highly soluble composition containing cosmetic actives and its preparation and application

Abstract

The present invention relates to a highly soluble composition containing cosmetic actives, its preparation and application, belonging to the technical field of cosmetics. The highly soluble composition containing cosmetic actives of the present invention comprises cosmetic actives and a solvent; the cosmetic actives are selected from one or more of glycyrrhetinic acid, asiatic acid and madecassic acid; the solvent comprises hexylene glycol, methyl glucamine and water. Methyl glucamine has multiple hydroxyl groups in its structure and has good water solubility. By combining the amino group in its structure with the carboxyl group on the cosmetic actives, the hydrophilicity of the cosmetic actives is increased. Hexylene glycol has the characteristics of being amphiphilic for oil and water and can play a bridging role in dissolving the cosmetic actives, promoting the combination of the cosmetic actives and methyl glucamine, thus playing a synergistic effect. At the same time, the amount of solvent used can be greatly reduced, and the dissolution efficiency of the cosmetic actives can be greatly improved, thereby realizing the application value in cosmetics.

Description

Technical Field

[0001] The present invention belongs to the technical field of cosmetics, and particularly relates to a highly soluble composition containing cosmetic active substances, its preparation and application. Background Art

[0002] Many highly effective raw materials in cosmetics have excellent skin care effects, but their application in cosmetics is restricted due to difficult dissolution. For example, glycyrrhetinic acid has a highly effective soothing and anti-allergic effect, is soluble in ethanol, chloroform, pyridine, acetic acid, and insoluble in water; asiatic acid / asiaticoside has various physiological activities such as antioxidant, anti-inflammatory, and repair effects, is soluble in dimethyl sulfoxide, ethanol, and methanol, and slightly soluble in water. Therefore, improving the solubility of cosmetic active substances remains a research hotspot.

[0003] Currently, there are mainly two methods for dissolving cosmetic active substances on the market. One is lipid encapsulation, which has high requirements for equipment and high production costs. The other is solubilization with surfactants such as PEG-40 hydrogenated castor oil. However, the solubilization with surfactants results in a sticky skin feel, high dosage, high irritation, and is prone to generating unwanted foams in the formulation.

[0004] Therefore, it is of great significance to develop a method that can efficiently, conveniently, and safely dissolve cosmetic active substances. Summary of the Invention

[0005] To solve the above technical problems, the present invention provides a highly soluble composition containing cosmetic active substances, its preparation and application.

[0006] The first object of the present invention is to provide a highly soluble composition containing cosmetic active substances, including cosmetic active substances and a solvent; the cosmetic active substances are selected from one or more of glycyrrhetinic acid, asiatic acid, and asiaticoside; the solvent includes hexylene glycol, methyl glucamine, and water.

[0007] In an embodiment of the present invention, the mass ratio of the cosmetic active substances to the solvent is 0.01 - 20:80 - 99.99.

[0008] In an embodiment of the present invention, the mass ratio of the cosmetic active substances to the solvent is 0.1 - 10:90 - 99.9.

[0009] In an embodiment of the present invention, the mass ratio of hexylene glycol, methyl glucamine, and water is 0.01 - 50:0.01 - 20:30 - 99.9.

[0010] In an embodiment of the present invention, the mass ratio of hexylene glycol, methyl glucamine, and water is 0.1 - 40:0.1 - 10:40 - 99.9.

[0011] The second object of the present invention is to provide a method for preparing the high-solubility composition containing cosmetic active substances, comprising the following steps:

[0012] S1. Add cosmetic active substances to hexylene glycol, heat and stir until completely dissolved to obtain a first mixed solution;

[0013] S2. Add methyl glucamine and water to the first mixed solution obtained in S1, and stir until completely dissolved to obtain the high-solubility composition containing cosmetic active substances.

[0014] In an embodiment of the present invention, in S1, the heating temperature is 50°C - 80°C.

[0015] In an embodiment of the present invention, after S2, it further includes a step of stirring and cooling; the temperature after stirring and cooling is 20°C - 40°C.

[0016] The third object of the present invention is to provide a cosmetic, comprising the high-solubility composition containing cosmetic active substances.

[0017] In an embodiment of the present invention, the cosmetic includes essence, lotion and cream.

[0018] The technical solution of the present invention has the following advantages compared with the prior art:

[0019] (1) In the high-solubility composition of the present invention, methyl glucamine has multiple hydroxyl groups in its structure and has good water solubility. Through the combination of the amino group in its structure and the carboxyl group on the cosmetic active substance, the hydrophilicity of the cosmetic active substance is increased. Hexylene glycol has the characteristics of being amphiphilic and can play a bridging role in dissolving the cosmetic active substance, promoting the combination of the cosmetic active substance and methyl glucamine, thereby playing a synergistic effect. The combination of hexylene glycol and methyl glucamine has an obvious synergistic solubilization effect on the cosmetic active substance at a specific ratio, and at the same time can greatly reduce the amount of solvent used, greatly improving the dissolution efficiency of the cosmetic active substance, so as to realize its application value in cosmetics.

[0020] (2) The preparation method of the present invention selects hexylene glycol, methyl glucamine and water as solvents, maximizing the dissolution of cosmetic active substances. No special equipment is required, only simple heating and stirring are needed. The process cost is low, the process is safe and easy to operate, and it does not contain surfactants and is not limited by the formula dosage form, greatly improving the application prospect of this type of cosmetic active substance. Description of the Drawings

[0021] In order to make the content of the present invention easier to be clearly understood, the following further details the present invention according to specific embodiments of the present invention in combination with the drawings, wherein:

[0022] Figure 1 This is the display diagram of the compositions of Examples 1-10 of the present invention after being placed at 5°C for 2 weeks. From left to right are Example 1 to Example 10 in sequence;

[0023] Figure 2 This is the display diagram of the compositions of Comparative Examples 1-4 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 1 to Comparative Example 4 in sequence;

[0024] Figure 3 This is the display diagram of the compositions of Comparative Examples 5-8 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 5 to Comparative Example 8 in sequence;

[0025] Figure 4 This is the display diagram of the compositions of Comparative Examples 9-12 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 9 to Comparative Example 12 in sequence;

[0026] Figure 5 This is the display diagram of the compositions of Comparative Examples 13-16 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 13 to Comparative Example 16 in sequence;

[0027] Figure 6 This is the display diagram of the compositions of Comparative Examples 17-20 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 17 to Comparative Example 20 in sequence;

[0028] Figure 7 This is the display diagram of the compositions of Comparative Examples 21-24 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 21 to Comparative Example 24 in sequence;

[0029] Figure 8 This is the display diagram of the compositions of Comparative Examples 25-30 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 25 to Comparative Example 30 in sequence;

[0030] Figure 9 This is the display diagram of the compositions of Comparative Examples 31-36 of the present invention after being placed at 5°C for 2 weeks. From left to right are Comparative Example 31 to Comparative Example 36 in sequence. Detailed implementation manners

[0031] The present invention will be further described below in conjunction with the accompanying drawings and specific embodiments, so that those skilled in the art can better understand the present invention and be able to implement it, but the exemplified embodiments do not limit the present invention.

[0032] In the present invention, unless otherwise specified, the technical and scientific terms used in the present invention have the same meanings as those commonly understood by those skilled in the technical field to which the present invention belongs.

[0033] In the present invention, unless otherwise specified, the experimental methods used in the embodiments of the present invention are all conventional methods without special instructions. The materials, reagents, etc. used can be obtained from commercial channels without special instructions.

[0034] Examples 1 - 10

[0035] The highly soluble composition containing cosmetic actives of the present invention comprises cosmetic actives and a solvent; the cosmetic actives are selected from one or more of glycyrrhetinic acid, asiatic acid, and madecassic acid; the solvent comprises hexylene glycol, methyl glucamine, and water. The specific formulation and dosage (parts by mass) are shown in Table 1 as follows:

[0036] Table 1

[0037]

[0038] Specifically, it includes the following steps:

[0039] S1. Add the cosmetic actives to hexylene glycol, heat to 75 °C, and stir until completely dissolved to obtain a first mixed solution;

[0040] S2. Add methyl glucamine and water to the first mixed solution, stir until completely dissolved, and stir and cool to room temperature to obtain the highly soluble composition containing cosmetic actives.

[0041] To investigate the stability of the compositions of Examples 1 - 10, their conditions after being placed at 5 °C for 2 weeks were respectively recorded, and the recording results are as Figure 1 and shown in Table 1. It can be seen from Figure 1 and Table 1 that whether it is a single cosmetic active or a composite cosmetic active, hexylene glycol and methyl glucamine can dissolve it well at a relatively low proportion.

[0042] Comparative Examples 1 - 4

[0043] Basically the same as Example 1, the difference lies in that the formulation and dosage (parts by mass) of the composition are different, as specifically shown in Table 2:

[0044] Table 2

[0045] Component Asiatic acid Methyl glucamine Water Dissolution at 75°C Dissolution after two weeks at 5°C Comparative Example 1 0.5 2 97.5 Turbid A large amount of crystals precipitated Comparative Example 2 0.5 5 94.5 Turbid A large amount of crystals precipitated Comparative Example 3 0.5 10 89.5 Turbid A large amount of crystals precipitated Comparative Example 4 0.5 20 79.5 Turbid A large amount of crystals precipitated

[0046] To investigate the dissolution and stability of the compositions of Comparative Examples 1 - 4, their dissolution conditions at 75 °C and their conditions after being placed at 5 °C for 2 weeks were respectively recorded, and the recording results are as Figure 2 and shown in Table 2. It can be seen from Figure 2As can be seen from Table 2, asiatic acid has poor solubility in a single methylglucamine solution, and increasing the amount of methylglucamine does not significantly increase the solubility of asiatic acid; moreover, crystals precipitate after being placed at 5°C for 2 weeks, indicating that the solubility and stability of this group of compositions are both very poor.

[0047] Comparative Examples 5-8

[0048] Basically the same as Example 1, the difference lies in the formulation and dosage (parts by mass) of the composition, specifically as shown in Table 3:

[0049] Table 3

[0050] Component Asiatic acid Hexylene glycol Water Dissolution at 75°C Dissolution after two weeks at 5°C Comparative Example 5 0.5 2 97.5 Dissolved More crystals precipitated Comparative Example 6 0.5 10 89.5 Dissolved A small amount of crystals precipitated Comparative Example 7 0.5 30 69.5 Dissolved A small amount of crystals precipitated Comparative Example 8 0.5 60 39.5 Dissolved A small amount of crystals precipitated

[0051] To investigate the dissolution and stability of the compositions of Comparative Examples 5-8, their dissolution at 75°C and their conditions after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 3 and shown in Table 3. As can be seen from Figure 3 and Table 3, although asiatic acid can dissolve in a single hexylene glycol solution, crystals precipitate after being placed at 5°C for 2 weeks, indicating that the stability of this group of compositions is poor.

[0052] Comparative Examples 9-12

[0053] Basically the same as Example 1, the difference lies in the formulation and dosage (parts by mass) of the composition, specifically as shown in Table 4:

[0054] Table 4

[0055] Component Madecassic acid Methyl glucamine Water Dissolution at 75°C Dissolution after two weeks at 5°C Comparative Example 9 0.5 2 97.5 Turbid More crystals precipitated Comparative Example 10 0.5 5 94.5 Turbid More crystals precipitated Comparative Example 11 0.5 10 89.5 Turbid More crystals precipitated Comparative Example 12 0.5 20 79.5 Turbid More crystals precipitated

[0056] To investigate the dissolution and stability of the compositions of Comparative Examples 9-12, their dissolution at 75°C and their conditions after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 4 and shown in Table 4. As can be seen from Figure 4 and Table 4, madecassic acid cannot be completely dissolved in a single methylglucamine solution, and increasing the amount of methylglucamine does not significantly increase the solubility of madecassic acid; moreover, crystals precipitate after being placed at 5°C for 2 weeks, indicating that the solubility and stability of this group of compositions are both very poor.

[0057] Comparative Examples 13-16

[0058] Basically the same as Example 1, the difference lies in the formulation and dosage (parts by mass) of the composition, specifically as shown in Table 5:

[0059] Table 5

[0060] Component Madecassic acid Hexylene glycol Water Dissolution at 75°C Dissolution after two weeks at 5°C Comparative Example 13 0.5 2 97.5 Dissolved More crystals precipitated Comparative Example 14 0.5 10 89.5 Dissolved A small amount of crystals precipitated Comparative Example 15 0.5 30 69.5 Dissolved A small amount of crystals precipitated Comparative Example 16 0.5 60 39.5 Dissolved A small amount of crystals precipitated

[0061] To investigate the dissolution and stability of the compositions of Comparative Examples 13 - 16, their dissolution at 75°C and the situation after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 5 shown in Table 5. It can be seen from Figure 5 Table 5 that although asiatic acid can dissolve in the individual solution of hexylene glycol, crystals precipitate after being placed at 5°C for 2 weeks, indicating that the stability of this group of compositions is poor.

[0062] Comparative Examples 17 - 20

[0063] are basically the same as Example 1, except that the formulation and dosage (parts by mass) of the composition are different, as specifically shown in Table 6:

[0064] Table 6

[0065] Component Glycyrrhetinic acid Methyl glucamine Water Dissolution at 75°C Dissolution after two weeks at 5°C Comparative Example 17 0.5 2 97.5 Turbid More crystals precipitated Comparative Example 18 0.5 5 94.5 Turbid More crystals precipitated Comparative Example 19 0.5 10 89.5 Turbid More crystals precipitated Comparative Example 20 0.5 20 79.5 Turbid More crystals precipitated

[0066] To investigate the dissolution and stability of the compositions of Comparative Examples 17 - 20, their dissolution at 75°C and the situation after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 6 shown in Table 6. It can be seen from Figure 6 Table 6 that the solubility of glycyrrhetinic acid in the individual solution of methylglucamine is poor, and increasing the dosage of methylglucamine does not significantly increase the solubility of glycyrrhetinic acid; moreover, crystals precipitate after being placed at 5°C for 2 weeks, indicating that the solubility and stability of this group of compositions are both very poor.

[0067] Comparative Examples 21 - 24

[0068] are basically the same as Example 1, except that the formulation and dosage (parts by mass) of the composition are different, as specifically shown in Table 7:

[0069] Table 7

[0070] Component Glycyrrhetinic acid Hexylene glycol Water Dissolution at 75°C Dissolution after two weeks at 5°C Comparative Example 21 0.5 2 97.5 Incompletely dissolved Abundant precipitation Comparative Example 22 0.5 10 89.5 Dissolved More precipitation Comparative Example 23 0.5 30 69.5 Dissolved A small amount of precipitation Comparative Example 24 0.5 60 39.5 Dissolved Trace precipitation

[0071] To investigate the dissolution and stability of the compositions of Comparative Examples 21 - 24, their dissolution at 75°C and the situation after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 7 shown in Table 7. It can be seen from Figure 7 Table 7 that glycyrrhetinic acid can dissolve only at a certain ratio in the individual solution of hexylene glycol, and crystals precipitate after being placed at 5°C for 2 weeks, indicating that the stability of this group of compositions is poor.

[0072] Comparative Examples 25 - 30

[0073] are basically the same as Example 1, except that the formulation and dosage (parts by mass) of the composition are different, as specifically shown in Table 8:

[0074] Table 8

[0075] Component Comparative Example 25 Comparative Example 26 Comparative Example 27 Comparative Example 28 Comparative Example 29 Comparative Example 30 Hexylene glycol 4 20 2 10 2 10 Triethanolamine 1 5 1 5 1 5 Water 94.5 74.5 96.5 84.5 96.5 84.5 Glycyrrhetinic acid 0.5 0.5 - - - - Asiatic acid - - 0.5 0.5 - - Madecassic acid - - - - 0.5 0.5 Dissolution at 75°C Dissolved Dissolved Dissolved Dissolved Dissolved Dissolved Dissolution after two weeks at 5°C More precipitation Less precipitation More precipitation Less precipitation More precipitation Less precipitation

[0076] To investigate the dissolution and stability of the compositions of Comparative Examples 25 - 30, their dissolution at 75°C and the situation after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 8 and Table 8 shown. From Figure 8 and Table 8, it can be seen that replacing methylglucamine with the combination of triethanolamine and hexylene glycol which also has basic amino functional groups cannot achieve the stabilizing effect of methylglucamine and hexylene glycol on cosmetic actives, even if the dosage is increased.

[0077] Comparative Examples 31 - 36

[0078] Basically the same as Example 1, the difference lies in the formulation and dosage (parts by mass) of the composition, as specifically shown in Table 9:

[0079] Table 9

[0080]

[0081]

[0082] To investigate the dissolution and stability of the compositions of Comparative Examples 31 - 36, their dissolution at 75°C and the situation after being placed at 5°C for 2 weeks were respectively recorded, and the recording results are as Figure 9 and Table 9 shown. From Figure 9 and Table 9, it can be seen that replacing hexylene glycol with butylene glycol which is also used as a solvent cannot achieve the synergistic effect of hexylene glycol even if the dosage is increased.

[0083] From the comparison between the examples and the comparative examples, it can be seen that the solubility of cosmetic actives in a single hexylene glycol or methylglucamine solution is not ideal; the combination of hexylene glycol and methylglucamine has an obvious synergistic solubilizing effect on cosmetic actives, and at the same time can greatly reduce the usage amount of the solvent, greatly improving the dissolution efficiency of cosmetic actives, thereby realizing their application value in cosmetics. This is because methylglucamine has multiple hydroxyl groups in its structure and has good water solubility. By combining the amino group in its structure with the carboxyl group on the cosmetic active, the hydrophilicity of the cosmetic active is increased. Hexylene glycol has the characteristics of being amphiphilic and can play a bridging role in dissolving cosmetic actives, promoting the combination of cosmetic actives and methylglucamine, thus playing a synergistic effect.

[0084] Obviously, the above embodiments are merely examples for clear illustration and are not limitations on the implementation manners. For those of ordinary skill in the art, other different forms of changes or modifications can be made based on the above description. It is not necessary and impossible to enumerate all the implementation manners here. And the obvious changes or modifications derived therefrom are still within the protection scope of the present invention.

Claims

1. A highly soluble composition containing cosmetic active substances, characterized in that, It is composed of a cosmetic active ingredient and a solvent; the cosmetic active ingredient is selected from one or more of glycyrrhetinic acid, asiatic acid and madecassic acid; the solvent is composed of hexylene glycol, methyl glucamine and water; the mass ratio of the cosmetic active ingredient to the solvent is 0.01-20:80-99.99; the mass ratio of hexylene glycol, methyl glucamine and water is 0.01-50:0.01-20:30-99.

9.

2. The highly soluble composition containing a cosmetic active substance according to claim 1, characterized in that, The mass ratio of the cosmetic active ingredient to the solvent is 0.1-10:90-99.

9.

3. The highly soluble composition containing a cosmetic active substance according to claim 1, characterized in that, The mass ratio of hexylene glycol, methyl glucamine and water is 0.1-40:0.1-10:40-99.

9.

4. A method for preparing a highly soluble composition containing a cosmetic active ingredient according to any one of claims 1-3, characterized in that, It includes the following steps S1. Add the cosmetic active ingredient to hexylene glycol, heat and stir until completely dissolved to obtain a first mixture. S2. Add methyl glucamine and water to the first mixture obtained in S1, and stir until completely dissolved to obtain the highly soluble composition containing the cosmetic active ingredient.

5. The preparation method of the highly soluble composition containing cosmetic active substances according to claim 4, characterized in that, In S1, the heating temperature is 50°C - 80°C.

6. The preparation method of the highly soluble composition containing a cosmetic active substance according to claim 4, characterized in that, After S2, it further includes a step of stirring and cooling; the temperature after stirring and cooling is 20°C - 40°C.

7. A cosmetic, characterized in that, It includes the highly soluble composition containing the cosmetic active ingredient according to any one of claims 1-3.

8. The cosmetic according to claim 7, characterized in that, The cosmetic includes essence, lotion and cream.

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