Oil-soluble composition as well as preparation method and application thereof

Abstract

The embodiment of the invention provides an oil-soluble composition as well as a preparation method and application thereof, and relates to the technical field of skin care products. The oil-soluble composition provided by the embodiment of the invention comprises the following components in percentage by mass: 5-50% of alkanet root extract; 5%-39% of dracocephalum dracocephalum extract; 0.01%-30% of vegetable oil; and 0.01%-40% of a softening and moistening agent. The oil-soluble composition as well as the preparation method and the application of the oil-soluble composition have excellent anti-inflammatory and soothing effects on skin.

Description

Technical Field

[0001] This application relates to the technical field of skin care products. Specifically, it relates to an oil-soluble composition, a preparation method thereof, and an application thereof. Background Art

[0002] Inflammation is a protective immune response of the body to external harmful stimuli, usually triggered by factors such as microbial infection, oxidative stress, and cell damage. Inducible nitric oxide synthase (iNOS) plays an important role in the inflammatory response. Its activation leads to the generation of a large amount of nitric oxide (NO), which can cause vasodilation, cell damage, and excessive release of cytokines, thereby aggravating inflammation. TRPV1 is an ion channel located in the nervous system and is involved in the conduction of sensory signals, especially pain and temperature perception. During inflammation, after the capsaicin receptor (TRPV1) is activated, it will trigger a series of neuroinflammatory reactions, resulting in pain and other discomfort symptoms. Cyclin-dependent protein kinase (CDK1) mainly regulates cell division in the G2 / M phase of the cell cycle and plays an important role in the inflammatory response. Its overactivation may lead to abnormal proliferation of immune cells and abnormal immune responses, further exacerbating chronic inflammation. The regulation of these three targets is interrelated. Controlling their activities and expressions can effectively reduce the pathological changes caused by inflammation and provide potential targets for anti-inflammatory treatment.

[0003] Therefore, there is a need for a composition that can simultaneously regulate the above three targets to achieve an anti-inflammatory effect. Summary of the Invention

[0004] The purpose of the embodiments of this application is to provide an oil-soluble composition, a preparation method thereof, and an application thereof, which have excellent anti-inflammatory and soothing effects on the skin.

[0005] In a first aspect, the embodiments of this application provide an oil-soluble composition, and its components by mass percentage include:

[0006]

[0007] In the above technical solution, the extracts of Lithospermum erythrorhizon and Dracaena cochinchinensis provide active ingredients, and vegetable oil and emollient are used as the oil phase matrix to adjust the viscosity and enhance the solubility of lipophilic active ingredients such as shikonin and dracoresinotannol in the extracts of Lithospermum erythrorhizon and Dracaena cochinchinensis, thereby improving the transdermal absorption efficiency.

[0008] Lithospermum erythrorhizon and Dracaena cochinchinensis are traditional Chinese medicinal materials with a variety of pharmacological activities, especially outstanding in anti-inflammatory, antioxidant and anti-tumor aspects. The main medicinal part of Lithospermum erythrorhizon is the root, and the extract of Lithospermum erythrorhizon root usually contains shikonin, alkannin, tannins and flavonoids. Dracaena cochinchinensis is a traditional precious Chinese medicine, known as the "sacred medicine for promoting blood circulation". The extract of Dracaena cochinchinensis mainly contains dracorhodin perchlorate, dracorubin and other bioactive components, which are widely used in anti-inflammatory, hemostatic, promoting wound healing and other aspects.

[0009] In this application, the extract of Lithospermum erythrorhizon root and the extract of Dracaena cochinchinensis are used in combination. The anti-inflammatory active ingredient shikonin of the extract of Lithospermum erythrorhizon root and the anti-inflammatory active ingredient dracorhodin perchlorate of the extract of Dracaena cochinchinensis have a synergistic inhibitory effect on anti-inflammatory. The binding energies with three conventional soothing anti-inflammatory related receptors (iNOS receptor, TRPV1 receptor, CDK1 receptor) are all relatively low, with strong biological activity, and regulate the inflammatory response, thus playing a synergistic inhibitory effect on anti-inflammatory. Specifically, shikonin inhibits iNOS and reduces the synthesis of inflammatory molecules. Dracorhodin perchlorate relieves neurogenic inflammation through the regulatory effect of TRPV1 receptor or regulates the cell cycle through the inhibitory effect of CDK1 to prevent excessive proliferation of inflammatory cells. When both bind to multiple receptors and regulate related signaling pathways simultaneously, they can exert a stronger anti-inflammatory effect than when used alone, and their combined action may significantly enhance the effect.

[0010] In one possible implementation, its components include by mass percentage:

[0011]

[0012]

[0013] In one possible implementation, the vegetable oil includes at least one of wild soybean oil, jojoba oil, and olive oil;

[0014] And / or, the emollient includes at least one of hydrogenated polydecene, isododecane, squalane, glyceryl trioctanoate, glyceryl tridecanoate, and ethylhexyl palmitate.

[0015] In the above technical solution, the above vegetable oil can not only be used as an oil phase matrix, but also has the effects of moisturizing and antioxidant. The wild soybean oil in it contains unsaturated fatty acids (such as linoleic acid, oleic acid), which can form a closed protective film on the skin surface to reduce water loss, thus playing a moisturizing effect; the wild soybean oil contains natural vitamin E and polyphenolic substances, which can neutralize free radicals and delay oxidative damage, playing an antioxidant effect.

[0016] The above emollient can not only serve as an oil-phase matrix but also improve stability. Among them, hydrogenated polydecene, as a synthetic ester, can reduce greasiness, enhance ductility, ensure the uniform dispersion of shikonin and dracorhodin, and also improve the stability of the composition to prevent delamination or precipitation.

[0017] In a possible implementation, its components by mass percentage further include:

[0018] Octyldodecanol 0.00779%-0.779%;

[0019] Ribes nigrum seed oil 0.00126%-0.126%;

[0020] Rosmarinus officinalis leaf extract 0.00005%-0.005%.

[0021] In the above technical solution, the above components are used as auxiliary synergistic components. Among them, octyldodecanol has both emollient and emulsifying and stabilizing functions, can adjust the viscosity of the composition, promote the transdermal absorption of active ingredients such as shikonin and dracorhodin, and can enhance the ductility of the oil phase and reduce greasiness when combined with the emollient. Ribes nigrum seed oil is rich in γ-linolenic acid (Omega-6), supplements essential fatty acids for the skin, and assists in repairing the barrier function. Rosmarinus officinalis leaf extract contains carnosic acid and rosmaridiphenol, and acts as a fat-soluble antioxidant to prevent the oxidative rancidity of the oil phase.

[0022] In a possible implementation, its components by mass percentage further include:

[0023] Antioxidant 0.005%-0.1%;

[0024] Anti-inflammatory ingredient 0.0001%-0.1%.

[0025] In the above technical solution, it is used as an auxiliary synergistic component.

[0026] In a possible implementation, the antioxidant includes at least one of tocopherol, vitamin E derivative, and coenzyme Q10;

[0027] And / or, the anti-inflammatory ingredient by mass percentage includes:

[0028] Unsaponifiables of sunflower seed oil 0.0003%-0.03%;

[0029] Sunflower seed oil 0.00005%-0.005%;

[0030] Cardiospermum halicacabum extract 0.00005%-0.005%.

[0031] In the above technical solution, the unsaponifiable matter of sunflower seed oil contains phytosterols (mainly β-sitosterol), inhibits inflammatory factors (such as IL-6, TNF-α), and reduces the irritation that may be caused by a high concentration of Lithospermum erythrorhizon extract. The unsaponifiable matter of sunflower seed oil and the free fatty acids of sunflower seed oil form a sebum-like complex, simulating the natural barrier structure and synergistically enhancing the anti-inflammatory effect. The Cardiospermum halicacabum extract contains saponins and flavonoid components, reduces the swelling reaction by inhibiting the NF-κB pathway, and its anti-inflammatory target forms a multi-pathway synergy with the Dracaena cochinchinensis extract (sanguisorbine regulates the MAPK pathway). The unsaponifiable matter of sunflower seed oil and the triterpenoids in the Cardiospermum halicacabum flower extract jointly inhibit the COX-2 pathway and enhance the anti-inflammatory effect.

[0032] In a possible implementation, the Lithospermum erythrorhizon extract includes shikonin, and the content of shikonin in the Lithospermum erythrorhizon extract is 90 - 130 μg·mL -1 ; the content of shikonin in the oil-soluble composition is 33 - 55 μg·mL -1 .

[0033] In the above technical solution, the content of the anti-inflammatory active ingredient shikonin in the Lithospermum erythrorhizon extract is high.

[0034] In a possible implementation, the Dracaena cochinchinensis extract includes sanguisorbine, and the content of sanguisorbine in the Dracaena cochinchinensis extract is 60 - 100 μg·mL -1 ; the content of sanguisorbine in the oil-soluble composition is 23.2 - 40 μg·mL -1 .

[0035] In the above technical solution, the content of the anti-inflammatory active ingredient sanguisorbine in the Dracaena cochinchinensis extract is high, and it plays a better synergistic effect with the anti-inflammatory active ingredient shikonin in the Lithospermum erythrorhizon extract.

[0036] In a second aspect, an embodiment of the present application provides a preparation method of the oil-soluble composition provided in the first aspect, which mixes and emulsifies each component.

[0037] In a third aspect, an embodiment of the present application provides an application of the oil-soluble composition provided in the first aspect in skin care products. Description of the Drawings

[0038] In order to more clearly illustrate the technical solutions of the embodiments of the present application, the following will briefly introduce the drawings required to be used in the embodiments of the present application. It should be understood that the following drawings only show some embodiments of the present application, and therefore should not be regarded as limiting the scope. For those of ordinary skill in the art, other related drawings can be obtained based on these drawings without creative efforts.

[0039] Figure 1It is a matching binding diagram of shikonin and iNOS receptor;

[0040] Figure 2 It is a matching binding diagram of shikonin and TRPV1 receptor;

[0041] Figure 3 It is a matching binding diagram of shikonin and CDK1 receptor;

[0042] Figure 4 It is a matching binding diagram of dracorhodin perchlorate and iNOS receptor;

[0043] Figure 5 It is a matching binding diagram of dracorhodin perchlorate and TRPV1 receptor;

[0044] Figure 6 It is a matching binding diagram of dracorhodin perchlorate and CDK1 receptor. Detailed implementation manners

[0045] To make the objectives, technical solutions and advantages of the embodiments of the present application clearer, the technical solutions in the embodiments of the present application will be clearly and completely described below. For those not specified in the embodiments, the conventional conditions or the conditions recommended by the manufacturer are followed. For the reagents or instruments not specified by the manufacturer, they are all conventional products that can be obtained through commercial purchase.

[0046] The oil-soluble composition of the embodiments of the present application, its preparation method and applications will be specifically described below.

[0047] The embodiments of the present application provide an oil-soluble composition, and its components by mass percentage include: 20%-50% of purple gromwell root extract; 20%-39% of dragon's blood extract; 0.01%-30% of vegetable oil; 0.01%-40% of emollient.

[0048] In some embodiments of the present application, the components of the oil-soluble composition by mass percentage include: 30%-50% of purple gromwell root extract, optionally 40%-45%; 29%-39% of dragon's blood extract, optionally 30%-35%; 5%-25.6% of vegetable oil; 5%-15.4% of emollient.

[0049] Exemplarily, the components of the oil-soluble composition by mass percentage include: 20%, 25%, 30%, 35%, 40%, 45%, 50% of purple gromwell root extract or an intermediate value between any two of the above values; 20%, 25%, 29%, 35%, 39% of dragon's blood extract or an intermediate value between any two of the above values; 0.01%, 5%, 10%, 15%, 20%, 25.6%, 30% of vegetable oil or an intermediate value between any two of the above values; 0.01%, 5%, 10%, 15.4%, 20%, 25%, 30%, 40% of emollient or an intermediate value between any two of the above values.

[0050] In some embodiments of the present application, the vegetable oil includes at least one of wild soybean oil, jojoba oil, and olive oil;

[0051] And / or, the emollient mainly refers to synthetic ester emollients, including at least one of hydrogenated polydecene, isododecane, squalane, glyceryl tricaprylate, glyceryl tricaprate, and ethylhexyl palmitate.

[0052] In some embodiments of the present application, the components of the oil-soluble composition further include, by mass percentage: octyldodecanol 0.00779% - 0.779%; ribes nigrum seed oil 0.00126% - 0.126%; rosemary leaf extract 0.00005% - 0.005%.

[0053] In some embodiments of the present application, the components of the oil-soluble composition further include, by mass percentage: antioxidant 0.005% - 0.1%; anti-inflammatory ingredient 0.0001% - 0.1%.

[0054] In some embodiments of the present application, the antioxidant includes at least one of tocopherol (vitamin E), vitamin E derivatives, and coenzyme Q10.

[0055] In some embodiments of the present application, the anti-inflammatory ingredient includes phytosterol components and natural anti-inflammatory extracts. As an implementation manner, the anti-inflammatory ingredient includes, by mass percentage: the components of the oil-soluble composition further include: sunflower seed oil unsaponifiables 0.0003% - 0.03%; sunflower seed oil 0.00005% - 0.005%; cardiospermum halicacabum extract 0.00005% - 0.005%. The cardiospermum halicacabum extract refers to the extract of flowers, leaves, and vines.

[0056] As an embodiment, the components of the oil-soluble composition by mass percentage include: Lithospermum erythrorhizon extract 5%-50%; Dracaena cochinchinensis extract 5%-39%; Glycine soja oil 0.01%-30%; hydrogenated polydecene 0.01%-40%; octyldodecanol 0.00779%-0.779%; Ribes nigrum seed oil 0.00126%-0.126%; Rosmarinus officinalis leaf extract 0.00005%-0.005%; tocopherol (vitamin E) 0.005%-0.1%; unsaponifiables of sunflower seed oil 0.0003%-0.03%; sunflower seed oil 0.00005%-0.005%; Cardiospermum halicacabum extract 0.00005%-0.005%. This oil-soluble composition not only has the aforementioned technical effects, but also Glycine soja oil and tocopherol have a synergistic effect; hydrogenated polydecene and octyldodecanol synergistically improve the spreading property of the system and reduce the greasiness; hydrogenated polydecene and tocopherol prevent the oxidative degradation of active ingredients through antioxidant action; Ribes nigrum seed oil and tocopherol can form an antioxidant-barrier repair linkage (replenishing essential fatty acids in a timely manner after free radicals are scavenged); rosmarinol quickly neutralizes highly reactive oxygen free radicals, and tocopherol continuously protects the lipid layer, jointly preventing the oxidative rancidity of the oil phase and prolonging the stability of the formulation.

[0057] In other embodiments, other vegetable oils can be used to partially or completely replace Glycine soja oil, other emollients can be used to partially or completely replace hydrogenated polydecene, other antioxidants can be used to partially or completely replace tocopherol (vitamin E), and other combinations of anti-inflammatory components can be used.

[0058] In some embodiments of the present application, the Lithospermum erythrorhizon extract includes shikonin (the anti-inflammatory active ingredient), and the content of shikonin in the Lithospermum erythrorhizon extract is 90 - 130 μg·mL -1 ; the content of shikonin in the oil-soluble composition is 33 - 55 μg·mL -1 .

[0059] In some embodiments of the present application, the Dracaena cochinchinensis extract includes dracorhodin perchlorate (the anti-inflammatory active ingredient), and the content of dracorhodin perchlorate in the Dracaena cochinchinensis extract is 60 - 100 μg·mL -1 ; the content of dracorhodin perchlorate in the oil-soluble composition is 23.2 - 40 μg·mL -1 .

[0060] In addition, the embodiments of the present application also provide a preparation method of the aforementioned oil-soluble composition, which mixes and emulsifies each component.

[0061] In some embodiments of the present application, the Radix Arnebiae (Radix Lithospermi) extract and Dracaena cochinchinensis extract can be obtained by supercritical CO2 extraction. The fat-soluble components are separated using the solubility of supercritical CO2 to obtain an extract with a high content of anti-inflammatory active ingredients. As an implementation method, the preparation methods of the Radix Arnebiae (Radix Lithospermi) extract and Dracaena cochinchinensis extract are as follows: After drying the Radix Arnebiae (Radix Lithospermi) or Dracaena cochinchinensis, it is loaded into the extraction kettle, and the parameters are set: pressure 25 - 35 MPa, temperature about 50 °C, and CO2 flow rate 20 - 30 L / h. The extract is collected in the separation kettle.

[0062] In addition, other plant extracts (such as wild soybean oil, blackcurrant seed oil, rosemary leaf extract, sunflower oil unsaponifiables, sunflower oil, Cardiospermum halicacabum extract, etc.) can also be extracted by supercritical CO2 extraction respectively.

[0063] In addition, the embodiments of the present application also provide an application of the aforementioned oil-soluble composition in skin care products.

[0064] The components of the oil-soluble composition in the embodiments of the present application are all oil-soluble and are suitable for oil-soluble products. In some embodiments of the present application, the oil-soluble composition can be applied to a cream, and an emulsifier (such as glyceryl stearate) and an aqueous phase component need to be additionally added to form a cream. In addition, essence oil, lotion, ointment and other products can also be formed based on the oil-soluble formula, and other additives need to be added accordingly.

[0065] The features and properties of the present application will be further described in detail below in conjunction with the embodiments.

[0066] Example 1

[0067] This example provides an oil-soluble composition, and its components are calculated by mass percentage as follows: Radix Arnebiae (Radix Lithospermi) extract 42%; Dracaena cochinchinensis extract 33%; wild soybean oil 12.3%; hydrogenated polydecene 12.2%; octyldodecanol 0.4%; blackcurrant seed oil 0.037%; sunflower oil unsaponifiables 0.01%; Cardiospermum halicacabum flower / leaf / vine extract 0.001%; tocopherol (vitamin E) 0.05%; sunflower oil 0.001%; rosemary leaf extract 0.001%.

[0068] Among them, the Radix Arnebiae (Radix Lithospermi) extract, Dracaena cochinchinensis extract, wild soybean oil, blackcurrant seed oil, sunflower oil unsaponifiables, Cardiospermum halicacabum flower / leaf / vine extract, sunflower oil, and rosemary leaf extract are all extracted by supercritical CO2 extraction;

[0069] Tocopherol (vitamin E), hydrogenated polydecene, and octyldodecanol are commercially available finished products purchased.

[0070] In this example, the above components are mixed, and the prepared oil-soluble composition is denoted as A.

[0071] Example 2

[0072] This embodiment provides a method for preparing an oil-soluble composition, and its components are as follows by mass percentage:

[0073] Gromwell root extract: 50%; Dragon's blood extract: 39%; Wild soybean oil: 5%; Hydrogenated polydecene: 5%; Octyldodecanol: 0.779%; Blackcurrant seed oil: 0.126%; Unsaponifiable matter of sunflower oil: 0.03%; Cardiospermum halicacabum flower / leaf / vine extract: 0.005%; Tocopherol (vitamin E): 0.05%; Sunflower oil: 0.005%; Rosemary leaf extract: 0.005%.

[0074] The sources of the components in this embodiment are the same as those in Example 1, and the oil-soluble composition prepared in this embodiment is denoted as B.

[0075] Example 3

[0076] This embodiment provides an oil-soluble composition, and its components are as follows by mass percentage: Gromwell root extract: 30%; Dragon's blood extract: 29%; Wild soybean oil: 25.58%; Hydrogenated polydecene: 15.39%; Octyldodecanol: 0.005%; Blackcurrant seed oil: 0.002%; Unsaponifiable matter of sunflower oil: 0.003%; Cardiospermum halicacabum flower / leaf / vine extract: 0.005%; Tocopherol (vitamin E): 0.005%; Sunflower oil: 0.005%; Rosemary leaf extract: 0.005%.

[0077] The sources of the components in this embodiment are the same as those in Example 1, and the oil-soluble composition prepared in this embodiment is denoted as C.

[0078] Example 4

[0079] This embodiment provides an oil-soluble composition, which is different from that in Example 1 in that jojoba oil is used to replace wild soybean oil.

[0080] Example 5

[0081] This embodiment provides an oil-soluble composition, which is different from that in Example 1 in that squalane is used to replace hydrogenated polydecene.

[0082] Example 6

[0083] This embodiment provides an oil-soluble composition, and its components are as follows by mass percentage: Gromwell root extract: 33%; Dragon's blood extract: 33%; Wild soybean oil: 17%; Hydrogenated polydecene: 17%.

[0084] Comparative Example 1

[0085] This comparative example provides an oil-soluble composition, which is different from that of Example 1 in that the components of this comparative example are as follows by mass percentage: chamomile extract 42%; dragon's blood extract 33%; wild soybean oil 12.3%; hydrogenated polydecene 12.2%; octyldodecanol 0.4%; blackcurrant seed oil 0.037%; sunflower oil unsaponifiables 0.01%; Cardiospermum halicacabum flower / leaf / vine extract 0.001%; tocopherol (vitamin E) 0.05%; sunflower oil 0.001%; rosemary leaf extract 0.001%.

[0086] Among them, the chamomile extract is obtained by supercritical CO2 extraction, and the sources of the remaining components are the same as those in Example 1.

[0087] The oil-soluble composition prepared in this comparative example is denoted as M1.

[0088] Comparative Example 2

[0089] This comparative example provides an oil-soluble composition, which is different from that of Example 1 in that the components of this comparative example are as follows by mass percentage: camellia seed extract 42%; dragon's blood extract 33%; wild soybean oil 12.3%; hydrogenated polydecene 12.2%; octyldodecanol 0.4%; blackcurrant seed oil 0.037%; sunflower oil unsaponifiables 0.01%; Cardiospermum halicacabum flower / leaf / vine extract 0.001%; tocopherol (vitamin E) 0.05%; sunflower oil 0.001%; rosemary leaf extract 0.001%.

[0090] Among them, the camellia seed extract is obtained by supercritical CO2 extraction, and the sources of the remaining components are the same as those in Example 1.

[0091] The oil-soluble composition prepared by the preparation method provided in this comparative example is denoted as M2.

[0092] Comparative Example 3

[0093] This comparative example provides an oil-soluble composition, which is different from that of Example 1 in that the components of this comparative example are as follows by mass percentage: purple gromwell root extract 42%; guaiac wood extract 33%; wild soybean oil 12.3%; hydrogenated polydecene 12.2%; octyldodecanol 0.4%; blackcurrant seed oil 0.037%; sunflower oil unsaponifiables 0.01%; Cardiospermum halicacabum flower / leaf / vine extract 0.001%; tocopherol (vitamin E) 0.05%; sunflower oil 0.001%; rosemary leaf extract 0.001%.

[0094] Among them, the guaiac wood extract is obtained by supercritical CO2 extraction, and the sources of the remaining components are the same as those in Example 1.

[0095] The oil-soluble composition prepared in this comparative example is denoted as M3.

[0096] Comparative Example 4

[0097] This comparative example provides an oil-soluble composition, which is different from that of Example 1 in that the components of this comparative example are as follows by mass percentage: Lithospermum erythrorhizon extract 42%; Lotus extract 33%; Glycine soja oil 12.3%; Hydrogenated polydecene 12.2%; Octyldodecanol 0.4%; Ribes nigrum seed oil 0.037%; Sunflower oil unsaponifiables 0.01%; Cardiospermum halicacabum flower / leaf / vine extract 0.001%; Tocopherol (vitamin E) 0.05%; Sunflower oil 0.001%; Rosemary leaf extract 0.001%.

[0098] Among them, the lotus extract is obtained by supercritical CO2 extraction method, and the sources of the remaining components are the same as those in Example 1.

[0099] The oil-soluble composition prepared in this comparative example is denoted as M4.

[0100] Comparative Example 5

[0101] This comparative example provides an oil-soluble composition, which is different from that of Example 1 in that the components of this comparative example are as follows by mass percentage: Chamomile extract 42%; Guaiacum extract 33%; Glycine soja oil 12.3%; Hydrogenated polydecene 12.2%; Octyldodecanol 0.4%; Ribes nigrum seed oil 0.037%; Sunflower oil unsaponifiables 0.01%; Cardiospermum halicacabum flower / leaf / vine extract 0.001%; Tocopherol (vitamin E) 0.05%; Sunflower oil 0.001%; Rosemary leaf extract 0.001%.

[0102] Among them, the chamomile extract and the guaiacum extract are obtained by supercritical CO2 extraction method, and the sources of the remaining components are the same as those in Example 1.

[0103] The oil-soluble composition prepared in this comparative example is denoted as M5.

[0104] The oil-soluble compositions of the foregoing Examples 1-3 and Comparative Examples 1-5 were tested below.

[0105] Test Example 1

[0106] In this test example, the oil-soluble compositions A-C prepared in Examples 1-3 were analyzed and detected for their components, and the contents of shikonin and dracorhodin were determined by HPLC method. Chromatographic conditions: Chromatographic column: Agilent C18 (250 mm × 4.6 mm, 5 μm); Mobile phase for shikonin content determination: Methanol-water (85:15); Flow rate: 1.0 mL·min -1 ; Column temperature: 40 °C; Detection wavelength 516 nm; Injection volume: 5 μL. Prepared into 10 - 50 μg·mL -1A series of shikonin standard solutions were used to calculate the content of shikonin by the external standard method. Mobile phase for the determination of dracorhodin content: acetonitrile - 0.05 mol / L sodium dihydrogen phosphate solution (35∶65); flow rate: 1.0 mL·min -1 ; column temperature: 40 °C; detection wavelength 440 nm; injection volume: 5 μL. A series of dracorhodin standard solutions with a concentration of 5 - 20 mg·mL -1 were prepared, and the content of dracorhodin was calculated by the external standard method. The detection results are shown in Table 2.

[0107] Table 2 Composition of the oil-soluble composition

[0108] sample <![CDATA[Shikonin (μg·mL -1 )]]> <![CDATA[Dracorhodin (mg·mL -1 )]]> A 46.2 26.4 B 55 40 C 33 23.2

[0109] As can be seen from the results in Table 2, by comparing the oil-soluble compositions A - C prepared in Examples 1 - 3, it can be observed that the contents of shikonin and dracorhodin are positively correlated with the contents of purple perilla root extract and dragon's blood extract.

[0110] Test Example 2 (Molecular Docking)

[0111] 1. Experimental materials

[0112] Receptors: PDB structures of iNOs, TRPV1, and CDK1 proteins.

[0113] Ligands: shikonin, dracorhodin.

[0114] Operation and analysis software: Chem 3D, PyMOL; Autodock Vina, AutodockTools

[0115] 2. Experimental methods and procedures

[0116] Search for the small molecule structures in PubChem and download the structures in 3d.sdf format; for the molecular structures not available in PubChem, draw and save them using ChemDraw. Select the MM2 force field in Chem 3D for energy minimization and save as PDB format. Perform molecular docking calculations using the Autodock Vina software: match the ligand with the receptor, delimit a search area within the residues of the receptor amino acids to be tested, calculate the grid energy by scanning different atoms respectively, continuously adjust the conformation, position, and orientation of the ligand, and perform scoring and ranking to obtain the conformation with the lowest energy as the output result. Execute the molecular docking operation using AutodockTools and start PyMOL to analyze the results.

[0117] Table 3 Experimental results

[0118]

[0119]

[0120] The first group detected shikonin, and its binding energy with the iNOS receptor was -9.1 Kcal / mol( Figure 1 ), and its binding energy with the TRPV1 receptor was -9.1 Kcal / mol( Figure 2 ), and its binding energy with the CDK1 receptor was -9.3 Kcal / mol( Figure 3 ). The second group detected dracorhodin perchlorate, and its binding energy with the iNOS receptor was analyzed to be -10.9 Kcal / mol( Figure 4 ), and its binding energy with the TRPV1 receptor was -8.7 Kcal / mol( Figure 5 ), and its binding energy with the CDK1 receptor was -10 Kcal / mol( Figure 6 ). Comparing and analyzing the binding energies of the above molecular docking with -5 Kcal / mol indicated that the above molecular docking results were reliable.

[0121] The above results confirmed that the binding energies of shikonin and dracorhodin perchlorate with three conventional soothing and anti-inflammatory related receptors (iNOS receptor, TRPV1 receptor, CDK1 receptor) were all low (less than -8 kcal / mol), with strong biological activities and the ability to regulate inflammatory responses.

[0122] Experimental Example 3

[0123] Relieving skin redness caused by capsaicin

[0124] 1) Preparation before testing

[0125] a. Testing instruments: VapoMeter, SkinColorCatch.

[0126] b. Subject criteria: 31 healthy volunteers were screened, aged 25 - 60 years old.

[0127] c. Test site: The inner side of the forearms of both hands, marking a 3×3 cm 2 test area, and 2 areas were marked on the same arm simultaneously, with an interval of 1 cm between the areas.

[0128] d. Test substances: The test sample was a 5% oil-soluble composition, and the blank control group was water.

[0129] e. Environmental conditions: The test should be carried out in an environment with a temperature of (21 ± 1) °C and a relative humidity of (50 ± 10)%, and the subjects should sit still in the test environment for 30 min before evaluation and testing.

[0130] 2) Determination

[0131] a. Pre - use detection: Use an instrument to detect the initial transepidermal water loss rate (TEWL) and erythema value (Erythema) of each product area and the control area. Measure them in parallel 3 times and take the average value as the baseline value.

[0132] b. Sample application method: The test samples and blank controls are randomly distributed on the left and right arms. The test specimens are evenly coated on the test area at a dosage of 2.0 ± 0.1 mg / cm2.

[0133] c. Capsaicin stimulation: Treat the above - mentioned test areas with 0.075% capsaicin (model group and sample group) for 30 min, measure the transepidermal water loss rate (TEWL) and erythema (Erythema), and evaluate the repair status by comparing the test results of the sample group and the model group.

[0134] Table 4 Experimental results

[0135] group <![CDATA[ΔTEWL (g / h / m 2 )]]> ΔErythema model group 21.2 41.5 A 13.5 33.8 B 13.3 33.5 C 14.8 34.2 M1 18.4 38.6 M2 18.9 39.5 M3 18.5 39.1 M4 19.1 39.7 M5 18.1 38.9

[0136] As can be seen from the above table, compared with the model group, the examples can effectively relieve the increase in transdermal water loss and erythema caused by capsaicin stimulation, while the comparative examples have a very limited effect on relieving the increase in TEWL and Erythema. The effects of the examples are better than those of the comparative examples.

[0137] In summary, the examples have the effect of relieving the increase in skin erythema value caused by capsaicin stimulation and have a soothing effect on repairing skin irritation.

[0138] In conclusion, the oil - soluble composition, its preparation method and application in the embodiments of the present application have excellent anti - inflammatory and soothing effects on the skin.

[0139] The above are only the embodiments of the present application and are not used to limit the protection scope of the present application. For those skilled in the art, the present application can have various changes and modifications. Any modification, equivalent replacement, improvement, etc. made within the spirit and principle of the present application shall be included in the protection scope of the present application.

Claims

1. An oil-soluble composition, characterized in that, Its components by mass percentage include:

2. The oil-soluble composition according to claim 1, characterized in that, Its components by mass percentage include:

3. The oil-soluble composition according to claim 1 or 2, characterized in that, The vegetable oil includes at least one of wild soybean oil, jojoba oil, and olive oil; And / or, the emollient includes at least one of hydrogenated polydecene, isododecane, squalane, glyceryl tricaprylate, glyceryl tricaprate, and ethylhexyl palmitate.

4. The oil-soluble composition according to claim 1, wherein Its components by mass percentage further include: Octyldodecanol 0.00779% - 0.779%; Ribes nigrum seed oil 0.00126% - 0.126%; Rosmarinus officinalis leaf extract 0.00005% - 0.005%.

5. The oil-soluble composition according to claim 1, characterized in that, Its components by mass percentage further include: Antioxidant 0.005% - 0.1%; Anti-inflammatory component 0.0001% - 0.1%.

6. The oil-soluble composition according to claim 5, wherein The antioxidant includes at least one of tocopherol, vitamin E derivatives, and coenzyme Q10; And / or, the anti-inflammatory component by mass percentage includes: Sunflower oil unsaponifiables 0.0003% - 0.03%; Sunflower oil 0.00005% - 0.005%; Cardiospermum halicacabum extract 0.00005% - 0.005%.

7. The oil-soluble composition according to claim 1, wherein The purple gromwell root extract includes shikonin, and the content of shikonin in the purple gromwell root extract is 90-130 μg·mL -1 ; the content of shikonin in the oil-soluble composition is 33-55 μg·mL -1 .

8. The oil-soluble composition according to claim 7, wherein, The dragon's blood extract includes dracorhodin, and the content of dracorhodin in the dragon's blood extract is 60 - 100 μg·mL -1 ; the content of dracorhodin in the oil-soluble composition is 23.2 - 40 μg·mL -1 .

9. A method for preparing an oil-soluble composition according to any one of claims 1 to 8, characterized in that, It mixes and emulsifies each component.

10. Use of an oil-soluble composition according to any one of claims 1 to 8 in skin care products.

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