A supramolecular anti-aging composition suitable for sensitive skin population, and a preparation method and application thereof

Abstract

The present application relates to the field of medical devices, the field of medical or toiletry formulations, the field of biopharmaceutical manufacturing technology and the field of formulation manufacturing technology, in particular to a supramolecular anti-aging composition suitable for sensitive skin population and a preparation method and application thereof. Active ingredients, inclusion materials, emulsifiers and solvents; the active ingredients include: silymarin, silatrane and phytol; the silymarin includes silybin, silychristin and silydianin; the inclusion material includes at least one of hydroxypropyl-alpha-cyclodextrin and hydroxypropyl-beta-cyclodextrin; the emulsifier includes at least one of oleyl polyether-20, Tween 80 and PPG-13-decyltetradecyl alcohol polyether-24; the solvent includes water and polyhydric alcohol. The composition provided by the present application has excellent anti-aging efficacy and stability, and has good effect of reducing allergy, and is suitable for sensitive population.

Description

Technical Field

[0001] This invention relates to the fields of medical devices, medical or cosmetic preparations, biopharmaceutical manufacturing technology, and formulation manufacturing technology, specifically to a supramolecular anti-aging composition suitable for people with sensitive skin, its preparation method, and its application. Background Technology

[0002] Silymarin is a class of flavonoid lignan compounds extracted from the seeds of the silymarin plant (Silybum marianum) of the Asteraceae family. Its main active components include silybin, isosilybin, silymarinine, and silymarinine. Modern pharmacological studies have shown that silymarin has significant anti-aging biological effects, mainly reflected in three aspects: (1) potent antioxidant activity: it can effectively scavenge free radicals, inhibit lipid peroxidation, and slow down cellular oxidative damage; (2) collagen metabolism regulation: it promotes the synthesis of type I, type III, and type XVII collagen, while inhibiting the degradation of collagen by matrix metalloproteinases (MMPs); (3) anti-inflammatory and barrier repair: it inhibits the release of pro-inflammatory factors such as IL-1α, IL-6, and TNF-α, and improves the skin's immune barrier function.

[0003] Silymarin is poorly soluble in water and tends to crystallize in water-based formulations (such as medical dressings or cosmetics). It also exhibits slight precipitation in ethanol-based formulations (such as medical dressings or cosmetics), especially during stable storage.

[0004] Nanoemulsion technology is one of the methods to improve the solubility of milk thistle. It mainly improves solubility and permeability by reducing particle size. Although this system can improve solubility, it has problems such as easy stratification during long-term storage of nanoemulsions, reliance on high concentrations of synthetic emulsifiers, and potential damage to the skin barrier with long-term use.

[0005] Therefore, there is still an urgent need for a composition with good stability and anti-aging effects. Summary of the Invention

[0006] To address the aforementioned technical problems, the present invention provides the following technical solutions.

[0007] In a first aspect, the present invention provides a composition.

[0008] A composition comprising: an active ingredient, an inclusion material, an emulsifier, and a solvent; said active ingredient comprising: silymarin, silanetriol, and phytol; said silymarin comprising silybin, silymarinine, and silymarinine; said inclusion material comprising at least one of hydroxypropyl-α-cyclodextrin and hydroxypropyl-β-cyclodextrin; said emulsifier comprising at least one of oleyl alcohol polyether-20, Tween 80, and PPG-13-decyltetradecyl alcohol polyether-24; said solvent comprising water and a polyol;

[0009] in,

[0010] The weight ratio of silybin, silybinin and silybinin in the silybin is (2.5~4.3):1:(0.1~0.25).

[0011] The weight ratio of silymarin to silanetriol is (1~10):(0.5~5).

[0012] The weight ratio of silymarin to phytol is (1~10):(1~2).

[0013] Based on the total mass of the composition, the total content of the active ingredient is 3wt% to 17wt%, the content of the inclusion material is 5wt% to 30wt%, the content of the emulsifier is 2wt% to 15wt%, the content of the polyol is 9wt% to 25wt%, and the content of water is 43wt% to 63wt%.

[0014] Silanetriol is a class of organosilicon compounds that possesses the natural bioactive form of silicon in the human body. Its small molecular structure gives it extremely high skin affinity and permeability, allowing it to be directly utilized by the skin. Simultaneously, it can regulate the skin's immune response, effectively relieving irritation caused by external stimuli; it can also promote the synthesis of collagen and elastin by fibroblasts. In this invention, the inventors discovered that silanetriol can associate with milk thistle within the cavity of the inclusion material provided by this invention to form a supramolecular hydrogen bond network, reducing the crystallization tendency of silymarin.

[0015] Phytol (CAS 7541-49-3) is an unsaturated higher alcohol containing 20 carbon atoms, with the molecular formula C64-32 ... 20 H 40 O, belongs to the diterpenoid class of compounds. This substance is naturally present in the molecular structure of chlorophyll and has attracted attention in the skincare industry due to its unique biological activity. It is known as "phytoretinol" and provides anti-aging effects similar to retinol but is generally gentler. It can activate RXR / PPAR receptors, promote collagen production, terminate free radical chain reactions, and inhibit inflammatory factors such as IL-1β and NF-κB.

[0016] In some embodiments, the polyol includes at least one selected from dipropylene glycol, 1,2-pentanediol, 1,3-butanediol, hexyldecyl alcohol, 1,2-propanediol, 1,3-propanediol, 1,2-hexanediol, and methylpropanediol.

[0017] In some embodiments, the polyol comprises a first polyol and a second polyol; wherein the first polyol comprises at least one of dipropylene glycol, methyl propylene glycol, or 1,3-butanediol; and the second polyol comprises 1,2-pentanediol.

[0018] In some embodiments, the weight ratio of the first polyol to the second polyol is (4~20):5. In some embodiments, the weight ratio of the first polyol to the second polyol is 4:5, 5:5, 6:5, 7:5, 8:5, 9:5, 10:5, 11:5, 12:5, 13:5, 14:5, 15:5, 16:5, 17:5, 18:5, 19:5, 20:5, or any value between any two of these values.

[0019] In some embodiments, the total content of the active ingredient is 3wt% to 17wt%, the content of the inclusion material is 5wt% to 30wt%, the content of the emulsifier is 2wt% to 15wt%, the content of the polyol is 9wt% to 25wt%, and the balance is water, calculated based on the total mass of the composition.

[0020] In some embodiments, silanetriol is methylsilanetriol.

[0021] In some embodiments, the weight ratio of silybin and silybinin in silymarin is (2.5~4.3):1:(0.1~0.25), where (2.5~4.3) can be 2.5, 3, 3.5, 4, 4.3, or any value within the range of any two values; and (0.1~0.25) can be 0.1, 0.2, 0.25, or any value within the range of any two values.

[0022] In some embodiments, the weight ratio of silymarin to silanetriol is (1~10):(0.5~5), where (1~10) can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, or any value within the range of any two values; and (0.5~5) can be 0.5, 1, 2, 3, 4, 5, or any value within the range of any two values.

[0023] In some embodiments, the weight ratio of silymarin to phytol is (1~10):(1~2), where (1~10) can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, or any value within the range of any two values; where (1~2) can be 1, 1.5, 2, or any value within the range of any two values.

[0024] In some embodiments, the weight ratio of silybin to silybinin in silymarin is 2.5:1 to 4.3:1; the weight ratio of silybinin to silybinine in silymarin is 1:0.1 to 1:0.25; the weight ratio of silymarin to silanetriol is 1:1 to 8:1; and the weight ratio of silymarin to phytol is 1:1 to 5:1.

[0025] In some embodiments, the weight ratio of silybin to silybinin in the silybin is 2.5:1, 3:1, 3.5:1, 4:1, 4.3:1, or any value within the range of any two of these values.

[0026] In some embodiments, the weight ratio of silymarin to silymarin in the silymarin is 1:0.1, 1:0.15, 1:0.2, 1:0.25, or any value within the range of any two of these values.

[0027] In some embodiments, the weight ratio of silymarin to silanetriol is 1:1, 1.5:1, 2:1, 2.5:1, 3:1, 3.5:1, 4:1, 4.5:1, 5:1, 5.5:1, 6:1, 6.5:1, 7:1, 8:1, or any value within a range of any two of these ratios.

[0028] In some embodiments, the weight ratio of silymarin to phytol is 1:1, 1.5:1, 2:1, 2.5:1, 3:1, 3.5:1, 4:1, 4.5, 5:1, or any value within a range of any two of these values.

[0029] In some embodiments, the weight ratio of silybin to silybinine in silybin is 4.3:1, the weight ratio of silybinine to silybinine in silybin is 1:0.2, the weight ratio of silybin to silanetriol is 4:3, and the weight ratio of silybin to phytol is 2:1.

[0030] In some embodiments, the weight ratio of silybin to silybinine in silybin is 2.5:1, the weight ratio of silybinine to silybinine in silybin is 1:0.25, the weight ratio of silybin to silanetriol is 2:1, and the weight ratio of silybin to phytol is 5:1.

[0031] In some embodiments, the weight ratio of silybin to silybinine in silybin is 3:1, the weight ratio of silybinine to silybinine in silybin is 1:0.1, the weight ratio of silybin to silanetriol is 1:1, and the weight ratio of silybin to phytol is 1:1.

[0032] In some embodiments, the weight ratio of silybin to silybinine in silybin is 4.3:1, the weight ratio of silybinine to silybinine in silybin is 1:0.2, the weight ratio of silybin to silanetriol is 8:1, and the weight ratio of silybin to phytol is 2:1.

[0033] In some embodiments, the weight ratio of silybin to silybinine in silybin is 4.3:1, the weight ratio of silybinine to silybinine in silybin is 1:0.2, the weight ratio of silybin to silanetriol is 4:1, and the weight ratio of silybin to phytol is 2:1.

[0034] In some embodiments, the first polyol is at least one selected from dipropylene glycol, methylpropanediol, or 1,3-butanediol. In some embodiments, the first polyol is both dipropylene glycol and methylpropanediol. In some embodiments, the first polyol is 1,3-butanediol.

[0035] In some embodiments, the first polyol is dipropylene glycol and methylpropanediol, and the second polyol is 1,2-pentanediol; the weight ratio of the first polyol to the second polyol is (4~10):5. In some embodiments, the first polyol is dipropylene glycol and methylpropanediol, and the second polyol is 1,2-pentanediol; the weight ratio of the first polyol to the second polyol is 4:5, 5:5, 6:5, 7:5, 8:5, 9:5, 10:5, or any value between any two of these values.

[0036] In some embodiments, the first polyol is 1,3-butanediol, the second polyol is 1,2-pentanediol, and the weight ratio of the 1,3-butanediol to the 1,2-pentanediol is 20:5.

[0037] In some embodiments, the total content of the active ingredient, calculated by the total mass of the composition, is 3 wt%, 4 wt%, 5 wt%, 6 wt%, 7 wt%, 8 wt%, 9 wt%, 10 wt%, 11 wt%, 12 wt%, 13 wt%, 14 wt%, 15 wt%, 16 wt%, 17 wt%, or any value within a range of any two of these values.

[0038] In some embodiments, the content of the inclusion material, calculated by the total mass of the composition, is 5 wt%, 10 wt%, 15 wt%, 20 wt%, 25 wt%, 30 wt%, or any value within a range of any two of these values.

[0039] In some embodiments, the content of the emulsifier, calculated by the total mass of the composition, is 2 wt%, 3 wt%, 4 wt%, 5 wt%, 6 wt%, 7 wt%, 8 wt%, 9 wt%, 10 wt%, 11 wt%, 12 wt%, 13 wt%, 14 wt%, 15 wt%, or any value within a range of any two of these values.

[0040] In some embodiments, the content of the polyol, calculated by the total mass of the composition, is 9 wt%, 10 wt%, 15 wt%, 17 wt%, 20 wt%, 25 wt%, or any value within a range of any two of these values.

[0041] In some embodiments, the water content, calculated by the total mass of the composition, is 43 wt%, 44 wt%, 45 wt%, 46 wt%, 47 wt%, 48 wt%, 49 wt%, 50 wt%, 51 wt%, 52 wt%, 53 wt%, 53.5 wt%, 54 wt%, 55 wt%, 56 wt%, 57 wt%, 58 wt%, 59 wt%, 60 wt%, 61 wt%, 62 wt%, 63 wt%, or any value within a range of any two of these values.

[0042] In some embodiments, the composition comprises the following components in the following proportions: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water, calculated by the total mass of the composition.

[0043] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% oleyl alcohol-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0044] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 10 wt% silymarin, 5 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0045] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 10 wt% silymarin, 5 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 2.5:1:0.25.

[0046] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 1 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 1 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0047] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 1 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 1 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of silymarin:silymarinine:silymarinine = 3:1:0.1.

[0048] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 0.5 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0049] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 0.5 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, and the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0050] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 5 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0051] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 5 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of silymarin:silymarinine:silymarinine = 4.3:1:0.2.

[0052] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 30 wt% hydroxypropyl-β-cyclodextrin, 2 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0053] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 30 wt% hydroxypropyl-β-cyclodextrin, 2 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0054] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 10 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 2 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0055] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 10 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 2 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0056] In some embodiments, the composition comprises, by total mass, the following components in the amounts of: 4 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 10 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 15 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0057] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 10 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 15 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0058] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 20 wt% 1,3-butanediol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water.

[0059] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 20 wt% 1,3-butanediol, 2 wt% phytol, 10 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0060] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 30 wt% hydroxypropyl-β-cyclodextrin, 2 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% Tween-80, 5 wt% 1,2-pentanediol, with the balance being water.

[0061] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 1 wt% silanetriol, 30 wt% hydroxypropyl-β-cyclodextrin, 2 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% Tween-80, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0062] In some embodiments, the composition comprises, by total mass, the following components in the amounts of: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% Tween-80, with the balance being water.

[0063] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% Tween-80, and the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of silymarin:silymarinine:silymarinine = 4.3:1:0.2.

[0064] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% PPG-13-decyltetradecyl alcohol polyether-24, with the balance being water.

[0065] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% PPG-13-decyltetradecyl alcohol polyether-24, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0066] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% PPG-13-decyltetradecyl alcohol polyether-24, with the balance being water.

[0067] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-β-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% PPG-13-decyltetradecyl alcohol polyether-24, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0068] In some embodiments, the composition comprises the following components in the following proportions: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-α-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% oleyl alcohol polyether-20, 5 wt% 1,2-pentanediol, with the balance being water, calculated by the total mass of the composition.

[0069] In some embodiments, the composition comprises, by total mass, the following components in the following amounts: 4 wt% silymarin, 3 wt% silanetriol, 15 wt% hydroxypropyl-α-cyclodextrin, 8 wt% dipropylene glycol, 2 wt% methyl propylene glycol, 2 wt% phytol, 5 wt% oleyl alcohol-20, 5 wt% 1,2-pentanediol, with the balance being water; wherein the silymarin is composed of silymarin, silymarin, and silymarin in a weight ratio of 4.3:1:0.2.

[0070] In a second aspect, the present invention provides a method for preparing the composition described in the first aspect.

[0071] A method for preparing the composition according to the first aspect, comprising:

[0072] (1) Silymarin and silanetriol were dissolved in ethanol to obtain phase A;

[0073] (2) Dissolve the inclusion material in water to obtain phase B;

[0074] (3) Mix phase A obtained in step (1) and phase B obtained in step (2), stir, and dry to obtain solid powder;

[0075] (4) The solid powder obtained in step (3) is mixed with a polyol and stirred, and then mixed with phytol and stirred to obtain mixture 1; the polyol in step (4) includes at least one of dipropylene glycol, 1,3-butanediol, hexyldecyl alcohol, 1,2-propanediol, 1,3-propanediol, methylpropanediol and 1,2-hexanediol.

[0076] (5) Mix the emulsifier with the polyol to obtain phase E, and then mix it with the mixture 1 obtained in step (4), homogenize it, and obtain mixture 2; the polyol in step (5) includes 1,2-pentanediol;

[0077] (6) Mix water and the mixture 2 obtained in step (5) to obtain the composition.

[0078] In some embodiments, the weight ratio of the sum of silymarin and silanetriol to the weight of ethanol in step (1) is (15~2):10. In some embodiments, the weight ratio of the sum of silymarin and silanetriol to the weight of ethanol in step (1) is 15:10, 14:10, 13:10, 12:10, 11:10, 10:10, 9:10, 8:10, 7:10, 6:10, 5:10, 4.5:10, 4:10, 3:10, 2:10, or any value within a range of any two of these values.

[0079] In some embodiments, the weight ratio of the encapsulating material to water in step (2) is 1:1.

[0080] In some embodiments, the weight ratio of polyol to emulsifier in step (5) is (15~2):5. In some embodiments, the weight ratio of polyol to emulsifier in step (5) is 15:5, 14:5, 13:5, 12:5, 11:5, 10:5, 9:5, 8:5, 7:5, 6:5, 5:5, 4:5, 3:5, 2:5 or any value within the range of any two of these values.

[0081] Thirdly, the present invention provides a formulation product.

[0082] A pharmaceutical preparation, characterized in that it comprises the composition described in the first aspect or the composition prepared by the preparation method described in the second aspect.

[0083] In some embodiments, the formulation product includes a medical device or a cosmetic.

[0084] In some embodiments, the medical device includes medical dressings.

[0085] In some embodiments, the cosmetic is a functional cosmetic.

[0086] In some embodiments, the formulation product is used for anti-aging.

[0087] Fourthly, the present invention provides an application.

[0088] The use of a composition described in the first aspect or a composition prepared by the preparation method described in the second aspect in the preparation of an anti-aging pharmaceutical product.

[0089] In some embodiments, the formulation product includes a medical device or a cosmetic.

[0090] In some embodiments, the medical device includes medical dressings.

[0091] In some embodiments, the cosmetic is a functional cosmetic.

[0092] Beneficial effects

[0093] Compared with the prior art, the technical solution provided by the present invention has at least one of the following beneficial technical effects:

[0094] (1) The composition provided by the present invention has excellent anti-aging effects and stability, and has a good effect on reducing allergies, making it suitable for sensitive people.

[0095] (2) The composition provided by the present invention has a significant promoting effect on type I and type III collagen genes and a significant inhibitory effect on matrix metalloproteinase MMP-1.

[0096] (3) The silymarin, silanetriol and phytol provided by the present invention work synergistically to promote the growth of type I and type III collagen genes and inhibit the matrix metalloproteinase MMP-1, resulting in an unexpected synergistic effect.

[0097] (4) Compared with other weight ratios of silymarin and silanetriol, the weight ratio of silymarin and silanetriol provided by this invention (weight ratio of silymarin and silanetriol = (10~1): (5~1)) is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has unexpected technical effects.

[0098] (5) Compared with other weight ratios of silymarin and phytol, the weight ratio of silymarin and phytol provided by this invention (weight ratio of silymarin and silanetriol = (10~1): (2~1)) is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, with unexpected technical effects.

[0099] (6) Compared with silymarin which uses only one of silybin, silybinin and silybinine, the present invention preferably uses silymarin which contains silybin, silybinin and silybinine, which is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has an unexpected synergistic effect.

[0100] (7) Compared with other weight ratios of silybin, silytin and silynin in silybin, the weight ratio of silybin, silytin and silynin in silybin provided by the present invention (silybin: silytin: silynin (weight ratio) = (2.5~4.3):1:(0.1~0.25)) is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has unexpected technical effects.

[0101] (8) In the technical solution provided by the present invention, silymarin and silanetriol associate to form a supramolecular hydrogen bond network, which reduces the crystallization tendency of silymarin; then the inclusion material provided by the present invention is used to encapsulate and improve bioavailability, greatly improve solubility, and further solve the problems of transparency and precipitation; the addition of phytol further stabilizes the supramolecular co-crystal system, and silanetriol and phytol play an unexpected synergistic effect in avoiding the crystallization of silymarin and improving the stability of the composition.

[0102] (9) Neither silanetriol nor phytol alone can achieve the technical effect of preventing silymarin crystallization and improving the stability of the composition.

[0103] (10) Compared with other weight ratios of silymarin and silanetriol, the weight ratio of silymarin and silanetriol provided by the present invention (weight ratio of silymarin and silanetriol = (10~1): (5~1)) is more conducive to avoiding crystallization of silymarin and improving the stability of the composition, and has unexpected technical effects.

[0104] (11) Compared with other weight ratios of silymarin and phytol, the weight ratio of silymarin and phytol provided by the present invention (weight ratio of silymarin and silanetriol = (10~1): (2~1)) is more conducive to avoiding silymarin crystallization and improving the stability of the composition, and has unexpected technical effects.

[0105] (12) Compared with silymarin using only one of silybin, silybinin and silybinin, the present invention preferably uses silymarin containing silybin, silybinin and silybinin, which is more conducive to avoiding silymarin crystallization and improving the stability of the composition, and has unexpected synergistic effect.

[0106] (13) Compared with other weight ratios of silybin, silytin and silynin in silybin, the weight ratio of silybin, silytin and silynin in silybin provided by the present invention (silybin: silytin: silynin (weight ratio) = (2.5~4.3):1:(0.1~0.25)) is more conducive to avoiding crystallization of silybin and improving the stability of the composition, and has unexpected technical effects.

[0107] (14) Compared with other inclusion materials (such as hydroxypropyl-α-cyclodextrin or sulfobutyl-γ-cyclodextrin), the inclusion material of the present invention preferably uses hydroxypropyl-β-cyclodextrin, which is more conducive to avoiding the crystallization of silymarin and improving the stability of the obtained composition, and has unexpected technical effects.

[0108] (15) Compared with other emulsifiers, the emulsifier of the present invention preferably uses oleyl alcohol polyether-20, which is more conducive to avoiding the crystallization of silymarin and improving the stability of the obtained composition, and has unexpected technical effects.

[0109] Terminology Explanation

[0110] In the foregoing description of this invention, all figures disclosed herein, whether or not the words “approximately” or “about” are used, are approximate values. Based on the disclosed figures, the value of each figure may vary by less than ±10% or by a difference that is considered reasonable by those skilled in the art, such as ±1%, ±2%, ±3%, ±4%, or ±5%.

[0111] The term “room temperature” refers to ambient temperature, which is between approximately 15°C and approximately 35°C, or approximately 20°C and approximately 30°C, or approximately 25°C.

[0112] The terms “optional,” “optional,” or “optionally” refer to events or situations that may, but are not necessarily, occur as described below.

[0113] The term “and / or” should be understood to mean any one of the options or any combination of two or more of the options.

[0114] The term "wt%" indicates a percentage by mass.

[0115] "Supramolecular" refers to a complex aggregate of two or more molecules that are bonded together by non-covalent interactions. These molecules are bonded together by interactions such as hydrogen bonds and electrostatic interactions, and spontaneously assemble into an ordered and functional molecular aggregate.

[0116] In the description of this specification, the references to terms such as "one embodiment," "some embodiments," "example," "specific example," or "some examples," etc., indicate that a specific feature, structure, material, or characteristic described in connection with that embodiment or example is included in at least one embodiment or example of the present invention. In this specification, the illustrative expressions of the above terms do not necessarily refer to the same embodiment or example. Furthermore, the specific features, structures, materials, or characteristics described may be combined in any suitable manner in one or more embodiments or examples. Moreover, without contradiction, those skilled in the art can combine and integrate the different embodiments or examples described in this specification, as well as the features of different embodiments or examples.

[0117] Silymarin: Its CAS number is 22888-70-6.

[0118] The CAS number for the Mizuhitate is 33889-69-9.

[0119] Silymarin: Its CAS number is 29782-68-1.

[0120] PEG-60 hydrogenated castor oil: also known as: polyoxyethylene (60) hydrogenated castor oil.

[0121] PPG-13-decyltetradecyl alcohol polyether-24: also known as polypropylene glycol-13-decyltetradecyl alcohol-24. Detailed Implementation

[0122] To enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting embodiments are further disclosed below to provide a more detailed description of the present invention.

[0123] All reagents used in this invention can be purchased commercially or prepared by the methods described in this invention.

[0124] Silanetriol: Methylsilanetriol (CH6O3Si), CAS number 2445-53-6.

[0125] Example 1: Composition

[0126] Ingredient list: see Table 1.

[0127] Table 1: Ingredient List for Example 1

[0128]

[0129] Preparation method:

[0130] (1) Mix the components of phase A, heat to 70°C (or 60°C~80°C), stir, dissolve, and obtain phase A;

[0131] (2) Mix the components of phase B, heat to 60°C (or 50°C~65°C), stir, dissolve, and obtain phase B;

[0132] (3) Mix phase A obtained in step (1) and phase B obtained in step (2), stir for 30 min, and dry under reduced pressure at 60℃ (or 55℃~65℃) to obtain solid powder;

[0133] (4) The solid powder obtained in grinding step (3) is mixed with phase C, heated to 70°C (or 60~80°C) and stirred for 30 min, then mixed with phase D and stirred at 60°C (or 60~70°C) for 10 min to obtain mixture 1;

[0134] (5) Mix the components of phase E to obtain phase E, then mix it with mixture 1 and homogenize it to obtain mixture 2;

[0135] (6) Heat phase F to 65°C (or 60-70°C), and then mix it with the mixture 2 obtained in step (5); to obtain the composition.

[0136] Comparative Example 1: Contains no active ingredients

[0137] Comparative Example 1: The only difference from Example 1 is that silymarin, silanetriol and phytol are not added, and the weight of water in phase F is adjusted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0138] Comparative Examples 2-4: Investigation of Single Active Ingredients

[0139] Comparative Example 2: The only difference from Example 1 is that silanetriol and phytol are not added (i.e., the active ingredient is only silymarin), and the weight of water in phase F is adapted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0140] Comparative Example 3: The only difference from Example 1 is that silymarin and phytol are not added (i.e., the active ingredient is only silanetriol), and the weight of water in phase F is adapted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0141] Comparative Example 4: The only difference from Example 1 is that silanetriol and silymarin are not added (i.e., the active ingredient is only phytol), and the weight of water in phase F is adapted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0142] Comparative Examples 5-7: Investigation of Dual Active Ingredients

[0143] Comparative Example 5: The only difference from Example 1 is that phytol is not added (i.e., the active ingredients are only silymarin and silanetriol), and the weight of water in phase F is adapted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0144] Comparative Example 6: The only difference from Example 1 is that silanetriol is not added (i.e., the active ingredients are only silymarin and phytol), and the weight of water in phase F is adapted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0145] Comparative Example 7: The only difference from Example 1 is that silymarin is not added (i.e., the active ingredients are only silanetriol and phytol), and the weight of water in phase F is adapted to make the sum of the weights of the other components in the composition, except for ethanol in phase A and water in phase B, 100. All other conditions are the same as in Example 1.

[0146] Comparative Examples 8-9: Investigation of the ratio of silymarin to silanetriol

[0147] Comparative Example 8: The only difference from Example 1 is that the weight parts of silanetriol are changed to 6 and the weight parts of silymarin are changed to 1, that is, the weight ratio of silymarin to silanetriol is 1:6, and other conditions are the same as in Example 1.

[0148] Comparative Example 9: The only difference from Example 1 is that the weight of silanetriol is changed to 0.5 and the weight of silymarin is changed to 6.5, that is, the weight ratio of silymarin to silanetriol is 13:1, and other conditions are the same as in Example 1.

[0149] Comparative Examples 10-11: Investigation of the ratio of silymarin to phytol

[0150] Comparative Example 10: The only difference from Example 1 is that the weight of phytol is changed to 0.4 and the weight of silymarin is changed to 5.6, that is, the weight ratio of silymarin to phytol is 14:1, and other conditions are the same as in Example 1.

[0151] Comparative Example 11: The only difference from Example 1 is that the weight parts of phytol are changed to 5 and the weight parts of silymarin are changed to 1, that is, the weight ratio of silymarin to phytol is 1:5, and other conditions are the same as in Example 1.

[0152] Comparative Examples 12-16: Investigation of Silymarin Ratio

[0153] Comparative Example 12: The difference from Example 1 is that silymarin and silymarinine are replaced with silybin, that is, silymarin contains only silybin.

[0154] Comparative Example 13: The difference from Example 1 is that silybin and silybinine are replaced with silybinin, that is, silybinin contains only silybinin.

[0155] Comparative Example 14: The difference from Example 1 is that silybin and silybinine are replaced with silybinine, that is, silybinine is the only component of silybin.

[0156] Comparative Example 15: The difference from Example 1 is that the silymarin in Comparative Example 15 is composed of silybin: silybinin: silybinin = 2.9:1:0.3 (weight ratio).

[0157] Comparative Example 16: The difference from Example 1 is that the silymarin in Comparative Example 16 is composed of silybin: silybinin: silybinin = 2.1:1:0.2 (weight ratio).

[0158] Examples 2 to 12:

[0159] Ingredient list: see Tables 2 to 4.

[0160] Table 2:

[0161]

[0162] Table 3:

[0163]

[0164] Preparation method: Refer to the preparation method in Example 1.

[0165] Table 4:

[0166]

[0167] Preparation method: Refer to the preparation method in Example 1.

[0168] Experimental Example 1: Examination of Anti-aging Effect

[0169] Type I collagen accounts for 80%-90% of the collagen in the dermis of the skin. It forms strong, tightly packed bundles, providing the skin with strong support and tensile strength, maintaining its firmness, elasticity, and plumpness. Type III collagen is a key protein in maintaining skin structure and function. It not only regulates the thickness of collagen fibers and enhances skin resilience but also effectively promotes wound repair and tissue regeneration. The loss of type III collagen in the human body is an important marker of skin aging. Therefore, evaluating the effects of products on promoting type I and III collagen through aging models can provide crucial scientific evidence for the anti-aging and repair efficacy of these products.

[0170] MMP-1 is a collagenase primarily responsible for degrading type I and type III collagen in the skin. These collagens are major components of skin structure, maintaining skin firmness and elasticity. External factors such as UV radiation, inflammation, and oxidative stress can stimulate the overexpression of MMP-1, leading to excessive collagen degradation and accelerating the skin aging process. Therefore, this study investigates the inhibition of MMP-1 gene expression to verify its anti-aging effects.

[0171] To compare the anti-aging effects of this embodiment, qPCR experiments were performed on the embodiment and the comparative example.

[0172] Testing process:

[0173] (1) Cell seeding: HSF cells (human skin fibroblast cell line, Fenghui Biotechnology) in logarithmic growth phase were selected, and the cells were collected after trypsin digestion and made into a cell suspension. Cells were counted using a cell counter and prepared into 1.2×10⁻⁶ cells using complete culture medium (manufacturer: Thermo Fisher Scientific; brand: Gibco; catalog number: 11995). 5 Cell suspension of 1 / mL was seeded into 12-well plates, with 1 mL added to each well, and cultured at 37℃ in a 5% CO2 incubator for 24±2 h.

[0174] (2) Cell loading: Discard the culture medium in the cell culture plate and load the sample (the sample group is loaded with the final concentration of the composition at 0.01wt% of the detection concentration; no composition is added to the negative control group, and the other operations are the same as the sample group). After loading the sample, place the cell culture plate in a CO2 incubator and continue to culture for 24±2 h.

[0175] (3) RNA extraction: RNA was collected and its concentration was determined according to the instructions of the total RNA extraction kit (manufacturer: Beijing Solarbio Science & Technology Co., Ltd.).

[0176] (4) Detection: Prepare the reverse transcription reaction system according to the steps (Table 5) of the instructions of the total RNA extraction kit (manufacturer: Beijing Solarbio Science & Technology Co., Ltd.), and prepare the following mixture in the qPCR tube (Table 6); proceed step by step according to the pre-denaturation, cycling reaction and melting curve (Table 7).

[0177] Table 5: Preparation of reverse transcription reaction system according to the table below

[0178]

[0179] Table 6: Prepare the following mixture in qPCR tubes

[0180]

[0181] Table 7: Perform qPCR reactions according to the following procedures:

[0182]

[0183] Note: Tables 5, 6, and 7 are the reagents and procedures from the instructions for the total RNA extraction kit (manufacturer: Beijing Solarbio Science & Technology Co., Ltd.).

[0184] (5) Calculation and analysis of results:

[0185] Based on the formula for calculating relative gene expression levels:

[0186]

[0187] Among them: internal reference gene: refers to the gene used as an internal reference in molecular experiments. Its expression is relatively constant in various tissues and cells. The internal reference gene in this test is GAPDH (glyceraldehyde-3-phosphate dehydrogenase).

[0188] NC average: refers to the average ΔCT value of the negative control group, the purpose of which is to eliminate minor errors that may be caused by the experimental procedure itself.

[0189] Fold expression: refers to the relative fold increase in gene expression, which directly reflects the expression level of the target gene in the experimental group (see Table 8 for results).

[0190] The relevant test results were calculated, and the results are shown in Table 8.

[0191] Table 8: Relative Expression Levels of Type I Collagen, Type III Collagen, and MMP-1 Genes

[0192]

[0193] in conclusion:

[0194] (1) As can be seen from the results of Examples 1-12 in Table 8, the composition provided by the present invention has a significant promoting effect on type I and type III collagen genes and a significant inhibitory effect on matrix metalloproteinase MMP-1.

[0195] (2) As can be seen from the results of Example 1, Comparative Example 1 and Comparative Examples 2 to 4 in Table 8, the silymarin, silanetriol and phytol provided by the present invention have a synergistic effect on promoting type I and type III collagen genes and inhibiting matrix metalloproteinase MMP-1.

[0196] (3) As can be seen from the results of Example 1, Comparative Example 1 and Comparative Examples 5 to 7 in Table 8, silymarin, silanetriol and phytol cannot achieve a synergistic effect in promoting type I and type III collagen genes and inhibiting matrix metalloproteinase MMP-1.

[0197] (4) As can be seen from the results of Comparative Examples 8 to 9 in Table 8, compared with other weight ratios of silymarin and silanetriol, the weight ratio of silymarin and silanetriol provided by this invention (weight ratio of silymarin and silanetriol = (10~1): (5~1)) is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has unexpected technical effects.

[0198] (5) As can be seen from the results of Example 1 and Comparative Examples 10 to 11 in Table 8, compared with other weight ratios of silymarin and phytol, the weight ratio of silymarin and phytol provided by the present invention (weight ratio of silymarin and silanetriol = (10~1): (2~1)) is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has unexpected technical effects.

[0199] (6) As can be seen from the results of Example 1 and Comparative Examples 12 to 14 in Table 8, compared with silymarin using only one of silybin, silybinin and silybinine, the present invention preferably uses silymarin containing silybin, silybinin and silybinine, which is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has an unexpected synergistic effect.

[0200] (7) As can be seen from the results of Example 1 and Comparative Examples 15 to 16 in Table 8, compared with other weight ratios of silybin, silytin and silynin in silybin, the weight ratio of silybin, silytin and silynin in silybin provided by the present invention (silybin:silytin:silynin (weight ratio) = (2.5~4.3):1:(0.1~0.25)) is more conducive to improving the promoting effect on type I and type III collagen genes and the inhibitory effect on matrix metalloproteinase MMP-1, and has unexpected technical effects.

[0201] Comparative Examples 17-18: Investigation of Inclusion Materials

[0202] Comparative Example 17: The only difference from Example 1 is that hydroxypropyl-β-cyclodextrin is replaced with methyl-β-cyclodextrin, and all other conditions are the same as in Example 1.

[0203] Comparative Example 18: The only difference from Example 1 is that hydroxypropyl-β-cyclodextrin is replaced with sulfobutyl-γ-cyclodextrin, and all other conditions are the same as in Example 1.

[0204] Comparative Examples 19-20: Investigation of Emulsifier Types

[0205] Comparative Example 19: The only difference from Example 1 is that oleyl alcohol polyether-20 is replaced with PEG-60 hydrogenated castor oil, and the other conditions are the same as in Example 1.

[0206] Comparative Example 20: The only difference from Example 1 is that oleyl alcohol polyether-20 is replaced with polyglycerol-10 stearate, and the other conditions are the same as in Example 1.

[0207] Experimental Example 2: Stability Study - Appearance and Crystallinity

[0208] The compositions obtained in each example and comparative example were placed at room temperature (25±0.5℃), high temperature (45±0.5℃), and frozen (-15±0.5℃) for three months. The appearance and crystallinity (whether precipitation occurred) were tested before (day 0) and after the placement. The results are shown in Table 9.

[0209] Table 9: Stability results at 0 days and 3 months

[0210]

[0211] Note: No abnormality indicates that compared with day 0, there is no change in color, and the product is uniformly transparent, without crystallization, turbidity, or stratification.

[0212] in conclusion:

[0213] (1) As can be seen from the results of Examples 1-12 in Table 9, the composition provided by the present invention has excellent stability.

[0214] (2) As can be seen from the results of Example 1 and Comparative Examples 2 to 4 in Table 9, in the technical solution provided by the present invention, silymarin associates with silanetriol to form a supramolecular hydrogen bond network, which reduces the crystallization tendency of silymarin; then, the inclusion material provided by the present invention is used to encapsulate and improve bioavailability, greatly improve solubility, and further solve the problems of transparency and precipitation; the addition of phytol further stabilizes the supramolecular co-crystal system, and silanetriol and phytol play an unexpected synergistic effect in avoiding the crystallization of silymarin and improving the stability of the composition.

[0215] (3) As can be seen from the results of Example 1 and Comparative Examples 5 to 6 in Table 9, neither silanetriol nor phytol alone can achieve the technical effect of preventing silymarin crystallization and improving the stability of the composition.

[0216] (4) As can be seen from the results of Example 1 and Comparative Examples 8 to 9 in Table 9, compared with other weight ratios of silymarin and silanetriol, the weight ratio of silymarin and silanetriol provided by the present invention (weight ratio of silymarin and silanetriol = (10~1): (5~1)) is more conducive to avoiding crystallization of silymarin and improving the stability of the composition, and has unexpected technical effects.

[0217] (5) As can be seen from the results of Example 1 and Comparative Examples 10 to 11 in Table 9, compared with other weight ratios of silymarin and phytol, the weight ratio of silymarin and phytol provided by the present invention (weight ratio of silymarin and silanetriol = (10~1): (2~1)) is more conducive to avoiding crystallization of silymarin and improving the stability of the composition, and has unexpected technical effects.

[0218] (6) As can be seen from the results of Example 1 and Comparative Examples 12 to 14 in Table 9, compared with silymarin using only one of silybin, silybinin and silybinin, the present invention preferably uses silymarin containing silybin, silybinin and silybinin, which is more conducive to avoiding silymarin crystallization and improving the stability of the composition, and has an unexpected synergistic effect.

[0219] (7) As can be seen from the results of Example 1 and Comparative Examples 15 to 16 in Table 9, compared with other weight ratios of silybin, silytin and silynin in silybin, the weight ratio of silybin, silytin and silynin in silybin provided by the present invention (silybin: silytin: silynin (weight ratio) = (2.5~4.3):1:(0.1~0.25)) is more conducive to avoiding crystallization of silybin and improving the stability of the composition, and has unexpected technical effects.

[0220] (8) As can be seen from the results of Example 1 and Comparative Examples 17 to 18 in Table 9, compared with other inclusion materials (such as hydroxypropyl-α-cyclodextrin or sulfobutyl-γ-cyclodextrin), the inclusion material of the present invention preferably uses hydroxypropyl-β-cyclodextrin, which is more conducive to avoiding the crystallization of silymarin and improving the stability of the obtained composition, and has unexpected technical effects.

[0221] (9) As can be seen from the results of Example 1, Comparative Examples 19 to 20 in Table 9, compared with other emulsifiers, the emulsifier of the present invention preferably uses oleyl alcohol polyether-20, which is more conducive to avoiding the crystallization of silymarin and improving the stability of the obtained composition, and has unexpected technical effects.

[0222] Experimental Example 3: Closed Patch Test

[0223] Using the closed patch test method, approximately 0.020 mL to 0.025 mL (liquid) of the test substance was placed in the patch applicator, and a hypoallergenic adhesive tape was applied to the flexor side of the subject's forearm. After 24 hours, the test substance was removed, and skin reactions were observed at 0.5 hours, 24 hours, and 48 hours after removal. The results were recorded according to the skin reaction grading standards in the currently effective technical specification "Cosmetic Safety Technical Specification" (2015 edition) (see Table 10) (results are shown in Table 11).

[0224] Table 10: Skin Reaction Grading Standards

[0225]

[0226] Table 11: Results of Cosmetic Patch Tests on Human Skin

[0227]

[0228] Conclusion: As can be seen from the experimental results in Table 11, the examples have a significant effect in reducing irritation and have no skin reaction. They have the effect of reducing skin allergies, indicating that the composition prepared by the present invention has a good effect in reducing allergies and is suitable for sensitive people.

[0229] Experiment 4: Human Testing of Anti-wrinkle Effect

[0230] The wrinkle area of ​​the subjects was measured before using the VISIA 7 facial image analyzer (Canfield, USA) and recorded as the initial value. The wrinkle area was measured again after 30 minutes, 14 days and 28 days of continuous use and recorded as the termination value. Finally, the wrinkle area change rate was calculated as follows: wrinkle area change rate (%) = (initial value - termination value corresponding to the test time point) / initial value × 100%. The higher the wrinkle area change rate, the better the anti-aging effect of the cosmetic.

[0231] Table 12: Change rate of wrinkle area in experimental cases

[0232]

[0233] Conclusion: According to Table 12, the results of Examples 1 and 8 show that the supramolecular milk thistle anti-aging composition can effectively achieve cosmetic anti-aging effects at 30 min, 14 days and 28 days, and significantly reduce the proportion of wrinkle area.

[0234] The method of this invention has been described through preferred embodiments. Those skilled in the art will readily be able to modify or appropriately alter and combine the methods and applications described herein within the scope, spirit, and context of this invention to implement and apply the technology of this invention. Those skilled in the art can refer to the content herein to appropriately improve process parameters. It should be particularly noted that all similar substitutions and modifications are obvious to those skilled in the art and are considered to be included within the scope of this invention.

Claims

1. A composition, characterized in that, include: The active ingredient comprises an active ingredient, an incorporating material, an emulsifier, and a solvent; the active ingredient is silymarin, silanetriol, and phytol; the silymarin is silybin, silymarinine, and silymarinine; the incorporating material is at least one of hydroxypropyl-α-cyclodextrin and hydroxypropyl-β-cyclodextrin; the emulsifier is at least one of oleyl alcohol polyether-20, Tween 80, and PPG-13-decyltetradecyl alcohol polyether-24; the solvent comprises water and a polyol. in, The weight ratio of silybin, silybinin and silybinin in the silybin is (2.5~4.3):1:(0.1~0.25). The weight ratio of silymarin to silanetriol is (1~10):(0.5~5). The weight ratio of silymarin to phytol is (1~10):(1~2). Based on the total mass of the composition, the total content of the active ingredient is 3wt% to 17wt%, the content of the inclusion material is 5wt% to 30wt%, the content of the emulsifier is 2wt% to 15wt%, the content of the polyol is 9wt% to 25wt%, and the content of water is 43wt% to 63wt%.

2. The composition according to claim 1, wherein the polyol comprises at least one selected from dipropylene glycol, 1,2-pentanediol, 1,3-butanediol, hexyldecyl alcohol, 1,2-propanediol, 1,3-propanediol, 1,2-hexanediol, and methylpropanediol.

3. The composition according to claim 1, wherein the polyol comprises a first polyol and a second polyol; in, The first polyol includes at least one of dipropylene glycol, methylpropanediol, or 1,3-butanediol; The second polyol includes 1,2-pentanediol.

4. The composition according to claim 3, wherein the weight ratio of the first polyol to the second polyol is (4~20):

5.

5. The composition according to any one of claims 1 to 4, wherein, based on the total mass of the composition, the total content of the active ingredient is 3 wt% to 17 wt%, the content of the inclusion material is 5 wt% to 30 wt%, the content of the emulsifier is 2 wt% to 15 wt%, the content of the polyol is 9 wt% to 25 wt%, and the balance is water.

6. The composition according to any one of claims 1 to 4, wherein the silanetriol is methylsilanetriol.

7. The composition according to any one of claims 1 to 4, wherein the weight ratio of silybin to silybinin in the silymarin is 2.5:1 to 4.3:1; The weight ratio of silymarin to silymarin in the silymarin is 1:0.1 to 1:0.25; The weight ratio of silymarin to silanetriol is 1:1 to 8:1; The weight ratio of silymarin to phytol is 1:1 to 5:

1.

8. A method for preparing the composition according to any one of claims 1 to 7, characterized in that, include: (1) Silymarin and silanetriol were dissolved in ethanol to obtain phase A; (2) Dissolve the inclusion material in water to obtain phase B; (3) Mix phase A obtained in step (1) and phase B obtained in step (2), stir, and dry to obtain solid powder; (4) The solid powder obtained in step (3) is mixed with a polyol and stirred, and then mixed with phytol and stirred to obtain mixture 1; the polyol in step (4) includes at least one of dipropylene glycol, 1,3-butanediol, hexyldecyl alcohol, 1,2-propanediol, 1,3-propanediol, methylpropanediol and 1,2-hexanediol. (5) Mix the emulsifier with the polyol to obtain phase E, and then mix it with the mixture 1 obtained in step (4), homogenize it, and obtain mixture 2; the polyol in step (5) includes 1,2-pentanediol; (6) Mix water and the mixture 2 obtained in step (5) to obtain the composition.

9. A pharmaceutical preparation, characterized in that, The composition includes the composition according to any one of claims 1 to 7 or the composition prepared by the preparation method according to claim 8.

10. The use of a composition according to any one of claims 1 to 7 or a composition prepared by the preparation method according to claim 8 in the preparation of an anti-aging pharmaceutical product.

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