CN113041182A

CN113041182A - Collagenase inhibitor, anti-aging skin lightening lotion containing collagenase inhibitor and preparation method

Info

Publication number: CN113041182A
Application number: CN201911381292.7A
Authority: CN
Inventors: 杨登亮; 李传茂; 李华真; 张楚标; 曾伟丹; 张伟杰
Original assignee: GUANGZHOU BAIYUN LIANJIA FINE CHEMICAL FACTORY; Guangdong Danz Group Co Ltd; Guangzhou Keneng Cosmetic Research Co Ltd
Current assignee: GUANGZHOU BAIYUN LIANJIA FINE CHEMICAL FACTORY; Guangdong Danz Group Co Ltd; Guangzhou Keneng Cosmetic Research Co Ltd
Priority date: 2019-12-27
Filing date: 2019-12-27
Publication date: 2021-06-29

Abstract

The invention provides a collagenase inhibitor, an anti-aging skin-lightening lotion containing the collagenase inhibitor and a preparation method of the collagenase inhibitor. The collagenase inhibitor comprises: the collagenase inhibitor comprises a red pomegranate bark extract and a purslane extract, wherein the red pomegranate bark extract is added in an amount of 26-74% and the purslane extract is added in an amount of 26-74% based on the total mass of the collagenase inhibitor. The collagenase inhibitor of the present invention has an excellent inhibitory effect on collagenase activity and has no side effects on the human body.

Description

Collagenase inhibitor, anti-aging skin lightening lotion containing collagenase inhibitor and preparation method

Technical Field

The invention relates to a collagenase inhibitor, an anti-aging skin-brightening lotion containing the collagenase inhibitor and a preparation method, and belongs to the field of cosmetics.

Background

Collagen is mainly produced by fibroblasts in the dermis layer, is a main component of the dermis layer, and can maintain the structure of the skin and endow the skin with toughness and elasticity. The collagen content and distribution determine the youth or not of the skin. However, abnormal reduction of collagen content causes thinning of the dermis, skin sagging, loss of elasticity, appearance of wrinkles, and affects the quality of life of people. With the ongoing and intensive research on collagen, researchers have found that collagenase plays an important role in the dynamic balance of skin collagen, and its overexpression and abnormal activation are one of the major causes of skin aging. Therefore, inhibiting the activity of collagenase can block the degradation of collagen of skin, increase the content of collagen, and realize the anti-aging effect.

The main approaches to skin anti-aging and skin care include the following aspects, with respect to factors affecting the collagen content of the skin: (1) increasing collagen synthesis by stimulating proliferation of fibroblasts in the dermis layer; (2) increasing the total amount of collagen in the dermis by stimulating the speed of synthesizing collagen by fibroblasts through active factors; (3) the degradation speed of the collagen is slowed down by inhibiting the catalytic activity of collagenase, a key enzyme for degrading the collagen in the dermis, so that the anti-aging purpose is achieved; (4) through sun protection, the damage of ultraviolet rays in sunlight to collagen in the skin is prevented, and the photoaging of the skin is slowed down; (5) the induced expression of collagenase and abnormal cross-linking of biomacromolecules is slowed down by scavenging excess oxygen free radicals in the skin using antioxidants.

In order to prevent skin from sagging, losing elasticity, wrinkling, etc., and keep skin young, anti-aging products mixed with various components such as hydrolyzed collagen, hyaluronic acid, polypeptide, retinol and its derivatives have been proposed in the prior art. However, if these ingredients are used in large amounts, problems arise in the actual anti-aging effect, the feeling of use, and safety. If the molecular weight of the hydrolyzed collagen is too large, the hydrolyzed collagen is not easy to permeate the skin barrier of the human body to reach the dermis; hyaluronic acid cannot essentially slow down the loss of collagen; the polypeptide and the retinol have certain irritation and safety risks to the skin, and the like.

With the increase of attention of people to skin health, the development of a natural anti-aging agent with safety, stability, obvious effect and high cost performance has become one of the main research directions of the current pharmaceutical and cosmetic industries, and has a very good development prospect.

Disclosure of Invention

Problems to be solved by the invention

In view of the prior art, the hydrolyzed collagen has too high molecular weight and is not easy to reach the dermis layer through the skin barrier of the human body; hyaluronic acid cannot essentially slow down the loss of collagen; the invention firstly provides a collagenase inhibitor and a preparation method thereof, and the polypeptide and the retinol have certain irritation and safety risks to skin.

Furthermore, the invention also provides anti-aging skin-brightening lotion containing the collagenase inhibitor, and the anti-aging skin-brightening lotion has excellent anti-aging effect.

Furthermore, the invention also provides a preparation method of the anti-aging skin-brightening lotion, which is simple to operate and easy to obtain raw materials.

Means for solving the problems

The present invention provides a collagenase inhibitor comprising: the collagenase inhibitor comprises a red pomegranate bark extract and a purslane extract, wherein the red pomegranate bark extract is added in an amount of 26-74% and the purslane extract is added in an amount of 26-74% based on the total mass of the collagenase inhibitor.

The collagenase inhibitor according to the present invention, wherein the mass ratio of the pomegranate bark extract to the purslane extract is 1:0.36 to 2.8, preferably 1:0.37 to 2.5, more preferably 1:0.4 to 2.2, further preferably 1:0.45 to 2, further preferably 1:0.5 to 1.8, and further preferably 1:0.6 to 1.5.

The collagenase inhibitor according to the present invention, wherein the collagenase is interstitial collagenase.

The present invention also provides a method for preparing a collagenase inhibitor according to the present invention, comprising the step of mixing the components of a collagenase inhibitor.

The invention also provides anti-aging skin-brightening lotion which comprises the collagenase inhibitor and the penetration enhancer; the addition amount of the collagenase inhibitor is 0.01-10% of the total mass of the anti-aging skin-brightening water; the addition amount of the penetration enhancer is 0.01-10%.

The anti-aging skin lightening lotion comprises one or more of propylene glycol, bis-diethoxydiol cyclohexane 1, 4-dicarboxylate and chitosan.

The anti-aging skin brightening lotion further comprises one or the combination of more than two of a humectant, a thickening agent, a preservative, a skin conditioning agent, a solubilizer, a skin whitening agent, a soothing agent and an aromatic;

preferably, the addition amount of the humectant is 0.01-20% by mass of the total anti-aging skin-brightening lotion; the addition amount of the thickening agent is 0.02-0.8%; the addition amount of the preservative is 0.01-1.5%; the addition amount of the skin conditioner is 0.01-5%; the addition amount of the solubilizer is 0.01-0.5%; the addition amount of the skin whitening agent is 0.01-5%; the addition amount of the allergy relieving agent is 0.01-5%; the addition amount of the aromatic is 0.005-0.5%.

The anti-aging skin brightening lotion comprises one or more of a giant kelp extract, oat peptide, ceramide 2, a sea oak extract, a chlorella fermentation product, hydrolyzed collagen, hydrolyzed wheat protein, a green algae extract, a brown algae extract, allantoin, a lactobacillus/soybean fermentation product extract, a mistletoe ginkgo leaf extract, a cogongrass rhizome extract, a cactus extract, trehalose, a clitocybe antarctica extract and a bonafillar spirulina extract.

The anti-aging skin lightening lotion comprises one or the combination of more than two of niacinamide, magnolia sieboldii extract, kojic acid and derivatives thereof, arbutin and derivatives thereof and vitamin C; and/or the presence of a gas in the gas,

the soothing agent comprises one or more of Hamamelis virginiana flower water, centella asiatica extract, ginger root extract, bisabolol, and dipotassium glycyrrhizinate.

The invention further provides a preparation method of the anti-aging skin-brightening water, which comprises the step of mixing the components of the anti-aging skin-brightening water.

ADVANTAGEOUS EFFECTS OF INVENTION

The collagenase inhibitor of the present invention has an excellent inhibitory effect on collagenase activity and has no side effects on the human body.

The anti-aging skin brightening lotion disclosed by the invention is mild in formula, and can effectively improve the skin elasticity, so that an anti-aging effect is achieved.

The preparation method of the anti-aging skin-brightening lotion is simple to operate, the raw materials are easy to obtain, and the anti-aging skin-brightening lotion can be produced in batches.

Drawings

FIG. 1 is a graph showing the logarithmic mass concentration-collagenase activity inhibition ratio of the pomegranate rind extract according to comparative examples 1 to 5 of the present invention;

FIG. 2 is a graph showing the logarithmic mass concentration of the purslane extract of comparative examples 6-10 of the present invention versus collagenase activity inhibition rate;

FIG. 3 is a graph showing the log mass concentration of collagenase inhibitors versus the collagenase activity inhibition rate for examples 1-5 of the present invention;

FIG. 4 is a graph showing the relationship between the content of pomegranate rind extract and the interaction coefficient in collagenase inhibitors according to examples 1 to 5 of the present invention.

FIG. 5 is a graph showing the comparison of the skin elasticity change rate of examples 1 to 5 of application and comparative examples 1 to 8 of the present invention.

Detailed Description

Various exemplary embodiments, features and aspects of the invention will be described in detail below. The word "exemplary" is used exclusively herein to mean "serving as an example, embodiment, or illustration. Any embodiment described herein as "exemplary" is not necessarily to be construed as preferred or advantageous over other embodiments.

Furthermore, in the following detailed description, numerous specific details are set forth in order to provide a better understanding of the present invention. It will be understood by those skilled in the art that the present invention may be practiced without some of these specific details. In other instances, methods, means, devices and steps which are well known to those skilled in the art have not been described in detail so as not to obscure the invention.

It should be noted that:

in the present specification, the meaning of "may" or "may" includes both the meaning of performing a certain process and the meaning of not performing a certain process.

In the present specification, the numerical range represented by "numerical value a to numerical value B" means a range including the end point numerical value A, B.

All units used in the present invention are international standard units unless otherwise stated, and numerical values and numerical ranges appearing in the present invention should be understood to include errors allowed in industrial production.

In the present specification, reference to "some particular/preferred embodiments," "other particular/preferred embodiments," "embodiments," and the like, means that a particular element (e.g., feature, property, and/or characteristic) described in connection with the embodiment is included in at least one embodiment described herein, and may or may not be present in other embodiments. In addition, it is to be understood that the described elements may be combined in any suitable manner in the various embodiments.

A first aspect of the invention provides a collagenase inhibitor comprising: the collagenase inhibitor comprises a red pomegranate bark extract and a purslane extract, wherein the red pomegranate bark extract is added in an amount of 26-74% and the purslane extract is added in an amount of 26-74% based on the total mass of the collagenase inhibitor.

The inventors of the present invention found that using a combination of purslane extract and pomegranate rind extract, an excellent synergistic effect can be produced, and thus collagenase activity can be inhibited to achieve an anti-aging effect.

Specifically, in the invention, the mass ratio of the red pomegranate bark extract to the purslane extract is 1: 0.36-2.8, preferably 1: 0.37-2.5, more preferably 1: 0.4-2.2, further preferably 1: 0.45-2, further preferably 1: 0.5-1.8, and further preferably 1: 0.6-1.5. When the mass ratio of the pomegranate rind extract to the purslane extract is within the above range, a synergistic effect can be further exhibited, and the collagenase activity inhibition effect is excellent.

The method for preparing the collagenase inhibitor of the present invention is not particularly limited, and may be a method generally used in the art, and specifically may include a step of mixing the components of the collagenase inhibitor. For example, the red pomegranate bark extract and the purslane extract are mixed uniformly by adopting a conventional mixing mode.

Collagenase

Collagenases belong to one class of Matrix Metalloproteinases (MMPs). Matrix metalloproteinases are a family of endopeptidases with a zinc ion-dependent biological activity and the ability to degrade the extracellular Matrix (ECM). Collagenase mainly acts to degrade collagen and elastin in dermis, and its Tissue Type Inhibitor (TIMPs) specifically inhibits the activity of collagenase by covalently binding with its highly conserved zinc binding site, co-regulates the metabolism of the matrix, and maintains the structure of the dermis.

The collagenase includes interstitial collagenase (MMP-1), polymorphonuclear collagenase (MMP-8) and collagenase 3 (MMP-13). Among them, interstitial collagenase, also known as collagenase-1, has various functions and can act on different substrates. Interstitial collagenase degrades several matrix molecules, such as aggrecan, multipotent glycans, basement membrane proteoglycans, casein, nidogen, serine protein inhibitors, and mucin-C. Thus, interstitial collagenases play a key role in the physiological repair of the extracellular matrix. The invention is mainly based on the important function of interstitial collagenase in the skin aging process, and inhibits the activity of interstitial collagenase, thereby reducing the inflammatory reaction and wrinkles of the skin, and being used as a way for delaying aging to realize the anti-aging function.

It is noted that the collagenase inhibitor of the present invention is intended to inhibit collagenase activity, rather than collagenase expression, for example: inhibiting the activity of interstitial collagenase.

Pomegranate rind extract

Pomegranate (Punica grandium L.) is deciduous shrub or tree of the genus Punica (Punicaceae) of the family Punicaceae. Native balkan peninsula to iran and its neighborhood, both temperate and tropical areas of the world are cultivated. China has cultivation in the south and north, and the planting area is large in Jiangsu, Henan and other fields. Pomegranate is one kind of pomegranate.

The pomegranate rind contains abundant chemical substances, such as tannins, alkaloids, flavonoids, amino acids and organic acids, which have pharmacological and health promoting effects on human body, and can be used for treating anthelmintic, hemostatic, dysentery and toothache. The red pomegranate bark extract is rich in pomegranate bark polyphenol, which comprises ellagitannin, ellagic catechin, chlorogenic acid, etc. The substances have effects of resisting oxidation, scavenging free radicals, preventing sunburn, whitening skin, etc.

In the invention, the added amount of the pomegranate bark extract is 26-74% by the total mass of the collagenase inhibitor. When the addition amount of the pomegranate bark extract is 26-74%, the collagenase activity can be effectively inhibited. Specifically, the addition amount of the pomegranate bark extract may be 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, etc.

Purslane extract

Purslane (Portulaca oleracea L.) is an annual herb of Portulacaceae (Portulacaceae) Portulaca, and is produced in all parts of China. Purslane is fertile and fertile in soil, drought and waterlogging resistant, strong in vitality and widely distributed in temperate and tropical areas all over the world.

The purslane has the effects of clearing away heat and toxic materials, cooling blood and stopping bleeding, and has strong antioxidation besides the effects of resisting bacteria, reducing blood fat, relaxing muscles, resisting inflammation, promoting wound healing and the like. The water extract of purslane has obviously improved activity on liver superoxide dismutase (SOD), whole blood glutathione peroxidase (GSH-Px) and Catalase (CAT) of old mice, and the purslane has obvious antioxidant effect.

In the invention, the purslane extract is added in an amount of 26-74% by mass based on the total mass of the collagenase inhibitor. When the addition amount of the purslane extract is 26-74%, the collagenase activity can be effectively inhibited. Specifically, the purslane extract may be added in an amount of 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, etc.

The second aspect of the invention provides an anti-aging skin-lightening lotion, which comprises the collagenase inhibitor and a penetration promoter according to the first aspect of the invention; the anti-aging skin-brightening lotion can inhibit the activity of collagenase, particularly the activity of interstitial collagenase by adding a proper amount of collagenase inhibitor, so that the anti-aging skin-brightening lotion has an excellent anti-aging effect and can improve the skin elasticity. In order to promote the absorption of collagenase inhibitors into the skin, the anti-aging skin-lightening lotion also uses penetration promoters. By using a penetration enhancer, the collagenase inhibitor of the present invention can be exerted to a greater extent.

Wherein, the addition amount of the collagenase inhibitor is 0.01-10% based on the total mass of the anti-aging skin-brightening water, such as: 0.5%, 1%, 2%, 3%, 5%, 6%, 7%, 8%, etc. When the collagenase inhibitor is added in an amount of 0.01-10%, the elasticity of the skin after the collagenase inhibitor is used is increased. When the addition amount of the collagenase inhibitor is less than 0.01%, the collagenase inhibitor cannot play a role in resisting aging; when the addition amount of the collagenase inhibitor is more than 10%, the content of the collagenase inhibitor is too high, the cost is too high, and the corresponding anti-aging effect is not obviously improved.

The addition amount of the penetration enhancer is 0.01-10% of the total mass of the anti-aging skin-brightening lotion. When the addition amount of the penetration enhancer is less than 0.01%, the penetration enhancing effect is not significant. When the addition amount of the penetration enhancer is more than 10%, the penetration enhancer cannot further function.

In the present invention, the penetration enhancer includes one or a combination of two or more of propylene glycol, bis-diethoxydiol cyclohexane 1, 4-dicarboxylate, and chitosan. The invention preferably uses the combination of propylene glycol and bis-diethoxydiol cyclohexane 1, 4-dicarboxylate, and the propylene glycol and bis-diethoxydiol cyclohexane 1, 4-dicarboxylate have synergistic effect, so that the absorption effect of collagenase inhibitor can be more excellent.

When a combination of propylene glycol and bis-diethoxydiol cyclohexane 1, 4-dicarboxylate is used as the penetration enhancer, the addition amount of propylene glycol is 0.01-5% and the addition amount of bis-diethoxydiol cyclohexane 1, 4-dicarboxylate is 0.01-5% based on the total mass of the anti-aging skin lightening lotion. When the addition amount of the propylene glycol is 0.01-5% and the addition amount of the bis-diethoxydiol cyclohexane 1, 4-dicarboxylate is 0.01-5%, the absorption effect of the collagenase inhibitor can be effectively improved. For example: the amount of propylene glycol added is 0.1%, 0.5%, 1%, 1.5%, 2.5%, 3.5%, 4.5%, etc., and the amount of bis-diethoxydiol cyclohexane 1, 4-dicarboxylate added is 0.1%, 0.5%, 1%, 1.5%, 2.5%, 3.5%, 4.5%.

The anti-aging skin brightening lotion can also comprise one or the combination of more than two of humectant, thickener, preservative, skin conditioner, solubilizer, skin whitening agent, soothing agent and aromatic. The anti-aging skin-brightening lotion has mild formula composition, and can fully exert the efficacy of the collagenase inhibitor. Specifically, the method comprises the following steps:

the addition amount of the humectant is 0.01-20% by the total mass of the anti-aging skin-brightening lotion. When the addition amount of the humectant is 0.01-20%, the humectant can play a role in moisturizing and hydrating. In order to further exert the efficacy of the moisturizer, the amount of the moisturizer of the present invention added may be preferably 1 to 19%, 4 to 18%, 6 to 17%, 8 to 16%, 10 to 15%, or the like. When the content of the humectant is less than 0.01%, the moisturizing effect is not obvious; when the content of the humectant is more than 20%, the anti-aging toner has sticky feeling.

In the invention, the humectant comprises one or more of dipropylene glycol, butanediol, panthenol, glycerol, polyethylene glycol-32, glyceryl polyether-26 and sodium hyaluronate. The anti-aging skin-brightening lotion has excellent moisturizing performance by using a combination of a plurality of humectants.

The addition amount of the thickening agent is 0.02-0.8% of the total mass of the anti-aging skin-brightening lotion. When the addition amount of the thickener is between 0.02 and 0.8 percent, the low-viscosity feeling and excellent use feeling are achieved, the dispersibility is good, and the absorption is fast. When the addition amount of the thickening agent is less than 0.02%, the anti-aging skin-brightening lotion is thin in texture and does not have any sticky feeling; when the thickener is added in an amount of more than 0.8%, the anti-aging skin-lightening lotion is too thick and heavy, which may increase the burden on the skin.

In the invention, the thickening agent comprises one or more than two of acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer, hydroxyethyl cellulose, xanthan gum, hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, carbomer and acryloyldimethyl taurate/VP copolymer.

The addition amount of the solubilizer is 0.01-0.5% based on the total mass of the anti-aging skin-brightening lotion. The solubilizer is used in the anti-aging and skin brightening water to lead the skin feel to be smooth. Preferably, the solubilizer is added in an amount of 0.05-0.4%, 0.08-0.3%, etc. In the present invention, the solubilizer includes one or more of polysorbate-20, PEG-40 hydrogenated castor oil, and PPG-26-buteth-26.

In order to further improve the efficacy of the anti-aging skin-brightening lotion, the anti-aging skin-brightening lotion further comprises a skin conditioner. The skin conditioner is added, so that the effects of moisturizing and moisturizing can be further achieved, and the generation of wrinkles can be reduced. In addition, the skin conditioner can also properly reduce the adhesive force of stratum corneum cells, accelerate the renewal of epidermal cells and enhance the repair capacity of skin.

The addition amount of the skin conditioner is 0.01-5% of the total mass of the anti-aging skin-brightening lotion; for example, it may be 0.5%, 1%, 2%, 3%, 4%, etc. When the addition amount of the skin conditioner is less than 0.01%, the content is too low to play a corresponding effect; when the skin conditioning agent is added in an amount of more than 5%, the cost is too high.

Specifically, the skin conditioner comprises one or more of a giant kelp extract, oat peptide, ceramide 2, a fucus extract, a chlorella fermentation product, hydrolyzed collagen, hydrolyzed wheat protein, a chlorella extract, a brown algae extract, allantoin, a lactobacillus/soybean fermentation product extract, a mistletoe ginkgo leaf extract, a cogongrass rhizome extract, a cactus extract, trehalose, a Plectranthus antarctica extract and a Bonnate spirulina extract.

The kelp extract is derived from kelp, and the kelp can increase the content of natural plant protein by the mass propagation of kelp cells. The giant kelp extract has the effects of supplementing cell nutrition and effectively preserving moisture.

The ceramide 2 can be used for improving the sebaceous membrane and inhibiting the secretion of active sebaceous glands, so that the skin is balanced in water and oil, the self-protection function of the skin is enhanced, and the skin care cream is suitable for young skin which is greasy and has requirements. The composition has good effects in moisturizing and repairing skin, is an important skin-activating component in horny layer, and can enhance skin barrier and rebuild cells.

Allantoin can reduce the adhesion of stratum corneum cells, accelerate epidermal cell renewal, and enhance skin repair ability, and has high safety.

Pleurotus Antarctica (Durvileavantartica) grows on the cold coast of Antarctica, and therefore, the extract of Pleurotus Antarctica is extremely resistant to severe cold, pollution and radiation. The refined component of the Antarctic iced sea brown algae can adjust the cell activity, help the cells to keep the optimal water content in various environments, enhance the immunity, resist skin inflammation and promote metabolism, continuously supplement the required moisture for the skin, preserve moisture and relieve dryness, and has extremely high skin care value.

The Bonnate spirulina extract is a pure natural extract product, can moisten skin, enable the skin to be elastic, moisturize, smooth and tender, provide nutrient components for the skin, fade the phenomenon of darkness and enable the skin to be young and active.

The anti-aging skin brightening lotion can also be added with a small amount of skin whitening agent. The skin whitening agent is added to play a role in brightening the skin color and achieve a certain whitening effect. The addition amount of the skin whitening agent is 0.01-5% of the total mass of the anti-aging skin brightening lotion; for example, it may be 0.5%, 1%, 2%, 3%, 4%, etc. When the amount of the skin whitening agent added is less than 0.01%, the content is too low to exert the corresponding effect.

Specifically, the skin whitening agent comprises one or more of niacinamide, magnolia sieboldii extract, kojic acid and derivatives thereof, arbutin and derivatives thereof and vitamin C.

The anti-aging skin brightening lotion can also be added with a small amount of soothing agents. By adding the allergy relieving agent, the skin can be calmed, so that the skin has certain allergy relieving effect on the injury red swelling of the facial skin, and the skin can be helped to resist inflammation, relieve and promote cell repair.

The addition amount of the soothing and sensitizing agent is 0.01-5% of the total mass of the anti-aging skin-brightening lotion; for example, it may be 0.5%, 1%, 2%, 3%, 4%, etc. When the addition amount of the allergy relieving agent is less than 0.01 percent, the allergy relieving effect is not obvious. When the addition amount of the allergy relieving agent is more than 5%, the further allergy relieving effect cannot be achieved, and the cost is too high.

The hamamelis virginiana flower water in the allergy-relieving agent belongs to high-concentration plant original dew, has light herbal fragrance, and has the effects of controlling oil, conditioning, astringing, tightening pores, removing stasis and relieving swelling. Can be used for caring skin and soothing skin.

In addition, the anti-aging skin-brightening lotion can be properly added with a pH regulator, an antioxidant and a chelating agent. Generally, the addition amount of the pH regulator is 0-1% based on the total mass of the anti-aging skin-brightening lotion; the addition amount of the antioxidant is 0-2%; the addition amount of the chelating agent is 0-1%. The pH regulator comprises one or more of aminomethyl propanol, arginine, citric acid, sodium citrate, and sodium hydroxide. The antioxidant can be one or more of vitamin E, tocopherol acetate, butylated hydroxytoluene, lycopene, etc. The chelating agent may be EDTA-2Na and/or EDTA-4Na, etc.

Finally, the preservative in the anti-aging and skin-brightening water is added in an amount of 0.01-1.5%. The preservative can comprise one or the combination of more than two of phenoxyethanol, methyl hydroxybenzoate, propyl hydroxybenzoate, benzoic acid and salts thereof. In addition, the anti-aging brightening toner also contains a perfume. The addition amount of the aromatic is 0.005-0.5% by total mass of the anti-aging skin-brightening water. The aromatic may be a perfume, etc.

In a third aspect of the invention, a preparation method of the anti-aging skin-lightening lotion provided by the invention comprises the step of mixing the components of the anti-aging skin-lightening lotion.

Specifically, the preparation method of the anti-aging skin-brightening lotion can comprise the following steps:

1. adding water, humectant, thickener, part of skin conditioner, part of penetration enhancer, optionally chelating agent, optionally pH regulator and part of antiseptic into a stirring pot, stirring and heating to 80-85 deg.C;

2. cooling to 40-50 deg.C, adding collagenase inhibitor, solubilizer, residual skin conditioner, residual penetration enhancer, skin whitening agent, soothing agent, aromatic, optional antioxidant, and residual antiseptic, and stirring;

3. cooling to 35-40 deg.C, discharging after qualified inspection, and standing for 12-48 hr;

4. and (5) after the inspection is qualified, subpackaging, packaging, inspecting again, and warehousing the finished product.

Examples

Embodiments of the present invention will be described in detail below with reference to examples, but those skilled in the art will appreciate that the following examples are only illustrative of the present invention and should not be construed as limiting the scope of the present invention. The examples, in which specific conditions are not specified, were conducted under conventional conditions or conditions recommended by the manufacturer. The reagents or instruments used are not indicated by the manufacturer, and are all conventional products commercially available.

The red pomegranate peel extract was purchased from: quzhou City exhibition-macro biotechnology Co., Ltd;

purslane extracts were purchased from: quzhou Guangzhou Zhanhong Biotech Co., Ltd

Comparative examples 1 to 5

Pomegranate rind extract is provided as collagenase inhibitor. Dissolving the red pomegranate peel extract in 5 groups of deionized water with different volumes to obtain 5 groups of test solutions, wherein the concentrations of the 5 groups of test solutions are 4000 mu g/mL, 3200 mu g/mL, 2400 mu g/mL, 1600 mu g/mL and 800 mu g/mL respectively. The log mass concentration of the pomegranate rind extract is shown in table 2 below and fig. 1.

Comparative examples 6 to 10

Purslane extract is provided as a collagenase inhibitor. The purslane extract was dissolved in 5 groups of deionized water of volumes corresponding to comparative examples 1-5 to give 5 groups of test solutions, the concentrations of the 5 groups of test solutions were 4000. mu.g/mL, 3200. mu.g/mL, 2400. mu.g/mL, 1600. mu.g/mL, 800. mu.g/mL, respectively. The logarithmic mass concentration of the purslane extract is shown in table 2 below and fig. 2.

Examples 1 to 5

Pomegranate rind extract and purslane extract are provided as collagenase inhibitors. The collagenase inhibitor is obtained by mixing the pomegranate rind extract and the purslane extract in a mass ratio of 3:1 (example 1), 2:1 (example 2), 1:1 (example 3), 1:2 (example 4), and 1:3 (example 5). The collagenase inhibitors of examples 1 to 5 were dissolved in 5 sets of deionized water in volumes corresponding to those of comparative examples 1 to 5, respectively. Examples 1-5 can give 5 sets of test solutions (not corresponding, tabulated separately) at concentrations corresponding to comparative examples 1-5. Wherein, the content (mass%) of the pomegranate bark extract and the purslane extract in the collagenase inhibitor is shown in the following table 1, and the logarithmic mass concentration of the collagenase inhibitor is shown in the following table 3.

TABLE 1

Collagenase activity inhibition assay

The forskolin phenol reagent can be reduced by phenolic compounds to be blue (a mixture of molybdenum blue and tungsten blue) under alkaline conditions, and because the protein molecules contain amino acid containing phenolic groups (such as tyrosine, tryptophan and the like), the protein and the hydrolysate thereof can be subjected to the reaction, so that the protease activity can be measured by utilizing the principle. Generally, casein is used as a substrate, the casein is hydrolyzed by collagenase under certain pH value and temperature conditions, the enzymolysis reaction is stopped by trichloroacetic acid after a period of time, the supernatant is taken after the casein precipitate is removed by centrifugation or filtration, and Na is used₂CO₃Alkalizing, adding Folin phenol reagent, developing, wherein the shade of blue is proportional to the amount of tyrosine in the filtrate, and measuring with spectrophotometer at 650nm wavelength to calculate the activity of collagenase.

In the test, all collagenases used were matrix collagenase (MMP-1), purchased from: shanghai ze leaf Biotech Co., Ltd.

Collagenase activity is measured as the activity of collagenase that catalyzes the production of tyrosine by casein. The method specifically comprises the following steps:

taking 1 test tube, respectively adding 0.25mL of deionized water and 0.25mL (32U/mL) of collagenase, then adding 0.5mL (1.0%, w/v) of a substrate casein solution, immediately mixing the solutions, preserving the heat in a water bath at 37 ℃ for 10min, then adding 1mL (6.5%, w/v) of a trichloroacetic acid solution, mixing the solutions uniformly, standing the mixture for 10min, centrifuging the mixture for 5min at 10000rpm, taking 0.5mL of a supernatant sample in the test tube, respectively adding 0.5mL (mass concentration: 10%) of a sodium bicarbonate test solution into another test tube, and shaking the test tube uniformly. After 10 minutes, respectively adding 0.5ml of forinophenol test solution (diluted by 2 times by 1mol/L acid concentration of the forinophenol test solution), immediately mixing uniformly, and standing for 30 minutes at room temperature; the supernatant 1 of the experimental group was obtained and the absorbance at a wavelength of 650nm was measured and recorded as A1.

② taking another 1 test tube, respectively adding 0.25mL of deionized water and 0.25mL (32U/mL) of collagenase, then adding 1mL (6.5%, w/v) of trichloroacetic acid solution and immediately mixing, preserving heat in 37 ℃ water bath for 10min, then adding 0.5mL (1.0%, w/v) of substrate casein solution and mixing, standing for 10min, centrifuging at 10000rpm for 5min, taking 0.5mL of supernatant sample in the test tube, respectively adding 0.5mL (mass concentration: 10%) of sodium bicarbonate test solution into another test tube, and shaking uniformly. After 10 minutes, respectively adding 0.5ml of forinophenol test solution (diluted by 2 times by 1mol/L acid concentration of the forinophenol test solution), immediately mixing uniformly, and standing for 30 minutes at room temperature; control supernatant 2 was obtained and the absorbance measured at 650nm and recorded as A2.

③ respectively adding 0.25mL (32U/mL) of collagenase into 35 test tubes, then respectively adding 0.25mL (1.0%, w/v) of the test solution of the comparative examples 1-10 and the examples 1-5, and mixing uniformly, then adding 0.5mL (1.0%, w/v) of the casein solution of the substrate and immediately mixing uniformly, after preserving heat in a water bath at 37 ℃ for 10min, then adding 1mL (6.5%, w/v) of trichloroacetic acid solution and mixing uniformly, standing for 10min, centrifuging at 10000rpm for 5min, respectively taking 0.5mL of the supernatant sample in 35 test tubes, respectively adding 0.5mL of sodium bicarbonate test solution into another 35 test tubes, respectively adding 0.5mL (mass concentration: 10%) of sodium bicarbonate test solution, and shaking uniformly. After 10 minutes, respectively adding 0.5ml of forinophenol test solution (diluted by 2 times by 1mol/L acid concentration of the forinophenol test solution), immediately mixing uniformly, and standing for 30 minutes at room temperature; 35 groups of experimental group supernatants 3 were obtained and absorbance was measured at 650nm and recorded as A3.

And fourthly, respectively adding 0.25mL (32U/mL) of collagenase into 35 test tubes, then respectively adding 0.25mL of the test solution of the comparative examples 1-10 and the examples 1-5, uniformly mixing, then adding 1mL (6.5%, w/v) of trichloroacetic acid solution, immediately uniformly mixing, keeping the temperature in a water bath at 37 ℃ for 10min, then adding 0.5mL (1.0%, w/v) of casein solution as a substrate, uniformly mixing, standing for 10min, centrifuging at 10000rpm for 5min, respectively taking 0.5mL of supernatant samples in the 35 test tubes, respectively adding 0.5mL (mass concentration: 10%) of sodium bicarbonate test solution into the other 35 test tubes, and uniformly shaking. After 10 minutes, respectively adding 0.5ml of forinophenol test solution (diluted by 2 times by 1mol/L acid concentration of the forinophenol test solution), immediately mixing uniformly, and standing for 30 minutes at room temperature; 35 control group supernatant 4 was obtained and absorbance was measured at 650nm and recorded as A4.

The inhibition rate is [1- (A3-A4)/(A1-A2) ] x 100%

In the formula: a1 is the absorbance of supernatant 1 of experimental group without adding collagenase inhibitor;

a2 is the absorbance of control supernatant 2 without collagenase inhibitor;

a3 is the absorbance of supernatant 3 of experimental group containing collagenase inhibitor;

a4 is the absorbance of control supernatant 4 containing collagenase inhibitor.

The inhibition rates of the red pomegranate peel extract (comparative examples 1-5) and the purslane extract (comparative examples 6-10) on the collagenase activity were calculated respectively. Combining the logarithmic mass concentration-collagenase activity inhibition ratio relationship chart (figure 1 and figure 2), and calculating the corresponding mass concentration (IC) when the inhibition ratio of the pomegranate bark extract is 50%_50A) The mass concentration (IC) corresponding to 50% inhibition rate of herba Portulacae extract_50B) The results are shown in Table 2.

TABLE 2

Then, the collagenase activity inhibition rates of the collagenase inhibitors of examples 1 to 5 were measured. And calculating the mass concentration (IC) of the pomegranate bark extract when the complex action of the pomegranate bark extract and the purslane extract generates equivalent inhibition rate (50%) by combining a relation graph (figure 3) of logarithmic mass concentration-collagenase activity inhibition rate_50a) Mass concentration of purslane extract ((IC) when the combined action of pomegranate rind extract and purslane extract produces equivalent inhibition rate (50%))_50b) The results are shown in Table 3.

The effect of the combined effect of the pomegranate rind extract and the purslane extract can be evaluated by the interaction coefficient γ, and the specific results are shown in table 3.

γ＝IC_50a/IC_50A+IC_50b/IC_50B

Wherein, IC_50ARepresents the corresponding mass concentration when the inhibition rate of the pomegranate bark extract is 50%;

IC_50Brepresents the mass concentration corresponding to 50% inhibition rate of the purslane extract;

IC_50awhen the compound action of the pomegranate bark extract and the purslane extract generates equivalent inhibition rate (50 percent), the pomegranate bark is extractedMass concentration of the substance;

IC_50bthe mass concentration of the purslane extract is shown when the compound action of the pomegranate rind extract and the purslane extract generates equivalent inhibition rate (50%).

Wherein γ ═ 1, indicates that the red pomegranate bark extract and the purslane extract exhibit a simple additive effect; gamma is less than 1, the pomegranate bark extract and the purslane extract show a synergistic effect, and the smaller the gamma value is, the stronger the synergistic effect is; gamma is more than 1, the pomegranate bark extract and the purslane extract show antagonistic effect, and the larger the gamma value is, the larger the antagonistic effect is.

TABLE 3

Note: in Table 3, examples 1 and 5 are embodied in the present invention as reference examples 1 and 5, which can be compared with examples 2 to 4.

As can be seen from table 3, the collagenase inhibitor of the present invention has an interaction coefficient of less than 1, and the interaction coefficient value thereof may be 0.8 or less, and even 0.7 or less, so that the pomegranate rind extract and the purslane extract may exhibit excellent synergistic effects.

Application examples 1 to 5

The anti-aging skin-brightening lotion is prepared according to the content (mass percentage) of each component in the anti-aging skin-brightening lotion formula of the application examples 1-5 in the following table 4 and according to the following production process steps. The production process comprises the following steps:

1. adding A, B and C phase raw materials into a stirring pot, stirring and heating to 82-85 ℃;

2. cooling to 42 ℃, adding D, E, F phase and stirring evenly;

3. cooling to 37 ℃, discharging after the inspection is qualified, and standing for 24 hours;

Note: the A, B, C, D, E, F phases in the process are respectively

Phase A: water;

phase B: butylene glycol, propylene glycol, glycerin, hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, ceramide 2, ammonium acryloyldimethyl taurate/VP copolymer, sodium hyaluronate, panthenol, dipropylene glycol;

and C phase: methylparaben, allantoin, glyceryl polyether-26, polyethylene glycol-32;

phase D: PEG-40 hydrogenated castor oil, essence;

phase E: phenoxyethanol, nicotinamide, bis-diethoxydiol cyclohexane 1, 4-dicarboxylate;

and (3) phase F: pomegranate rind extract, purslane extract, Bonnate spirulina extract, Hamamelis virginiana flower water, Antarctic Pleurosperma extract, and Macrocystis extract.

The pomegranate peel extract and the purslane extract used in the formula are collagenase inhibitors;

butanediol, glycerol, sodium hyaluronate, panthenol, dipropylene glycol, glyceryl polyether-26, and polyethylene glycol-32 as humectant;

hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer and acryloyl dimethyl ammonium taurate/VP copolymer are thickening agents;

the giant kelp extract, ceramide 2, Bonnate spirulina extract, Antarctic Pleurotus extract and allantoin are skin conditioners;

PEG-40 hydrogenated castor oil is a solubilizer; hamamelis virginiana flower water is a soothing sensitizer;

propylene glycol and bis-diethoxydiethylene glycol cyclohexane 1, 4-dicarboxylate are permeation enhancers;

niacinamide is a skin whitening agent; phenoxyethanol and methyl hydroxybenzoate as antiseptic; the essence is an aromatic.

TABLE 1

Application of comparative examples 1 to 8

Skin lightening lotions were prepared according to the contents (mass percentages) of the components in the skin lightening lotion formulations of comparative application examples 1 to 8 in the following table 5 in the same manner as in application examples 1 to 5.

TABLE 5

Skin elasticity test

Method for testing skin elasticity: the test principle is based on the principle of suction and stretching, where a negative pressure is generated on the skin surface to be tested to suck the skin into a specific test probe, and the depth of the skin sucked into the test probe is measured by a non-contact optical test system. The test probe includes a transmitter and receiver of light, the ratio of which (the ratio of transmitted light to received light) is proportional to the depth of skin being absorbed, thus obtaining a time-dependent curve of the length of skin stretched.

Measuring the skin elasticity of the subject by using a probe PVM600 and a skin elasticity measuring instrument MPA580 of German CK company, selecting a parameter R2 as a comparison index (R2: the ratio of the skin rebound quantity without negative pressure to the maximum stretching quantity with negative pressure is closer to 1, the skin elasticity is better) and measuring for 3 times in total, and taking an average value; the improvement of the skin elasticity of the tested area by the product was evaluated by measuring the change in the skin elasticity value R2 before and after use of the product.

The number of the subjects is 33, the test period is 8 weeks, the anti-aging skin-lightening lotion prepared by the application examples 1-5 and the skin-lightening lotion prepared by the application comparative examples 1-8 are selected as test samples in the test, 13 different areas are divided on the forearm of the subject, the anti-aging skin-lightening lotion prepared by the application examples 1-5 and the skin-lightening lotion prepared by the application comparative examples 1-8 are smeared on different areas on the inner side of the forearm every morning and evening, and the smearing amount is about 2mg/cm²And the position of application of each test sample was kept constant during the test period, and then the skin elasticity of the test area before the test and at 8 weeks of use was measured, respectively, to further characterize the rate of change in skin elasticity, and the results of the specific rate of change in elasticity (averaged) are shown in table 6 and fig. 5.

TABLE 6

As can be seen from table 6 and fig. 5, the application examples 1 to 5 of the present application have a large change rate of elasticity, i.e., increased skin elasticity, and thus, the use of the red pomegranate bark extract and the purslane extract is effective in improving skin aging.

In the application comparative examples 1 to 8 of the present application, the change rate of skin elasticity is small, and thus, the anti-aging effect is relatively poor in the application comparative examples 1 to 8.

The above examples of the present invention are merely examples for clearly illustrating the present invention and are not intended to limit the embodiments of the present invention. Other variations and modifications will be apparent to persons skilled in the art in light of the above description. And are neither required nor exhaustive of all embodiments. Any modification, equivalent replacement, and improvement made within the spirit and principle of the present invention should be included in the protection scope of the claims of the present invention.

Claims

1. A collagenase inhibitor comprising: the collagenase inhibitor comprises a red pomegranate bark extract and a purslane extract, wherein the red pomegranate bark extract is added in an amount of 26-74% and the purslane extract is added in an amount of 26-74% based on the total mass of the collagenase inhibitor.

2. The collagenase inhibitor according to claim 1, wherein the mass ratio of the pomegranate bark extract to the purslane extract is 1: 0.36-2.8, preferably 1: 0.37-2.5, more preferably 1: 0.4-2.2, further preferably 1: 0.45-2, further preferably 1: 0.5-1.8, and still further preferably 1: 0.6-1.5.

3. Collagenase inhibitor according to claim 1 or 2, characterised in that the collagenase is a interstitial collagenase.

4. A method of preparing a collagenase inhibitor according to any one of claims 1-3, comprising the step of mixing the components of a collagenase inhibitor.

5. An anti-aging skin lightening lotion, comprising the collagenase inhibitor according to any one of claims 1 to 3 and a penetration enhancer; the addition amount of the collagenase inhibitor is 0.01-10% of the total mass of the anti-aging skin-brightening water; the addition amount of the penetration enhancer is 0.01-10%.

6. The anti-aging skin lightening lotion according to any one of claim 5, wherein the penetration enhancer comprises one or a combination of two or more of propylene glycol, bis-diethoxydiol cyclohexane 1, 4-dicarboxylate and chitosan.

7. The anti-aging skin lightening lotion according to claim 5 or 6, further comprising one or a combination of more than two of a humectant, a thickener, a preservative, a skin conditioner, a solubilizer, a skin whitening agent, a soothing agent and a fragrance;

8. The anti-aging skin lightening lotion according to claim 7, wherein the skin conditioner comprises one or a combination of two or more of a giant kelp extract, avenin, ceramide 2, a fucus extract, a chlorella fermentation product, hydrolyzed collagen, hydrolyzed wheat protein, a chlorella extract, a brown algae extract, allantoin, lactobacillus/soybean fermentation product extract, a mistletoe ginkgo leaf extract, a cogongrass rhizome extract, a cactus extract, trehalose, a Pleurotus Antarctica extract, and a Bonadius spirulina extract.

9. The anti-aging skin lightening lotion according to claim 7 or 8, wherein the skin whitening agent comprises one or a combination of more than two of niacinamide, magnolia sieboldii extract, kojic acid and derivatives thereof, arbutin and derivatives thereof, and vitamin C; and/or the presence of a gas in the gas,

10. A method for preparing the anti-aging skin lightening lotion according to any one of claims 5 to 9, which comprises the step of mixing the components of the anti-aging skin lightening lotion.