A sustained-release whitening composition and its preparation method and application

Abstract

The present invention provides a sustained-release whitening composition and its preparation method and application. In parts by mass, the sustained-release whitening composition includes 15-22 parts of nicotinamide, 0.3-0.8 parts of carnosine, 0.12-0.25 parts of rhizome extracts of osmanthus fragrans, 27-43 parts of polyols, 0.015-0.045 parts of glyceryl caprylate, 0.018-0.05 parts of beta-glucan and water supplemented to a total mass of 100 parts. The sustained-release whitening composition of the present invention can slowly release nicotinamide, carnosine and rhizome extracts of osmanthus fragrans into the skin, has good transdermal absorption, sustained release and long-acting whitening effects, and the sustained-release whitening composition of the present invention is non-irritating to the skin and is suitable for application in the preparation of cosmetics.

Description

Technical Field

[0001] The invention belongs to the technical field of cosmetic raw materials, and particularly relates to a sustained-release whitening composition and a preparation method and application thereof. Background Art

[0002] As living standards continue to improve, people hope that their skin condition is getting better and better, and they are constantly pursuing healthy and fair skin. Existing surveys show that consumers spend more than $1 billion on skin whitening products every year. Commonly used whitening active substances include hydroquinone and its derivatives, vitamin C and its derivatives, kojic acid and its derivatives, glycyrrhizic flavonoids, azelaic acid, etc. These active substances can, to a certain extent, inhibit tyrosinase activity or block the oxidation pathway of tyrosine to produce melanin, thereby reducing the production of melanin and achieving the effect of whitening the skin. However, when these whitening active substances act on cells, they only work for a short time, resulting in poor whitening effects of the active substances. Summary of the invention

[0003] In order to overcome the problems of short action time and poor whitening effect of whitening active substances on the skin in the above-mentioned prior art, the first aspect of the present invention is to provide a sustained-release whitening composition.

[0004] The sustained-release whitening composition of the present invention is achieved by the following scheme:

[0005] A sustained-release whitening composition comprises, by weight: 15-22 parts of niacinamide, 0.3-0.8 parts of carnosine, 0.12-0.25 parts of rhizome extract of Phyllostachys glabra, 27-43 parts of polyol, 0.015-0.045 parts of glyceryl caprylate, 0.018-0.05 parts of beta-glucan and water to make up to 100 parts by weight.

[0006] The present invention prepares a sustained-release whitening composition through the above components. The sustained-release whitening composition uses glyceryl caprylate, beta-glucan and polyol as wall materials. After high-speed shearing and high-pressure homogenization, water-soluble substances nicotinamide and carnosine are wrapped in the wall materials to form nano-alcohol bodies, i.e., sustained-release whitening compositions. Nano-alcohol bodies can slowly release active substances to better exert skin care effects. In the present invention, there is a synergistic effect between the active substances nicotinamide, carnosine and the rhizome extract of Osmanthus fragrans, and the sustained-release whitening composition formed by the three can better and longer exert skin care effects.

[0007] Optionally, in some embodiments, the sustained-release whitening composition comprises, in parts by mass: 17.8-19.8 parts of niacinamide, 0.5-0.75 parts of carnosine, 0.16-0.22 parts of ophiopogon rhizome extract, 30-40 parts of polyols, 0.025-0.032 parts of glyceryl caprylate, 0.028-0.04 parts of β-glucan and water to make up the total parts by mass of 100.

[0008] Optionally, in some embodiments, the polyol includes at least one of propylene glycol and butanediol.

[0009] More preferably, in some embodiments, the polyol includes glycerol and butylene glycol; based on the total mass parts of the sustained-release whitening composition, the glycerol is 15-25 parts, and the butylene glycol is 12-18 parts.

[0010] In the present invention, the polyol is used as the solvent of the alcohol phase and the wall material of the nano-alcohol body, so that the finally formed nano-alcohol body has better permeability, and the active substances such as nicotinamide can be better absorbed through the skin.

[0011] Optionally, in some embodiments, the molecular weight of the β-glucan is 6000 kDa-10000 kDa.

[0012] More preferably, in some embodiments, the molecular weight of the β-glucan is 7000 kDa-9000 kDa.

[0013] In the present invention, the β-glucan with a molecular weight of 6000 kDa-10000 kDa has a longer molecular chain and poorer water solubility, and can better encapsulate nicotinamide and other active substances to exert a sustained-release effect.

[0014] Optionally, in some embodiments, the preparation method of the Osmanthus fragrans rhizome extract is:

[0015] S1, crushing the rhizomes of Bamboo Stalks to obtain Bamboo Stalk Rhizomes powder;

[0016] S2, mixing the rhizome powder of the bamboo with water, and heating the mixture to obtain a mixed solution;

[0017] S3, adding a composite enzyme to the mixed solution for enzymolysis to obtain an enzymolysis solution;

[0018] S4, performing enzyme inactivation treatment and filtering treatment on the enzymatic hydrolyzate to obtain the rhizome extract of Bambusa occidentalis.

[0019] More preferably, in some embodiments, in step S1, the pulverization process is ultrasonic cell pulverization.

[0020] In the present invention, ultrasonic cell pulverization can break the cells of the rhizome of Phyllostachys raphanus, and the active substances can be better dissolved during the subsequent extraction, so that the rhizome extract of Phyllostachys raphanus has better skin care effect.

[0021] More preferably, in some embodiments, in step S1, the conditions for ultrasonic cell pulverization are: frequency 20-30 kHz, pulverization time 20-50 s, and number of cycles 4-8 times.

[0022] More preferably, in some embodiments, in step S2, the mass ratio of the Bambusa occidentalis rhizome powder to water is 1:(40-80).

[0023] More preferably, in some embodiments, in step S2, the temperature of the heating treatment is 70-90° C., and the time of the heating treatment is 1-3 h;

[0024] More preferably, in some embodiments, in step S3, the amount of the complex enzyme added is 0.5-1.0% of the mass of the mixed solution.

[0025] More preferably, in some embodiments, in step S3, the composite enzyme comprises cellulase and pectinase, and the mass ratio of the cellulase to the pectinase is (2-4):1.

[0026] More preferably, in some embodiments, in step S3, the temperature of the enzymatic hydrolysis is 40-50°C, and the time of the enzymatic hydrolysis is 3-5h.

[0027] More preferably, in some embodiments, in step S4, the temperature of the enzyme inactivation treatment is 75-95° C., and the time of the enzymatic treatment is 20-40 min.

[0028] More preferably, in some embodiments, in step S4, the filtration treatment is diatom filter filtration.

[0029] In the present invention, the extract of the rhizome of Bambusa occidentalis prepared by the above method has a synergistic effect with niacinamide and carnosine, and the three together form a sustained-release whitening composition, which can better exert the whitening effect.

[0030] In a second aspect, the present invention provides a method for preparing the above-mentioned sustained-release whitening composition.

[0031] A method for preparing a sustained-release whitening composition, comprising:

[0032] B1. Evenly mix water, niacinamide, carnosine and rhizome extract of Phyllostachys occidentalis to obtain a mixture A;

[0033] B2, mixing the polyol, glyceryl caprylate and β-glucan uniformly to obtain a mixture B;

[0034] B3, adding the mixture A to the mixture B, mixing and reacting, and then performing high-speed shear dispersion to obtain a coarse nanocomposite;

[0035] B4. Performing high-pressure homogenization on the crude nanocomposition to obtain a sustained-release whitening composition.

[0036] Optionally, in some embodiments, the speed at which the mixture B is added to the mixture A in step B3 is 0.8-2.2 mL / min.

[0037] Optionally, in some embodiments, the temperature of the mixed reaction in step B3 is 40-50° C., the speed of the stirring paddle is 80-150 rpm, and the time of the mixed reaction is 15-30 min.

[0038] Optionally, in some embodiments, the rotation speed of the high-speed shear dispersion in step B3 is 8000-12000 rpm, and the time of the high-speed shear dispersion is 5-15 min.

[0039] Optionally, in some embodiments, the high-pressure homogenization treatment in step B4 is a high-pressure microfluidization homogenization treatment.

[0040] More preferably, in some embodiments, the conditions of the high-pressure microfluidization homogenization treatment are: pressure 1.3-1.8 MPa, and number of cycles 2-6 times.

[0041] In the present invention, the mixture A is an aqueous phase, the mixture B is an alcohol phase, the aqueous phase is added to the alcohol phase, and after high-speed shear dispersion and high-pressure homogenization treatment, nano-alcohol bodies are formed. The nano-alcohol bodies wrap the whitening composition and have a sustained-release effect, so it is a sustained-release whitening composition, which can slowly release water-soluble active substances to achieve better skin care effects.

[0042] In a third aspect, the present invention provides use of the sustained-release whitening composition in the preparation of cosmetics.

[0043] The sustained-release whitening composition is used in cosmetics in an amount of 1-100% by mass. Cosmetics adding the sustained-release whitening composition within this range are safe and non-irritating to the skin and have good whitening effects.

[0044] In a fourth aspect, the present invention provides a whitening essence, which comprises, by mass percentage, 12-20% of a sustained-release whitening composition, 0.08-0.22% of allantoin, 0.08-0.15% of sodium hyaluronate, 0.03-0.08% of disodium EDTA, 0.01-0.03% of Ningxia wolfberry fruit extract, 0.02-0.06% of sophora flavescens root extract, 0.01-0.05% of pyracantha fruit extract, and 0.015-0.035% of arginine ferula. Salt, 0.12-0.25% 1-methylhydantoin-2-imide, 0.1-0.5% cornus extract, 0.002-0.006% phenoxyethanol, 0.0002-0.001% ethylhexylglycerol, 0.8-2.0% α-arbutin, 0.3-0.8% 1,2-pentanediol, 0.02-0.06% caprylhydroxamic acid, 0.002-0.007% p-hydroxyacetophenone and water supplemented to 100% of the total mass percentage of the whitening essence.

[0045] Optionally, in some embodiments, the whitening essence includes, by mass percentage: 16% sustained-release whitening composition, 0.15% allantoin, 0.1% sodium hyaluronate, 0.05% disodium EDTA, 0.015% Ningxia wolfberry fruit extract, 0.04% Sophora flavescens root extract, 0.02% Pyracantha fortuneana fruit extract, 0.025% arginine ferulate, 0.175% 1-methylhydantoin-2-imide, 0.3% Cornus officinalis extract, 0.004% phenoxyethanol, 0.00035% ethylhexylglycerin, 1.3% α-arbutin, 0.5% 1,2-pentanediol, 0.045% caprylhydroxamic acid, 0.0045% p-hydroxyacetophenone, and water to make up to 100% of the total mass percentage of the whitening essence.

[0046] In a fifth aspect, the present invention provides a method for preparing the above-mentioned whitening essence, comprising:

[0047] (1) adding the sustained-release whitening composition, allantoin, sodium hyaluronate, disodium EDTA and water into a feeder, stirring evenly, and keeping warm to obtain a mixture 1;

[0048] (2) After the temperature is lowered once, add the Ningxia wolfberry fruit extract, the Sophora flavescens root extract, the Pyracantha fortuneana fruit extract, arginine ferulate, 1-methylhydantoin-2-imide, the Cornus officinalis extract, phenoxyethanol and ethylhexylglycerin to the mixture 1, and stir evenly to obtain a mixture 2;

[0049] (3) After the second cooling, α-arbutin, 1,2-pentanediol, caprylhydroxamic acid and p-hydroxyacetophenone are added to the mixture 2 and stirred evenly to obtain a whitening essence.

[0050] Optionally, in some embodiments, the stirring temperature in step (1) is 55-65°C.

[0051] Optionally, in some embodiments, the insulation time in step (1) is 8-20 minutes.

[0052] Optionally, in some embodiments, the temperature of the first cooling in step (2) is 40-50°C.

[0053] Optionally, in some embodiments, the stirring temperature in step (2) is 40-50°C.

[0054] Optionally, in some embodiments, the temperature of the secondary cooling in step (3) is 30-38°C.

[0055] Optionally, in some embodiments, the stirring temperature in step (3) is 30-38°C.

[0056] Compared with the prior art, the present invention has the following advantages and beneficial effects:

[0057] (1) The present invention uses encapsulation technology to encapsulate niacinamide and carnosine using glyceryl caprylate, β-glucan, and polyol as wall materials. The formed composition can slowly release the active substances, thereby enhancing the action time of the active substances in the skin, so that the final product has a better whitening effect.

[0058] (2) The sustained-release composition of the present invention contains a plant extract, namely, a Bamboo rhizome extract. The Bamboo rhizome extract obtained by enzymatic hydrolysis has a synergistic effect with niacinamide and carnosine, which can better exert the whitening effect of the composition.

[0059] (3) The sustained-release composition of the present invention is safe and non-irritating, and is suitable for use in the preparation of cosmetics. DETAILED DESCRIPTION

[0060] The present invention is further described in detail below in conjunction with the examples, but the embodiments of the present invention are not limited thereto. If the specific conditions are not specified in the examples, they are carried out according to conventional conditions or conditions recommended by the manufacturer. If the manufacturer of the reagents or instruments used is not specified, they are all conventional products that can be purchased commercially.

[0061] Unless otherwise specified, the reagents used in the examples can be purchased from the market.

[0062] Unless otherwise specified, all percentages mentioned in the present invention are by mass percentages.

[0063] The rhizome of the bamboo shoots of the present invention is a dried rhizome of the bamboo shoots.

[0064] The bamboo leaves described in the present invention are dried bamboo leaves.

[0065] The green bamboo leaves described in the present invention are dried green bamboo leaves.

[0066] The ultrasonic cell pulverization described in the present invention is processed by an ultrasonic cell pulverizer. The ultrasonic cell pulverizer is purchased from Ningbo Xinzhi Biotechnology Co., Ltd., model number is JY92-ⅡN. Ultrasonic cell pulverizers obtained from other commercial channels are also suitable for the present invention.

[0067] The cellulase and pectinase described in the present invention were purchased from Guangxi Nanning Dongheng Huadao Biotechnology Co., Ltd.

[0068] The Ningxia wolfberry fruit extract, Sophora flavescens root extract and Pyracantha fortuneana fruit extract described in the present invention were purchased from Shanghai Jiakai Biotechnology Co., Ltd.

[0069] The Cornus officinalis extract of the present invention was purchased from Guangdong Gexin Biotechnology Co., Ltd.

[0070] Example 1

[0071] A sustained-release whitening composition, comprising, by weight:

[0072] 15 parts of niacinamide, 0.3 parts of carnosine, 0.25 parts of rhizome extract of Phyllostachys glabra, 15 parts of glycerol, 12 parts of butylene glycol, 0.015 parts of glyceryl caprylate, 0.05 parts of beta-glucan and 57.385 parts of deionized water.

[0073] The molecular weight of the β-glucan in this example is 8000 kDa-10000 kDa.

[0074] The preparation method of the extract of the rhizome of Osmanthus fragrans in this embodiment is as follows:

[0075] S1, crushing the dried rhizome of Phyllostachys raphis by ultrasonic cell crusher (the conditions are frequency 30kHz, crushing time 20s, and number of cycles 4 times) to obtain rhizome powder of Phyllostachys raphis;

[0076] S2, mixing the rhizome powder of Bambusa occidentalis with 80 times the mass of deionized water, and heating at 90° C. for 1 h to obtain a mixed solution;

[0077] S3, adding 1% of complex enzyme (the mass ratio of cellulase to pectinase is 2:1, i.e. 0.667% of cellulase and 0.333% of pectinase) to the mixed solution, and performing enzymolysis at 40° C. for 5 h to obtain an enzymolysis solution;

[0078] S4. The enzymatic hydrolyzate was kept at 75° C. for 40 min to inactivate the enzyme, and then filtered through a diatom filter to obtain a rhizome extract of Phyllostachys ostreatus.

[0079] The preparation method of the sustained-release whitening composition described in this embodiment is:

[0080] B1. Evenly mix water, niacinamide, carnosine and rhizome extract of Phyllostachys occidentalis to obtain a mixture A;

[0081] B2, mixing glycerol, butylene glycol, glyceryl caprylate and β-glucan to obtain a mixture B;

[0082] B3, adding mixture B to mixture A at a rate of 2.2 mL / min, mixing and reacting for 15 min at 40° C. and a stirring paddle speed of 150 rpm, and after the reaction, high-speed shear dispersion (condition: a speed of 12000 rpm, time of 5 min) was performed to obtain a crude nanocomposite;

[0083] B4. The crude nanocomposition was subjected to high-pressure microfluidization homogenization treatment at a treatment condition of 1.3 MPa and a cycle number of 6 times to obtain a sustained-release whitening composition.

[0084] Example 2

[0085] A sustained-release whitening composition, comprising, by parts by mass:

[0086] 22 parts of niacinamide, 0.8 parts of carnosine, 0.12 parts of rhizome extract of Phyllostachys glabra, 25 parts of glycerol, 18 parts of butylene glycol, 0.045 parts of glyceryl caprylate, 0.018 parts of beta-glucan and 34.017 parts of deionized water.

[0087] The molecular weight of the β-glucan in this example is 6000 kDa-8000 kDa.

[0088] The preparation method of the extract of the rhizome of Osmanthus fragrans in this embodiment is as follows:

[0089] S1, crushing the rhizome of Bambusa glabra by ultrasonic cell crusher (the conditions are frequency 20kHz, crushing time 50s, and number of cycles 8 times) to obtain Bambusa glabra rhizome powder;

[0090] S2, mixing the rhizome powder of Bambusa occidentalis with 40 times the mass of deionized water, and heating at 70° C. for 3 h to obtain a mixed solution;

[0091] S3, adding 0.5% of complex enzyme (the mass ratio of cellulase to pectinase is 4:1, i.e. 0.4% of cellulase and 0.1% of pectinase) to the mixed solution, and performing enzymolysis at 50° C. for 3 h to obtain an enzymolysis solution;

[0092] S4. The enzymatic hydrolyzate was kept at 95° C. for 20 min to inactivate the enzyme, and then filtered through a diatom filter to obtain a rhizome extract of Phyllostachys ostreatus.

[0093] The preparation method of the sustained-release whitening composition described in this embodiment is:

[0094] B1. Evenly mix water, niacinamide, carnosine and rhizome extract of Phyllostachys occidentalis to obtain a mixture A;

[0095] B2, mixing glycerol, butylene glycol, glyceryl caprylate and β-glucan to obtain a mixture B;

[0096] B3, mixture B was added to mixture A at a rate of 0.8 mL / min, and the mixture was mixed and reacted at 50°C and a stirring speed of 80 rpm for 30 min. After the reaction, the mixture was dispersed by high-speed shear (the condition was a speed of 8000 rpm and a time of 5 min) to obtain a crude nanocomposite;

[0097] B4. The crude nanocomposition was subjected to high-pressure microfluidization homogenization treatment at a treatment condition of 1.8 MPa and a cycle number of 2 times to obtain a sustained-release whitening composition.

[0098] Example 3

[0099] A sustained-release whitening composition, comprising, by parts by mass:

[0100] 18.75 parts of niacinamide, 0.63 parts of carnosine, 0.19 parts of rhizome extract of Phyllostachys glabra, 19.38 parts of glycerol, 14.75 parts of butylene glycol, 0.028 parts of glyceryl caprylate, 0.034 parts of beta-glucan and 46.238 parts of deionized water.

[0101] The molecular weight of the β-glucan in this example is 7000 kDa-9000 kDa.

[0102] The preparation method of the extract of the rhizome of Osmanthus fragrans in this embodiment is as follows:

[0103] S1, crushing the rhizome of Bambusa glabra by ultrasonic cell crusher (the conditions are frequency 25kHz, crushing time 40s, and number of cycles 6 times) to obtain Bambusa glabra rhizome powder;

[0104] S2, mixing the rhizome powder of Bambusa occidentalis with 60 times the mass of deionized water, and heating at 80° C. for 2 h to obtain a mixed solution;

[0105] S3, adding 0.8% of complex enzyme (the mass ratio of cellulase to pectinase is 3:1, i.e. 0.6% of cellulase and 0.2% of pectinase) to the mixed solution, and performing enzymolysis at 45° C. for 4 h to obtain an enzymolysis solution;

[0106] S4. The enzymatic hydrolyzate was kept at 85° C. for 30 min to inactivate the enzyme, and then filtered through a diatom filter to obtain a rhizome extract of Phyllostachys ostreatus.

[0107] The preparation method of the sustained-release whitening composition described in this embodiment is:

[0108] B1. Evenly mix water, niacinamide, carnosine and rhizome extract of Phyllostachys occidentalis to obtain a mixture A;

[0109] B2, mixing glycerol, butylene glycol, glyceryl caprylate and β-glucan to obtain a mixture B;

[0110] B3, mixture B was added to mixture A at a rate of 1.5 mL / min, and the mixture was mixed and reacted at 45°C and a stirring speed of 100 rpm for 20 min. After the reaction, the mixture was dispersed by high-speed shear (the conditions were a speed of 10000 rpm and a time of 10 min) to obtain a crude nanocomposite;

[0111] B4. The crude nanocomposition was subjected to high-pressure microfluidization homogenization treatment at a treatment condition of 1.5 MPa and a cycle number of 4 times to obtain a sustained-release whitening composition.

[0112] Example 4

[0113] A sustained-release whitening composition, comprising, by parts by mass:

[0114] 17.8 parts of niacinamide, 0.75 parts of carnosine, 0.22 parts of rhizome extract of Phyllostachys glabra, 24 parts of glycerol, 16 parts of butylene glycol, 0.025 parts of glyceryl caprylate, 0.04 parts of beta-glucan and 41.165 parts of deionized water.

[0115] The molecular weight of the β-glucan in this example is 7000 kDa-9000 kDa.

[0116] The preparation method of the rhizome extract of Osmanthus fragrans in this embodiment is the same as that in Example 3.

[0117] The preparation method of the sustained-release whitening composition of this embodiment is the same as that of Example 3.

[0118] Embodiment 5-10

[0119] The preparation methods of the Osmanthus fragrans rhizome extract and the sustained-release whitening composition in Examples 5-10 are the same as those in Example 3, except that only the contents of some components in the sustained-release whitening composition are different from those in Example 3. The contents of the components of the sustained-release whitening composition of Examples 5-10 are shown in Table 1.

[0120] Table 1

[0121]

[0122] Comparative Examples 1-5

[0123] The preparation methods of the Osmanthus fragrans rhizome extract and the sustained-release whitening composition in Comparative Examples 1-5 are the same as those in Example 3, except that only the contents of some components in the sustained-release whitening composition are different from those in Example 3. The contents of the components of the sustained-release whitening compositions of Comparative Examples 1-5 are shown in Table 2.

[0124] Table 2

[0125] Components / mass Example 3 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Niacinamide 18.75 18.85 19.17 0 18.75 18.75 Carnosine 0.63 0.72 0 13.13 0.63 0.63 Osmanthus fragrans rhizome extract 0.19 0 0.4 6.44 0.19 0.19 Glycerol 19.38 19.38 19.38 19.38 19.38 19.38 Butanediol 14.75 14.75 14.75 14.75 14.75 14.75 Glyceryl Caprylate 0.028 0.028 0.028 0.028 0.062 0 β-Glucan 0.034 0.034 0.034 0.034 0 0.062 water 46.238 46.238 46.238 46.238 46.238 46.238 total 100 100 100 100 100 100

[0126] Comparative Example 6

[0127] The difference between Comparative Example 6 and Example 3 is that in Comparative Example 6, the β-glucan with a molecular weight of 7000kDa-9000kDa in Example 3 is replaced with β-glucan with a molecular weight of 3000kDa-5000kDa, and the remaining steps and parameters are the same as those in Example 3. The preparation method of the extract of Osmanthus fragrans rhizome is the same as that in Example 3.

[0128] Comparative Example 7

[0129] The difference between Comparative Example 7 and Example 3 is that in Comparative Example 7, 19.38 parts of glycerol and 14.75 parts of butylene glycol in Example 3 are replaced by 19.38 parts of glycerol and 14.75 parts of hexylene glycol, and the remaining steps and parameters are the same as those in Example 3. The preparation method of the extract of Rhizome of Phyllostachys occidentalis is the same as that in Example 3.

[0130] Comparative Example 8

[0131] The difference between Comparative Example 8 and Example 3 is that in Comparative Example 8, 0.028 parts of glyceryl caprylate in Example 3 are replaced by 0.028 parts of propylene glycol caprylate, and the remaining steps and parameters are the same as those in Example 3. The preparation method of the extract of Rhizoma Osmanthus fragrans is the same as that in Example 3.

[0132] Comparative Example 9

[0133] The preparation method of the rhizome extract of Bamboo Shoots in Comparative Example 9 is different from that in Example 3, and the remaining steps and parameters are the same as those in Example 3. The preparation method of the rhizome extract of Bamboo Shoots in Comparative Example 9 is as follows:

[0134] S1, crushing the rhizome of Bambusa glabra by ultrasonic cell crusher (the conditions are frequency 25kHz, crushing time 40s, and number of cycles 6 times) to obtain Bambusa glabra rhizome powder;

[0135] S2, mixing the rhizome powder of Phyllostachys cinnamomea with 10 times by mass of a 10% ethanol aqueous solution, and soaking and extracting the mixture at 40° C. for 48 hours each time to prepare an ethanol extract;

[0136] S3, filtering the ethanol extract and concentrating it 50 times, purifying it with a macroporous adsorption resin, eluting it with a 75% ethanol aqueous solution, and collecting the eluate;

[0137] S4, after the eluate is concentrated 15 times, add 0.5 times the volume of 1,3-butanediol, stir evenly, let stand for 36 hours, and collect the supernatant;

[0138] S5. Centrifuge the supernatant (rotation speed 8000 rpm, time 20 min) to obtain a supernatant, which is the extract of the rhizome of Osmanthus fragrans.

[0139] Comparative Example 10

[0140] Comparative Example 10: 0.19 parts of the rhizome extract of Bamboo Sinensis in Example 3 were replaced by 0.19 parts of the leaf extract of Bamboo Sinensis, and the remaining steps and parameters were the same as those in Example 3. The preparation method of the leaf extract of Bamboo Sinensis was the same as that of the rhizome extract of Bamboo Sinensis, except that the rhizome of Bamboo Sinensis of the same mass was replaced by the leaf of Bamboo Sinensis of the same mass.

[0141] Comparative Example 11

[0142] Comparative Example 11: 0.19 parts of the rhizome extract of Bambusa glabra in Example 3 were replaced by 0.19 parts of the green bamboo leaf extract, and the remaining steps and parameters were the same as those of Example 3. The preparation method of the green bamboo leaf extract was the same as that of the rhizome extract of Bambusa glabra, except that the same mass of the rhizome of Bambusa glabra was replaced by the same mass of the green bamboo leaf.

[0143] Application Example 1-3 A whitening essence

[0144] Comparative Examples 1-3 are used to provide a whitening essence, wherein the formula of the whitening essence is as shown in Table 3.

[0145] Table 3

[0146]

[0147]

[0148] The preparation method of the whitening essence of Application Example 1-3 is as follows:

[0149] (1) The sustained-release whitening composition, allantoin, sodium hyaluronate, disodium EDT and water were added to a feeder, stirred evenly at 60° C., and kept warm for 15 minutes to obtain a mixture 1.

[0150] (2) Cooling the mixture to 45° C., adding the Ningxia wolfberry fruit extract, the Sophora flavescens root extract, the Pyracantha fortuneana fruit extract, the arginine ferulate, the 1-methylhydantoin-2-imide, the Cornus officinalis extract, the phenoxyethanol and the ethylhexylglycerin to the mixture 1, and stirring the mixture at 45° C. to obtain the mixture 2.

[0151] (3) The mixture was cooled to 35° C., α-arbutin, 1,2-pentanediol, caprylhydroxamic acid, and p-hydroxyacetophenone were added to the mixture 2, and the mixture was stirred at 35° C. to obtain a whitening essence.

[0152] Test Example 1: Safety Performance Test

[0153] The skin irritation of the sustained-release whitening composition was tested in accordance with the "Technical Specification for Safety of Cosmetics" (2015 edition) to evaluate the safety of the composition for use on the skin.

[0154] Test samples: compositions of Examples 1-10 and Comparative Examples 1-11.

[0155] Test steps: 84 rabbits were selected and randomly divided into 21 groups, with 4 rabbits in each group, and one test sample was used. 24 hours before the test, the hair on both sides of the rabbit's back spine was cut off without damaging the surface, and the shaved area was 3cm×3cm as the test area. About 0.5g of the test sample was applied directly to the test area, and then covered with two layers of gauze (2.5cm×2.5cm) and a layer of cellophane or the like, and then fixed with non-irritating tape and bandage. The skin on the other side was used as a control. A closed test was used with an application time of 4h. The other side was used as a blank control. It was applied continuously for 7 days. Observe the skin reaction at the application site 24h, 48h and 72h after application, and perform skin reaction scoring in accordance with Table 1 of Part 4 (page 491) of the "Technical Specifications for Safety of Cosmetics" (2015 edition). Make a comprehensive evaluation based on the average score of the test animals, and determine the skin irritation intensity in accordance with Table 2 of Part 4 (page 492) based on the average of the highest scores at each observation time point of 24h, 48h and 72h, and evaluate the irritation of the test sample to the skin.

[0156] The test results are shown in Table 4.

[0157] Table 4

[0158] Group strength Group strength Example 1 Non-irritating Comparative Example 1 Non-irritating Example 2 Non-irritating Comparative Example 2 Non-irritating Example 3 Non-irritating Comparative Example 3 Non-irritating Example 4 Non-irritating Comparative Example 4 Non-irritating Example 5 Non-irritating Comparative Example 5 Non-irritating Example 6 Non-irritating Comparative Example 6 Non-irritating Example 7 Non-irritating Comparative Example 7 Non-irritating Example 8 Non-irritating Comparative Example 8 Non-irritating Example 9 Non-irritating Comparative Example 9 Mild irritation Example 10 Non-irritating Comparative Example 10 Non-irritating / / Comparative Example 11 Non-irritating

[0159] The test results show that the sustained-release whitening compositions of Examples 1-10 are not irritating to the skin and will not cause irritation to the skin when directly applied to the skin surface. The composition of Comparative Example 9 is slightly irritating, indicating that the extraction method of the rhizome extract of Osmanthus fragrans affects the safety of the final product. A large amount of ethanol is used in the extraction process of the rhizome extract of Osmanthus fragrans in Comparative Example 9, resulting in the final product being easily irritated to the skin.

[0160] Test Example 2: Transdermal Performance Test

[0161] Test samples: whitening compositions of Examples 1-10 and Comparative Examples 1-11; the control group is a niacinamide aqueous solution with a mass fraction of 18.75%.

[0162] Test steps: In vitro transdermal experiments were performed using a vertical diffusion cell with pig skin as the model. Commercially available fragrant pig skin was fixed between the upper and lower chambers of the Franz transdermal absorption diffusion cell, with the stratum corneum facing upwards and the receiving cell (diffusion area 2cm 2 , volume 12mL) is filled with physiological saline, and the receiving solution is just in contact with the dermis, and 5g of the test sample is placed in the sample pool. Stirring is maintained at a constant speed of 180rpm at a constant temperature (37℃±0.1)℃. 0.5mL of the receiving solution is taken into an EP tube at 4, 8, and 24h, and the content of nicotinamide in the receiving solution is determined by high performance liquid chromatography (HPLC). Based on the original content of nicotinamide in the sustained-release whitening composition, the transdermal absorption rate of nicotinamide is calculated.

[0163] The test results are shown in Table 5.

[0164] Table 5

[0165] Nicotinamide penetration rate (%) 4h 8h 24h Control group 2.2 3.5 3.7 Example 1 10.3 15.8 25.1 Example 2 10.9 17.1 27.6 Example 3 12.7 21.4 32.3 Example 4 11.2 19.5 29.2 Example 5 12.2 20.1 31.2 Example 6 12.5 20.6 31.5 Example 7 9.5 16.4 26.4 Example 8 11.1 18.8 29.2 Example 9 12 19.5 29.6 Example 10 10.1 16.7 25.9 Comparative Example 1 9.2 14.5 21.4 Comparative Example 2 8.1 13.9 20.1 Comparative Example 3 0 0 0 Comparative Example 4 5.5 9.3 12.7 Comparative Example 5 7.2 12.5 17.9 Comparative Example 6 4.5 8.8 14.5 Comparative Example 7 3.5 6.1 8 Comparative Example 8 7.8 13.2 18.5 Comparative Example 9 9 12.3 18.9 Comparative Example 10 6.8 10.4 13.8 Comparative Example 11 7.4 11.6 16.3

[0166] As shown in the table above, in the control group, the nicotinamide solution is directly subjected to the transdermal test. At 4h and 8h, part of the nicotinamide can still penetrate the skin, but the permeability of 24h is only slightly higher than that of 8h, indicating that nicotinamide is difficult to further absorb at this time. Compared with the control group, the permeability of the nicotinamide in the embodiment of the present invention is higher, and the data of 8h and 24h are compared. It can be seen that the nicotinamide in the sustained-release whitening composition of the embodiment of the present invention can continue to penetrate the skin, indicating that the composition of the present invention has a sustained-release effect. Compared with the control group and comparative examples 1-11, the sustained-release composition of embodiments 1-10 of the present invention has a higher permeability of nicotinamide in 4h, 8h, and 24h hours, respectively, indicating that the sustained-release composition of the present invention has a better transdermal absorption effect. Comparative examples 3, 5, 6 and comparative examples 1-3 show that the ratio of nicotinamide, carnosine and rhizome extract of cassia twig has a certain influence on the permeability of the final product. When the composition contains nicotinamide, carnosine and rhizome extract of cassia twig simultaneously, the transdermal absorption effect of the composition is better. Comparative Examples 3, 7, 8 and Comparative Example 7 show that the type of polyol has an effect on the transdermal absorption effect of the active substance of the final product. With glycerol and hexylene glycol (Comparative Example 7) as the types of polyols, the transdermal absorption effect of the final product is worse than that of glycerol (Example 7) alone. In the present invention, the polyol is preferably at least one of glycerol and butanediol, and the most preferred combination of glycerol and butanediol. Comparative Examples 3, 9, 10 and Comparative Examples 4, 5, 8 show that the amount of glycerol caprylate and β-glucan added and the type of caprylate affect the transdermal absorption effect of the final product. The present invention preferably uses glycerol caprylate and β-glucan as the wall material of the sustained-release whitening composition. Comparative Example 3 and Comparative Example 6 show that the molecular weight of β-glucan has an effect on the transdermal absorption effect of the final product. The molecular weight of β-glucan is too low, and the encapsulation of the wall material of the composition is poor, which is not conducive to the absorption of active substances such as nicotinamide. From the comparison of Example 3 and Comparative Examples 9-11, it can be seen that the extraction method of the bamboo extract, the part of the bamboo extracted and the type of plant have an impact on the transdermal absorption effect of the final product. The present invention preferably uses the bamboo rhizome extract prepared by enzymatic hydrolysis to form a sustained-release whitening composition.

[0167] Test Example 3: Whitening Effect Test

[0168] Test samples:

[0169] Sample group: the sustained-release whitening composition of Examples 1-10 and Comparative Examples 1-11, prepared into a solution with a mass fraction of 5% with deionized water; blank control group: deionized water; positive control group: according to the mass fractions of niacinamide, carnosine, and rhizome extract of Osmanthus fragrans in Example 3, a mixed solution was prepared at a mass fraction of 5% (i.e., the mixed solution contained 0.9375 parts of niacinamide, 0.0315 parts of carnosine, and 0.0095 parts of rhizome extract of Osmanthus fragrans).

[0170] Test steps: 58 volunteers with no damage, scars, or pigmentation problems on the inside of their arms were selected, and 4 test areas were selected on the inside of the left and right hands of the volunteers (two on each arm, and the area of ​​each test area was 3cm×3cm), for a total of 232 test areas. 230 test areas were selected and randomly divided into 23 groups, and one test sample was applied to each test area in each group (two test areas were discarded). 0.5 ml of the test sample was applied to each test area each time, twice a day, for 3 consecutive weeks, during which no other skin care products were used in the test area. After applying the sample for 1, 2, and 3 weeks, the changes in the skin melanin content in the test area were detected by an instrument, and the percentage of reduction in the skin melanin content was recorded to evaluate the whitening effect of the test sample. The more the skin melanin content is reduced, the better the whitening effect of the test sample.

[0171] The percentage of reduction in skin melanin content (%) = skin melanin content before use - skin melanin content after use for n weeks / skin melanin content before use × 100%.

[0172] n=1,2,3.

[0173] The test results are shown in Table 6.

[0174] Table 6

[0175] Melanin content reduction percentage (%) Week 1 Week 2 Week 3 Blank control group 0.1 0 -0.1 Positive control group 6.5 7.8 8.7 Example 1 5.8 11.2 16.1 Example 2 5 9.5 15.7 Example 3 6.1 13.5 19.5 Example 4 6 11.6 18.8 Example 5 5.9 10.5 17.9 Example 6 5.7 10.1 16.2 Example 7 6.1 10.9 16.3 Example 8 6.2 11.8 18 Example 9 6.3 13.2 18.6 Example 10 6.4 10.9 17.1 Comparative Example 1 3.5 6.5 9.6 Comparative Example 2 3.1 6 8.8 Comparative Example 3 1.2 2.3 3.5 Comparative Example 4 6.1 8.1 9.8 Comparative Example 5 6.3 8.5 10.4 Comparative Example 6 6 7.4 9.2 Comparative Example 7 5.9 7.6 11.8 Comparative Example 8 6.2 8.7 10.2 Comparative Example 9 3.8 5.7 8.5 Comparative Example 10 3.8 7.7 11.2 Comparative Example 11 3.2 5.1 8.2

[0176] As shown in Table 6, the blank control group does not contain active substances, so it does not have a whitening effect. The 0.1% float in the data is an experimental error. The positive control group contains nicotinamide, carnosine and rhizome extract of Bamboo cycads in the same content as in Example 3. In the first week, it shows the best whitening effect. At the same time, compared with the data of the first week, when the ratio of nicotinamide, carnosine and rhizome extract of Bamboo cycads (enzymatic method) in the composition is 18.75:0.63:0.19, the whitening effect of the composition is the best, indicating that there is a synergistic effect between nicotinamide, carnosine and rhizome extract of Bamboo cycads by enzymatic method, and the three can be used together to improve the whitening effect of the composition. When other mass ratios are used, or the plant extracts are replaced, the whitening effect of the composition becomes worse. In Examples 1-10 and Comparative Examples 1-11, Comparative Example 3 does not contain nicotinamide, and its whitening effect is the worst. Comparing the data of the 2nd and 3rd weeks, it can be seen that as the use time is extended, the sustained-release whitening composition shows a better whitening effect. The whitening effects of Examples 1-10 and Comparative Examples 4-8 are better than those of the positive control group. Comparative Examples 3, 7, 8 and Comparative Example 7 show that the type of polyol affects the sustained-release effect of the sustained-release composition, and ultimately affects the long-lasting whitening effect of the composition. In the present invention, the polyol is preferably at least one of glycerol and butylene glycol, and most preferably a combination of glycerol and butylene glycol. Comparative Examples 3, 9, 10 and Comparative Examples 6 and 8 show that the types of caprylate and β-glucan affect the sustained-release effect of the final product, and ultimately affect the long-lasting whitening effect of the composition. In the present invention, caprylate is preferably glycerol caprylate and β-glucan, and β-glucan is selected as β-glucan with a molecular weight of 6000kDa-10000kDa.

[0177] Test Example 4: Soothing Effect Test

[0178] Test principle: The neutrophils of zebrafish embryos and human neutrophils are very similar in morphology, biochemistry and physiological functions. The cells are highly similar in morphology, biochemistry and physiological functions. When damage occurs or pathogens invade, neutrophils are the first white blood cells to appear at the site of damage or invasion, and their main function is to clear infection or remove harmful substances. Copper sulfate is used to induce damage to the neuromast cells in the lateral line area of ​​zebrafish embryos, causing neutrophil aggregation. The greater the damage to the zebrafish neuromast cells, the more neutrophils aggregate; if the tested sample has a soothing effect, the number of neutrophils will decrease. Compare the changes in the number of neutrophils in the lateral line area of ​​the fish embryos in the test sample group and the blank control group, and calculate the inhibition rate of zebrafish embryo neutrophils to evaluate the soothing effect of the test sample (raw material, formula or product).

[0179] Test sample: The sustained-release whitening composition of Examples 1-10 and Comparative Examples 1-11 was prepared into a solution with a mass fraction of 5% using fish embryo culture medium.

[0180] Test steps (test sample set):

[0181] (a) Six fish embryos were selected and placed in a culture dish (six fish embryos for each test sample). 5 mL of the fish embryo culture medium (containing 0.16 mg / L copper sulfate pentahydrate) of the test sample was added to the culture dish and cultured at 28° C. for 50 min.

[0182] (b) The fish embryos of the test group were fixed in paraformaldehyde for at least 1 hour, then treated with PBST solution, and then stained with Sudan black staining solution for 1 hour, and finally treated with bleaching solution to obtain fixed and stained fish embryos.

[0183] (c) The fish embryos were placed sideways, observed and photographed under a microscope, and the number of neutrophils in the lateral line region of the tail three quarters of the way from the anus of each fish embryo was counted. The counting results were averaged, with one decimal place retained, and the neutrophil aggregation inhibition rate was calculated.

[0184] The test steps of the blank control group were similar to those of the test sample group, with the only difference being that in step (a), 5 mL of the test sample's fish embryo culture medium (containing 0.16 mg / L copper sulfate pentahydrate) was replaced with 5 mL of fish embryo culture medium (containing 0.16 mg / L copper sulfate pentahydrate), i.e., no test sample was added to the blank control group.

[0185] Neutrophil aggregation inhibition rate (%) = (CT) / C×100%

[0186] C is the number of neutrophils in fish embryos of the blank control group; T is the number of neutrophils in fish embryos of the test sample group.

[0187] The higher the neutrophil aggregation inhibition rate is, the better the soothing effect of the test sample is. The test results are shown in Table 7.

[0188] Table 7

[0189]

[0190] The test results show that the sustained-release whitening compositions of the embodiments of the present invention and the comparative examples all show a certain soothing effect. Comparative Examples 3, 5, 6 and Comparative Examples 1-3, Comparative Examples 9-11 show that in the sustained-release whitening composition of the present invention, there is a synergistic effect between nicotinamide, carnosine and the enzymatic hydrolysis of the rhizome extract of Phyllostachys glabra. The combination of the three has a better soothing effect on the final product. The soothing effect of the final product is poor if one of the components is missing, or the preparation method of the rhizome extract of Phyllostachys glabra is replaced, or the components of the plant are replaced. Comparative Examples 3, 7-10 and Comparative Examples 4-7 show that the types of caprylic acid ester and β-glucan and the type of polyol have an effect on the soothing effect of the final product. Among them, Comparative Examples 3, 7, 8 and Comparative Example 7 show that the type of polyol has relatively less effect on the soothing effect. The polyol of the present invention is preferably at least one of glycerol and butylene glycol, and the remaining wall materials are preferably glycerol caprylate and β-glucan with a molecular weight of 6000kDa-10000kDa.

[0191] The above embodiments are preferred implementation modes of the present invention, but the implementation modes of the present invention are not limited to the above embodiments. Any other changes, modifications, substitutions, combinations, and simplifications that do not deviate from the spirit and principles of the present invention should be equivalent replacement methods and are included in the protection scope of the present invention.

Claims

1. A sustained-release whitening composition, characterized in that: The composition comprises, by weight: 15-22 parts of niacinamide, 0.3-0.8 parts of carnosine, 0.12-0.25 parts of rhizome extract of Phyllostachys glabra, 27-43 parts of polyol, 0.015-0.045 parts of glyceryl caprylate, 0.018-0.05 parts of β-glucan, and water to make up to 100 parts by weight; The polyol comprises glycerol and butylene glycol; based on the total mass of the sustained-release whitening composition, the glycerol is 15-25 parts, and the butylene glycol is 12-18 parts; The molecular weight of the β-glucan is 6000 kDa-10000 kDa; The preparation method of the Osmanthus fragrans rhizome extract comprises: S1, crushing the rhizomes of Bamboo Stalks to obtain Bamboo Stalk Rhizomes powder; S2, mixing the rhizome powder of the bamboo with water, and heating the mixture to obtain a mixed solution; S3, adding a composite enzyme to the mixed solution for enzymolysis to obtain an enzymolysis solution; S4, performing enzyme inactivation treatment and filtering treatment on the enzymatic hydrolyzate to obtain the rhizome extract of Phyllostachys occidentalis; wherein, In step S3, the complex enzyme includes cellulase and pectinase, and the mass ratio of the cellulase to the pectinase is (2-4):

1.

2. The sustained-release whitening composition according to claim 1, characterized in that The invention comprises, by weight: 17.8-19.8 parts of niacinamide, 0.5-0.75 parts of carnosine, 0.16-0.22 parts of rhizome extract of Phyllostachys glabra, 30-40 parts of polyol, 0.025-0.032 parts of glyceryl caprylate, 0.028-0.04 parts of beta-glucan and water to make up the total weight of 100 parts.

3. A method for preparing the sustained-release whitening composition according to any one of claims 1 or 2, characterized in that: include: B1. Evenly mix water, niacinamide, carnosine and rhizome extract of Phyllostachys occidentalis to obtain a mixture A; B2, mixing the polyol, glyceryl caprylate and β-glucan uniformly to obtain a mixture B; B3, adding the mixture A to the mixture B, mixing and reacting, and then performing high-speed shear dispersion to obtain a coarse nanocomposite; B4. Performing high-pressure homogenization on the crude nanocomposition to obtain a sustained-release whitening composition.

4. The preparation method according to claim 3, characterized in that: Including at least one of (I)-(IV): (I) In step B3, the mixture B is added to the mixture A at a rate of 0.8-2.2 mL / min; (II) The temperature of the mixed reaction in step B3 is 40-50°C, the speed of the stirring blade is 80-150 rpm, and the time of the mixed reaction is 15-30 min; (III) The rotation speed of the high-speed shear dispersion in step B3 is 8000-12000 rpm, and the time of the high-speed shear dispersion is 5-15 min; (IV) The high-pressure homogenization treatment in step B4 is a high-pressure microfluidization homogenization treatment; the conditions of the high-pressure microfluidization homogenization treatment are: pressure 1.3-1.8 MPa, and the number of cycles is 2-6 times.

5. Use of the sustained-release whitening composition according to any one of claims 1 or 2 in the preparation of cosmetics.

6. A whitening essence, characterized in that: In percentage by mass, including 12-20% The sustained-release whitening composition according to any one of claims 1 or 2, 0.08-0.22% allantoin, 0.08-0.15% sodium hyaluronate, 0.03-0.08% disodium EDTA, 0.01-0.03% Ningxia wolfberry fruit extract, 0.02-0.06% sophora flavescens root extract, 0.01-0.05% pyracantha fruit extract, 0.015-0.035% arginine ferulate, 0.12-0.25% 1 -methylhydantoin-2-imide, 0.1-0.5% cornus officinalis extract, 0.002-0.006% phenoxyethanol, 0.0002-0.001% ethylhexylglycerol, 0.8-2.0% α-arbutin, 0.3-0.8% 1,2-pentanediol, 0.02-0.06% caprylhydroxamic acid, 0.002-0.007% p-hydroxyacetophenone and water supplemented to 100% of the total mass percentage of the whitening essence.

7. A method for preparing the whitening essence according to claim 6, characterized in that: include: (1) adding the sustained-release whitening composition, allantoin, sodium hyaluronate, disodium EDTA and water into a feeder, stirring evenly, and keeping warm to obtain a mixture 1; (2) After the temperature is lowered once, add the Ningxia wolfberry fruit extract, the Sophora flavescens root extract, the Pyracantha fortuneana fruit extract, arginine ferulate, 1-methylhydantoin-2-imide, the Cornus officinalis extract, phenoxyethanol and ethylhexylglycerin to the mixture 1, and stir evenly to obtain a mixture 2; (3) After the second cooling, α-arbutin, 1,2-pentanediol, caprylhydroxamic acid and p-hydroxyacetophenone are added to the mixture 2 and stirred evenly to obtain a whitening essence.

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