WO2022218171A1 - Application d'une composition d'extrait d'ananas dans le blanchiment - Google Patents

Application d'une composition d'extrait d'ananas dans le blanchiment Download PDF

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WO2022218171A1
WO2022218171A1 PCT/CN2022/084837 CN2022084837W WO2022218171A1 WO 2022218171 A1 WO2022218171 A1 WO 2022218171A1 CN 2022084837 W CN2022084837 W CN 2022084837W WO 2022218171 A1 WO2022218171 A1 WO 2022218171A1
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pineapple
parts
extract composition
oil
water
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PCT/CN2022/084837
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English (en)
Chinese (zh)
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刘继涛
吴迪
安全
刘平平
权强华
王昌涛
石秀芹
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云南白药集团健康产品有限公司
云南白药集团股份有限公司
北轻家化(黄山)科技有限公司
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Publication of WO2022218171A1 publication Critical patent/WO2022218171A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9794—Liliopsida [monocotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9728—Fungi, e.g. yeasts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9755—Gymnosperms [Coniferophyta]
    • A61K8/9767—Pinaceae [Pine family], e.g. pine or cedar
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59—Mixtures
    • A61K2800/592—Mixtures of compounds complementing their respective functions
    • A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18

Definitions

  • the invention belongs to the field of cosmetics, and particularly relates to a whitening application of a pineapple extract composition.
  • Natural cosmetics are more and more popular nowadays. Natural cosmetics, in addition to natural ingredients, do not add flavors, preservatives and other potentially irritating ingredients.
  • enzymolysis can transform macromolecular components into small molecules, which are accompanied by the production of other active substances such as polysaccharides and polypeptides.
  • Plants contain a variety of enzymes, including protease, cellulase, amylase, esterase, etc.
  • the enzymes contained in plants can be used to hydrolyze macromolecular proteins into oligopeptides, and starch and cellulose into oligosaccharides. , lipolysis into glycerol, fatty acid.
  • the application of these products in cosmetics is more conducive to the skin's absorption of functional ingredients, and finally achieves a certain effect.
  • the object of the present invention is to overcome the defects in the prior art and provide a whitening application of the pineapple extract composition.
  • alpha-MSH refers to: melanin.
  • PBS refers to: Phosphate Buffered Saline.
  • t-test refers to: T-test.
  • B16 cells refers to: B16 mouse melanoma cells.
  • ITA refers to: Skin Color Measurement.
  • VISIA CR refers to: Facial Image Analyzer.
  • the first aspect of the present invention provides the application of a pineapple extract composition in the preparation of a product with a whitening effect
  • the pineapple extract composition is prepared by extracting the raw materials of the following components: pineapple, oat , highland barley, barley, tremella polysaccharide and water;
  • the parts by mass of each component in the pineapple extract composition are: 0.1-10 parts of pineapple, 0.1-10 parts of oats, 0.1-5 parts of highland barley, 0.1-5 parts of coix seed, 0.05-2 parts of Tremella polysaccharide, water 100 copies;
  • the pineapple extract composition is prepared by the following method:
  • step (1) gained oat, highland barley, coix seed and water are mixed and left standstill to obtain mixed pretreatment solution;
  • step (4) adding Tremella polysaccharide to the supernatant obtained in step (4), and homogenizing to obtain the pineapple extract composition.
  • step (1) wherein, in step (1), the oats, highland barley, and barley are pulverized and passed through an 80-mesh sieve.
  • the ratio of pineapple to water is 1:0.1 ⁇ 20g/mL, preferably 1:0.2 ⁇ 10g/mL, more preferably 1:0.5 ⁇ 5g/mL mL, more preferably 1:1 g/mL.
  • the standing time is 12-60 hours, preferably 12-48 hours, and most preferably 24 hours.
  • the addition ratio of the pineapple treatment solution obtained in step (2) and the mixed pretreatment solution obtained in step (3) is 1:1 to 500 g/mL, preferably 1 : 5 to 200 g/mL, more preferably 1:10 to 100 g/mL, still more preferably 1:20 to 50 g/mL.
  • the heating temperature is 20-90°C, preferably 25-85°C, more preferably 30-80°C, further preferably 40-75°C;
  • the heating time is 0.5 to 5 hours, preferably 0.5 to 4 hours, more preferably 1 to 3 hours, further preferably 1 to 2 hours; and/or
  • the stirring rate is 100-800 r/min, preferably 100-500 r/min, more preferably 100-400 r/min, further preferably 200-300 r/min.
  • the ratio of the Tremella polysaccharide to the supernatant obtained in step (4) is 1:1 ⁇ 1000g/mL, preferably 1:100 ⁇ 800g/mL ; more preferably 1:100 to 500 g/mL, most preferably 1:200 to 400 g/mL; and/or
  • the homogenization time is 1 to 60 minutes, preferably 5 to 50 minutes, more preferably 5 to 30 minutes, and further preferably 10 to 20 minutes.
  • the method further comprises the following steps:
  • the sterilization treatment method is heat sterilization
  • the heating sterilization temperature is 60-90°C, preferably 70-80°C, most preferably 75°C; and/or the heating sterilization time is 1-5 hours, preferably 1-3 hours , most preferably 2 hours.
  • the product with whitening effect comprises:
  • the pineapple extract composition is a pineapple extract composition
  • the cosmetic ingredients are selected from one or more of the following: olive oil, matsutake mushrooms, green thorn fruit oil, betaine, Ganoderma lucidum, and Rhodiola rosea.
  • the whitening effect is inhibition of tyrosinase activity
  • the whitening effect is to inhibit the synthesis of melanin.
  • the dosage form of the product with whitening effect is selected from one or more of the following: cream, lotion, water, gel, oil, powder, mud, aerosol , paste, film;
  • the cosmetic product is a cream, mask, lotion or essence.
  • step (c) adding the oil phase mixture prepared in step (b) to the water phase mixture prepared in step (a), and homogenizing to obtain the cosmetic product.
  • the water phase ingredients include vegetable oil and an antibacterial agent; and/or in the step (b), the oil phase ingredients include vegetable oil and emulsification agent;
  • the vegetable oil is selected from one or more of the following: glycerin, green thorn fruit oil, olive oil, peony seed oil, macadamia nut oil, babassu oil, toona japonica oil;
  • the antibacterial agent is selected from one or more of the following: hexanediol, methylparaben, propylparaben, phenoxyethanol; and/or
  • the emulsifier is selected from one or more of the following: wheat emulsifier, polyglycerol-3 diisostearate, dipolyhydroxystearic acid, and yeoleyl glucoside.
  • the ratio of the sterilized pineapple extract composition, vegetable oil and antibacterial agent is 80 ⁇ 95:1 ⁇ 10:0.01 ⁇ 1g/ g/g, preferably 89 ⁇ 93:2 ⁇ 5:0.05 ⁇ 0.2g/g/g;
  • the ratio of the vegetable oil to the emulsifier is 1 ⁇ 10:2 ⁇ 15g/g, preferably 2 ⁇ 5:5 ⁇ 10g/g; and/or
  • the ratio of the oil phase mixture to the water phase mixture is 2-25:0.5-5g/g, preferably 5-10:1-2g/g;
  • the heating temperature is 70-120°C, more preferably 70-100°C, further preferably 80-90°C; and /or
  • the homogenization time is 15-45 minutes, more preferably 20-40 minutes, and even more preferably 25-35 minutes.
  • the preparation method of the pineapple extract composition of the present invention comprises the following steps:
  • Tremella polysaccharide is added, and the mask liquid is obtained by homogenization.
  • the ratio of the oats to water is 1:1 ⁇ 500g/mL, preferably 1:10 ⁇ 300g/mL, more preferably 1:20 ⁇ 150g/mL, most preferably 1:80g/mL mL;
  • the ratio of highland barley to water is 1:1 ⁇ 400g/mL, preferably 1:10 ⁇ 350g/mL, more preferably 1:30 ⁇ 200g/mL, most preferably 1:100g/mL;
  • the ratio of coix seed and water is 1:1 ⁇ 400g/mL, preferably 1:20 ⁇ 300g/mL, more preferably 1:50 ⁇ 200g/mL, most preferably 1:100g/mL;
  • the ratio of the pineapple extract to (1) extract is 1:1 ⁇ 200g/mL, preferably 1:1 ⁇ 150g/mL, more preferably 1:1 ⁇ 100g/mL, most preferably 1:1 ⁇ 100g/mL. Preferably 1:50g/mL;
  • the heating temperature is 1-150°C, preferably 1-120°C, more preferably 20-90°C, most preferably 75°C;
  • the heating time is 0.1 to 4 hours, preferably 0.5 to 3 hours, more preferably 0.5 to 2 hours, and most preferably 1 hour
  • the stirring rate is 10-1000 r/min, preferably 10-800 r/min, more preferably 20-500 r/min, most preferably 300 r/min.
  • the ratio of Tremella polysaccharide and extract is 1:1 ⁇ 2000g/mL, preferably 1:1 ⁇ 1000g/mL, more preferably 1:1 ⁇ 800g/mL, most preferably 1:1 ⁇ 1000g/mL 400g/mL
  • the homogenization speed is 1000 ⁇ 20000r/min, preferably 2000 ⁇ 15000r/min, more preferably 2500 ⁇ 10000r/min; the best is 6000r/min;
  • the homogenization time is 1 to 60 minutes, preferably 1 to 40 minutes, more preferably 1 to 30 minutes, and most preferably 20 minutes.
  • the invention provides an application of a pineapple extract composition in preparing a product with a whitening effect. Tests show that the pineapple extract composition of the invention has an inhibitory effect on B16-F10 tyrosinase activity.
  • Figure 1 shows the HPLC profile of sample 1 at 220 nm in Example 1.
  • FIG. 2 shows the HPLC profile of sample 2 at 220 nm in Example 1.
  • FIG. 3 shows the HPLC profile of the blank group at 220 nm in Example 1.
  • FIG. 4 shows the tyrosinase activity of the pineapple extract composition in Test Example 1 acting on B16-F10.
  • FIG. 5 is a graph showing an example of the change in pigmentation of the volunteer 1 after using the cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 5 is a graph showing an example of the change in pigmentation of the volunteer 1 after using the cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 6 is a graph showing an example of the change in pigmentation of Volunteer 2 after using Cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 6 is a graph showing an example of the change in pigmentation of Volunteer 2 after using Cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 7 is a graph showing an example of the change in pigmentation of Volunteer 3 after using Cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 7 is a graph showing an example of the change in pigmentation of Volunteer 3 after using Cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 8 is a graph showing an example of the change in pigmentation of volunteer 1 after using the cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 8 is a graph showing an example of the change in pigmentation of volunteer 1 after using the cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 9 is a graph showing an example of the change in pigmentation of Volunteer 2 after using the cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 9 is a graph showing an example of the change in pigmentation of Volunteer 2 after using the cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 10 is a graph showing an example of the change in pigmentation of Volunteer 3 after using Cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 10 is a graph showing an example of the change in pigmentation of Volunteer 3 after using Cream 2 prepared in Example 10 in Test Example 4.
  • Figure 11 shows the effect of the sample (facial cream 1) prepared in Example 9 in Test Example 4 on the skin melanin value (time point comparison), wherein, **, p ⁇ 0.01, indicating that compared with the background, it has extremely high Significant difference; n.s., p>0.05, indicating no significant difference compared with the background.
  • Figure 12 shows the effect of the sample (cream 2) prepared in Example 10 in Test Example 4 on the skin ITA value (time point comparison), wherein, **, p ⁇ 0.01, indicating that compared with the background, it has a very high Significant difference; n.s., p>0.05, indicating no significant difference compared with the background.
  • Figure 13 shows the proportion of consumers who are satisfied with the efficacy evaluation of consumers in Test Example 4.
  • Figure 14 shows the proportion of the overall number of satisfied consumers in Test Example 4.
  • Oatmeal (fried and cooked), purchased from Zhangjiakou Jianjun Oat Food Co., Ltd.;
  • Tyrosinase purchased from Sigma Ltd.
  • Homogenizer purchased from IKA Co., Ltd., model T25;
  • Skin elasticity test instrument purchased from Beijing Jinhongfan Trading Co., Ltd., model MPA580 multi-probe;
  • Facial image analyzer purchased from Beijing Jinhongfan Trading Co., Ltd., model VISIA CR.
  • This example is used to illustrate the selection of the pineapple enzyme solution of the present invention.
  • pineapple enzyme solution 1 is Barry pineapple
  • pineapple enzyme solution 2 is golden diamond pineapple.
  • Sample preparation use the mobile phase as the solvent to prepare a sample with a concentration of 5 mg/ml, and then filter it with a microporous membrane (0.45 ⁇ m) for injection.
  • Standard sample bovine serum albumin (Mr 67000), B12 (Mr 1335), and oxidized glutathione (Mr 614) were prepared into mixed standards, and the content of each substance was 5mg/ml.
  • Figures 1 to 3 show the HPLC chromatograms of sample 1, sample 2 and blank group in Example 1, respectively.
  • the peak time, area and molecular weight of sample 1, sample 2 and blank group are shown in Table 1 below.
  • the content of the polypeptide with a molecular weight of 1495.12 Da is 88.49%, and the content of the polypeptide with a molecular weight of 148.08 Da is 11.51%.
  • the results showed that compared with the blank group, the proportion of peptides with molecular weight below 1600 Da in the supernatant obtained by adding pineapple enzyme solution increased, especially in sample 1, under the action of protease in pineapple, the peptides with molecular weight below 1000 Da The content is 59.45%.
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:1 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • the pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:20 (g/ml), heated at 40° C. for 2 hours, and stirred at 300 rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:1 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • step (1) The pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:50 (g/ml), heated at 75°C for 1 hour, and stirred at 200rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:1 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • step (1) (2) the pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:30 (g/ml), heated at 50 ° C for 2 hours, and stirred at 250 rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:1 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • step (1) (2) the pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:40 (g/ml), heated at 60 ° C for 1 hour, and stirred at 300 rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:5 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • step (1) (2) the pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:100 (g/ml), heated at 80° C. for 3 hours, and stirred at 400 rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:10 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • step (1) (2) the pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:200 (g/ml), heated at 85 ° C for 4 hours, and stirred at 500 rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the preparation method of the pineapple extract composition of the present invention.
  • Oats, highland barley, and barley crush the oats, barley, and barley to 80 mesh for use.
  • Pineapple Wash, peel, and dice. 1:20 (g/ml) was mixed with water and beaten to obtain a pineapple pretreatment solution for later use.
  • step (1) (2) the pineapple pretreatment solution and the mixed pretreatment solution obtained in step (1) are mixed according to the mass ratio of 1:500 (g/ml), heated at 90 ° C for 5 hours, and stirred at 800 rad/min; cooled to room temperature, filtered to remove impurities, Leave the supernatant (opaque).
  • This example is used to illustrate the method for preparing a whitening cream using the pineapple extract composition of Example 3 of the present invention.
  • This example is used to illustrate the method for preparing a whitening cream using the pineapple extract composition of Example 8 of the present invention.
  • This example is used to prepare the whitening cream 3 which is compared with Example 9 and Example 10.
  • composition of the pineapple extract is replaced with water, and the other ingredients, proportions and operation steps remain unchanged, and the face cream 3 is prepared.
  • B16 melanoma cells were plated in 6-well plates, and the number of cells was 5 ⁇ 10 4 , and cultured overnight. Discard the old medium, replace with fresh serum-free medium, add 1 ⁇ M ⁇ -MSH for stimulation, establish a cell model, and add pineapple extract composition (pineapple 1) at 1.25%, and test after 48 hours. As a positive control, kojic acid was selected at a concentration of 100 ⁇ g/ml. The results are shown in Figure 4.
  • Figure 4 shows the tyrosinase activity of the pineapple extract composition acting on B16 melanoma cells
  • ⁇ -MSH is the model group
  • kojic acid is the positive control
  • pineapple 1 is the pineapple extract composition
  • Table 11 shows the significant difference analysis of tyrosinase activity after the pineapple extract composition acts on B16 melanoma cells in Test Example 1. There is a significant statistical difference between the model group and the blank group. The model is successfully established. The extract composition had a reduced effect on tyrosinase in the model group.
  • This test example is used to illustrate the tyrosinase inhibition rate of the pineapple extract composition (pineapple 1) in Examples 3 to 5 on B16.
  • Table 12 shows the analysis of significant differences in tyrosinase activity after the pineapple extract compositions prepared in Examples 3 to 5 acted on B16. There was a significant statistical difference between the model group and the blank group, and the model was successfully established.
  • the pineapple extract composition prepared by the invention has a significant inhibitory effect on tyrosinase activity.
  • This test example is used to illustrate the inhibitory effect of the pineapple extract composition in Examples 2 to 8 on melanin synthesis on B16 cells.
  • B16 cells with good logarithmic growth phase were inoculated into 6-well plates at a density of 1 ⁇ 10 5 cells/mL, and placed in an incubator at 37°C and cultured overnight in a 5% CO 2 environment; the medium was replaced with 1.5% Concentrations of the compositions prepared in Examples 2 to 8, the negative control group was untreated, and 1 mg/mL arbutin was used as a positive control. After culturing for 48 hours, the culture medium was aspirated, washed with PBS, and then digested with 250 ⁇ L trypsin.
  • Table 13 shows the results of the inhibitory effect of the pineapple extract composition prepared by the present invention on melanin synthesis acting on B16. It can be seen from the table that the pineapple extract composition has a significant inhibitory effect on melanin synthesis.
  • Example 2 sample name Tyrosinase inhibition rate (%) SD P-value control group 0 0 / Alpha Arbutin 41.88 1.56 0.000**
  • Example 2 25.76 1.44 0.002**
  • Example 3 24.51 2.21 0.011*
  • Example 4 24.19 1.43 0.011**
  • Example 5 25.64 1.52 0.01**
  • Example 6 17.65 1.3 0.032*
  • Example 7 15.38 2.63 0.021*
  • Example 8 13.74 1.71 0.165*
  • This test example is used to compare the whitening efficacy of the cream prepared in Example 9, Example 10 and the cream prepared in Example 11 on human body.
  • test site has not undergone skin treatment, cosmetic or other tests that may affect the results
  • the specified content can be completed according to the requirements of the test plan.
  • Test environment temperature: 20 ⁇ 2°C; humidity: (50 ⁇ 10)%, and real-time dynamic monitoring is performed.
  • the left face uses the example sample
  • the right face uses the comparative sample.
  • the skin melanin index, ITA, and VISIA CR of both cheeks were collected at 0d, 14d, and 28d, respectively. And fill in the questionnaire in Annex 1 at 28d. Monitoring is required to ensure that subjects correctly distinguish between the test product and the control product on both sides and the continuous use sample.
  • Figure 11 shows the effect of the sample (cream 1) prepared in Example 9 in Test Example 4 on the skin melanin index (time point comparison), wherein, **, p ⁇ 0.01, indicating that compared with the background, it has a very high Significant difference; n.s., p>0.05, indicating no significant difference compared with the background. It can be seen from Figure 11 that after the 28-day sample use cycle, the skin melanin value of the sample group was extremely significantly lower than the background. There was no significant difference between the skin melanin value of the control group and the background.
  • Figure 12 shows the effect of the sample (cream 2) prepared in Example 10 in Test Example 4 on the skin ITA value (time point comparison), wherein, **, p ⁇ 0.01, indicating that compared with the background, it has a very high Significant difference; n.s., p>0.05, indicating no significant difference compared with the background. It can be seen from Figure 12 that after 14 days of sample use cycle, the skin ITA value of the sample (cream 2) group is extremely significantly higher than the background. There was no significant difference between the skin ITA value of the control group and the background.
  • Figure 13 shows the proportion of consumers who are satisfied with the efficacy evaluation of consumers in Test Example 4.
  • 30 subjects compared the satisfaction of the sample and the control in four aspects of moisturizing, whitening effect, brightening skin tone, and lightening spots, and the results showed that the sample group (cream 1 ) was more satisfied than the control group in three aspects: whitening effect, brightening skin tone and lightening spots.
  • Figure 14 shows the proportion of the overall number of satisfied consumers in Test Example 4. It can be seen from Figure 14 that after the 28-day sample use period, 30 subjects were satisfied with the overall use effect, and the proportion of satisfied people in the sample group (cream 2) reached 80%, which was higher than that in the control group.
  • FIG. 5 is a graph showing an example of the change in pigmentation of the volunteer 1 after using the cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 6 is a graph showing an example of the change in pigmentation of Volunteer 2 after using Cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 7 is a graph showing an example of the change in pigmentation of Volunteer 3 after using Cream 1 prepared in Example 9 in Test Example 4.
  • FIG. 8 is a graph showing an example of the change in pigmentation of volunteer 1 after using the cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 9 is a graph showing an example of the change in pigmentation of Volunteer 2 after using the cream 2 prepared in Example 10 in Test Example 4.
  • FIG. 10 is a graph showing an example of the change in pigmentation of Volunteer 3 after using Cream 2 prepared in Example 10 in Test Example 4.
  • the facial cream prepared by using the pineapple extract composition of the present invention has a significant whitening effect compared to the base cream prepared by adding only water in Example 11 (comparative example). It showed a good whitening effect in terms of ITA value and stain area.

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Abstract

Application d'une composition d'extrait d'ananas dans la préparation d'un produit présentant un effet blanchissant, la composition d'extrait d'ananas étant préparée et obtenue par extraction de matières premières des constituants suivants : les ananas, l'avoine, l'orge de montagne, les graines de coix, les polysaccharides et l'eau de trémelles. Il a été prouvé par expérimentation que la composition d'extrait d'ananas présente un effet inhibiteur sur l'activité de la tyrosinase après action sur des cellules de mélanome B16-F10, et présente un effet inhibiteur considérable sur la synthèse de mélanine des cellules B16.
PCT/CN2022/084837 2021-04-16 2022-04-01 Application d'une composition d'extrait d'ananas dans le blanchiment WO2022218171A1 (fr)

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CN113274334B (zh) * 2021-04-16 2022-07-22 云南白药集团股份有限公司 具有抗衰老作用的菠萝提取液组合物、其制备方法和应用
CN113230166A (zh) * 2021-04-16 2021-08-10 云南白药集团股份有限公司 一种面膜液、其制备方法及应用
CN113197817A (zh) * 2021-04-16 2021-08-03 云南白药集团股份有限公司 一种菠萝提取液组合物的美白应用
CN113274333B (zh) * 2021-04-16 2022-07-26 云南白药集团股份有限公司 具有抗氧化作用的菠萝提取液组合物、其制备方法和应用
CN113197818A (zh) * 2021-04-16 2021-08-03 云南白药集团股份有限公司 一种面膜液的制备方法及面膜产品

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