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A composition for lightening skin and hair

A technology of composition and mixture, which is applied in skin care preparations, skin diseases, drug combinations, etc., and can solve problems such as high sensitization potential

Active Publication Date: 2016-03-09
SYMRISE GMBH & CO KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] Kojic acid (5-hydroxy-hydroxymethyl-4-pyrone) is a tyrosinase inhibitor that inhibits the catalytic activity of tyrosinase through the copper atom in the chelating enzyme; it is used in commercially available skin and Hair lightener but with high sensitization potential and triggers contact allergy

Method used

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  • A composition for lightening skin and hair
  • A composition for lightening skin and hair
  • A composition for lightening skin and hair

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0273] Pigmentation effects on melanoma cell cultures

[0274] Take 7.5×10 3 Concentration of cells / well B16V mouse melanoma cells were dispersed in 96-well microtiter plates. in RPMI medium at 37 °C and 5% CO 2 Cultured in medium for 24 hours, enriched with 10% fetal bovine serum, added various concentrations of test substances and 0.3 mM tyrosine and 10 nM α-MSH (α-melanostimulating hormone) and continued to culture for 96 hours. The maximum concentration of the test substance used corresponds to the IC of the cytotoxicity test 20 0.1 times the value. Only tyrosine and α-MSH were added to the control. After the cultivation, a sodium hydroxide solution (final concentration: 1M) was added to the culture medium and absorbance at 400 nm was measured 3 hours later (A).

[0275] Inhibition of pigmentation in the presence of test compounds was calculated using the following equation:

[0276] Pigmentation inhibition rate (%)=100-[(A 测试化合物 / A 对比样 )×100]

[0277] in

[0278...

Embodiment 2

[0285] Synergistic effect of melanin inhibition in vitro

[0286] The experimental process is described in Example 1. The results are shown in Table 2:

[0287] Table 2

[0288] melanin suppression

[0289]

[0290]

[0291] Synergy Index (SI) 1 Calculated according to the following Kull equation:

[0292] S I = C * D A + C * E B

[0293] in

[0294] A: Individual results for substance A

[0295] B: Individual results for substance B

[0296] C: Results of a mixture of A and B

[0297] D: Percentage of substance A in the mixture

[0298] E: Percentage of substance B in the mixture

[0299] Compared with the examples given in the literature, where A, B and C decreased values ​​(i.e. the minimum concentration of inhibition in the antimicrobial test) mean be...

Embodiment 3

[0302] In Vitro Skin Pigmentation

[0303] Pigmented pigskin was excised from animals (slaughtered for meat, as described in EP193927 for pigskin samples including sub-epidermal fat layer) and cut into 4x4x3mm pieces (lengthxwidthxthickness) and placed in soaking Air-liquid interface cultures on sterile cotton pads with 5 ml of custom-made DMEM (Dulbecco's Modified Eagle Medium). Sample at 37°C, 5% CO 2 Tested after 24 hours of acclimatization. O / W emulsions without (= control) and with test compound (described in more detail below) were applied topically And cultivated for 6 days. Tissue sections were prepared and pellets were melanin stained by the Fontana-Masson technique. Particles were quantified by image analysis. The results are shown in Tables 3.1 and 3.2.

[0304] chart 3.1

[0305] Pigmentation of sclareolide on skin in vitro

[0306] test substance

Dosage weight%

Melanin score compared to control

Sclareolactone

0.1％

-42％

...

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Abstract

Suggested is a composition comprising (a) sclareolide and (b1) at least one tyrosinase inhibitor; and / or (b2) at least one sun protection factor; and / or (b3) at least one anti-oxidants; and / or (b4) at least one anti-inflammatory agent; and / or (b5) at least one desquamating agent. on condition that compound a is present in an amount of from 0.00001 to 0.001 % b.w. - calculated on the total composition.

Description

field of invention [0001] The present invention relates to the field of cosmetics and relates to the use of sclareolide as a potent agent for lightening the skin and hair. Background technique [0002] Skin lightening active ingredients interfere with melanin metabolism or catabolism in various ways. Melanin, which is usually brown to black, is formed in the melanocytes of the skin and is transferred to the keratinocytes to give the skin or hair its melanin color. In mammals, brown-black eumelanins are mainly formed from hydroxyl-substituted aromatic amino acids such as L-tyrosine and levodopa (L-DOPA), and yellow-to-red pheomelanins are formed from sulfur-containing molecules. Starting from L-tyrosine, L-3,4-dihydroxyphenylalanine (L-DOPA) is formed by the copper-containing key enzyme tyrosinase, and in turn is converted to dopachrome by tyrosinase. Through a series of steps catalyzed by various enzymes, the latter is oxidized to form melanin. [0003] Skin lighteners ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61Q5/08A61Q19/02A61K8/49
CPCA61K8/4973A61K31/365A61Q5/00A61Q17/04A61Q19/00A61Q19/02A61K8/9789A61P17/16A61P19/00A61K8/31A61K8/33A61K8/34A61K8/342A61K8/35A61K8/37A61K8/44A61K8/492A61K8/498A61K8/58A61K8/602A61K8/675A61K8/922A61K2800/592A61Q5/08
Inventor 伊姆克·迈耶米丽娅姆·克努普费尔
Owner SYMRISE GMBH & CO KG
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