NON-THERAPEUTIC ORAL USE OF A COMPOSITION FOR WHITENING AND/OR LIGHTENING THE SKIN COMPRISING CYSTINE AND GLUTATHIONE IN A CYSTINE-GLUTATHIONE RATIO RANGING FROM 1.5 TO 4

20220016005 · 2022-01-20

Assignee

Inventors

Cpc classification

International classification

Abstract

The non-therapeutic, cosmetic, oral use of a composition as an active ingredient for whitening and/or lightening the skin and/or depigmenting the skin, in particular for reducing the size of brown spots, including at least cystine and glutathione in a cystine/glutathione ratio ranging from 1.5 to 4, the composition advantageously further comprising glycine and/or glutamine Preferably, the composition also includes at least one component selected from the group formed by zinc or one of its salts, copper or one of its salts, selenium or one of its salts, vitamins B, in particular B3, B5, B6 and/or B8, vitamin E, melon juice extracts, horsetail extracts and mixtures of these components.

Claims

1-15. (canceled)

16. A non-therapeutic, cosmetic, oral composition for whitening and/or lightening the skin and/or depigmenting the skin, comprising at least cystine and glutathione in a cystine/glutathione ratio ranging from 1.5 to 4.

17. The composition according to claim 16, wherein the amount of cystine in said composition is from 30 to 60% by weight based on the total weight of said composition.

18. The composition according to claim 16, wherein the cystine comprises less than 5 ppm of heavy metals.

19. The composition according to claim 16, wherein the amount of glutathione ranges from 10 to 30% by weight based on the total weight of said composition.

20. The composition according to claim 16, wherein the composition comprises glycine in a cystine/glycine ratio of from 7 to 9.5.

21. The composition according to claim 16, wherein the composition comprises glutamine in a cystine/glutamine ratio of from 3.5 to 5.0.

22. The composition according to claim 16, wherein the composition comprises calcium ascorbate in a cystine to calcium ascorbate ratio of from 3.5 to 5.5.

23. The composition according to claim 16, wherein the composition comprises at least one component selected from the group consisting of zinc or one of its salts, copper or one of its salts, selenium or one of its salts, one or more B vitamins, vitamin E, melon juice extracts, horsetail extracts and mixtures thereof.

24. The composition according to claim 16, wherein the composition comprises glycine in a cystine/glycine ratio of from 7 to 9.5, glutamine in a cystine/glutamine ratio of from 3.5 to 5.0, and calcium ascorbate in a cystine to calcium ascorbate ratio of from 3.5 to 5.5.

25. The composition according to claim 16, wherein the composition does not comprise gooseberry extract.

26. A method of preparing the composition used according to claim 24, comprising the following steps: providing cystine; providing glutathione; providing glycine; providing glutamine; providing calcium ascorbate; optionally providing at least one component selected from the group consisting of zinc or one of its salts, copper or one of its salts, selenium or one of its salts, B vitamins, vitamin E, melon juice extracts, horsetail extracts, and mixtures thereof; and mixing the cystine, the glutathione, the glycine, the glutamine, the calcium ascorbate and, optionally, the at least one component.

27. A non-therapeutic, cosmetic method for whitening and/or lightening and/or depigmenting the skin, comprising a step of administering to an individual orally a composition comprising at least cystine and glutathione in a cystine/glutathione ratio ranging from 1.5 to 4.

28. The method according to claim 27, wherein, the following daily doses of active material are administered: cystine in a content ranging from 0.001 to 2 g; glutathione in a content ranging from 0.001 to 1 g; glycine in a content ranging from 0.001 to 1 g; glutamine in an amount of 0.001 to 1 g; and calcium ascorbate in an amount of 0.001 to 1 g.

29. The method according to claim 27, wherein the following daily doses are administered: vitamin B3 in a content corresponding to a content ranging from 0.01 to 0.03 g of nicotinamide; vitamin B5 in a content corresponding to a content ranging from 0.010 to 0.015 g of calcium pantothenate; vitamin B6 in a content corresponding to a content ranging from 0.001 to 0.005 g of pyridoxine hydrochloride; vitamin B8 in a content corresponding to a content ranging from 0.0001 to 0.0005 g of biotin; zinc or a salt thereof in a zinc content of from 0.005 to 0.015 g; copper or a salt thereof in a copper content of from 0.001 to 0.002 g; vitamin E in a content corresponding to a content of from 0.005 to 0.1 g; melon juice extract in a content of from 0.005 to 0.015 g; and horsetail extract in a content of from 0.001 to 0.01 g.

30. A non-therapeutic, cosmetic method according to claim 27 for reducing the size of pigmentary brown spots.

Description

EXAMPLES

[0130] I/Compositions

[0131] A composition A according to the invention and a comparative composition B, both in capsule form, are prepared.

[0132] In table 1, the ingredients of composition A in mg, the percentage by weight of the ingredients in composition A, and the ingredients of composition B in mg are shown respectively.

[0133] To prepare compositions A and B, the ingredients are weighed and mixed at room temperature. The compositions A and B prepared in this way are stable and are put into capsules.

TABLE-US-00001 TABLE 1 Composition A Comparative according to the of weight in composition Ingredients invention in mg composition A B in mg L-Cystine 250.00 40.19 250.00 L-Glutathione 125.00 20.10 — L-Glutamine 60.00 9.65 60.00 Glycine 30.00 4.82 30.00 Vitamin E a.i. 50% 15.00 2.41 15.00 Calcium ascorbate 55.00 8.84 55.00 Melon juice 10.00 1.61 10.00 concentrate Dry extract of horsetail 5.00 0.80 5.00 aerial parts Cu-amino acid chelate 7.49 1.20 7.49 a.i. 10% Zn-amino acid chelate 24.99 4.02 24.99 a.i. 20% Se-amino acid chelate 3.50 0.56 3.50 a.i. 1% Vitamin B3 8.91 1.43 8.91 Vitamin B5 (Calcium 6.00 0.97 6.00 Pantothenate) Vitamin B6 1.05 0.17 1.05 (pyridoxine hydrochloride) Vitamin B8 (biotin) 0.15 0.02 0.15 Magnesium stearate 19.91 3.20 13.92 Maltodextrin — — 130.99 Capsule 118.00 0 118 Total ingredients + 740 100 740 capsule

[0134] Two other compositions were prepared: the placebo C and the comparative composition D presented below

[0135] Placebo C

[0136] The placebo C composition included 622 mg of magnesium stearate in a 118 mg capsule.

[0137] Composition D

[0138] Composition D comprising the following ingredients shown in Table 2 is prepared by mixing the ingredients at room temperature.

TABLE-US-00002 TABLE 2 Composition A Comparative according to the of weight in composition B Ingredients invention in mg composition A in mg L-Cystine 250.00 40.19 250.00 L-Glutathione 125.00 20.10 — L-Glutamine 60.00 9.65 60.00 Glycine 30.00 4.82 30.00 Vitamin E a.i. 50 % 15.00 2.41 15.00 Calcium ascorbate 55.00 8.84 55.00 Melon juice 10.00 1.61 10.00 concentrate Dry extract of horsetail 5.00 0.80 5.00 aerial parts Cu-amino acid chelate 7.49 1.20 7.49 a.i. 10% Zn-amino acid chelate 24.99 4.02 24.99 a.i. 20% Se-amino acid chelate 3.50 0.56 3.50 a.i. 1% Vitamin B3 8.91 1.43 8.91 Vitamin B5 (Calcium 6.00 0.97 6.00 Pantothenate) Vitamin B6 1.05 0.17 1.05 (pyridoxine hydrochloride) Vitamin B8 (biotin) 0.15 0.02 0.15 Magnesium stearate 19.91 3.20 13.92 Maltodextrin — — 130.99 Capsule 118.00 0 118 Total ingredients + 740 100 740 capsule

[0139] II/Measurements of the Activity of the CVompositions

[0140] The daily amounts shown in Table 3 were administered to each subject for 90 days.

TABLE-US-00003 TABLE 3 L-Cystine L-Glutathione L-Cysteine in mg in mg in mg Composition A according to the 500 250 — invention (2 capsules per day) Composition C Placebo (2 — — — capsules per day) Comparative composition B 500 (2 capsules per day) Comparative composition D (1 — 250 100 capsule per day)

[0141] The study was conducted on 120 subjects, double-blind, randomized: 30 subjects were given composition A, 30 subjects were given composition B, 30 subjects were given composition C and 30 subjects were given composition D.

[0142] The compositions were administered for 90 days.

[0143] Topics

[0144] The subjects selected met the following criteria: [0145] healthy subjects, [0146] age between 30 and 50 years, [0147] light skin corresponding to phototypes III and IV on the Fitzpatrick scale and presenting one or more brown spots on the face, i.e. at least one spot whose smallest dimension was at least 2.5 mm in diameter.

[0148] Skin colour was assessed spectrophotometrically using a CM 700D spectrophotometer/colourimeter (Konica-Minolta) by measuring the L*a*b* values and calculating the Individual Typology Angle (ITA) value.

[0149] The L* parameters of the ITA are used to measure the whitening/lightening of the skin.

[0150] Assessment of brown spot reduction was performed by measuring spot size on cross-polarized digital photographs.

[0151] Measurements were taken at D=0, D 45 (after 45 days of treatment) and D 90 (after 90 days of treatment).

[0152] Table 4 presents the evolution of each criterion (in %) compared to the beginning of the study at D0 and for each composition.

TABLE-US-00004 TABLE 4 Composition Composition Composition Placebo C comp. B comp. D A (2 capsules (2 capsules (2 capsules (1 capsule per day) per day) per day) per day) Brown spot −16.2%*.sup.∧ +4.3% +1.4% −4.4% size.sup.(1) at D 45 Brown spot −34.4%*.sup.∧ +4.4% +4.8% −3.6% size.sup.(1) at D 90 ITA measured  +2.2% −3.5% −1.8% −1.0% on the cheek.sup.(2) at D 45 ITA measured  +8.7%*.sup.∧ +0.5% −0.8% −1.0% on the cheek.sup.(2) at D 90 L*measured on  +0.6% −0.1% −0.1% +0.3% the cheek.sup.(3) at D 45 L* measured  +1.8%*.sup.∧ +0.4% −0.1% +0.1% on the cheek.sup.(3) at D 90 ITA measured  +5.1%* −2.6% −2.0% −1.1% on the wrist.sup.(2) at D 45 ITA measured  +6.7%* −0.7% +3.9% +2.0% on the wrist.sup.(2) at D 90 L*measured on  +0.8% −0.4% −0.5% −0.3% the wrist.sup.(3) at D 45 L* measured  +1.1%* −0.1% +0.4%   0.0% on the wrist.sup.(3) at D 90 .sup.(1)measurement of the evolution in % of the surface (mm2) of the brown spots, .sup.(2)measurement of the evolution of the individual typology angle ITA, .sup.(3)measurement of the evolution of the clarity L*, *statistically significant change compared to D0, .sup.∧the variations observed with composition A are significantly different from those observed with the 3 other compositions.

[0153] The composition according to the invention allows a significant reduction in the size of brown spots (−16.2% at 45 days and −34.4% at 90 days), part of the spots are no longer visible, the skin appears more even.

[0154] It also allows an increase in skin lightening/whitening measured by an increase in the L* parameter on both the cheek (+0.6% at 45 days and +1.8% at 90 days), and the wrist (+0.8% at 45 days and +1.1% at 90 days), and a significant increase in the ATI° on both the cheek (+2.2% at 45 days and +8.7% at 90 days) and the wrist (+5.1% at 45 days and +6.7% at 90 days)

[0155] The proportion of subjects showing a reduction in the surface area of brown spots at 90 days is 87% with composition A according to the invention, this value is high and significantly different from those obtained with the placebo composition C (40%), with composition B (50%) and with composition D (39%).

[0156] Similarly, the proportion of subjects showing skin lightening/whitening at 90 days with an increase in the ITA value on the cheek is 77%, which is significantly higher than those of the placebo composition C (43%), B (47%) and D (39%).

[0157] There is also a whitening/lightening effect on brown spots