GB2618220A - Retinol compositions, methods of their preparation and use - Google Patents

Retinol compositions, methods of their preparation and use Download PDF

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Publication number
GB2618220A
GB2618220A GB2307416.4A GB202307416A GB2618220A GB 2618220 A GB2618220 A GB 2618220A GB 202307416 A GB202307416 A GB 202307416A GB 2618220 A GB2618220 A GB 2618220A
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composition
retinol
skin
combinations
ingredient
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GB202307416D0 (en
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Ovenell Toni
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Int Waters Pty Ltd T/a Alpha H
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Int Waters Pty Ltd T/a Alpha H
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Priority claimed from AU2020903892A external-priority patent/AU2020903892A0/en
Application filed by Int Waters Pty Ltd T/a Alpha H filed Critical Int Waters Pty Ltd T/a Alpha H
Publication of GB202307416D0 publication Critical patent/GB202307416D0/en
Publication of GB2618220A publication Critical patent/GB2618220A/en
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    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
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Abstract

A composition including 0.01-0.2% w/w retinol, 5-20% w/w alpha hydroxy acid, at least one emollient, at least one aqueous solvent, at least one emulsifying agent, at least one antioxidant, optionally at least one emulsion stabiliser, and optionally at least one skin conditioning agent, wherein the composition has a pH of 3.5 to 4.5.

Claims (52)

1. A composition including 0.01-0.2% w/w one or more retinol ingredient, 5-20% w/w one or more alpha hydroxy acid, at least one emollient, at least one aqueous solvent, at least one emulsifying agent, at least one antioxidant, optionally at least one emulsion stabiliser, and optionally at least one skin conditioning agent, wherein the composition has a pH of 3.5 to 4.5.
2. The composition of claim 1 , wherein the pH is 3.9 to 4.1 , preferably the pH is about 4.
3. The composition of claim 1 or claim 2, wherein the one or more retinol ingredient is hydroxypinacolone retinoate, retinol, retinyl acetate, retinyl linoleate, retinyl palmitate, retinyl proprionate, or combinations thereof.
4. The composition of any one of the preceding claims, wherein the one or more retinol ingredient is hydroxypinacolone retinoate, retinol, or combinations thereof.
5. The composition of any one of the preceding claims, wherein the one or more retinol ingredient is hydroxypinacolone retinoate, retinyl palmitate, retinyl propionate, retinol, or combinations thereof.
6. The composition of any one of the preceding claims, wherein the alpha hydroxy acid is glycolic acid.
7. The composition of any one of the preceding claims, wherein the one or more retinol ingredient is 0.07-0.15% w/w of the composition, preferably is about 0.1% w/w of the composition.
8. The composition of any one of the preceding claims, wherein the composition is 12-16% w/w of one or more alpha hydroxy acid, preferably the composition is about 14% w/w of one or more alpha hydroxy acid
9. The composition of any one of the preceding claims, wherein the at least one emollient is 8-15% w/w of the composition and optionally selected from the group consisting of glycerin, dimethocone, dicaprylyl carbonate, helianthus annuus seed oil, hippophae rhamnoides fruit extract and combinations thereof. Optionally, at least one emollient comprises all of the group consisting of glycerin, dimethocone, dicaprylyl carbonate, helianthus annuus seed oil, and hippophae rhamnoides fruit extract.
10. The composition of any one of the preceding claims, wherein the aqueous solvent is water and the water is 40-70% w/w of the composition, preferably the composition is about 55% w/w water.
11. The composition of any one of the preceding claims, wherein the at least one emulsifying agent is 1.0-2.5% w/w of the composition, preferably about 2% w/w of the composition.
12. The composition of any one of the preceding claims, wherein at least one emulsifying agent is selected from the group consisting of cetyl alcohol, glyceryl stearate, PEG-100 stearate, and combinations thereof.
13. The composition of any one of the preceding claims, wherein the at least one antioxidant is optionally 0.5-2.0% w/w of the composition, preferably about 0.6% w/w.
14. The composition of any one of the preceding claims, wherein the at least one antioxidant is selected from the group consisting of ubiquinone (coenzyme Q10), ferulic acid, Tasmannia lanceolata fruit/leaf extract, and combinations thereof.
15. The composition of any one of the preceding claims, wherein the at least one emulsion stabiliser is 0.5-1 .5% w/w of the composition, preferably about 1 % w/w of the composition.
16. The composition of any one of the preceding claims, wherein the at least one emulsion stabiliser is sodium polyacryloyldimethyl taurate.
17. The composition of any one of the preceding claims, wherein the at least one skin conditioning agent is about 12-17% w/w of the composition.
18. The composition of any one of the preceding claims, wherein the at least one skin conditioning agent is selected from the group consisting of palmitoyl tripepetide-5, hydrolysed jojoba esters, tocopherol, hibiscus sabdariffa flower extract, ammonium glycyrrhizate, sodium hyaluronate, butylene glycol, propanediol and combinations thereof.
19. A composition including: - 0.05-0.2% w/w (preferably 0.1 % w/w) one or more retinol ingredient; or 0.5-2.0% w/w (preferably 1.0% w/w) of a retinol composition comprising 10% one or more retinol ingredient in 90% dimethyl isosorbide, - 10-20% w/w (preferably 14% w/w) one or more alpha hydroxy acid, - 0.001-0.003% w/w (preferably 0.002%) palmitoyl tripepetide-5, - 0.5-2.0% w/w (preferably 0.6%) of at least one antioxidant selected from ubiquinone (coenzyme Q10), ferulic acid, Tasmannia lanceolata fruit/leaf extract, and combinations thereof, - 8-15% w/w (preferably 10-11 % w/w) of at least one emollient, - 1.0-2.5% (preferably 2%) of at least one emulsifying agent, - 0.5-1.5% w/w of at least one emulsion stabiliser - at least one aqueous solvent; and - at least one skin conditioning agent, wherein the composition has a pH of 3.9 to 4.1 (preferably, the pH is about 4).
20. The composition of claim 19, wherein the at least one antioxidant includes: - 0.5-1.5% w/w (preferably 1 % w/w) Tazman Pepper (70% water, 28% glycerin and 2% Tasmannia lanceolata fruit/leaf extract), - 0.005-0.15% w/w (preferable 0.1% w.w) ubiquinone, and - 0.3-0.7% w/w (preferably 0.5% w/w) ferulic acid.
21. The composition of claim 19 or claim 20, wherein the at least one emollient is selected from glycerin, dimethocone, dicaprylyl carbonate, helianthus annuus seed oil, hippophae rhamnoides fruit extract, and combinations thereof.
22. The composition of any one of claims 19-21 , wherein the at least one emulsifying agent selected from cetyl alcohol, glyceryl stearate, PEG-100 stearate, and combinations thereof.
23. The composition of any one of claims 19-22, wherein the at least one emulsion stabiliser selected from sodium polyacryloyldimethyl taurate.
24. The composition of any one of claims 19-23, wherein the at least one aqueous solvent is 50-60% w/w of the composition (preferably about 55% w/w).
25. The composition of any one of claims 19-23, wherein the at least one skin conditioning agent selected from palmitoyl tripepetide-5, hydrolysed jojoba esters, tocopherol, hibiscus sabdariffa flower extract, ammonium glycyrrhizate, sodium hyaluronate, butylene glycol, propanediol and combinations thereof.
26. The composition of any one of claims 19-23, wherein the at least one skin conditioning agent is 5-20% w/w (preferably 12-17% w/w of the composition).
27. The composition of any one of claims 19-23, wherein 90, 95, 98, 99 or 99.5% w/w of the one or more retinol ingredient added to the composition remains retinol ingredient following preparation of the composition.
28. The composition of any one of claims 19-23, wherein 70, 80, 85 or 90% w/w of the one or more alpha hydroxy acid added to the composition remains alpha hydroxy acid following preparation of the composition.
29. The composition of any one of claims 19-23, wherein the composition is stored in an opaque inert packaging and 70, 80, 85, 90, 95, or 98% w/w of the one or more retinol ingredient added to the composition remains retinol ingredient following storage of the composition in its packaging at room temperature and relative humidity for 90 days.
30. The composition of any one of claims 19-23, wherein the composition is stored in an opaque inert packaging and 70, 80, 85 or 90% w/w of the one or more alpha hydroxy acid added to the composition remains alpha hydroxy acid following storage of the composition in its packaging at 40 +/- 2 °C at 75% relative humidity for 90 days. 39
31. The composition of any one of claims 19-23, wherein the composition is stored in an opaque inert packaging and at least 70% w/w (preferably at least 75% w/w) of the one or more retinol ingredient added to the composition remains retinol ingredient following storage of the composition in its packaging at room temperature and standard relative humidity for 12 months.
32. The composition of any one of claims 19-23, wherein the composition is stored in an opaque inert packaging and at least 70% w/w (preferably at least 80% w/w) of the one or more alpha hydroxy acid added to the composition remains alpha hydroxy acid following storage of the composition in opaque inert packaging at room temperature and standard relative humidity for 12 months.
33. A method of exfoliating the skin comprising application of a composition according to any one of claims 1-32 to the skin.
34. A method of exfoliating the skin and one or more of (i) skin lightening by breaking down of hyperpigmentation, (ii) reducing of pore numbers and/or pore size, (iii) improving the skin's texture, (iv) increasing collagen and/or elastin production in the skin, (v) reducing fine lines and/or wrinkles, (vi) reducing sebum production, (vii) improving acne breakouts and blemishes, (viii) increasing hydration and/or a plumping the skin comprising application of a composition according to any one of claims 1-30 to the skin.
35. The method of claim 33 or claim 34, wherein 0.3 ml of the composition is applied to the face, neck, decolletage and/or scalp.
36. The method of any one of claim 33-35, wherein the composition is applied once per day.
37. The method of any one of claim 33-36, wherein the composition has similar irritation levels to the use of the same composition containing no retinol.
38. The method of any one of claim 33-37, wherein the method results in exfoliation of the skin that is 30%, 40% or 50% faster than natural exfoliation of the skin.
39. A method of preparing the composition according to any one of claims 1-32 comprising: 40 (i) combining the one or more alpha hydroxy acid and the at least one aqueous solvent and, if needed, adjusting the pH to 3.8-4.2 using a pH adjuster; (ii) optionally combining the mixture prepared in step (i) with one or more water soluble emollients, one or more skin conditioning agents, one or more humectants, or combinations thereof; (iii) combining the at least one emulsifying agent, at least one oil phase emollient, and optionally at least one emulsion stabiliser with the mixture prepared in step (ii) and homogenising; (iv) combining the one or more antioxidants, one or more retinol ingredient, and optionally one or more heat or shear sensitive ingredients such as skin conditioning agents into the mixture prepared in step (iii); (v) if needed, adjusting the pH to 3.8-4.2 using a pH adjuster.
40. The method of claim 39, wherein the mixture is heated to 60-80 °C (preferably about 70 °C) after step (i) and then cooled after step (iii) 45 °C or less (preferably about 40 °C).
41. The method of claim 39 or claim 40, wherein the heat or sheer sensitive skin conditioning agents added in step (iv) are one or more of tocopherol, hibiscus sabdariffa flower extract, and palmitoyl tripepetide-5.
42. The method of any one of claims 39-41 , wherein one or more of glycerin, butylene glycol, propanediol and sodium hyalonurate are combined with mixture (i) in step (ii).
43. The method of claim 41 , wherein following the inclusion of the one or more of glycerin, butylene glycol, propanediol and hyaluronic acid, one or more humectant is added to the mixture.
44. The method of claim 43, wherein the humectant is methyl gluceth-20.
45. The method of claim 43 or claim 44, wherein humectant is added with one or more skin conditioner, preferably, ammonium glycyrrhizate. 41
46. The method of any one of claims 39-45, wherein the at least one emulsifying agent and at least one oil phase emollient are combined before mixing with mixture of step (ii).
47. The method of claim 46, wherein the at least one emulsifying agent and at least one oil phase emollient are heated to 60-80 °C (preferably about 70 °C) before combining with the mixture of step (ii).
48. The method of any one of claims 39-47, wherein the at least one oil phase emollient is dimethicone and/or dicaprylyl carbonate.
49. The method of any one of claims 39-48, wherein the at least one emulsifying agent and at least one oil phase emollient is added to the mixture of step (ii) and homogenised, then the emulsion stabiliser is added to the mixture and the mixture homogenised again.
50. The method of claims 49, wherein the emulsion stabiliser is combined to the mixture with the emollients helianthus annuus seed oil, and/or hippophae rhamnoides fruit extract, and/or the skin conditioner hydrolysed jojoba esters.
51. The method of any one of claims 39-50, wherein homogenisation is for 5 minutes.
52. The method of any one of claims 39-50, wherein the one or more retinol ingredient is the final ingredient added to the composition before the final pH adjustment.
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