Uvasorb complete compositions, systems and methods

Abstract

Compositions, methods and systems relating to sunscreen active filter mixtures. In one exemplary embodiment, the invention includes a mixture, in solution form, including all or some of the following components: a UVB filter, a UVA filter, a UVA-UVB gap filter; and / or a vehicle for increasing stability and minimizing recrystallization of components.

Description

[0001] Attorney Docket No. 030146.00071

[0002] UVASORB COMPLETE COMPOSITIONS, SYSTEMS AND METHODS

[0003] CROSS-REFERENCE TO RELATED APPLICATIONS

[0004] This application is a PCT Application, which claims priority under 35 U.S.C. § 119 to U.S. Provisional Patent Application No. 63 / 697,605, filed September 23, 2024, the contents of which are incorporated by reference herein in its entirety.

[0005] FIELD

[0006] This invention relates to highly concentrated, soluble and SPF-tunable mixtures of organic sunscreen active UV filters in a preferred vehicle, stable for months. The mixtures can be used in sunscreen formulations using cold and hot-process manufacturing techniques.

[0007] BACKGROUND

[0008] Sunscreen cream and lotion formulations are typically oil-in-water (o / w) emulsions, where the oil phase acts not only as an emollient, such as in classic cream and lotions, but also as the main solvent used to dissolve organic filter active ingredients (e.g., UVA / UVB filters). Those organic filters have known different solubility and typically require considerable thermal energy in order to be dispersed and dissolved in the oil phase. This challenge precludes any so-called “cold-processing” method to produce a sunscreen lotion thus negatively impacting energy costs, manufacturing time, and the “green” environmental footprint.

[0009] Currently, the only cold process technically possible is one employing inorganic UV filters (zinc and titanium oxides). These types of filters limit overall outcome regarding sensorial preferences in sunscreens (for example, whitening, stickiness, poor spreadability).

[0010] Furthermore, the solubility of organic filters is often compromised by other ingredients of the formula leading to incomplete dissolution and recrystallization of the filter, with a resulting inhomogeneity of the final formula during manufacturing and / or during stability and usage.

[0011] Having a highly concentrated, liquid, stable organic UV filter mixture has proven to be a challenge because of recrystallization and / or poor solubility of the organic filters when used at the high concentrations necessary to have a suitable raw material for the production of cream and lotions with different SPF values.

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[0014] The vehicle compatibility with other cosmetic ingredients and with a positive effect on the final sensorial attributes is also of paramount importance for the compliance and the success of the final sunscreen formula. Skin feeling is reported as one of the main reasons people do not apply / reapply sunscreens or choose a different brand based on feeling during application.

[0015] Accordingly, additional cold processing methods and sunscreen mixtures having preferred sensorial attributes are needed.

[0016] SUMMARY

[0017] Described herein are compositions, methods and systems relating to sunscreen mixtures. In one exemplary embodiment, the compositions include mixtures, in solution form, that may include all or some of the following components:

[0018] A highly efficient UVB filter (such as Uvasorb HEB);

[0019] A UVA filter (such as DHHB, Diethylamino hydroxybenzoyl hexyl benzoate);

[0020] A UVA-UVB gap filter (such as Bemotrizinol); and / or

[0021] A vehicle (in one embodiment, ethylhexyl pelargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio between two or more of these solvents).

[0022] One feature of the present invention may include the use of a highly concentrated liquid organic UVA / UVB filter blend. This feature provides for an SPF -tunable ingredient for sunscreen formulation. In one aspect of the invention, the use of about 10% to about 35% w / w of this UVA / UVB blend, referred to herein as “UVASORB COMPLETE,” “as is” in the final formula may obtain an SPF 15 to SPF50-60 sunscreen (in-silico calculation).

[0023] UVASORB COMPLETE carries also an excellent emollient as its vehicle that is responsible for its pleasant sensoriality and that may reduce the necessity of loading other light emollients in the formulation.

[0024] Those of skill in the art can readily determine a suitable amount of UVASORB COMPLETE to produce a lotion or cream with a desired SPF value - it is understood that to achieve a higher SPF value, one would need to use more UVASORB COMPLETE than if a lower SPF value is desired. Typically, the amount of UVASORB COMPLETE is up to around 47% w / w.

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[0027] Another feature of the present invention may include the use of a UVA / UVB filter blend with the correct ratio between UVB and UVA protection, according to COLIPA requirements. In certain embodiments described herein, the compositions provide for complete protection from UVB and UVA, with a requested ratio of UVB / UVA=3, though deviations of plus or minus 10% from this ratio can also be used.

[0028] Still another feature of the present invention may include the use of a UVA / UVB filter blend in a liquid form of with very low viscosity. This feature allows the filter to be readily pumped / dosed into the formula reactor during manufacturing, saving time and removing dust formation, as well as the necessity of powder dispensing / dumping systems.

[0029] Yet another feature described herein involves using a UVA / UVB filter blend in a liquid form that allows for the formation of sunscreen lotions without any heating step, though if a heating step is performed, the compositions are still within the scope of the embodiments discussed herein. An aspect includes using a UVA / UVB filter blend that facilitates cold processing of sunscreen lotions or creams.

[0030] Another feature of the present invention may include the use of a highly concentrated liquid organic UVA, or UVB, or UVA-UVB gap-filler filters. An aspect of the invention provides for the use of about 10% to about 35% w / w of this liquid single filter “as is” in the final formula.

[0031] In one exemplary embodiment, the composition can include a vehicle for a mixture, that vehicle being in the form of a solvent. Most of the solvents commonly used in current cosmetic formulations of sunscreens, while being able to support high concentration of UV organic filters, fail during stability because of re-crystallization and / or precipitation.

[0032] Common ester solvents were tested by the present inventors, as they are used routinely in commercial formulas because of the acceptable skin feeling, and desirable chemical and solubilization properties. Surprisingly, a novel ester, ethylhexyl pelargonate was found to be a powerful solubilizer, with a pleasant skin feeling and an extended resistance to re-crystallization. The solution described in Example #5 herein shows that the stability of compositions including this solvent is greater than 1 year. Extended stability is ongoing.

[0033] Another embodiment of the compositions is using ethylhexyl perlargonate as a vehicle for a mixture. Ethylhexyl pelargonate’s lightness and spreadability attributes allows the creation of

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[0035] 204360301.V1 Attorney Docket No. 030146.00071 pleasant cream and lotions, enhancing the customer perception of a very easy to spread and light product. This solvent vehicle also mitigates the stickiness induced buy the organic UV filters. Further, this solvent vehicle may be synthetic or 100% natural from upcycled raw materials.

[0036] In another exemplary embodiment, the vehicle is neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, ethylhexyl perlargonate or a mixture in any ratio of two or more of these solvents.

[0037] As used herein, "consisting essentially of is a transitional phrase that defines the scope of the compositions described herein. It limits the claim to the specified elements and those that do not materially affect the basic and novel characteristics of the compositions. The characteristics of the compositions are that they are stable solutions, as opposed to water-containing emulsions that, overtime, lack the type of stability that maintains the UV organic filters in the emulsion, such that they re-crystallize and / or precipitate. In one embodiment, the solutions are stable (i.e., no significant re-crystallization and / or precipitation of the UV organic filters in a month or more, three months or more, six months or more, or one year or more, where significant refers to no more than 5%, no more than 10%, no more than 15%, or no more than 20% of the UV organic filters). By way of example, addition of sufficient water to the organic solutions, such that would be present in an emulsion, materially affects the characteristics of the organic solutions described herein, as solutions and emulsions are entirely different compositions. They have significantly different properties, including but not limited to differences in shelf stability.

[0038] Other aspects and advantages of the invention will become apparent from a review of the detailed description below.

[0039] DETAILED DESCRIPTION

[0040] Embodiments described herein can be understood more readily by reference to the following detailed description, examples, and claims. Elements, components and methods described herein, however, are not limited to the specific embodiments presented in the detailed description, examples, and claims. In particular, these embodiments are merely illustrative of the principles of the present invention. Accordingly, this disclosure is not intended to embrace all such alternatives, modifications and variations that fall within the spirit and broad scope of the

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[0042] 204360301.V1 Attorney Docket No. 030146.00071 specification and in view of the claims.

[0043] All publications, patents and patent applications mentioned in this specification are incorporated herein in their entirety by reference, to the same extent as if each individual publication, patent, or patent application was specifically and individually indicated to be incorporated herein by reference. In addition, citation or identification of any reference in this application shall not be construed as an admission that such reference is available as prior art to the present invention. To the extent that section headings are used, they should not be construed as necessarily limiting.

[0044] In addition, all ranges disclosed herein are to be understood to encompass any and all subranges subsumed therein. For example, a stated range of “1.0 to 10.0” should be considered to include any and all subranges beginning with a minimum value of 1.0 or more and ending with a maximum value of 10.0 or less, e.g., 1.0 to 5.3, or 4.7 to 10.0, or 3.6 to 7.9. All ranges disclosed herein are also to be considered to include the end points of the range, unless expressly stated otherwise. For example, a range of “between 5 and 10,” from 5 to 10,” or “5-10” should generally be considered to include the end points 5 and 10.

[0045] Further, when the phrase “up to” is used in connection with an amount or quantity, it is to be understood that the amount is at least a detectable amount or quantity. For example a material present in an amount “up to” a specified amount can be present from a detectable amount and up to and including the specified amount.

[0046] Additionally, in any disclosed embodiment, the terms “substantially,” “approximately,” and “about” may be substituted with “within [a percentage] of’ what is specified, where the percentage includes 0.1, 1, 5, and 10 percent.

[0047] It is also to be understood that the article “a” or “an” refers to “at least one,” unless the context of a particular use requires otherwise.

[0048] 1. Sunscreen Compositions

[0049] In one embodiment, the sunscreen compositions are a mixture comprising sunscreens and various additional components. In one exemplary embodiment, the mixture comprises the following components:

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[0052] A highly efficient UVB filter (for example, Uvasorb HEB);

[0053] A UVA filter (for example, DHHB, Diethylamino hydroxybenzoyl hexyl benzoate):

[0054] A UVA-UVB gap filter (such as Bemotrizinol, also known as Tinosorb S or Bis- Ethylhexyloxyphenol Methoxyphenyl Triazine): and / or

[0055] A vehicle (such as ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol di capryl ate / di caprate, or a mixture in any ratio of two or more of these solvents).

[0056] UVAsorb HEB, also known as Iscotrizinol or Diethylhexyl Butamido Triazone, is a UVB sunscreen agent that is also effective against some UVA rays. It is an oil-soluble chemical sunscreen. The chemical formula for Iscotrizinol is shown below:

[0057] In some embodiments, one or more preservatives and / or fragrances are present in the compositions.

[0058] Representative preservatives include but are not limited to phenoxyethanol, parabens, and disodium EDTA. These preservatives can help prevent bacterial and fungal growth, extend shelf life, and maintain product stability. The preservatives are typically present in a range of about 0.1 to about 2% w / w.

[0059] Sunscreen products often include, as a fragrance, the scent of cocoa butter, coconut oil and / or jasmine, though other fragrances can be present. The amount of fragrance in sunscreen varies significantly, but is typically in the range of from about 0.3% and about 0.8%.

[0060] II . Methods of Making Sunscreen Compositions

[0061] The mixtures described herein can be prepared using a process comprising the steps of:

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[0063] 204360301.V1 Attorney Docket No. 030146.00071 a) Providing an appropriate amount of a vehicle (about 50% to about 70% w / w) that is put in a vessel and heated to about 80°C. b) Adding bemotrizinol at a concentration of between about 10% and about 20% w / w and waiting until dissolution; c) Adding di ethylamino hydroxybenzoyl hexyl benzoate at 0% to about 10% w / w and allowing to dissolve; and d) Adding Uvasorb HEB at about 20% to about 30% w / w and allowing to dissolve completely.

[0064] In one aspect of the above embodiment, the resulting solution is clear and stable for at least 1 year without sign of recrystallization. Should minor recrystallization occur over a long term, the crystals can be easily reverted (i.e. crystals quickly solubilize) with mild warming step of heating up to 40°C-50°C.

[0065] In another exemplary embodiment, the present invention may include a method for making a mixture, including the steps of: a) Providing an appropriate amount of vehicle (about 60% to about 70% w / w) in a vessel and heating to about 60°C; and b) Adding bemotrizinol at about 30% to about 40% w / w and waiting until dissolution.

[0066] In another exemplary embodiment, the present invention may include a method for making a mixture, including the steps of: a) Proving an appropriate amount of vehicle (about 60% to about 70% w / w) in a vessel and heating to about 60°C; and b) Adding diethylamino hydroxybenzoyl hexyl benzoate at about 30% to about 40% w / w and waiting until dissolution.

[0067] In another exemplary embodiment, the method includes the steps of: a) Proving an appropriate amount of vehicle (about 60% to about 70% w / w) in a vessel and heating to about 80°C; and b) Adding Uvasorb HEB at about 30% to about 40% w / w and waiting until dissolution.

[0068] Some embodiments described herein are further illustrated in the following non-limiting examples.

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[0071] EXAMPLES

[0072] Example#!

[0073] An appropriate amount of vehicle (isononyl isononanoate) (50% - 70% w / w) was put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and wait till dissolution; then Di ethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% w / w and allowed to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% w / w and allowed to dissolve completely.

[0074] Solution is heavily re-crystallizing / precipitating after 1 month, room temperature.

[0075] Example#2

[0076] An appropriate amount of vehicle (C12-15 alkyl benzoate) (50% - 70% w / w) is put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and allowed to dissolve; then Diethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% w / w and allowed to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% w / w and allowed to dissolve completely.

[0077] Solution is re-crystallizing / precipitating after 1 month, room temperature.

[0078] Example#3

[0079] An appropriate amount of vehicle (Capric / Caprylic Triglycerides) (50% - 70% w / w) is put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and allowed to dissolve; then Diethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% w / w and allowed to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% w / w and allowed to dissolve completely.

[0080] Solution is re-crystallizing / precipitating after 1 month, room temperature.

[0081] Example#4

[0082] An appropriate amount of vehicle (Octyl Palmitate) (50% - 70% w / w) is put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and allowed to dissolve; then Diethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% w / w and allowed to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% w / w and let to dissolve completely.

[0083] Solution is re-crystallizing / precipitating after 3 months, room temperature.

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[0086] Example#5

[0087] An appropriate amount of vehicle (EthylHexyl Pelargonate) (50% - 70% w / w) is put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and allowed to dissolve; then Diethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% w / w and allowed to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% w / w and allowed to dissolve completely.

[0088] Solution is stable after 12 months, room temperature.

[0089] Example#6

[0090] An appropriate amount of vehicle (Neopentyl Glycol Diheptanoate) (50% - 70% w / w) is put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and wait till dissolution; then Diethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% and let to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% and let to dissolve completely.

[0091] Solution is stable after 6 months, room temperature.

[0092] Example#7

[0093] An appropriate amount of vehicle (ethylhexyl perlargonate, or neopentyl glycol diheptanoate, or propylene glycol dicaprylate / dicaprate, or a mixture in any ratio between these solvents) (50% - 70% w / w) is put in a vessel and heated to 80°C. Bemotrizinol is added at a 10% to 20% w / w and allowed to dissolve; then Diethylamino hydroxybenzoyl hexyl benzoate is added at 0% to 10% w / w and allowed to dissolve. Lastly, Uvasorb HEB is added at 20% to 30% w / w and allowed to dissolve completely.

[0094] Solution is stable after 6 months, room temperature.

[0095] It is understood that the disclosure provides compositions and methods that can be used in a variety of applications and fields without limitation, for instance, in the cosmetic and / or pharmaceutical industry.

[0096] Those skilled in the art will appreciate that many modifications and substitutions may be made to the foregoing description without departing from the spirit and scope of the present disclosure.

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Claims

Attorney Docket No. 030146.00071WHAT IS CLAIMED IS:

1. A stable, highly concentrated solution comprising: a UVAB-UVA organic filter in a vehicle, wherein the UVAB-UVA organic filter comprises between about 20% and about 30% Uvasorb HEB w / w, between about 10% and about 15% bemotrizinol w / w, and between about 0% to about 10% DHHB w / w.

2. The solution of claim 1, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio of two or more of these solvents.

3. A stable, highly concentrated solution comprising: a UVB-UVA gap filler organic filter in a vehicle, the UVB-UVA gap filler organic filter comprising between about 30% and about 40% Bemotrizinol w / w.

4. The solution of claim 3, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio of two or more of these solvents.

5. A stable, highly concentrated solution comprising: a UVA organic filter in a vehicle, wherein the UVA organic filter comprises between about 30% to about 40% diethylamino hydroxybenzoyl hexyl benzoate w / w.

6. The solution of claim 5, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio of two or more of these solvents.

7. A stable, highly concentrated solution comprising: a UVB organic filter in a vehicle, wherein the UVB organic filter comprises between about 30% and about 40% Uvasorb HEB w / w.10204360301.V1Attorney Docket No. 030146.000718. The solution of claim 7, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio of two or more of these solvents.

9. A vehicle to keep organic UV filters in solutions over longer period of time without recrystallization / precipitation at high concentration, with enhanced sensorial attributes and acceptance for cosmetic industry comprising: a solvent selected from the group consisting of ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, and mixtures thereof.

10. A solution consisting essentially of: a UVAB-UVA organic filter in a vehicle, the UVAB-UVA organic filter comprising about 20% to about 30% Uvasorb HEB w / w, about 10% to about 15% bemotrizinol w / w, and from 0% to about 10% DHHB w / w.

11. The solution of claim 10, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, a mixture in any ratio of two or more of these solvents.

12. A solution consisting essentially of: a UVB-UVA gap filler organic filter in a vehicle, wherein the UVB-UVA gap filler organic filter comprises between about 30% and about 40% Bemotrizinol w / w.

13. The solution of claim 12, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio of two or more of these solvents.

14. A solution consisting essentially of: a UVA organic filter in a vehicle, the UVA organic filter constituted by about 30% to about 40% diethylamino hydroxybenzoyl hexyl benzoate w / w.11204360301.V1Attorney Docket No. 030146.0007115. The solution of claim 14, wherein the vehicle is ethylhexyl perlargonate, or neopentyl glycol diheptanoate, or propylene glycol di capryl ate / di caprate, or a mixture in any ratio of two or more of these solvents.

16. A stable, highly concentrated solution consisting essentially of: a UVB organic filter in a vehicle, the UVB organic filter constituted by about 30% to about 40% Uvasorb HEB w / w.

17. The solution of claim 16, wherein the vehicle is ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, or a mixture in any ratio of two or more of these solvents.

18. A solution consisting essentially of one or more UV filters and one or more solvents selected from the group consisting of ethylhexyl perlargonate, neopentyl glycol diheptanoate, propylene glycol dicaprylate / dicaprate, and mixtures thereof.12204360301.V1

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