Photoprotective system

Abstract

The present invention concerns a topical, cosmetic or pharmaceutical preparation containing a combination of 3 or 4 solar filters comprising:—one or two UVA filters to obtain a critical wavelength>370 nm, chosen from among: (i)—5,6,5,6-tetraphenyl-3, 3′-(1,4-phenylene)-bis[1,2,4]triazine; (ii) 1,1′-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl]phenyl]-methanone; (iii)—Butyl Methoxydibenzoylmethane (BMDBM), in a quantity less than 2% by weight with regard to the total weight of said composition; (iv)—Hexyl-[4-(diethylamino)-2-hydroxybenzoyl]benzoate, -2,4-Bis[4-(2-ethyl-hexyloxy)-2-hydroxyphenyl]-6-(4-methoxyphenyl)-1,3,5-triazine=(BEMT), —one or two filters chosen from among UVB filters, except octocrylene, PABA and ethylhexyl methoxycinnamate, said composition also containing a pharmaceutically or cosmetically acceptable excipient.

Claims

1. A topical, cosmetic or pharmaceutical composition comprising one or more pharmaceutically or cosmetically acceptable excipients and a combination of solar filters only consisting of 3 or 4 solar filters comprising: one or two solar UVA filters to obtain a critical wavelength>370 nm, chosen from among: i. 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine, ii. 1,1′-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl[phenyl]-methanone, iii. Butyl Methoxydibenzoylmethane (BMDBM), in a quantity less than 2% by weight with regard to the total weight of said composition, iv. Hexyl 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoate, with the proviso that 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine is necessarily present, 2,4-Bis[4-(2-ethylhexyloxy)-2-hydroxyphenyl]-6-(4-methoxyphenyl)-1,3,5-triazine (BEMT), and one or two solar filters chosen from among solar UVB filters, with the proviso that the solar filters do not include octocrylene, para-aminobenzoic acid (PABA) and ethylhexyl methoxycinnamate.

2. The composition according to claim 1, wherein the quantity of all the compounds of said combination of solar filters is less than 20% by weight with regard to the total weight of the topical composition.

3. The composition according to claim 1, wherein said one or two solar UVA filters are two UVA solar filters consisting of 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine combined with another UVA filter chosen from among: 1,1′-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl[phenyl]-methanone, BMDBM, and hexyl 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoate.

4. The composition according to claim 1, wherein said one or two solar UVA filters are two UVA solar filters consisting of 1,1′-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl]phenyl]-methanone combined with: 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine.

5. The composition according to claim 1, wherein the 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine content is between 1% and 5% by weight with regard to the total weight of the composition.

6. The composition according to claim 1, wherein the 1,1′-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl]phenyl]-methanone content is between 1% and 5% by weight with regard to the total weight of the composition.

7. The composition according to claim 1, wherein the hexyl 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoate content is between 1% and 10% by weight with regard to the total weight of the composition.

8. The composition according to claim 1, wherein the BEMT content is between 1% and 4% by weight with regard to the total weight of the composition.

9. The composition according to claim 1, wherein the combination of 3 or 4 solar filters comprises one or two solar UVB filters with the proviso that the solar filters do not include octocrylene, PABA and its derivatives, the cinnamate chemical family including ethylhexyl methoxycinnamate, homosalate, the benzophenone chemical family and the benzylidene camphor chemical family.

10. The composition according to claim 1, wherein said solar UVB filter is chosen from among the following compounds: diethylhexyl butamido triazone, ethylhexyl triazone, tris-biphenyl triazine, ethylhexyl salicylate, phenylbenzimidazole sulfonic acid and TiO.sub.2.

11. The composition according to claim 10, wherein the tris-biphenyl triazine content is between 3% and 7% by weight with regard to the total weight of the composition.

12. The composition according to claim 10, wherein the diethylhexyl butamido triazone content is between 1% and 5% by weight with regard to the total weight of the composition.

13. The composition according to claim 10, wherein the ethylhexyl triazone content is between 1% and 5% by weight with regard to the total weight of the composition.

14. The composition according to claim 10, wherein the TiO.sub.2 content is between 1% and 10% by weight with regard to the total weight of the composition.

15. The composition according to claim 1, wherein it also comprises the broad spectrum filter methylene bis-benzotriazolyl tetramethylbutyl-phenol (MBBT).

16. The composition according to claim 1, wherein the combination of solar filters consists of 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine, BEMT and tris-biphenyl triazine.

17. The composition according to claim 1, wherein the combination of solar filters consists of 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine, BEMT, tris-biphenyl triazine and diethylhexyl butamido triazone.

18. The composition according to claim 1, wherein the combination of solar filters consists of 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine, BEMT, tris-biphenyl triazine and BMDBM.

19. The composition according to claim 1, wherein the combination of solar filters consists of 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)-bis[1,2,4]triazine, BEMT, MBBT and diethylhexyl butamido triazone.

20. The composition according to claim 1, characterized in that it contains 3 solar filters in all.

21. The composition according to claim 1, characterized in that it contains 4 solar filters in all.

22. A method for photoprotecting skin and/or hair, said method comprising: applying on the skin and/or hair the composition according to claim 1.

23. The composition according to claim 1, wherein the quantity of all the compounds of said combination of solar filters is less than 16% by weight with regard to the total weight of the topical composition.

24. The composition according to claim 1, wherein the quantity of all the compounds of said combination of solar filters is less than 14% by weight with regard to the total weight of the topical composition.

25. The composition according to claim 1, wherein the hexyl 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoate content is between 1% and 6%.

Description

EVALUATION AND EXAMPLES OF COMPOSITION

(1) In vitro Method of Evaluating Total UV and UVA Photostability

(2) A) Material

(3) UV Spectrophotometer:

(4) The spectrophotometer measures the spectral transmittance through a plate with and without a layer of a sunscreen composition on its surface.

(5) The spectrophotometer should allow measurements comprised between 290 nm and 400 nm. To reduce variability between measurement readings and to compensate for the lack of uniformity of the product layer, it is recommended that the reading zone of the sites be at least 0.5 cm.sup.2.

(6) The spectrophotometer used for these measurements is the Labsphere® UV-1000S or 2000S.

(7) Plate:

(8) The plate is the material onto which the sunscreen composition is applied. This material must be transparent to UV, non-fluorescent, photostable and inert with regard to the compounds of the compositions tested. For this protocol, polymethyl methacrylate (PMMA) plates proved ideal.

(9) UV Source:

(10) The UV source is a solar simulator with a xenon arc lamp diffusing a visible+UVA+UVB spectrum. The UV source used for this study is Suntest CPS+ (Atlas).

(11) B) Method:

(12) Measuring Transmission Through an Untreated Plate:

(13) Firstly, it is necessary to determine UV transmission through a control plate. This is prepared by spreading a few microliters of glycerin so that the surface of the plate is completely covered.

(14) Sample Application:

(15) The sample to be tested is applied onto the PMMA plate in an amount of 1.3 mg/cm.sup.2 (actual quantity remaining on the plate). To guarantee the accuracy of the amount and the reproducibility of the results, the application zone is larger than 10 cm.sup.2.

(16) The sample to be tested is applied in the form of a large number of small drops of the same volume, distributed over the entire surface of the plate.

(17) In order to ensure that the quantity of the product is correct, a method of validating the quantity of product applied must be adopted (for example: weigh the plate before and after application of the product).

(18) After application of the defined quantity of sample, the sample should be spread over the entire plate as quickly as possible (less than 30 seconds).

(19) The sample is then placed for 15 minutes in the dark at room temperature in order to promote the formation of a homogenous film.

(20) Measuring Transmission Through a Plate Treated with a Sample:

(21) The plate treated with the sample is analyzed with the spectrophotometer and the mean value of UV radiation transmission through the sample is determined for each wavelength from 290 nm to 400 nm (using the monochromatic absorbance data measured on the different areas of the plate).

(22) Number of Measurements:

(23) At least three PMMA plates should be prepared for each sample. Each plate should be measured in at least nine different regions unless almost the entire surface is measured by spectrophotometry.

(24) C) Calculation of Photostability:

(25) Calculation of SPF and UVA (PPD) in vitro from absorbance data A(λ) before and after irradiation with doses of 5 and 10 MED.

(26) $SPF\mathrm{in}\mathrm{vitro}=\frac{{\int }_{\lambda =290\mathrm{nm}}^{\lambda =400\mathrm{nm}}E\left(\lambda \right)*S\left(\lambda \right)*d\lambda }{{\int }_{\lambda =290\mathrm{nm}}^{\lambda =400\mathrm{nm}}E\left(\lambda \right)*S\left(\lambda \right)*{10}^{-A\left(\lambda \right)}*d\lambda }$
Wherein: E(λ)=Erythemal effectiveness spectrum S(λ)=Solar spectral irradiance A(λ)=Sample absorbance dλ=Wavelength variation (1 nm)

(27) $PPD\mathrm{in}\mathrm{vitro}=\frac{{\int }_{\lambda =320\mathrm{nm}}^{\lambda =400\mathrm{nm}}P\left(\lambda \right)*I\left(\lambda \right)*d\lambda }{{\int }_{\lambda =320\mathrm{nm}}^{\lambda =400\mathrm{nm}}P\left(\lambda \right)*I\left(\lambda \right)*{10}^{-A\left(\lambda \right)}*d\lambda }$
Wherein: P(λ)=PPD action spectrum (Persistent Pigment Darkening) I (λ)=Solar spectral irradiance A (λ)=Sample absorbance dλ=Wavelength variation (1 nm)

(28) Calculation of photostability from the following formulas:

(29) $\mathrm{Total}UV\mathrm{photostability}=\frac{SPF\mathrm{before}\mathrm{irradiation}}{SPF\mathrm{after}\mathrm{irradiaton}}$$UVA\mathrm{photostability}=\frac{PPD\mathrm{before}\mathrm{irradiation}}{PPD\mathrm{after}\mathrm{irradiation}}$

(30) In vitro Method for Evaluating COLIPA UVA and Critical Wavelength:

(31) In vitro COLIPA UVA and critical wavelength are determined according to the COLIPA method, Guidelines March 2011.

Example 1

(32) TABLE-US-00001 Ingredients % 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)- 4 bis[1,2,4]triazine Bis-Ethylhexyloxyphenol Methoxyphenyl 3 Triazine Tris-biphenyl triazine 5 Glycerin 10.0 Demineralized water QSP 100 Na2EDTA 0.1 Xanthan gum 0.3 C12-C15 alkyl benzoate 10.0 Octyl palmitate 5.0 Preservatives qs Stearyl alcohol 2.5 Glycerol monostearate 2.5 Potassium cetyl phosphate 1.8

(33) Results

(34) TABLE-US-00002 Parameter measured: Composition 1 SPF in vitro 66 COLIPA UVA 27.4 Critical wavelength nm 378 UVA photostability 5 MED 100% Total UV photostability 5 MED 100%

Example 2

(35) TABLE-US-00003 Ingredients % 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)- 4 bis[1,2,4]triazine Bis-Ethylhexyloxyphenol Methoxyphenyl 3 Triazine Methylene Bis-Benzotriazolyl 4 Tetramethylbutylphenol Diethylhexyl Butamido Triazone 2 Glycerin 10.0 Demineralized water QSP 100 Na2EDTA 0.1 Xanthan gum 0.3 C12-C15 alkyl benzoate 10.0 Octyl palmitate 5.0 Preservatives qs Stearyl alcohol 2.5 Glycerol monostearate 2.5 Potassium cetyl phosphate 1.8

(36) Results

(37) TABLE-US-00004 Parameter measured: Composition 2 SPF in vitro 50.6 COLIPA UVA 28.7 Critical wavelength nm 380 UVA photostability 5 MED 100% Total UV photostability 5 MED 100%

Example 3

(38) TABLE-US-00005 Ingredients % 5,6,5,6-tetraphenyl-3,3′-(1,4-phenylene)- 3 bis[1,2,4]triazine BMDBM 1 Bis-Ethylhexyloxyphenol Methoxyphenyl 3 Triazine Tris-biphenyl triazine 5 Glycerin 10.0 Demineralized water QSP 100 Na2EDTA 0.1 Xanthan gum 0.3 C12-C15 alkyl benzoate 10.0 Octyl palmitate 5.0 Preservatives qs Stearyl alcohol 2.5 Glycerol monostearate 2.5 Potassium cetyl phosphate 1.8

(39) Results

(40) TABLE-US-00006 Parameter measured: Composition 3 SPF in vitro 86.3 COLIPA UVA 31.2 Critical wavelength nm 378 UVA photostability 5 MED  93% Total UV photostability 5 MED 100%

Example 4

(41) TABLE-US-00007 Ingredients % 1,1′-(1,4-piperazinediyl)bis[1-[2-[4- 2.5 (diethylamino)-2-hydroxybenzoyl]phenyl]- methanone Bis-Ethylhexyloxyphenol Methoxyphenyl 4 Triazine Tris-biphenyl triazine 5 Glycerin 10.0 Demineralized water QSP 100 Na2EDTA 0.1 Xanthan gum 0.3 C12-C15 alkyl benzoate 10.0 Octyl palmitate 5.0 Preservatives qs Stearyl alcohol 2.5 Glycerol monostearate 2.5 Potassium cetyl phosphate 1.8