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Formulations of low oil content comprising diphenylmethane derivatives

A pharmaceutical preparation and preparation technology, applied in the field of preparations containing diphenylmethane derivatives with low oil content, can solve the problem of whitening skin toxicology acceptability, skin tolerance and/or stability without predictable relationship, etc. problem, to achieve high bioavailability, effective activity, improve skin whitening activity

Inactive Publication Date: 2009-02-11
SYMRISE GMBH & CO KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, there was no predictable relationship between the skin lightening and hair bleaching effects, toxicological acceptability, skin tolerance and / or stability of the potential active compounds

Method used

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  • Formulations of low oil content comprising diphenylmethane derivatives
  • Formulations of low oil content comprising diphenylmethane derivatives
  • Formulations of low oil content comprising diphenylmethane derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0342] In Vivo Study of Skin Lightening Effect of Styryl Resorcinol (Formula 3)

[0343] From the following studies it was found that the diphenylmethane derivative of formula 1 has a particularly good skin whitening effect when it is applied to the skin in a formulation with a low oil phase content.

[0344] Asian volunteers (Fitzpatrick skin, type III) were treated with emulsions A-F with a size of 1.5 cm on the back 2 skin for 7 days, 2 times a day. The volunteers were irradiated with UV-A light on day 8 (4 different doses produced weak, mild, moderate and strong pigmentation, respectively). Treatment with Emulsions A-F was repeated for another 14 days. Skin color was measured visually on days 8 and 21 (L * value).

example 1

[0347] Preparation instructions :

[0348] Separately heat phases A and B to about 80°C. Add Phase B to Phase A using an Ultra-Turrax mixer and emulsify. The emulsion was stirred with a paddle stirrer until cooled, the stirring speed decreased as the temperature decreased. The pH of the emulsion was adjusted to about 5.6-5.8 with sodium hydroxide solution.

[0349] Formulation II :

[0350] The formulation is very high in water and low in lipids.

[0351] Furthermore, no customary emulsifiers but surface-modified polymers are used here. (=hydrogel cream preparation)

[0352]

Substances used

INCI name

emulsion

D. emulsion

E. emulsion

f A.

Neo Pcl wssl.N

Trideceth-9

(Trideceth-9)

PEG-5

Ethylhexanoate 1.5

1.5

1.5

...

Embodiment 2

[0360] Example 2 : Study on the antioxidant capacity of styryl resorcinol (Formula 3; CARN 85-27-8; 4-(1-phenylethyl)-1,3-dihydroxybenzene) by ABTS method

[0361] Phenolic compounds generally have very good antioxidant activity. To test the degree of antioxidant potential also possessed by styryl resorcinol (Formula 3; CARN 85-27-8; 4-(1-phenylethyl)-1,3-dihydroxybenzene), the ABTS method was used to study said substance. For qualitative and quantitative evaluation of the antioxidant potential, its activity was compared with that of α-tocopherol, a highly active and versatile antioxidant.

[0362] Description of the ABTS method experiment

[0363] ABTS method is a cell-free in vitro test for evaluating antioxidant capacity (document: Re R, Pellegrini N, Proteggente A, Pannala A, Yang M, Rice-Evans C.1999. "Antioxidant activity applying an improved ABTS radical cation decolorization assay" ; Free Radic. Biol. Med. 26:1231-7). This method exploits the inherent coloratio...

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Abstract

The present invention relates to specific (cosmetic) formulations for improving the bioavailability and activity of skin- or hair-lightening or senile keratosis-reducing diphenylmethane derivatives (tyrosinase inhibitors) of the following formula (1).

Description

technical field [0001] The present invention relates to specific (cosmetic) preparations for enhancing the activity of diphenylmethane derivatives of the formula 1 (tyrosine bioavailability and activity of enzyme inhibitors): [0002] [0003] in [0004] R1 is [0005] -hydrogen, [0006] -methyl, [0007] - linear or branched saturated or unsaturated alkyl groups having 2 to 4 carbon atoms, [0008] -OH or [0009] -halogen, [0010] R2 is [0011] -hydrogen, [0012] - methyl or [0013] - linear or branched saturated or unsaturated alkyl groups having 2 to 5 carbon atoms, [0014] R3 is [0015] - methyl or [0016] - linear or branched saturated or unsaturated alkyl groups having 2 to 5 carbon atoms, [0017] as well as [0018] R4 and R5 independently of each other are [0019] -hydrogen, [0020] -methyl, [0021] - linear or branched saturated or unsaturated alkyl groups having 2 to 5 carbon atoms, [0022] -OH or [0023] -halogen. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/34A61Q5/08A61Q19/02A61Q19/08
CPCA61K8/347A61Q5/08A61K2800/782A61Q19/02A61P17/12
Inventor 加布里埃莱·菲尔哈伯格哈德·施毛斯扎比内·朗格卡林·沙佩尔
Owner SYMRISE GMBH & CO KG
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