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Over-additive effect of the cooling efficacy of Frescolat X-Cool in combination with WS3/WS5

IP.com Disclosure Number: IPCOM000216726D
Publication Date: 2012-Apr-16
Document File: 86 page(s) / 1M

Publishing Venue

The IP.com Prior Art Database

Abstract

The present invention primarily relates to the topical use of a mixture of cooling compounds, consisting of Frescolat X-Cool and WS3 or WS5. The invention aims on using the above mentioned mixture in cosmetic formulations with indented cooling properties on human skin.

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Symrise AG

Mühlenfeldstraße 1, 37603 Holzminden

Over-additive effect of the cooling efficacy of Frescolat X-Cool in combination with WS3/WS5

The present invention primarily relates to the topical use of a mixture of cooling compounds, consisting of Frescolat X-Cool and WS3 or WS5. The invention aims on using the above mentioned mixture in cosmetic formulations with indented cooling properties on human skin.

Background of the invention:

In the area of personal care cooling substances are used for application onto the skin, hair and mucous membranes. Cooling substances are for use in lotions and creams, skin cleansers, shampoos, hair conditioners, cleaning tissues, sanitary towels, tampons, nappies as well as other cosmetic products such as lipsticks or Eau de Toilette. Numerous natural and synthetic substances with cooling properties are described. Among these l-menthol, originally found in peppermint oil, is the most known substance. Menthol and its derivatives bind to and thus activate the TRPM8 (Transient Receptor Potential Melastatin 8) receptor (alias CMR = Cold Menthol Receptor 1) that belongs to the family of TRPs (Transient Receptor Potential Ion Channels). Along with other receptors of the TRP-family, it is expressed in specialized peripheral sensoric neurons and in the neighboring dermal keratinozytes. Four monomers of the channelprotein together form a pore. When activated by low temperatures or binding of cooling compounds the channel allows the influx of calcium and sodium ions. This resulting change of the cellular charge generates an action potential which will be converted in the brain into a sensation of cold (Clapham DE et al 2005, Pharmacological reviews, 57 (4), 427-450; Peier AM et al 2005, Cell, 108 (5), 705-15). Numerous menthol derivatives are described, to e able to activate TRPM8 (British Patent 1971 # 1315761 Watson H.R., J. Soc. Cosmet. Chem. 29, 1978, 185-200; Furrer S.M., Chem. Percept. 1, 2008, 119-126) Aside from this, cooling structures are described, which are not based on menthol, such as Icilin (Wei E.T., J. Pharm. Pharmacol. 35, 1983, 110-112; WO 2004/026840), WS-23 or substances such as mentioned in WO 2007/019719.

In the light of this background it is the object of the present invention to provide a way of creating a cooling sensation with a mixture of two known cooling compounds that generates a stronger cooling effect as expected by the addition of both (over-additive effect).

This way should be open for topical applications and applications of care products.

This object is achieved by using Frescolat X-Cool in combination with WS5 / WS3

(i)            N-ETHYL-OXALAMIDACID-MENTHYLESTER (Frescolat X-COOL)

 (ii) WS-3 (N-Ethyl-p-menthane-3-carboxamide)

(iii) WS-5 [Ethyl 3-(p-menthane-3-carboxamido)acetate]

Topical applications in terms of the present text are applications where the intended substance combination is brought into contact with the skin. It is especially preferred that the evaluation of a cooling effe...