Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-09-09
1995-12-19
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
424 59, A61K 31495, A61K 742
Patent
active
054768535
DESCRIPTION:
BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATION
This application is based upon PCT application Ser. No. PCT/EP 93/00634, filed Mar. 16, 1993, which claims priority from European patent application Ser. No. 92.200,828.9, filed on Mar. 23, 1992.
The present invention concerns the use of an agent as an anti-irritant, cosmetic compositions comprising said agent, processes for preparing said compositions and a method of reducing irritation of the skin.
An uneasy irritating sensation or itching feeling in the upper surface of the skin is a phenomenon affecting many people at some time, even though it does not indicate any health problem. Said irritation or itching feeling may result from having a sensitive or hypersensitive skin, e.g. in the case of a dry or broken skin, from exposure to light, insect bites, contact with irritating plants such as poison ivy, friction or contact with clothes or tissues.
The present invention is concerned with the use of a compound having the formula ##STR2## or a cosmetically acceptable acid addition salt form thereof, for preventing or reducing irritation or itching of the skin of human beings.
The present invention is also concerned with a method of preventing or reducing irritation or itching of the skin of human beings, which comprises administering topically to the skin of said human beings a compound having the formula (I) or a cosmetically acceptable acid addition salt thereof, in an amount effective in preventing or reducing the irritation or itching feeling.
The compound of formula (I), 1-[3-[4-(diphenylmethyl)-1-piperazinyl]propyl]-1H-benzimidazole is a known compound and its preparation as well as its properties are described in U.S. Pat. No. 3,472,854.
The compound of formula (I) is preferably used as such or in a cosmetically acceptable acid addition salt form. Said salt forms can conveniently be prepared by treating the base form with an appropriate acid such as, for example, hydrohalic acids, e.g. hydrochloric or hydrobromic acid; sulfuric acid; nitric acid; phosphoric acid and the like; or organic acids, such as, for example, acetic, propanoic, hydroxyacetic, 2-hydroxy-propanoic, 2-oxopropanoic, ethanedioic, propanedioic, butanedioic, (Z)-2-butenedioic, (E)-2-butenedioic, 2-hydroxybutanedioic, 2,3-dihydroxybutanedioic, 2-hydroxy-1,2,3-propanetricarboxylic, methanesulfonic, ethanesulfonic, benzenesulfonic, 4-methylbenzenesulfonic, cyclohexanesulfamic, 2-hydroxybenzoic, 4-amino-2-hydroxybenzoic and the like acids. The term acid addition salt form as used hereinabove also comprises the solvates which the compound compound (I) and its acid addition salts are able to form. Examples of such solvates are, e.g. the hydrates, alcoholates and the like.
The compound of formula (I) when used in cosmetic compositions at a concentration of 0.05% to 2% (by weight based on the total weight of said cosmetic compositions), preferably 0.5% to 2%, prevents or takes away irritation or itching in the upper surface of the skin. Moreover, because of the beneficial inflammation modulating properties of compound (I), the rash and redness associated with certain instances of irritation can be prevented or diminished.
The compound (I) can be applied to the skin when necessary or convenient, e.g. at each washing occasion or thereafter; or before, during or after sunbathing. The topical administration may be repeated until a cosmetically beneficial reduction of the irritation is obtained. No special precautions are needed other then those which normally apply when using cosmetic agents.
Compound (I) is advantageously used in a micronized form, e.g. as material having an average particle size of less than 100 microns. Said micronized form has the advantage of dissolving better and more rapidly due to its high surface area, and penetrating well into the upper layers of the skin. Micronized forms of the compound (I) can be prepared following art-known micronization techniques, e.g. by milling in an appropriate mill and sieving through appropriate sieves.
The compound (I) is most preferably applied to the
REFERENCES:
patent: 3472854 (1969-10-01), Archer
patent: 4011322 (1977-03-01), Rahtz et al.
patent: 4250176 (1981-02-01), Vandenberk et al.
patent: 4377578 (1983-03-01), Vandenberk et al.
Merck Manual, 15th Edition, pp. 2516-2517, 1987.
Janssen Pharmaceutica N.V.
Metz Charles J.
Tsang Cecilia
LandOfFree
Agent for use as an anti-irritant does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Agent for use as an anti-irritant, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Agent for use as an anti-irritant will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-992236