Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
1998-02-18
2001-04-17
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C514S827000, C514S828000, C514S829000, C514S830000, C514S848000, C514S886000, C514S887000, C514S969000
Reexamination Certificate
active
06217885
ABSTRACT:
The present invention relates to antipruritic cosmetic and/or pharmaceutical compositions for use on human or animal skin.
Insect stings and the associated itching are not only unpleasant, but can also lead to inflammations due to scratching on the itching areas of the skin. The scars often heal with difficulty and are visible for a long time or permanently. Alleviation of the itching is therefore particularly important in order to avoid complications.
It is known from the literature that ethoxylated compounds, such as, for example, laureth-9 (Fiedler, Lexikon der Hilfsstoffe für Pharmazie und Kosmetik und angrenzende Gebiete [Dictionary of auxiliaries for pharmaceuticals and cosmetics and related fields], publisher: Editio Cantor Aulendorf, 3rd edition, volume 1, page 540) or polyoxyethylene (20)-sorbitan monolaurate (manufacturer's data) or substances from other classes of substance, for example citric acid esters (Fiedler, Lexikon der Hilfsstoffe fir Pharmazie und Kosmetik und angrenzende Gebiete [Dictionary of auxiliaries for pharmaceuticals and cosmetics and related fields], publisher: Editio Cantor Aulendorf, 3rd edition, volume 1, page 309), have a certain local anesthetic action. This has also been confirmed in experiments on reducing itching after insect stings (see tables).
Nevertheless, previous antipruritic cosmetic and/or pharmaceutical compositions were not satisfactory because their actions subside rapidly.
The object of the present invention was to provide antipruritic cosmetic and/or pharmaceutical compositions for use on human or animal skin which alleviate swelling of the skin, allow swollen skin to detumesce, prevent reddening, and finally alleviate the itching over a relatively long period of time.
It should furthermore be ensured that the antipruritic cosmetic and/or pharmaceutical compositions according to the invention
1. do not impair the biological processes of the skin,
2. the active compounds do not have a pronounced intrinsic smell,
3. the active compounds are harmless in the event of an overdose or if used otherwise not as intended,
4. the active compounds do not become concentrated in or on the skin after repeated use,
5. the active principles can be incorporated easily into customary cosmetic or dermatological formulations, for example solutions, gels, balms, creams, foams or sticks,
6. the active compounds do not irritate the skin,
7. the active compounds do not interact with clothing materials.
It has now been found, and therein lies the achievement of all the abovementioned objects, that the use of an active complex comprising one or more mild local anesthetics, one or more astringents, for example the tanning agent tannin, and/or, if appropriate, a substance having an antiinflammatory action persists for much longer than was to be expected from the sum of the activity of the individual components. While the average antipruritic action of laureth-9 persists for about 30 minutes, tannin by itself indeed caused the skin to detumesce and alleviated reddening, but acted against the itching only indirectly (for less than 10 minutes after the application), and glycyrrhizinate and bisabolol also acted against the itching for only about 5 minutes, the action of the combination of the individual components persisted for up to 3 hours (average per 5 subjects: 130 to 140 minutes).
The compositions according to the invention are therefore outstandingly suitable for alleviating itching, for example after insect stings, contact with stinging nettles and jellyfish, and with allergic skin reactions. They counteract reddening of the skin and additionally have a detumescent action. It has furthermore been found that the cosmetic and/or pharmaceutical dermatological agents according to the invention display a potent action against development of erythema after excessive UV irradiation.
Preferred compositions according to the invention comprise
1. one or more local anesthetics of the series consisting of laureth-9, polyoxyethylene (20)-sorbitan monolaurate, triethyl citrate, acetyl-triethyl citrate, tributyl citrate or acetyl-tributyl citrate,
2. one or more astringents from the series consisting of tannin, walnut leaf extract, aluminum lactate or sodium tartrate and/or, if appropriate,
3. one or more substances having an antiinflammatory action from the series consisting of Dragosantol®, bisabolol, panthenol, pantothenyl alcohol, glycyrrhetin derivatives, glycyrrizin derivatives or liquorice extract.
Particularly preferred compositions according to the invention comprise
1. one or more local anesthetics of the series consisting of laureth-9, polyoxyethylene (20)-sorbitan monolaurate, triethyl citrate, acetyl-triethyl citrate, tributyl citrate or acetyl-tributyl citrate,
2. one or more astringents from the series consisting of tannin, walnut leaf extract, aluminum lactate or sodium tartrate and/or, if appropriate,
3. one or more substances having an antiinflammatory action from the series consisting of Dragosantol®, bisabolol, panthenol, dexpanthenol, pantothenyl alcohol, dipotassium glycyrrhizinate, glycyrrhizinic acid or salts thereof, glycyrrhetic acid or salts thereof, stearyl glycyrrhetinate or liquorice extract.
The active complex comprising laureth-9, tannin, dipotassium glycyrrhizinate and/ or bisabolol is particularly preferred.
All the components are known from the literature. Some of the contents are briefly described specifically:
Laureth-9 is a polyethylene glycol (9)-monododecyl ether (polydocanol), an adduct of 9 mol of ethylene oxide onto dodecyl alcohol; it corresponds to the formula
C
13
H
25
—(O—CH
2
—CH
2
)
n
—OH
(n has an average value of 9), and the average molecular weight is about 600.
Dragosantol® is a trade name for a synthetically prepared, colorless to pale yellowish-colored, faintly smelling liquid,
(−)-&agr;-bisabolol [(−)-6-methyl-2-(4-methyl-3-cyclohexenyl)-5-hepten-2-ol]
glycyrrhetic acid (3&bgr;-hydroxy-11-oxoolean-12-en-30-oic acid, common name: enoxolone, biosone).
R=H: glycyrrhetic acid
The antipruritic cosmetic and/or pharmacological compositions according to the invention comprise the additives and solutions customary for topical use, preferably as liquid, semi-solid or solid formulations.
Drops, tinctures or sprays, each of which comprise the active compound mixtures described above in the form of a solution, suspension, emulsion or dispersion, are possible for the liquid formulation.
Possible semi-solid formulations are, for example, gels, ointments, creams or foams, while solid formulations include, for example, powders, dusting powders, granules, pellets or microcapsules. If the active compound mixtures described above are available as a pharmaceutical and/or cosmetic composition in the form of a liquid presentation form, it is advisable to use for these, as far as possible, those diluents which do not irritate the skin when used topically. This applies in particular, for example, to water, monohydric alcohols, preferably ethanol, isopropanol or n-propanol, polyhydric alcohols, in particular glycerol and/or propanediol, polyglycols, in particular polyethylene glycols and/or Miglyol, glycerol formal, dimethylisosorbitol, naturally occurring and synthetic oils and/or esters.
In addition to the abovementioned diluents, base masses, such as, for example, bentonite, Veegum, guar flour and/or cellulose derivatives, in particular methylcellulose and/or carboxymethylcellulose, are also suitable for the preparation of semi-solid presentation forms, such as, for example, gels, ointments, creams and foams. Instead of the abovementioned base masses or in addition to the abovementioned base masses, possible base masses are also polymers of vinyl alcohols, vinylpyrrolidones, alginates, pectins, polyacrylates, solid and/or liquid polyethylene glycols, paraffins, fatty alcohols, vaseline, waxes, fatty acids and/or fatty acid esters.
For the preparation of solid formulations which are also suitable for topical use, such as, for example, the abovementioned powders, dusting powders,
Koch Sabine
Roder Klaus
Bayer Aktiengesellschaft
Norris & McLaughlin & Marcus
Page Thurman K.
Ware Todd D.
LandOfFree
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