Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
1999-06-25
2001-05-15
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S195110, C424S070100
Reexamination Certificate
active
06231877
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to an improvement to the composition for preventing ageing of the skin, which is the subject of patent PCT/FR 97/02017, filed on Nov. 10, 1997 in the name of the Applicant.
The invention similarly applies both to natural ageing and to phenomena of accidental ageing of the skin due to the manifold attacking factors to which the skin is subjected daily, in particular solar radiation. 2. Description of the Prior Art
In general, it is known that free radicals (aggressive particles possessing a free electron) are the main agents incriminated in skin damage caused, for example, either by prolonged exposure to solar radiation and thus to the ultraviolet rays included in this radiation, or even by metabolic and enzymatic reactions which take place in the body.
Radical attack initiates chain reactions which stop only when two free radicals become mutually inactivated.
Lipid peroxidation (lipoperoxidation) is a typical case of a radical-induced chain reaction.
Oxidation of the membrane lipids results in the formation of lipoperoxides, which decompose into various fragmentation products, some of which are highly aggressive.
One of the most important and most aggressive fragmentation products is an aldehyde, malondialdehyde (MDA), which exhibits formidable toxicity by transversely bridging proteins, intracellular lipids and DNA.
It thus appears that the free radicals and the cascade of chain reactions to which they give rise in the body play a very important role in the process of ageing of the skin.
With the aim of combating this radical action, the Applicant proposes a composition which uses the properties of Chrysanthellum indicum indicum, which, according to the abovementioned French patent:
has very good radical-scavenging properties, so as to obtain anti-ageing action both for natural and accidental ageing;
ensures effective protection against the reactions leading to the production of OH° radicals or radicals of oxoferryl type;
reduces the fall in the ATP content of the keratinocytes after irradiation, so as to obtain a repairing effect.
Hitherto, as many scientific publications affirm, the studies carried out on Chrysanthellum indicum revealed the clinical effects in essentially circulatory and digestive pathologies (exclusively medical field).
Only French patent No. 87/10502 proposed a cosmetic composition comprising an extract of Chrysanthellum indicum containing from 1% to 10% extract of Chrysanthellum indicum, for applications such as shampoos and hair lotions, dermal emulsions, body milks, lipsticks or even cosmetic compositions in the form of aerosols.
Besides the fact that that document does not mention the prevention of ageing of the skin, the concentrations recommended therein give products which are entirely inappropriate and even incompatible with normal cosmetic use, since, at these concentrations, emulsions for topical use exhibit, in particular:
a dark brown coloration which causes the skin to be treated and that of the fingers used to carry out the application to be dyed an intense mustard-yellow colour. The strong intensity of this dyeing is attenuated on rinsing, but leaves a dark yellow coloration after washing.
Poor stability over time: a concentration of water in the bottom of the container and considerable release of oil at the surface are observed from 24 hours onwards.
A strong odour of plant extract.
OBJECT OF THE INVENTION
A subject of the invention is thus, more particularly, a composition based on Chrysanthellum indicum in which the radical-scavenging effect is enhanced, without needing to increase the content of Chrysanthellum indicum, which must remain at a sufficiently low level in order to avoid the drawbacks mentioned above.
SUMMARY OF THE INVENTION
To this end, the invention proposes to use synergistic radical-scavenging effects, i.e. the effects obtained by combining one or more molecules with the Chrysanthellum indicum.
Now, it is known that such a combination can give:
a) either weaker activity than addition of the activity of each of the products, on account of an antagonistic effect (one product reducing the activity of the other) or of a saturation effect (impossibility of exceeding the maximum effect reached) or even a harmful effect (predominant antagonistic effect);
b) or an activity which is equal to the sum of the activities of each of the products tested separately;
c) or to higher activity than the sum of the activities of the products tested separately (synergistic effect).
d)
DESCRIPTION OF THE PREFERRED EMBODIMENTS
In practice, as much as it is conceivable that there may be an activity threshold which cannot be exceeded, it is implausible to hope to obtain additional effects, even partial effects. The demonstration of synergistic effects, for its part, is very rare.
As regards Chrysanthellum indicum, no synergistic radical-scavenging effect involving it was known hitherto and there was no indication to predict that it would be possible to demonstrate a synergistic effect between Chrysanthellum indicum and other molecules, or even that this type of combination would allow the already excellent performance levels to be improved.
Now, the studies conducted by the Applicant have revealed such a synergistic effect.
The aims of these studies, carried out in vitro, were:
on the one hand, to measure the effects of four compounds:
extract of Chrysanthellum indicum,
extract of green tea,
extract of Ginkgo biloba,
DL-&agr;-tocopheryl acetate, with respect to the peroxidation of linoleic acid by OH° and peroxyferryl radicals,
on the other hand, to investigate any potentiation between Chrysanthellum indicum and one of the other compounds.
To this end, each of the compounds was subjected to the lipid peroxidation initiation treatment below:
Peroxidation of a linoleic acid emulsion was induced by radicals of the type: hydroxyl OH° and oxyferryl. Linoleic acid (10 mg) was emulsified with 0.2% of 3-[(3-cholamidopropyl)dimethylammonio]-1-propane-sulphonate (CHAPS), in a pH 7.3 phosphate buffer (50 ml).
The OH° radicals are produced using a source of gamma irradiation. Under these conditions, the irradiation is carried out at 20° C. for 18 hours (source
131
Cs, total dose: 180 grays/18,000 rads).
The oxyferryl radicals are generated by adding 10 &mgr;l of haemoglobin to a linoleic acid emulsion (2 ml) for 3 hours (incubation at 40° C.).
These tests were carried out in 10 ml leakproof bottles in the presence or absence of two control antioxidants. Each test was performed in triplicate.
At the end of the reaction under the various conditions mentioned above, the lipid peroxidation is measured by means of determining the pentane (nmol) resulting from the decomposition of the lipid peroxides. The emission of pentane is directly proportional to the peroxidation. The pentane is measured by gas chromatography: 0.1 ml of the atmosphere from the flask in which the reaction took place are injected using a Hamilton syringe into a Varian 3600 type chromatograph.
This chromatograph is equipped with a GF molecular sieve alltech column (length: 1m; ID: ⅛″) at 140° C., the carrier gas used being nitrogen (40 ml/min). The method is calibrated using pure pentane.
The results of these measurements are given in Tables I and II below.
TABLE I
“Anti-oxyferryl” effect (release of pentane, in nmol)
Concen-
Concen-
tration
Green
Ginkgo
tration
(&mgr;g/ml)
Chrysanthellum
tea
biloba
Tocopherol
(&mgr;M)
0.00
100.00
100.00
100.00
100.00
0.00
0.15
101.39
110.83
122.77
93.02
1.00
1.50
97.70
93.85
104.63
82.17
2.50
15.00
82.77
87.61
93.00
72.33
5.00
150.00
40.77
44.93
65.73
57.07
7.50
300.00
11.17
24.33
35.47
36.80
10.00
TABLE II
“Anti-hydroxyl” effect (release of pentane)
Concen-
Concen-
tration
Green
Ginkgo
tration
(&mgr;g/ml)
Chrysanthellum
tea
biloba
Tocopherol
(&mgr;M)
0.00
100.00
100.00
100.00
100.00
0.00
0.15
101.41
108.43
115.43
119.67
1.00
1.50
86.67
97.30
100.37
66.76
2.50
15.00
30.50
36.93
98.87
13.70
5.00
150.00
12.73
23.03
53.87
7.67
7.50
300.00
7.97
12.10
29.90
Fritsch Marie-Claire
Vacher Anne-Marie
Drucker William A.
Howard S.
Lanatech Laboratoire Nature et Technique
Page Thurman K.
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