Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Reexamination Certificate
1998-02-06
2001-02-20
Tate, Christopher (Department: 1651)
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
C424S401000, C424S626000, C424S078020, C424S078030, C514S844000, C514S937000, C514S944000, C514S460000, C514S557000
Reexamination Certificate
active
06190664
ABSTRACT:
This invention relates to compositions showing a depigmenting activity and to their uses.
STATE OF THE ART
The brown marks are localized hyperpigmentations which are caused by an excess of melanin.
The skin melanic marks which become more pronounced or which appear with the age, are experienced as an esthetical trouble which is always hard to bear on a psychological level.
Depending on their origin, hyperpigmentations are classified into two main groups:
1) Hyperpigmentation Bound to Melanocytar Hyperactivity and Hyperpigmentation Bound to Melanocytar Proliferation
a) Ephelids
Commonly called brown blotches, they appear during childhood, mainly on clear skins and are preferentially located on the uncovered parts of the epidermis. They intensify after expositions to the sun.
Histologically, the number of melanocytes is normal but the amount of melanin is increased.
b) Lentigine or Solar Lentigo
They are rounded and flat marks of very small size, having a taint from brown yellow to black, appearing during childhood. It is practically impossible to differentiate them from the ephelids when they are not of very dark colour.
c) Senile Lentigo
They are brown marks appearing on the back side of the hands, on the forearms and on the face after the fifties. Histologically it is noted a melanic hyperpigmentation of the basal layer of epidermis with an increase of the number of melanocytes.
d) Melasma
It is a pigmental layer extending in a almost always symetrical manner on the forehead and the cheeks, more frequently appearing in the brown ladies. It may appear in three opportunities:
during pregnancy: it is chloasma,
during the intake of oestroprogestative agents,
in an idiopathic manner.
2) Hyperpigmentation by Pigmentar Incontinence
This is a hyperpigmentation consecutive to photosensibilization.
This is the classical dermatosis as a charm or perfume dermitis. They are brown, more or less dark, marks, laid out in packs or in runnings at the location where the perfumes and the cosmetics are applied before a sun exposition. They gradually and spontaneously disappear in several months.
SUMMARY OF THE INVENTION
It hence exists a need for a composition having a high depigmenting activity at low concentration, showing a good skin tolerancy.
Therefore this invention has as a subject matter, dermo-cosmetic compositions, wherein they contain as an ingredient a combination endowed with depigmenting activity:
a) An Acid Mixture Comprising
i) at least an &agr;-hydroxylated acid or one of the derivatives thereof,
ii) at least one compound selected from the group consisting of kojic acid, caffeic acid, azelaic acid, aminobutyric acid, fusaric acid, 5-hydroxy 2-hydroxymethyl-&ggr;-pyridone, and the derivatives thereof,
(b) at least one active ingredient from a plant extract from at least one plant selected from white mulberry, liquorice, skull cap, grapefruit, birch, heather, strawberry tree, bearberry, lemon, lettuce, oarweed, cucumber, ginseng, hop, sweet corn, fever few, sage, soya, elder, spirulina, lime, ferocious aloe, yukinoshita, bloodwort, hoelen, wood rose, &agr;-orizanol, burnet, Ginkgo biloba, tanlex VB, Eclipsa alba, with the proviso that when the composition contains kojic acid and liquorice, it contains at least another component from a vegetal extract.
Preferably ascorbic acid will be excluded from the usable acids mentioned under a). Among the derivatives of acids i) and ii) it needs to be cited the salts, mainly the alkali or earth alkaline metal salts and particularly the ammonium salts. Among the derivatives it may also cited the esters mainly the esters with the polyols for example the sugars.
It may particularly be contemplated co-esters with two acid derivatives on a same polyol.
Among the usable &agr;-hydroxylated acids, it has to be cited malic and citric acid, lactic acid, and glycolic acid; the concentration thereof is advantageously comprised between 0.1 and 45% in relation to the total weight of the composition.
Acids ii) providing more advantageous results according to the invention, are kojic acid, caffeic acid, or 5-hydroxy 2-hydroxymethyl-&ggr;-pyridone, the last compound being more particularly preferred. It will be then preferably used, these compounds or the salts thereof, alone or in a mixture to constitute the non &agr;-hydroxylated acid moiety of the depigmenting compositions.
Some particularly advantageous combinations are those comprising a mixture of kojic acid, Burnet and Eclipsa alba. The latter may be combined with &agr;-hydroxylated acids and optionally other components of vegetal extracts.
The active ingredient of a vegetal extract may be obtained by extraction from the plant or a part of the plant but it may be possible to obtain this component by chemical synthesis when this has been identified. This synthesis may be complete or be hemisynthesis.
The active ingredient is preferably brought by a vegetal extract obtained from white mulberry, liquorice, scuttellaria, grapefruit, birch, heather, strawberry tree, bearberry, lettuce, soja, Aloe ferox, yukinoshita, rose fruit, burnet and/or Eclipsa alba.
When they are obtained by extraction, the active components of the vegetal extracts may be obtained through a step of extraction in a hydroalcoholic medium from the stems, the leaves and/or the roots of the plants. In most of the cases, the hydroalcoholic extract containing the active ingredient and other components may be used as such, but it is obviously possible to eliminate from this extract the unuseful or noxious components if any and that by known methods such as selective precipitation, extraction by solvent and/or chromatography.
The nature of the active ingredient may very largely vary as a function of the activity of the two moieties, particularly as a function of the activity of the vegetal active component. It is so when the acidic mixture may constitute from 0.1 to 99% by weight of the active ingredient, the vegetal extract constituting thereby the complement.
Preferably the ratio by weight between the acidic moiety and the active component of the vegetal extract is comprised between 50/50 and 70/30.
The compositions according to the present invention may contain other active ingredients disregarding them in the preceding percentages. So, according to one of the aspects of the invention, the composition may further contain at least one compound selected among the ceramides, the vectorizing macromolecules, or component promoting the penetration.
As previously mentioned, the acidic mixture may at least be partially grafted on sucro esters. The concentration into actives in the composition will preferably be comprised between 1 and 20%.
A composition according to the invention shows particularly the following formulation:
Kojic acid: from 1 to 15%
Glycolic acid: from 20 to 30%
and from 20 to 35% of the vegetal extracts resulting from Tanlex VB, (extraction solvent is a mixture of water and butylene glycol). Yukinoshita, Naringin, Sohakuhi Bg (extraction solvent is butylene glycol), white mulberry, Lemon Bg, and the remainder in carrier suitable for this formulation.
Finally, melanin protects the skin from the noxious effects of the UV rays. Taking account of the fact that the compositions according to the invention, reduce the production of melanin, it is of interest to add to the cosmetic formulation sun protective agents, very efficient to avoid the damages incurred by the skin exposed to the sun without protection.
These sun protective agents may be organic and/or mineral filters known from the skilled scientists. Among the latters it may be cited the particles of metallic oxide, namely of titanium, iron, cerium, aluminum, etc., and of talc.
The selection of the type of retained filter, its content and optionally its granulometry will be determined by the desired final consistency of the formulation.
The compositions according to the invention may be presented in the form mainly of a lotion, a gel, an emulsion, a cream, an unguent and contain pharmaceutically and/or cosmetologically acceptable suitable carriers. Among these carriers it may be
Bierman, Muserlian and Lucas
C 3 D
Tate Christopher
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