Title:  Antioxidant and/or antielastase composition based on lupine oil

United States Patent:  6,146,616

Assignee:  Laboratories Pharmascience (Courbevioe, FR)

Filed:  December 24, 1998

PCT NO:  PCT/FR98/00827

102(e) Date:  December 24, 1998

PCT PUB. Date:  October 29, 1998

Foreign Application Priority Data:  Apr 24, 1997[FR] (97 05067)

The invention concerns an antioxidant and/or antielastase composition containing lupine oil or one or several fractions thereof, its use in cosmetics, pharmaceutics and as food additive. More particularly it concerns a composition containing a mixture of lupine oil and wheat germ concentrate, preferably in a proportion of 70 wt. % of lupine oil and 38 wt. % of wheat germ concentrate.

Description of the Invention

The subject of the present invention is new compositions based on lupine oil, or on fractions thereof, especially concentrates and unsaponifiable matter.

Lupine oil may be extracted especially from lupine meals and/or seeds.

Lupine is a close relative of the pea, broad bean, soybean and French bean. The seed is traditionally used as human food for its high protein content. It is also incorporated into ruminant feed in the form of a whole plant or of its seeds and is also frequently used as green manure. More particularly, four species of lupine are of real agronomic importance: white lupine (lupinus albus), blue lupine (lupinus angusti-folius), yellow lupine (lupinus luteus) and South American lupine (lupinus mutabilis).

Plants constitute an abundant lipid source and the extraction of vegetable oil has already been widely carried out. The oil can then be used directly, or in the form of some of its fractions. Among the fractions which can be obtained from a vegetable oil, there may be mentioned the unsaponifiable matter or the concentrates.

According to the European Pharmacopeia, 2nd edition, page V.3.4.7, the term "unsaponifiable" applies to the nonvolatile substances obtained by extraction, with an organic solvent, of a solution of the substance to be examined after saponification of a vegetable or animal oil.

Moreover, the so-called molecular distillation method makes it possible to concentrate oils derived in particular from plants (vegetable oils), and to obtain concentrates in which the concentration of unsaponifiable matter may reach, for example, the order of 10% to 20% by weight, or even greater, this concentration being of the order of 1% to 2% by weight in the original oils.

Vegetable oils have thus been the subject of various uses, mainly in cosmetology. For example, Patent FR 92 07830 describes the preparation of compositions based on unsaponifiable fractions of wheatgerm and sesame oils for a cosmetic use, these concentrates being obtained by molecular distillation according to a preferred method described in the patent.

As regards lupine oil, no cosmetic or pharmaceutical use has been envisaged up to date. European Patent Publication EP-A-441672 describes a process for the extraction of constituents of a plant material which make it possible in particular to obtain a lupine oil without any trace of alkaloid. This document describes in particular the treatment of the bitter lupine seeds and aims essentially to enhance the value of a protein cake free of the bitterness characteristic of bitter lupine seeds.

The inventors have now observed that, surprisingly, a composition containing lupine oil or one or more fractions thereof had a number of properties paving the way to a variety of applications in the cosmetic, pharmaceutical or food domain.

The studies on which the invention is based have made it possible to demonstrate that lupine oil or its fractions exert especially an antioxidant and antielastase activity.

The subject of the present invention is therefore an antioxidant and/or antielastase composition containing lupine oil or one or more fractions thereof. The lupine oil may be extracted from lupine meals and/or seeds.

The lupine oil may be obtained by any known method, in particular by direct pressing of the lupine seeds.

So-called sweet lupine species, that is to say free of bitterness, will be preferably used as raw material for the production of the lupine oil or of its fractions. There may be mentioned especially white lupine, blue lupine, yellow lupine and South American lupine, in particular white lupine (lupinus albus). The lupine oil extracted from this lupine variety is then free of undesirable alkaloids.

The invention relates more particularly to a composition comprising lupine oil in the form of a fraction consisting of a lupine oil concentrate obtained by molecular distillation of said oil.

According to a preferred embodiment, the compositions based on lupine oil according to the invention comprise one or more lupine oil fractions in the form of unsaponifiable matter as contained in a lupine oil concentrate obtained by molecular distillation of said oil.

Advantageously, the quantity by weight of the unsaponifiable fraction in the lupine oil concentrate is about 30% to about 70%, preferably about 45% to about 65% and still more preferably of the order of 60%.

The inventors have observed that lupine oil has a particularly high content of polyphenol, .beta.-carotene and tocopherol derivatives and it is known that the polyphenol derivatives contribute to the oxidation-stability of a composition containing them. Advantageously, the subject of the invention is an antioxidant and/or antielastase composition which contains a lupine oil fraction comprising phenol derivatives. More generally, the invention also relates to any antioxidant and/or antielastase composition which contains phenol derivatives extracted from lupine oil. Preferably, the content of phenol derivatives is equal to at least 20 ppm.

The subject of the invention is also a composition in which the lupine oil or its fractions are in the form of a mixture with wheatgerm oil or one or more of its fractions. In this case, the wheatgerm oil fraction used may also be a concentrate obtained by molecular distillation of said oil or alternatively an unsaponifiable fraction contained in such a concentrate. Surprisingly, the inventors have now established that wheatgerm oil or its fractions could be advantageously used in combination with lupine oil or its fractions.

Preferably, when the two types of oil are present in a composition according to the invention, the lupine oil is in the form of a mixture with a wheatgerm oil concentrate.

According to a preferred embodiment of the invention, the quantities by weight of concentrate of wheatgerm oil and of lupine oil vary respectively between about 10% and about 90% and between about 90% and about 10% so that the quantities of these two oils is 100% in total.

Surprisingly, it has moreover been observed that in a certain composition ratio, the antioxidant, in particular anti-free radical, activity was substantially better.

Accordingly, a preferred composition according to the invention is that in which the quantities by weight of the concentrate of wheatgerm oil and of lupine oil are respectively 30% and 70%.

The invention also relates to the cosmetic use of a composition according to the invention, especially as antioxidant, anti-free radical agent, antielastase agent, agent for protecting against UVA and/or B, agent for protecting DNA against damage, especially oxidative damage. By virtue of the activities demonstrated for the compositions according to the invention, it is possible to use the compositions according to the invention for cosmetic or pharmaceutical purposes, especially for photoprotection, against actinic aging or otherwise, and for protecting the skin against oxidative attacks including pollution.

The invention also relates to the compositions according to the invention as a pharmaceutical, especially dermatological, product and more particularly as an agent intended for the prevention or for the treatment of the effects of UVA and/or UVB radiation on the skin, at the epidermal, dermal, cellular or extracellular levels, as a pharmaceutical product for the prevention and treatment of the effects of oxidation, of elastase and of free radicals on the skin, or alternatively as an agent having an activity of protecting DNA against damage, especially oxidative damage.

The subject of the invention is also a method of cosmetic treatment comprising the application of an antioxidant or antielastase composition or of a cosmetic composition according to the invention on the skin surface of an individual.

Under another aspect, the invention relates to a cosmetic or pharmaceutical composition comprising a composition according to the invention, preferably in combination with a physiologically acceptable vehicle.

The cosmetic or pharmaceutical compositions thus defined are capable of being used in particular as an antisun product for protecting against UVB and/or A radiation and/or infrared radiation, a restructuring or toning cream, a product, especially a cream, for the prevention and the regression of vibices, a nutritive cream, antiwrinkle cream (for combating aging of the skin, epidermis and dermis) and protective day cream, contour of the lips and of the eyes, regenerative and protective lipsticks. For these uses, the cosmetic compositions according to the invention are advantageously formulated for a topical use, especially in the form of creams, emulsions, ointments, sticks or gels.

The cosmetic or pharmaceutical compositions according to the invention may have a total content by Weight of lupine oil or its fractions and wheatgerm oil or its fractions of the order of 0.5 to 10% approximately, preferably from about 1% to about 5%.

The antioxidant activity of the compositions according to the invention, demonstrated by the oxidation-stability especially of the lupine oil and of the corresponding concentrate, is particularly advantageous because it offers possibilities of additional uses as a dietary supplement taking advantage of this antioxidant activity.

Finally, the subject of the invention is also a process for preparing the compositions described above. Different variations may be envisaged depending on the compositions. Thus, for example, there may be mentioned:

the mixture of two concentrates of lupine oil and of wheatgerm oil as obtained by the molecular distillation method, for example, as described in the review "Parfumerie Cosmetique et Arome" [Cosmetic Perfumery and Fragrance] (1985, No. 61, page 91-96);

the preliminary mixing of lupine and wheatgerm oils followed by molecular distillation of the mixture according to the process described above;

the mixture of lupine oil and of a wheatgerm oil concentrate obtained by molecular distillation.

The wheatgerm oil concentrate is advantageously prepared according to the molecular distillation process described in Patent FR 92 07830. According to this process, the oil is spread in a thin layer on the heated surface of a conical rotor revolving at high speed. A high vacuum is maintained in the distillation chamber. Under these conditions, there is evaporation, and not boiling, from the hot surface, of the constituents of the unsaponifiable matter whose separation becomes possible in relation to the glycerides, the advantage being that the oil and the unsaponifiable matter, which are reputed to be fragile, are not degraded during the operation.

Claim 1 of 29 Claims

What is claimed is:

1. A composition comprising lupine oil or one or more of its fractions for use as an antioxidant and/or antielastase.

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