Process for the preparation of a solid dispersion of at...

Drug – bio-affecting and body treating compositions – Live skin colorant containing – Lip

Reissue Patent

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C106S270000, C252S391000, C424S059000, C424S063000, C424S401000, C424SDIG005, C514S784000, C514S785000, C514S787000, C514S844000, C514S943000

Reissue Patent

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RE037198

ABSTRACT:

The present invention relates to a process for preparing a solid dispersion containing, in the dispersed state, a significant amount of polyhydric alcohol (“polyol”) in a fatty body, the resulting dispersion being intended for cosmetic or pharmaceutical use.
Cosmetic or pharmaceutical solid fatty products, conventionally employed principally in the form of sticks, for example, lip sticks, exhibit the disadvantage of not having hydrating characteristics.
To reduce this disadvantage, attempts have been made to incorporate water when preparing these emulsified products.
In this regard mention can be made of French patent application No. 73 26446 (2.237.615) which describes a water-in-oil emulsion containing 1 to 50 percent by weight of water.
However, this type of composition poses water evaporation problems.
The composition described in this patent application also contains from 1 to 10 percent of a polyhydroxylated compound in order to obtain a uniform distribution of the dye substances in the water-in-oil emulsion.
The water evaporation problem of solid dispersions has been resolved, according to European patent application No. EP 374.332, by incorporating a silicone oil as well as an organopolysiloxane modified by a polyoxyalkylene.
The compositions thus modified can also contain small amounts of polyols as additional humectants.
However, no product containing water in any substantial amount has yet to be commercialized at the present time simply because of water loss problems which appear not yet to have been resolved in a satisfactory manner.
According to Japanese patent application publication No. 1-143.812, there is described the incorporation of a significant amount of polyvalent alcohols in a solid emulsion for cosmetic use by the expedient of a silicone oil and modified polyoxyalkylenated organopolysiloxane as an emulsifying agent.
Now, with this system, it is difficult to obtain good homogeneity of the formulation.
One goal of the present invention is to reduce the difficulties described above.
Following various studies, it has been noted, in an unexpected and surprising manner, that a significant amount of polyhydric alcohol can be incorporated in a solid dispersion by the use of, during the incorporation, a turbine rotating at a minimum speed which produces very small size particles.
The present invention relates then to a process for the preparation of a stable andanhydrous solid dispersion comprising from 20 to 95 percent and, preferably, from 40 to 85 percent of a fatty body, constituted by 10 to 50 percent of at least one wax having a melting point greater than 55° C., and from 4 to 50 percent of a dispersed polyhydric alcohol, preferably from 6 to 40 percent, and more particularly from 8 to 25 percent, characterized in that the said fatty body and the polyhydric alcohol are heated to a temperature between 65° and 95° C. and that a turbine operated at a rotation speed of at least 1500 rpm and preferably, between 2500 and 3500 rpm is employed to mix these heated components.
By the expression “solid dispersion” is meant a composition which is solid at a temperature between 0° and 50° C., which temperature corresponds to that of storage temperature and the temperature at which the cosmetic compositions is employed.
The present invention also relates a stable and anhydrous solid dispersion comprising from 20 to 95 percent of a fatty body, constituting the continuous phase, and from 4 to 50 percent, preferably, from 6 to 40 percent and more particularly from 8 to 25 percent, of a dispersed polyhydric alcohol characterized in that the average size of the polyhydric alcohol particles is less than or equal to 1 &mgr;m and preferably between 0.01 and 0.8 &mgr;m and in that the fatty body is constituted by 10 to 50 percent by weight of at least one wax having a melting point greater than 55° C.
The dispersion according to the present invention provides cosmetic products having excellent emollient properties on application to the skin.
The solid dispersion according to the invention are employed in molded fatty products such as lip rouge, complexion foundations, eye shadow formulations, cheek rouge and principally in products in the form of sticks.
According to one preferred embodiment, the solid dispersion, according to the invention can also contain up to 10 percent of a mineral or organic charge or filler such as talc, starch and the like.
It is also possible that the dispersion, according to the invention, contain up to about 30 percent (preferably from 0.1 to 20 percent) of a pigment and from 0.01 to 20 percent (preferably from 0.5 to 10 percent) of a hydrocarbon surfactant. The use of a hydrocarbon surfactant provides a finer dispersion and thus a more satisfactory stick.
In accordance with a more particularly preferred embodiment, it is possible to add to the dispersion, according to the invention, a sufficient amount of copolymer for increased stabilization against a moist atmosphere.
Such polymers must be liposoluble and have a low amount of hydrophilic units.
Among these, mention can be made of polyalkylenes (principally polyethylenes and polybutenes), polyacrylates and silicone polymers compatible with fatty bodies.
Among the polyalkylenes mention can be made of polybutene, principally that sold by Amoco under the trade name INDOPOL.
The weight ratio of the polymer to the polyhydric alcohol is generally less than 4 and is, preferably, between 0.25 and 2.
In accordance with the invention, the polyhydric alcohol can be a compound having 2-8 carbon atoms and from 2 to 6 hydroxy functions. Among these compounds mention can be made of ethylene glycol, glycerine, 1,2-propanediol, diglycerine, erythritol, arabitol, adonitol, sorbitol and dulcitol.
The polyhydric alcohol can also be a polyether alcohol having an average molecular weight between 150 and 600 and among these mention can be made of polyethylene glycol 300 and polyglycerine 500.
The polyhydric alcohol can optionally be enriched with hydrosoluble active agents such as amino acids (for example arginine, lysine, proline and serine), vitamins such as D,L Panthenol and sunscreen agents. These can be present in an amount of from 0.05 to 5 percent.
As indicated above, the fatty body in accordance with the invention is constituted of 10 to 50 weight percent of at least one wax whose melting point is greater than 55° C., the remainder being either a wax having a melting point lower than 55° C. or an oil or a mixture thereof. The final melting point of the entire mixture must be lower than 110° C. which does not preclude the use of certain constituents of the mixture having a higher melting point.
Among waxes having a melting point greater than 55° C., capable of being employed in accordance with the invention, mention can be made of animal, vegetable, mineral and synthetic waxes and various fractions of natural waxes, all these waxes having, as a general rule, a melting point between 55° and 110° C., and a needle penetration value, at 25° C., between about 3 and 40, as measured in accordance with the American standard, ASTM D5 or the French standard, NFT 004. The principle of the needle penetration measurement according to these two standards consists in measuring the depth, expressed in tenths of millimeters, at which penetrates a standardized needle (weighing 2.5 g, placed in a needle holder weighing 47.5 g, or a total of 50 g), placed on the wax for 5 minutes.
Among the animal waxes that can be employed, mention can be made, among others, of beeswax, lanolin wax, china insect wax and lanolin derivatives. Representative vegetable waxes include, among others, Carnauba wax, Candelilla wax, Ouricurry wax, cork fiber wax, sugar cane wax and Japan wax. Representative mineral waxes, include, in particular, paraffins, microcrystalline waxes, lignite waxes (Montan wax) and ozokerites. Representative synthetic waxes include, in particular, polyethylene waxes, waxes obtained by Fischer-Tropsch synthesis, and waxy polymers as well as their esters. All these waxes are well known to those skilled in the art.
Among the waxes ha

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