Lipid mixtures and their use

08-11-2001 дата публикации
Номер:
AU0000740624B2
Принадлежит: Johnson and Johnson GmbH
Контакты:
Номер заявки: 21-25-19992
Дата заявки: 02-02-1999

[1]

Lipid mixtures and their use The invention relates to lipid mixtures having a physiologically effective amount of polyunsaturated fatty acids and/or derivatives thereof and also to their use as such or in cosmetic or pharmaceutical preparations for topical application to the skin. The principal task of topically applied lipids, in the cosmetic or pharmaceutical field, is to enhance the barrier function, i.e. the protection function, of the skin and thus to prevent it from drying out or to prevent the entry of foreign substances. They also serve to improve the suppleness of the skin, the condition of its surface and its appearance. Moreover, substances present particularly in natural lipids, e.g. saturated and unsaturated fatty acids, lecithins, ceramides, etc., play an important role in physiologica! processes, e.g. metabolism, irritation, inflammation, allergic reactions, etc. The barrier function is often enhanced by using occlusive substances, e.g. paraffin oil and vaseline, which, although preventing the skin from drying out to a certain degree, are not, however, able to contribute to the physiologica! processes in the skin. Furthermore, their use is cosmetically unacceptable since they have poor spreadability and poor absorption and impart a greasy feel to the skin. Natura! lipids are able, depending on the composition, to influence skin physiology, but they are more difficult to spread than the specified occlusive substances, cannot be distributed particularly well and are absorbed more slowly than, for example, paraffin oil. US-A-5,445,822 describes a cosmetic composition comprising triglycerides containing from 40 to 70% of oleic acid, from 30 to 50% of polyunsaturated fatty acids, from 0.2 to 1% of 7-1inolenic acid and from 1 to 5% of -linolenic fatty acid, the ratio of n-6 fatty acids to n-3 fatty acids being from 10:1 to 30:1. There is no mention of the application properties, nor is there a further explanation as to the physiological effects of the composition. Any discussion of the prior art throughout the specification should in no way be considered as an admission that such prior art is widely known or forms part of common general knowledge in the field. It is an object of the present invention to overcome or ameliorate at least one of the disadvantages of the prior art, or to provide a useful alternative. In a broad aspect, the present invention comprises a lipid mixture having a physiologically effective content of polyunsaturated fatty acids and/or derivatives thereof, comprising an effective content of modified coconut oil which essentially comprises C10 to C14 fatty acids in the form ofmono-, diand triglycerides and has a cloud point of<5°C. Unless the context clearly requires otherwise, throughout the description and the claims, the words 'comprise', 'comprising', and the like are to be construed in an inclusive sense as opposed to an exclusive or exhaustive sense; that is to say, in the sense of "including, but not limited to". Preference is given to a lipid mixture in which the modified coconut oil is present in a concentration of from 5 to 40%, preferably from 10 to 30%, particularly preferably from 15 to 25%, based on the total weight of the lipid mixture. The polyunsaturated fatty acids advantageously comprise linoleic acid and - linolenic acid. It is intended that the ratio of linoleic acid to -linolenic acid, in precent by weight, is between 15:1 and 5:1, preferably between 13:1 and 7:1, particularly preferably between 11:1 and 9:1. It is intended that the polyunsaturated fatty acids are essentially present in the form of their triglycerides. Natural triglycerides having a high content of polyunsaturated fatty acids are advantageously present. According to a particular embodiment of the invention, the polyunsaturated fatty acids are prepared using soybean oil, sunflower oil, wheat germ oil, linseed oil, thistle oil, China oil, grapeseed oil, sesame oil or mixtures thereof. It is advantageous to use a mixture of at least two of the specified oils. The invention further relates to the use of the lipid mixture according to the invention as such Finally, the invention also relates to the use of the lipid mixture according to the invention as or in a pharmaceutical preparation for topical application to the skin, in particular for the treatment of dry skin, neurodermatitis, atopic eczema and similar skin conditions. Surprisingly, it has been found that the lipid mixture according to the invention has better application properties than the known occlusive substances, such as, for example, paraffin oil and vaseline, Or individual natural oils, and at the same time contributes to improving the physiologica! condition of the skin. An essential component of the lipid mixture according to the invention is a modified coconut oil, which essentially comprises CI0-C14 fatty acids in the form of mono-, diand triglycerides, and has a cloud point of < 5°C. A modified coconut oil of this type is known under the INCI name "cocoglycerides" and is commercially available, for example under the name Myritol 331. It is advantageously used in a concentration of from 5 to 40%, preferably from i0 to 30% and particularly preferably from 15 to 25%, based on the total weight of the lipid mixture. A direct comparison with the compositions in the aforementioned US-A-5,445,822 has shown that the triglycerides comprising oleic acid mentioned therein do not improve the application properties in this way. Moreover, the oxidation stability of the coconut oil used according to the invention is significantly higher than that of the triglycerides listed in the cited US Patent. The physiologically effective components used are lipids having a high content of linoleic acid and - linolenic acid, where the ratio of linoleic acid to - linolenic acid, in percent by weight, is between 15:1 and 5:1, preferably between 13:1 and 7:1 and particularly preferably between Ii:i and 9:1. Linoleic acid and - linolenic acid can either be used as such or in the form of their derivatives, e.g. monoesters, triglycerides or amides, etc. Triglycerides having a high content of linoleic acid and -linolenic acid are present in natural oils, such as, for example, soybean oil, sunflower oil, wheat germ oi!, linseed oi!, thistle oil, China oil, grapeseed oil or sesame oil. Particular preference is given to soybean oil, sunflower oil, wheat germ oil, linseed oil, thistle oil or China oil, with soybean oil, sunflower oil, wheat germ oil and linseed oil being the most preferred. In particular, it is possible to use mixtures of at least two of the specified oils. In addition, ylinolenic acid can be added to the lipid mixture as it is or in the form of oils such as starflower oil or evening primrose oil. It is preferable to add an antioxidant to the lipid mixtures. The antioxidants which are primarily suitable for this purpose are oil-soluble ones, such as, for example, tocopherol, mixtures of different tocopherols, ascorbyl palmitate, BHT, BHA and mixtures thereof, optionally with the addition of synergists, such as lecithin etc. Antioxidants of this type are commercially available, for example under the names Oxynex, Covi-ox T70 or Controx. Furthermore, it is possible to add other auxiliaries or additives, such as, for example, perfume or the like. The lipid mixtures according to the invention are either used as such, e.g. as body oils for cosmetic or pharmaceutical use, or as oil phases or constituents of oil phases in cosmetic or pharmaceutical preparations, such as, for example, emulsions of the water-in-oil type or of the oil-in-water type, microemulsions, nonaqueous preparations in the form of pastes, sticks, ointments, oil baths, hydrosurfactant preparations such as care shampoo and shower gels, etc. Substances which are customarily used in the formulation of such preparations can be added to the corresponding cosmetic or pharmaceutical preparations. These include, inter alia, emulsifiers, surfactants, emollients, structure formers, etc. Furthermore, it is possible, depending on the desired use, to incorporate further active substances, e.g. light protection filters, antibacterial substances, antiperspirants, deodorants, etc. The lipid mixtures according to the invention and the cosmetic or pharmaceutical preparations prepared therefrom are notable for excellent absorption, good spreadability and distribution properties and impart an exceptionally good and smooth feel to the skin at the same time as being very well tolerated. They are suitable, in particular, for use with dry skin, neurodermatitis, atropic eczema or similar skin conditions. People who suffer from atropic eczema usually avoid oiland fat-containing skincare products since such products worsen the condition of the skin rather than improve it. Surprisingly, it has now been found that the lipid mixtures according to the invention in the form of body oils or emulsions are not only very well tolerated by people with atopic eczema but that the disease phenomena can be reduced and the condition of the skin significantly improved. In an application test using a body oil according to the invention, participants who suffered from atopic eczema reported that the red areas and centres of inflammation disappeared within one week. People with dry skin reported a significant increase in the elasticity of the skin and a normalizing of the condition of the skin. The invention is illustrated in more detail below with reference to typical lipid mixtures and products prepared therefrom. Examples 1 to 6 give lipid mixtures according to the invention which were prepared by thoroughly mixing, by stirring, the individual components in the order given in a stainless steel container. Example i: Modified coconut oil 15.00% by weight Soybean oil 43.17 % by weight Wheat germ oil 41.63 % by weight Example 2: Modified coconut oil 20.00 % by weight Soybean oil 2.51% by weight Sunflower oil 71.89 % by weight Oxynex K 0.10 % by weight Example 3: Modified coconut oil i0 39 % by weight Sunflower oil 71 34 % by weight Linseed oil 6 87 % by weight Thistle oil ii 20 % by weight Oxynex K 0 i0 % by weight Perfume 0 i0 %by weight Example 4: Modified coconut oil 19 89% by weight Soybean oil 56 96% by weight Sunflower oil 12 86% by weight Wheat germ oil I0 00 % by weight Oxynex K 0 15 % by weight Perfume 0 15 % by weight Example 5: Modified coconut oil 19 86% by weight Soybean oil 24 86% by weight Sunflower oil 5O O8% by weight Linseed oil 5 OO% by weight Oxynex K 0 10% by weight Perfume 0 10% by weight Example 6: Modified coconut oil 20.02 % by weight Soybean oil 59.10 % by weight Sunflower oil 16.68 % by weight Wheat germ oil 4.00 % by weight Oxynex K 0.i0 % by weight Perfume 0.i0 % by weight Example 7: An oil-in-water emulsion was prepared by incorporating the lipid mixture from Example 4 into a solution of Pemulen TRI in water and propylene glycol. After the other ingredients, which are given the table below, had been added, the mixture was neutralized using sodium hydroxide solution and homogenized. Lipid mixture from Ex. 4 46 60 % bywelght Tocopheryl acetate 0 l0 % by weight Preservative 1 00 % by weight Pemulen TRI 0 35 % by weight Arlacel 83 0 i0 % by wexght Water 50 35 % by weight Propylene glycol 1 00 % by weight Na hydroxide 0 50 % by weight An oil according to Example 4 was tested by a panel of experts for its application properties compared with paraffin oil and individual natural oils. The properties of spreading and distribution were judged to be significantly better compared with the individual natura! oils; the properties of skin smoothness and absorption were significantly better compared with paraffin oil and the individual natural oils. The features of the invention disclosed in the description above and the claims may be essential either individually or in any combination for implementing the invention in its different variants.



[2]

(57) Abstract Lipid mixture having a physiologically effective content of polyunsaturated fatty acids and/or derivatives thereof, having a physiologically effective content of modified coconut oil which essentially comprises C10-C14 fatty acids in the form of mono-, diand triglycerides and has a cloud point of < 5 °C, and the use thereof as or in a cosmetic or pharmaceutical preparation.



1. Lipid mixture having a physiologically effective content of polyunsaturated fatty acids and/or derivatives thereof, comprising an effective content of modified coconut oil which essentially comprises C10 to C14 fatty acids in the form ofmono-, diand triglycerides and has a cloud point of<5°C.

2. Lipid mixture according to Claim 1, wherein the modified coconut oil is present in a concentration of from 5 to 40%, based on the total weight of the lipid mixture.

3. Lipid mixture according to Claim 1 or 2, wherein the modified coconut oil is present in a concentration of from 10 to 30%, based on the total weight of the lipid mixture.

4. Lipid mixture according to any one of the previous claims, wherein the modified coconut oil is present in a concentration of from 15 to 25%, based on the total weight of the lipid mixture.

5. Lipid mixture according to any one of the previous claims, wherein the polyunsaturated fatty acids are linoleic acid and cx-linolenic acid.

6. Lipid mixture according to any one of the previous claims, wherein the ratio of linoleic acid to ct-linolenic acid, in percent by weight, is between 15:1 and 5:1.

7. Lipid mixture according to any one of the previous claims, wherein the ratio of linoleic acid to cz-linolenic acid, in percent by weight, is between 13:1 and 7:1.

8. Lipid mixture according to any one of the previous claims, wherein the ratio of linoleic acid to cx-linolenic acid, in percent by weight, is between 11:1 and 9:1.

9. Lipid mixture according to any one of Claims 4 to 8, wherein the polyunsaturated fatty acids are essentially in the form of their triglycerides.

10. Lipid mixture accordingly to Claim 9, wherein natural triglycerides having a high content of polyunsaturated fatty acids are present.

11. Lipid mixture according to Claim 10, wherein the polyunsaturated fatty acids are prepared using soybean oil, sunflower oil, wheat germ oil, linseed oil, thistle oil, China oil, grapeseed oil, sesame oil or mixtures thereof.

12. Lipid mixture according to Claim 11, wherein a mixture of at least two of the specified oils is used.

3. Use of a lipid mixture according to one of the preceding claims as or in a cosmetic eparation.

14. Use of a lipid mixture according to any one of Claims 1 to 12 as or in a pharmaceutical preparation for topical application to the skin.

15. Use according to Claim 14 for the treatment of dry skin, neurodermatitis, atopic eczema and similar skin conditions.

16. A lipid mixture substantially as herein described with reference to any one of the embodiments of the invention illustrated in the accompanying drawings and/or examples.

17. Use of a lipid mixture in a cosmetic preparation substantially as herein described with reference to any one of the embodiments of the invention illustrated in the accompanying drawings and/or examples.