NL8800691A - DIETARY PREPARATION AND METHOD FOR PREPARING IT. - Google Patents

Description

NL 34928-Kp / vD 'v »* Dietary preparation and process for its preparation.

The present invention relates to dietary preparations.

In another aspect, the invention relates to a process for the preparation of such compositions.

It is known that the C | g_22 ω “3 unsaturated fatty acids have favorable biological properties. Among these substances, eicosapentanoic acid (EPA) and docosahexanoic acid (DHA) are excellent; the importance and multiple biological activity of both acids have been discussed by Dyerberg et al. / The Lancet 1_5, 117 (19 78) _7 -

The actions associated with the important role of the polyunsaturated fatty acids, mainly EPA and DHA, in hyperlipidaemia and thrombotic disorders have been discussed by Goodnight et al. / Arteriosclerosis 2, 87 (1982).

The active components of the fish oil, eicosapentanoic acid (EPA) and docosahexanoic acid (DHA), are precursors for the biosynthesis of the PG-3 series and at the same time they are competitive inhibitors of harmful metabolites, such as TXA2 and TXB2, from the so-called "arachidone acid stage, which is a chain of complex biochemical processes starting from arachidonic acid.

After many beneficial effects, a drawback of the polyunsaturated fatty acids is that they are a potential source of the particularly deleterious malondialdehyde (MDA) formed by radical peroxidation processes involving the so-called "ceroidal lipofuscinosis". central nervous system can be induced.

The utilization of EPA for food in the form of a cyclodextrin inclusion complex is described in French Patent No. 2,550,445.

Marschall et al. / Am. J. Clin. Nutr. 38, 895 (1983), 7 have studied the role of ω-3 polyunsaturated fatty acids in the synthesis of α-linolenic acid and prostaglandins as well as in dietary foods.

In addition to EPA and DHA, the fish oils contain significant amounts of saturated and low saturated fatty acids as well as .8800691 - 2 - ·>

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1 »non-hydrolyzable components, the removal of which is very important, since blood triglyceride levels and caloric intake are sensitively enhanced by the increase in dietary dose. In addition, steroids which are harmful from a dietary point of view, e.g. cholesterol as well as vitamin D (its precursor) and vitamin A, both susceptible to accumulation in the human organism, may also be present among the non-hydrolyzable components.

The dietary activity of the ω-3 polyunsaturated fatty acids and mainly EPA and DHA in relation to their frequent physiological connections have been discussed in many other publications ^ see eg ü. Barcelli: Thromb. Res. 39, 307 (1985); J.J. Jurkowski: JNCI 74, 1145 (1985); A.

15 Lembke: Milchwissenschaft £ 0.329 (1985).

It is further known that algae have been used by humans for nutritional and feed purpose for quite some time. Algae are mainly consumed by peoples from the Far East; more recently, however, they have also been used in dry or tablet form in developed countries.

Algae are the carriers of very valuable food materials, since their dry form contains in high concentration substances essential for a healthy life, such as vitamins, proteins, complexes of proteins with microelements, saccharides, polyunsaturated fatty acids and the like .

For example, a general and detailed overview of algae can be found in Zajic's book "Properties and 30 Products of Algae" (Edition Planum, New York, 1970).

Research into the biological effect of microelements and trace elements has been started in the last decades. It was hereby recognized that selenium is one of the most important essential substance in the living mechanism. The beneficial effect of selenium lies mainly in the activation of the glutathione peroxidase enzyme and more precisely in the activation of the prosthetic group of the enzyme, which is the most important endogenous inhibitor of the harmful processes. Selenium is produced in the human organism. 8 8 0 06 9 1 Ϋ · - 3 - not accumulated? as a result, selenium should be continuously supplemented. Selenium has hitherto been available in the form of inorganic compounds, mainly as selenium dioxide or sodium selenite.

5 Selenium as such has a hypotensive effect, improves the ischemic, hypoxic and infarct states of the heart and inhibits ceroid lipofuscinosis of the central nervous system? moreover, selenium has a favorable effect on periodontitis and has the chance of developing cancer diseases been reduced? in addition, selenium is considered as a mutagenic inhibitor. A number of abnormalities or diseases, such as hepatic necrosis, myonecrosis, destruction of the erythrocyte membrane, interstitial lesions, STG elevation in the ECG, kashiorcor syndrome (protein malnutrition) and multiple sclerosis have been shown to be induced by selenium deficiency.

A review of the biological action of selenium was published by Thressa et al. / Nutrition Review 35 ^ 7 (1977) J, R.I. Shamberger / J. or Env. Path, and Tox. 4, 305 20 (1980} /; and Masukawa et al / Êxperientia 39_, 405 (1983) 7 *

The object of the present invention is to develop a dietary preparation which removes the disadvantages of the biological action of the consumption of polyunsaturated fatty acids, while providing the combination of the beneficial properties of EPA, DHA, algae and selenium, which preparation based on its composition is able to balance at least part of unhealthy life behavior and adverse dietary habits.

The invention is based on the recognition that the above objectives can be fully achieved using a food composition containing a selenium-containing algae in addition to polyunsaturated fatty acids.

Accordingly, the present invention relates to dietary preparations characterized in that they contain 0.5 to 35% by weight of selenium-containing algae as well as 99.5 to 50% by weight of C-yg-22 unsaturated fatty acids with at least two double bonds or their derivatives, together with additives commonly used in the food industry, and optionally an antioxidant.

.8800691 Ύ - 4 - <1

The invention furthermore relates to a process for the preparation of the above-mentioned dietary preparation, characterized in that 0.5 to 50% by weight of selenium-containing algae and 99.5 to 50% by weight of c-yq -22 unsaturated (3- ige fatty acids.

5 with at least two double bonds or their derivatives were mixed with additives commonly used in the food industry and optionally with an antioxidant.

The selenium-containing alga is prepared in the manner as described in the associated patent application No. 10 Serial No. .......... (Hungarian patent application No. 575/88).

The starting material for the unsaturated fatty acids, which serve as active ingredients of the preparation, may be the oils from various sea or freshwater fish, mainly the oils of mackerel, cod, herring, sardine and squid as well as oils, which can be obtained from the liver of these fish, such as cod liver oil and shark liver oil.

As algae, mainly Chlorella or Scenedes mus strains are used, which are not only suitable for human consumption, but also have their own favorable biological effect.

The preparation is sensitive to oxidation. It is therefore suitable to use an active preservative, eg α-tocopherol (vitamin E), glutathione or a traditional antioxidant such as butylhydroxytoluene.

The homogenized preparation can be included in food products, tablets, capsules and the like. Here, the term "food product" means any useful products that can be administered orally or parenterally. The orally administered product may be in a confectionery (eg chocolate, cake), meat or butchery preparations, spices, margarine, milk, butter or fat products, oils and the like.

The main advantages of the preparation according to the invention can be summarized as follows.

a) Individual components of the preparation have important biological and nutritional properties per se and combine the beneficial properties of EPA and DHA as well as of selenium and algae.

.8800691-5 - if b) The composition according to the invention eliminates the possibility of "ceroidal lipofuscinosis", which occurs with the consumption of polyunsaturated fatty acids.

C) The use of a continuous dietary regimen is not necessary due to the consumption of the composition according to the invention, since it does not contain the above-described harmful fish oil components (saturated fatty acids, cholesterol, vitamins A and D).

D) Selenium is present in its natural form, enriched with algae, i.e. as a material of natural origin.

e) It is useful to prevent apoplectic and thromboembolic states of the cardiovascular system in order to prevent the development of infarction and apoplexy as well as to prevent atopically related or atopic abnormalities. The use of the preparation is moreover particularly favorable under developed conditions.

The preparation according to the invention is further elucidated by means of the following non-limiting Examples. The preparation of the ingredients used as basic materials is shown in Examples I, II and III, while the preparation of the preparations is described in the remaining Examples.

EXAMPLE I

10 kg of sardine oil was added at a temperature of 50-60 ° C to a solution of 2 kg of sodium hydroxide in 70 l of 95% ethanol. The mixture was then heated to reflux under nitrogen for 2 hours, then cooled to 10 ° C with stirring. The precipitated crystalline sodium salt of the saturated fatty acid was filtered off and washed with a little ethanol. The ethanolic filtrate was evaporated and 20 L of boiled water was added to the residue. The non-hydrolyzable compounds, such as cholesterol, were removed by extraction with 5 L of hexane. The extracted aqueous phase was acidified to a pH of 2 by adding dilute sulfuric acid and then extracted again with 151 hexane.

The organic phase was washed with water, dried over anhydrous .8800691 *% - 6 - sodium sulfate and evaporated to yield 3.2 kg of an oil concentrate with a DHA content of 36.8% and an EPA content of 31.8 %. This oil is brown and smells like fish. Thus, Fuller's soil was mixed with the oil-5 concentrate, which was then heated to 105 ° C under nitrogen for 10 min and filtered off hot. Deodorization was carried out by steam distillation under reduced pressure of 1.3 bar at 170 ° C for 3 hours to yield 1.6 kg of a pale yellow, odorless and tasteless oil with a practically unaltered composition.

EXAMPLE II

24 kg of cod liver oil were dissolved in 16 l of methanol at 60 ° C, after which 8 kg of 40% sodium hydroxide solution was added dropwise to this solution at a temperature between 50 and 60 ° C with stirring. The mixture was stirred at 60 ° C for an additional 45 min. Then 20 kg of 15% hydrochloric acid was added to the solution at about 60 ° C. After separation of the phases, the organic layer was extracted with 10 kg of 15% hydrochloric acid and then washed with about 180 l of warm tap water until neutral. The phases were separated and 100 L of acetone was added to the oil phase. The mixture was heated to about 45 ° C, after which a solution of 3.8 kg of lithium hydroxide monohydrate in 30 L of water was added.

After stirring for 30 min, the mixture was left overnight, followed by filtration, and the acetone filtrate was evaporated. The residue was acidified by adding 8 kg of 15% hydrochloric acid, then extracted three times with hexane and finally evaporated. The entire purification operation was performed under nitrogen.

This yielded 6.4 kg of purified fish oil with an iodine value of 258 and an acid number of 160.

1 kg of the cod liver oil thus purified was added dropwise to the solution of 3 kg of urea at 60 ° C in 9 l of methanol. The mixture was stirred at the same temperature for 2 hours. After cooling, the mixture is stored in a refrigerator at -18 ° C overnight, after which the mixture is filtered and the filtrate evaporated. Then 2.5 L hydrochloric acid (concentrated acid diluted 1: 1 with water) was added to the residue and the .8800631 * 4-7 mixture was stirred for an additional 15 min. After extracting with hexane, the organic phase was washed with water until neutral, then dried over anhydrous sodium sulfate and evaporated to yield 0.34 kg ω ~ 3 fatty acids with an iodine value of 315, EPA content of 24% and a DHA content of 42%.

EXAMPLE III

81 Bud-Pringsheim's culture medium was transferred to a 10 L algae culture glass bottle, into which 40 mg of sodium selenite was transferred. The system was sterilized at 121 ° C under an overpressure of 1 bar for 30 min.

The sterile solution was inoculated with a pure algae culture of selenium resistant Scenedesmus obtisiusculus. Sterile air containing 5% by volume of carbon dioxide was bubbled through the culture medium at 25 ° C under illumination with an electric discharge lamp operating at 4000 lux as well as at a wavelength of 440 to 520 and 640 to 700 yam. After a 14-day culture period, the alga was separated from the culture medium. .

The algae mass thus obtained was decomposed under the influence of sound waves at a temperature below 65 ° C, yielding 6 g of an algae powder with a selenium content of 1200 µg / g.

EXAMPLE IV

100 g of selenium-containing algae (with a selenium concentration of 260 yag / g of algae powder) was added with stirring to 150 g of an enriched cod liver oil (containing 22% EPA and 43% DHA). After homogenization, the mixture was preserved by adding 0.2% by weight of vitamin E.

EXAMPLE V

Preparation of a diet margarine preparation.

30 8 g 65% cod liver oil (containing 22% EPA and 43% DHA) and 1 g selenium containing algae (with a selenium concentration of 260 yag / g algae powder) were mixed with 250 g soft margarine, after which the mixture was homogenized.

EXAMPLE VI

The procedure described in Example IV was repeated, except that the following amounts of the starting materials were used: 400 g of 65% enriched cod liver oil (containing 22% EPA and 43% DHA); 8800691 * - 8 - ft * 70f6 g algae powder containing 1200 µg / g selenium; and 0.4 g of vitamin E.

The homogenate thus obtained was transferred into soft gelatin capsules or soft gelatin pearl-5 capsules with a capacity of 500 mg, after which they were packed in a blister pack.

EXAMPLE VII

Tablets of the following composition were prepared using known pharmaceutical devices and methods:

Cod liver oil enriched in EPA and DHA, (DHA content: containing 0.1% vitamin E as 200 mg con- 200 mg; serving EPA content: 22%) 15 selenium-containing algae 86 mg (selenium concentration: 380 µg / g algae powder) lactose 140 mg 20 starch 60 mg polyvinylpyrrolidone 3.5 mg magnesium stearate 3.5 mg

If desired, the tablets can be coated with sugar in a pelleting machine.

8800691

Claims (5)

Dietary preparation, characterized in that it contains 0.5 to 50% by weight of selenium-containing algae and 99.5 to 50% by weight of C-8-22 unsaturated fatty acids with at least two double bonds or their derivatives mixed with additives. Additives commonly used in the food industry and optionally with an antioxidant. Preparation according to claim 1, characterized in that the fatty acid derivatives are esters, alkaline earth metal salts or amine salts. 3. Preparation according to claim 1 or 2, characterized in that this preparation contains as unsaturated fatty acids 5,8,11,14,17-eicosapentanoic acid and 4,7,10,13,16,19-docosahexanoic acid. 4. A composition according to claim 1, characterized in that it contains as unsaturated fatty acids fatty acids obtained from sea fish oil. Process for the preparation of a dietary preparation according to claim 1, characterized in that 0.5 to 50% by weight of selenium-containing algae as well as 99.5 to 20% by weight of q22 unalloyed fatty acids with at least two double bonds or their derivatives are mixed with additives commonly used in the food industry and optionally with an antioxidant. 8800691