RU2251934C2 - Biologically active food additive - Google Patents

Abstract

FIELD: food-processing industry.

SUBSTANCE: biologically active food additive contains pectin, vaseline oil, flavor additive, preservative, polysaccharide and distilled water. Polysaccharide is selected from the group comprising agar-agar, agaroid, agaropectin, starch, and vegetable gum. Components are introduced in predetermined ratio into additive composition.

EFFECT: prolonged storage time and enhanced toning, antioxidant and immuno-modeling effect of additive.

2 cl, 1 dwg, 2 tbl

Description

The invention relates to biologically active food additives of the parapharmaceutical series, in particular to dietary supplements of therapeutic and prophylactic effect, contributing to the regulation of intestinal microbiocenosis, the functional activity of the liver at physiological boundaries and the restoration of natural lipid metabolism in the human body.

To determine the achieved level in the field under consideration, patents were studied for the corresponding classes of the International Classification and publications of leading experts over the past decade. Our patent information search and our previous studies in this direction have oriented us towards the development of dietary supplement for polysaccharide-oil composition.

It is known to use polysaccharides of various nature in dietary supplements and medicines to normalize the gastrointestinal tract / GIT /, stimulate its motor-secretory and evacuation functions, improve the intestinal microflora due to the sorption of certain toxins, metals, radionuclides and other substances harmful to the body. This ability to a certain extent applies both to pectins (A.P. Nechaev and other food additives - study guide, M., Kolos-Press, 2002, p. 66-67), and to a number of other polysaccharides (V.A. Tutelyan, B.P. Sukhanov and other biologically active additives in human nutrition, Tomsk, NTL, 1999, p.23).

RF patent 2104660, 1998, IPC A 23 L 1/30, 1/29; A 61 K 35/78, 7/00, the biologically active additive VIVATON C is protected for use in a number of industries, including the medical one, which has versatile biological properties. It is recommended for diseases of the gastrointestinal tract, nervous, endocrine and cardiovascular systems, as a radio and cancer protector.

The additive consists of vitamins, minerals (metal or phosphorus), food organic acids, glycosides and carbohydrates (mono-, di-, oligo- and polysaccharides) in the ratio, respectively (0.3-1.5) :( 0.45- 2.0) :( 1.0-3.0) :( 0.49-5.0) :( 0.5-2.9). Of the polysaccharides named glycogen, inulin, starch, fiber. Physiologically and biologically active substances — FAA and BAS — can additionally be introduced into its composition. The latter include brown and red algae, substances from them, as well as bran, gelling agents, such as pectin, guar, plant cellulose.

For the production of therapeutic and prophylactic agents, in particular suppositories, the ratio of carbohydrates to other components should be maintained within the range of 1-1.3, while preparing food jelly 1.2 -2.9. Thus, in all cases (when converted to percentage), the total amount of the carbohydrate portion in the patented dietary supplement ranges from 16.8 to 24.6 wt.%

55 names of plants serve as raw materials for this composition, with the addition of FAV and BAS, another 23 species.

When evaluating all the useful properties of the considered dietary supplement, it should be noted that its multicomponent composition has a different purpose and cannot solve the problems that our experts have faced. In addition, the high content of the carbohydrate part is noteworthy, even without additional introduction of physiologically and biologically active components into the composition.

Also known is a composition for food supplements (US Pat. RF 2141773, 1999, IPC A 23 L 1/30, 1/302, 304; A 61 K 35/78), which includes soluble dietary fiber, invert sugar and pantocrine in the ratio respectively (0.02-3.1) :( 99-45) :( 0.002-0.15). Pectin, alginates, and gelatin are used as dietary fiber, and honey, beet and fruit sugar, and pantocrine of animal origin are used as invert sugars. A preservative is also added to the composition - potassium sorbate, citric acid and, if necessary, a flavoring, for example honey. The content of dietary fiber polysaccharide nature is from 0.022 to 3.13 wt.% (When converted to percent).

Supplements have a pleasant taste and aroma and, according to the authors of the invention, can be used by people suffering from various diseases (see pages 3, 5, 6 of the description).

The technical result of the invention is the production of dietary supplements with tonic, antioxidant, anti-inflammatory, immunomodulating and general strengthening properties. The result is achieved by selecting the optimal ratio of the above components. At the same time, the synergism of the action of the components of the composition on the body is taken into account, which has a beneficial effect on the gastrointestinal tract, increases disease resistance, physical and mental performance of a person.

As for the inclusion of pectin or modified starch (dextrin) as a soluble dietary fiber, these polysaccharides are widely used in many products and dietary supplements for the preparation of jelly, marmalade or, for example, jelly concentrate - Golden Ball nutraceutical (V. B. Spirichev, Materials of the All-Russian Scientific and Practical Seminar, Tomsk, NTL, 2000, p.27).

However, the use of the composition described in RF patent 2141773 is in no way suitable for solving the problems of our invention formulated on pages 6 and 8 of this description.

As the closest in purpose and composition, we have chosen a biologically active drug, proposed in the description of the patent of the Russian Federation 2128991, 1999, IPC A 61 K 9 / 10.9 / 107, which is adopted as a prototype.

The drug can be used for the prevention and treatment of dyslipoproteinemia. Its action is aimed at reducing the absorption of bile acids (FAs) in the small intestine, blocking their enterohepatic circulation, approaching the norm of the lipid spectrum of blood plasma, stabilizing the atherosclerotic process with possible regression of atherosclerosis.

The composition of the emulsion preparation according to the prototype in wt.%:

liquid paraffin 40-84

pectin 0.1-6.0

methyl or carboxymethyl cellulose

(second polysaccharide of a different structure) 0.1-10

flavoring 0.1-20

preservative 0.01-0.07

distilled water - the rest

The composition may be added flavoring and sweetener non-sugar nature.

According to the description of the invention, the combination of components provides the therapeutic and prophylactic effect of the drug and “increased aggregative and sedimentation stability of the emulsion system” by introducing into the proposed preparation a second polysaccharide — cellulose ethers such as methyl or carboxymethyl cellulose. According to the authors, they are effective emulsifiers along with pectin (see page 5 of the description of the invention).

However, according to the code classification, neither pectin [E440] nor carboxymethyl cellulose [E466], including fermented [E469], are classified as emulsifiers. These are thickeners and stabilizers, and pectin, in addition, and a gelling agent. Emulsion properties in this composition are shown only by methyl cellulose (A.P. Nechaev et al. Food additives, M., Kolos-Press, 2002, p. 229 -230).

If we consider an alternative of two additional polysaccharides, each of which may be part of the drug according to US Pat. RF 2128991, then in this case there is the formation of a direct emulsion - liquid paraffin in water - M / W. At the same time, it remains possible to reverse the phases with a transition to the reverse water / oil emulsion - W / M. This process is characteristic of a concentrated dispersed phase and is one of the reasons for the destruction of emulsions even in the presence of emulsifiers (A.D. Zimon, N.F. Leshchenko, Colloid chemistry, M., Agar, 2001, p.235). In this case, the concentration of mineral oil is quite high 40 - 84 wt.%. Such emulsions are aggregatively unstable.

In addition, due to their chemical structure, cellulose ethers do not contain either cationic or anionic groups and are neutral, which makes it impossible to bind them into complexes with micelles of M / B or B / M emulsions (see explanation below).

As shown by clinical trials of the drug obtained by the patent prototype, each time freshly prepared formulations had a therapeutic effect when taken for 4-8 weeks on patients with impaired lipid metabolism in the body (see table 2). However, due to the thermodynamic instability of the colloidal (micellar) system, this drug was already destroyed in the stomach under the influence of body temperature with the release of free liquid paraffin, which acts as a strong laxative. As a result, many patients suffered from diarrhea and were denied the drug.

As you know, the lifetime of colloidal systems determines the possibility of their use. And the shelf life of the drug is very limited. Therefore, from a technical and economic point of view, such an emulsion preparation became unsuitable for further use and, accordingly, for production.

Our scientists faced the task of developing a stable composition of dietary supplements with a long shelf life, which would contribute to the restoration of natural lipid metabolism in the human body.

Conducted scientific and experimental studies have elucidated the causes of the instability of the emulsion preparation, protected US Pat. RF 2128991, and create a new improved composition of dietary supplements, which in its therapeutic and prophylactic effect is more effective than that proposed in the prototype.

As a result of studies, it was found that when dispersing vaseline oil in an aqueous medium, a direct M / B emulsion is formed, the micelles of which concentrate a rather high concentration of positive charges in the peripheral zone. Interacting with polysaccharides (containing dissociated acid groups, mainly carboxyl and sulfonyl, which carry anionic charges), the micelles of the M / B emulsion form fairly stable complex compounds. Pectin is also involved in this process, which contains a small amount of negatively charged carboxy groups and which creates, as a rule, synergistic mixtures with our polysaccharides.

Regarding the instability of the drug according to the prototype, we found out the following. In our opinion, it is precisely the insufficient content of negatively charged carboxy groups in pectin (a significant part of the carboxyls in it is methylated), on the one hand, and the neutral charge of the second polysaccharide, on the other hand, is not able to bind the M / B emulsion and especially B emulsion to the durable micelle complex / M. Despite the thickening and stabilizing properties of the polysaccharides used, the so-called. the emulsion structure, which includes in its composition an unstable emulsion M / B and / or B / M, is destroyed with time with the release of the oil phase. That is, after a short time, the drug loses its useful properties.

We have proposed a dietary supplement, having the following qualitative and quantitative composition in wt.%:

liquid paraffin 10-39

pectin 1.0-6.0

flavoring agent 5,0-20

preservative 0.01-0.07

polysaccharide selected from the group: agar-agar, agaropectin, agaroid, starch, gum plants, or mixtures thereof 1.0-10

distilled water - the rest

Among the gums of plants, carob gum, guaran, xanthan, gellan and gum arabic can be called.

It should be noted that the second polysaccharide is selected from the group of polymers containing negatively charged acid residues in its structure: galacturonic, guluronic, pyruvic, sulfuric, etc. Neutral polysaccharides included in the selected group, in particular starch, including starch and some gums plants can be included only in a mixture with an anionically charged polysaccharide.

Sorbic acid and / or metal benzoate are used as a preservative. If necessary, flavoring is added to the additive in an amount of 0.0001-0.001 wt.%, Most often with a content of vaseline oil 30-39 wt.%, For example vanillin, menthol.

As a flavoring additive, fruit and berry substrates of different consistencies are used.

The amount of the second polysaccharide or its mixture, like pectin, is taken in a certain ratio to the content of liquid paraffin and water, taking into account the properties and synergy of their action. The ratio of the components of the mixture in our proposal is necessary for the formation of a sustainable

a complex of vaseline-water emulsion with polysaccharides by ionic bond, on the one hand. On the other hand, it is sufficient for structuring a mixture of components and the formation of a stable and dense cohesive-dispersed system that functions as a membrane.

In order to present the mechanism of action of our dietary supplements, it is advisable to touch on biochemical processes in the body, the violation of which leads to dyslipoproteinemia.

Violation of lipid metabolism in the body occurs, as a rule, against the background of deep microecological changes in the digestive tract. By acting on the enzyme systems of cells synthesizing endogenous cholesterol, unwanted microorganisms lead to a change in natural cholesterol metabolism. Enhanced proliferation of bacteria in the small intestine, in particular anaerobic ones, with their ability to form toxic salts of bile acids (FA) interfere with their normal enterohepatic circulation (V.N. Babin et al., Russian Chemical Journal, 1994, 38. No. 6, p. 66 - 68). An excess of bacteria thus creates the conditions for the almost complete absorption of FAs into the blood in the small intestine and their recirculation to the liver through the portal blood flow. And this reduces the normal synthesis of FAs in the liver, causes depression of its reticuloendothelial cells (REC), which further violates lipid catabolism and forms hyperlipidemia.

Therefore, the preventive task of dietary supplement is to help restore the processes of FA synthesis in the liver and its entry into the intestine.

Passing through the gastrointestinal tract, vaseline oil in a micellar state dissolves bile acids (FA), and the colloidal structure, holding them, preventing absorption in the small intestine and recirculation into the liver through the portal bloodstream, transports them into the large intestine. Here FA undergoes microbial transformation, polysaccharides nourish saprophytic flora and actively absorb toxins of organic and inorganic nature. The content of dietary supplements with feces is eliminated from the colon.

The liver, without receiving returnable FAs, uses plasma cholesterol for the synthesis of new ones, reducing its blood content along with other indicators, and subsequently taking it from tissue depots. Thus, the natural fecal excretion of cholesterol is restored.

A method of producing a dietary supplement is to prepare an aqueous solution containing pectin, a second polysaccharide or a mixture thereof and a flavoring. Then vaseline oil is introduced into it with vigorous stirring, and after homogenizing the mixture, a preservative in the dissolved state, and, if necessary, a flavoring agent.

We have developed a dietary supplement that is inert for the body from the chemical point of view (unlike drugs), since its components are not absorbed in the digestive tract, do not form intermediate products that can turn into other compounds that change the metabolic processes in the body.

Shelf life of the product in the refrigerator is at least 12 months.

Examples of the prepared compositions of dietary supplements are summarized in table 1.

Evaluation of the results of a biochemical study of lipid metabolism gave the following indicators for plasma cholesterol for 2 months of taking drugs and supplements. The concentration of blood plasma cholesterol in the treatment of placebo decreased by 7%, hepatene - by 12%, probiotic hilak-fort - by 9%. Reception of dietary supplement weekly at a dose of 200 g gave a decrease in cholesterol by 26%.

Comparative results of changes in the composition of blood parameters when taking dietary supplements and the preparation of the prototype are shown in table 2 and are presented on the graph (see drawing). Clinical trials of dietary supplements thus confirmed the high efficiency of its use.

table 2
Comparative evaluation of the biochemical effectiveness of the drug according to the prototype and the new dietary supplement Analyzed Indicators Norm
mg / dl The prototype drug New dietary supplement Before receiving After taking Before receiving After taking Abs. % Abs. % Cholesterol <200 298.7 + 20.1 194.4 + 11.6 -34 312.7 + 34.7 170.8 + 39.1 -45 Triglycerides <80 225.3 + 31.1 163.5 + 19.2 -27 267.9 + 29.7 130.4 + 18.1 -51 High Density Lipoproteins > 40 47.4 ± 5.3 54.9 + 6.0 +15 36.2 ± 6.7 56.1 ± 5.1 +56 Low density lipoproteins <130 206.2 + 18.4 106.18 + 18.1 -52 244.4 ± 27.1 112.7 ± 19.0 -54

Table 2 is compiled from the summary data published in the following sources:

1. V.A. Roosters. Russian Medical Journal, 2002, No. 9, p. 81.

2. V.S. Saveliev et al. Russian Medical Journal, 2002, No. 4, 160.

3. V.A. Roosters. Russian Medical Journal, 2002, No. 4.163.

4. V.S. Saveliev, V.A. Petukhov, B.V. Boldin. Moscow, “VEDI”, 2002, 159 p.

Claims (2)

1. A biologically active food supplement containing pectin, liquid paraffin, flavoring agent, preservative, polysaccharide and distilled water, characterized in that a polysaccharide selected from the group: agar agar, agaroid, agaropectin, starch, gum plants is included in the dietary supplement or a mixture thereof in the following ratio of components, wt.%: Pectin 1.0-6.0 Petroleum jelly 10-39 Flavoring additive 5.0-20 Preservative 0.01-0.07 Olisaccharide selected from the group: agar-agar, agaroid, agaropectin, starch, plant gum 1.0-10 Distilled Water Else 2. The biologically active food supplement according to claim 1, characterized in that it may additionally contain a flavoring agent in an amount of 0.0001-0.001 wt.%.