Biologically active additive based on beta-carotene and method for producing microemulsions

 

(57) Abstract:

The invention relates to the field of medicine, food and agricultural industry. The proposed biologically active additive based on beta-carotene, including alpha-tocopherol acetate, zinc ascorbate, and pharmacologically acceptable excipient (vegetable oil or emulsifier, stabilizer and water). Method for obtaining a microemulsion of this Supplement, including homogenization of beta-carotene in a pre-heated emulsifier in the presence of an antioxidant and a stabilizer, followed by mixing the resulting solution with water (heated to a temperature not exceeding 50o(C) that impose additional ascorbate zinc. BAD and how you can get it allows you to extend the range of dietary supplements on the basis of beta-carotene by increasing the bioavailability of the active components, to compensate for a deficiency of zinc, increase absorption of beta-carotene. 2 S. p. f-crystals, 1 Il. , 1 table.

The invention relates to the field of medicine, food and agricultural industry.

Environmental degradation and social conditions led to the impoverishment of the body such valuable vital neenie of these components is the design of biologically active additives, for enhancing the resistance of the body and having a certain orientation, or which are included in foods, feeds, beverages, or used independently or in conjunction in various technological forms (Problems associated with patent protection of biologically active additives to food. I. Pavlyuchenko, Budantseva, I., Petrenas, A. Ulyanov, Intellect, property 4, 2000 ). Known vitamin tools to enhance natural resistance based or activity of one active ingredient or active ingredient complexes. For example, biologically active additive to patent 2076704 contains carotenoids in vegetable oil. Replacement of vitamin a in the well-known drugs on beta-carotene allows you to save all the positive properties of vitamin a, to eliminate the risk of manifestation of toxic effects with long-term use and overdose, for example, teratogenicity (RF patent 2076704, 10.04.97).

Use as a derivative of vitamin a And beta-carotene in vitamin Supplement for treatment of avitaminosis birds in complex with antioxidants in the form of alpha-tocopherol acetate in the presence of butylacetate and dimethyl sulfoxide on the basis of which eshiwani active components and butylacetate with food sunflower oil (application EN 93008967/14, BI 11/96).

However, studies have shown that just the introduction of beta-carotene in the presence of antioxidants is not enough. To enhance the absorption of vitamin a is necessary the presence of Zn ion, which provides transport of vitamin a through the mucous membrane of the intestine through a zinc-containing protein. So they began to seek for sharing, this synergistic pair.

So, best-known food additive to corn feed containing mineral, vitamin and protein components in the form of heat-treated soybean, fodder yeast, cake, fruits and berries, fodder concentrate lysine, vitamins A, D, E, b2beta-carotene, zinc, manganese, copper, cobalt, white salt, precipitate, limestone, dry coffee sludge, feed grains from ficiary and forage lignin (patent RU 2050145, 10.12.95). In the same direction is known premix for lactating cows, incorporating biologically active additive in the form of a mixture of microbial carotene, lysine feed, Lukonina, copper sulfate, zinc sulfate, manganese sulfate, cobalt chloride, aminosidine, ammonical phosphate, salt, philodina and pine flour (patent RU 1503732, 23.05.91).

Not the a), introduction trace elements in the form of inorganic salts, which drastically reduces the degree of bioavailability and the unpredictability of the behavior of such complex multicomponent systems in acidic and alkaline media in the presence of enzymes of the gastrointestinal tract.

Introduction micro - and macronutrients in the form of organic salts increases their bioavailability. Thus, the known vitamin feed additive, which is obtained by processing of the mother liquor ascorbic acid, iron sulfate, cobalt sulfate, zinc sulfate, followed by the application on wheat bran (Temporary instruction on the use of supplements of vitamin-mineral feed on the basis of ascorbic acid in livestock and poultry (in order extensive production experience in 1999-2001 ). Approved by the Deputy administrator's guide. Department of veterinary centuries Seliverstova 28.12.99 year ).

Pharmacological properties of the additive due to members of trace elements in easily digestible nutrient form in the presence of ascorbic acid. The degree of absorption of beta-carotene and trace elements is also influenced by the aggregate state entered additives. It is shown that the introduction of biologically active additives in the form of microemulsions predpochtitelnye as a prototype for the claimed composition with the content of beta-carotene, not less than 2%, incorporating the antioxidant alpha-tocopherol acetate 0.5%, ascorbinatoxydase component in the form of ascorbic acid 0.25% and pharmacologically applicable filler.

The use of additives in experiments on chickens showed that, apart from increase of resistance in the yolks of eggs increased content of carotenoids by 10.3%, vitamin a by 30.4% (Guidance on the application of "Between"-beta-carotene water-soluble developed LLP (AUG-LTD) , St. Petersburg, agreed with the chief Sanit. doctor MSCH-24 Federal health-biological and experimental problems of the Russian Federation Century So Lyamin 31.07.98,,, Moscow, approved by the technical Director belvitamini", 1998).

When all of the positive results achieved by the prototype, the disadvantages should be considered incomplete absorption of beta-carotene (vitamin a), which is caused by deficiency of the trace element zinc in diets of animals and birds in many regions of the Russian Federation related to biogeochemical areas characterized by zinkevicius.

As a prototype for the method selected is a method of obtaining a microemulsion of beta-carotene, including homogenization of beta-carotene in a pre-heated emulsifier in the presence of the Sabbath. Object of the invention is the expansion of the range of dietary supplements on the basis of beta-carotene due to the design composition with increased absorption of beta-carotene, especially in regions with zinc deficiency, and develop ways to obtain microemulsions of this Supplement.

Technical results are:

- increase the biological availability of the active components of the additive;

- prevention of Cinderella;

- increase the absorption of beta-carotene;

- the achievement of biocoordination result in the assimilation;

- ensuring the possibility of obtaining zinc-containing microemulsions based on beta-carotene.

Addressing the above objectives and the achievement of the technical result in relation to compositions made possible by the fact that in the known biologically active additive based on beta-carotene, including active ingredients: beta-carotene, the antioxidant alpha-tocopherol acetate, ascorbinatoxydase component and a pharmacologically acceptable excipient, as ascorbinatoxydase additive component includes biologically available organic salt in the form of zinc ascorbate in the following ratio, wt. %: beta-carotene 1-3, alpha-tocopherol acetate 0.5 and 0.9, ascorbate zinc 1,9-2,5 well as pharmacologically acceptable filler comprises a filler or vegetable oil, or a mixture of eMule is due to the formation of a chelate structure with the connection, involved in all metabolic processes.

Received a dietary Supplement combines the positive properties of the prototype, and it has stability when stored in connection with the use of as a derivative of retinol, beta-carotene, providing a stabilizing effect on the composition and extend the range of its validity. Beta-carotene prevents the risk of overdose of vitamin a, as the process of converting beta-carotene into vitamin a, which is strictly regulated by the activity of an enzyme of the carotenoid-15-15-dioxygenase and occurs when vitamin a deficiency in the blood, while the latter regulates the absorption of zinc by the body. Joint introduction synergists - zinc and vitamin a - helps to achieve biocoordination the result of assimilation. Presumably, the prolongation of the process of absorption is achieved by inclusion in the composition of the zinc ion is in the form of biologically available with less salt compared to the inorganic salt, the ratio of dissociation, which leads to a gradual release of zinc. At this speed the release of zinc comparable to the speed of biochemical reactions associated with protein with the formation of zinc-containing protein com which included a large area of the intestine, due to which more fully used biologically active components of the additive.

The presence of an antioxidant such as alpha-tocopherol acetate, enhances the antioxidant effect of beta-carotene, protects it from damage by preventing free radical processes.

The resulting composition has a novelty and a significant difference in comparison with analogues, determining technical level through the use of a pair of synergistic vitamin a-zinc (in a biologically available form) in the presence of an antioxidant, provides the formation of the ecosystem of the digestive tract and can be used long-term as a mass preventive adaptogenic funds in ecologically unfavorable regions and regions characterized by zinkevicius. Unlike multi-component analogues, including inorganic zinc salts, the proposed composition is made in the form of organic structure characterized by a formed internal communication, ensuring the normal course of metabolic processes.

The choice of pharmaceutically acceptable carrier or vegetable oil, or a mixture of emulsifier, stabilator, either in the form of water-soluble micro-emulsions, reflecting a new direction.

As a prototype for the preparation of microemulsions of the proposed drug selected patent 2077523 (patent RU 2077529, 20.04.97).

The solution of tasks and achievement of the technical result regarding methods made possible by the fact that in the known method of obtaining a microemulsion comprising homogenization of beta-carotene in a pre-heated emulsifier in the presence of an antioxidant and a stabilizer, followed by mixing the resulting solution with water, before the operation of the mixing water is heated to a temperature not exceeding 50oWith and contribute to it with stirring, addition of ascorbate zinc in the following ratio, wt. %: beta-carotene 1-3, antioxidant, 0.5 and 0.9, ascorbate zinc 1,9-2,5, emulsifier 19, stabilizer 0,002, water up to 100. The temperature rise over 50oWith entail loss of ascorbate zinc.

The proposed method allows to obtain a stable microemulsion water-soluble fat-soluble beta-carotene and put the drug in the category of water-dispersed, which is important in the conditions of modern production and in line with current trends.

and table in which, for clarity, reduced data examples.

The method is as follows. From collector 1 in a measuring Cup 2 download emulsifier, which is used as tween-80 in the presence of the stabilizer - butylacetate. From the volumetric capacity 2 emulsifier served in the reactor 3, equipped with a heat exchanger 4 and the agitator 5 is heated, add from the container 6 crystalline beta-carotene and dissolve it. Download from tank 7 alpha-tocopherol acetate, used as an antioxidant, and homogenize the mixture with stirring for 10 minutes. In parallel to the reactor 8, equipped with a stirrer 9 and the heat exchanger 10, heat water to a temperature not exceeding 50oWith, from the tank 11 download ascorbate zinc under stirring, after which the mixed emulsion of beta-carotene and ready solution of zinc ascorbate. The resulting preparation is filtered through a filter 12 and sent for packing.

Example 1.

Preparing a microemulsion of biologically active additives by the present method when the ratio of components, wt. %:

Beta-carotene - 1

Antioxidant (alpha tocopherol acetate) - 0,5

Ascorbate zinc - 1,9

Emulsifier (tween-80) - 19

Stabilizer (butylacetamide) -tx2">

Determination of the bioavailability and efficacy of the additive held in the control groups of laying hens, while in the study group daily in the drinking was added claimed the drug for 10 days according to the instruction for use.

At the end of the experiment investigated the liver birds on the accumulation of carotene, zinc, vitamin A.

The following results are obtained for the claimed composition:

Carotene, g/g - 18,9

Vitamin a, g/g - 151, 3mm

Zinc, mg/kg 17,7

The resulting emulsion is stable and does not separate during storage

Example 2.

Preparing a microemulsion of biologically active additives by the present method when the ratio of components, wt. %:

Beta-carotene - 2,0

Antioxidant (alpha tocopherol acetate) - 0,7

Ascorbate zinc - 2,2

Emulsifier (tween-80) - 19

Stabilizer (butylacetamide) - 0,002

Water Up to 100

which corresponds to the average values of the components in the claimed range.

When determining the bioavailability and efficacy of the additive as in example 1 showed that in liver birds contained:

Carotene, g/g - 27,4

Vitamin a, g/g - to 219.5

Zinc, mg/kg 22,1

The resulting emulsion is stable and not avci by the present method when the ratio of the components, wt. %:

Beta-carotene - 3

Antioxidant (alpha tocopherol acetate) - 0,9

Ascorbate zinc 2,5

Emulsifier (tween-80) - 19

Stabilizer (butylacetamide) - 0,002

Water Up to 100

that corresponds to the maximum value components in the claimed range.

When determining the bioavailability and efficacy of the additive as in example 1 showed that in liver birds contained:

Carotene, g/g - 38,7

Vitamin a, g/g - 315,4

Zinc, mg/kg - 49,0

The resulting emulsion is stable and does not separate during storage.

Example 4.

Preparing a microemulsion of biologically active additives by the present method when the ratio of components, wt. %:

Beta-carotene - 0,5

Antioxidant (alpha tocopherol acetate) - 0,4

Ascorbate zinc - 1,0

Emulsifier (tween-80) - 19

Stabilizer (butylacetamide) - 0,002

Water Up to 100

which corresponds to the beyond the minimum values within the claimed limits.

When determining the bioavailability and efficacy of the additive as in example 1 showed that in liver birds contained:

Carotene, g/g - 9,6

Vitamin a, g/g - br93.1

Zinc, mg/kg 13,2

The emulsion obtained ustoichivoi additives by the present method when the ratio of the components, wt. %:

Beta-carotene - 3,5

Antioxidant (alpha tocopherol acetate) - 1,2

Ascorbate zinc - 3,0

Emulsifier (tween-80) - 19

Stabilizer (butylacetamide) - 0,002

Water Up to 100

which corresponds to the beyond the maximum declared values of the components relative to the proposed limits.

When determining the bioavailability and efficacy of the additive as in example 1 showed that in liver birds contained:

Carotene, g/g - 39,9

Vitamin a, g/g - 328,9

Zinc, mg/kg - 60,7

The resulting microemulsion stable and does not separate during storage.

Example 6.

Preparing an oil solution of the inventive biologically active additive composition of the active components according to example 2, which corresponds to the average values of the components in the claimed range. As the filler used vegetable clarified butter.

" When determining the bioavailability and efficacy of the additive as in example 1 showed that in liver birds contained:

Carotene, g/g - 19,1

Vitamin a, g/g - 310,6

Zinc, mg/kg - 30,8

Example 7.

Prototype - dietary Supplement BETWEEN.

Prepare the microemulsion "Be the t) - 0,5

Ascorbic acid - 0,25

Emulsifier (tween-80) - 19

Stabilizer (butylacetamide) - 0,002

Water Up to 100

When determining the bioavailability and efficacy of the additive as in example 1 showed that in liver birds contains:

The results of analyses 7

Carotene, g/g 10.5V

Vitamin a, g/g - 120,1

Zinc, mg/kg 9,6

As can be seen from examples 2 and 7, the inventive composition allows to achieve better absorption compared to the prototype carotene 38.3%, vitamin a 38,08%, zinc at 43,44%.

Examples 1 and 3 demonstrate the industrial applicability of biologically active additives in the claimed range. Reducing the number of components below the stated limits (example 4) weakens the effectiveness of exposure; the increase in the number of components above the stated limits is not economically feasible (example 5). Examples 1 and 3 also showed the possibility of obtaining stable active microemulsions of the claimed supplements, not inferior to the properties of the microemulsion prototype using pharmacologically acceptable excipient in the form of an emulsion, stabilizer, water, shows that the industrial applicability of the claimed method.

Thus, the invention has Isakov the first and second paragraphs formula allows to provide biocoordination result in absorption, prevention of Cinderella, improving the absorption of beta-carotene, increased bioavailability of the active components of the additive, as well as to provide the possibilities of production of zinc-containing emulsion.

1. Biologically active additive based on beta-carotene, including active ingredients: beta-carotene, the antioxidant alpha-tocopherol acetate, ascorbinatoxydase component and a pharmacologically acceptable excipient, characterized in that as ascorbinatoxydase component it contains biologically assimilable organic salt of zinc ascorbate, and as a pharmacologically acceptable carrier or vegetable oil, or emulsifier, stabilizer and water in the following ratio, wt. %:

Beta-carotene - 1 - 3

Alpha-tocopherol acetate - 0,5 - 0,9

Organic salt of zinc ascorbate - 1,9 - 2,5

Pharmacologically acceptable excipient (vegetable oil or emulsifier, stabilizer, water) - the Rest is up to 100%

2. The way to obtain microemulsions biologically active additives based on beta-carotene, including homogenization beta mesovarium the resulting solution with water, characterized in that before mixing the homogenized mixture with water, the latter is heated to a temperature no higher than 40-50oWith and contribute to it with stirring, addition of ascorbate zinc in the following ratio, wt. %:

Beta-carotene - 1 - 3

Antioxidant - 0,5 - 0,9

Ascorbate zinc - 1,9 - 2,5

Emulsifier - 19,0

Stabilizer - 0,002

Water Up To 100

 

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