RU2182011C1 - Biologically active food additive to prevent reduction of immune system - Google Patents

Abstract

FIELD: medicine. SUBSTANCE: the suggested biologically active food additive designed in a tableted form contains a dry extract of purple Echinacea and physiologically acceptable fillers: magnesium stearate, finely divided powder of dry Echinacea grass, ascorbic acid and microcrystalline cellulose at the following ratio of ingredients, weight%: dry extract of Echinacea grass and/or roots 10.0-40.0, powder of dry Echinacea grass 20.0-70.0, ascorbic acid 1.0-4.0, magnesium stearate 0.3- 1.0, microcrystalline cellulose - up to 100%. The suggested additive is designed out of powders of ingredients divided to the size of particles being below 500 mcm. EFFECT: broadened list of medicinal preparations. 1 cl

Description

 The invention relates to medicine, namely to therapeutic and prophylactic agents that increase the body's defenses by stimulating the immune system.

 Among the plants used to increase the protective functions of the body by enhancing immunity, purple coneflower has been most recently known.

 All organs of the plant contain polysaccharides, essential oil. The main component of the essential oil is non-cyclic sesquiterpenes. Echinacoside glycoside, betaine, resins, organic acids (palmitic, linoleic, cerotinic), as well as phytosterols, were found in the roots. The main active substances with immunostimulating activity are Echinacea polysaccharides (A.M. Nosov. Medicinal plants. M., EKSMO-Press, 1999, 350 p.).

 As a result of chemical and pharmacological studies, it was found that various parts of Echinacea contain biologically active substances with antiviral and antimicrobial activity, as well as capable of stimulating the immune system and inhibiting the growth of malignant tumors. According to some researchers, the main area of application of echinacea drugs should be all diseases associated with acquired immunodeficiency or temporary immune weakening of the body. The stimulating effect of the plant on the immune system is manifested not only in adults, but also in children with an unstable immune system, as well as in elderly people, whose functions of this system are reduced due to general aging of the body.

 The plant has a high bactericidal effect and is used as an antiseptic for internal and external use. Preparations from it have an analgesic effect, stimulate tissue granulation, accelerate the healing of wounds and ulcers, burns, bedsores.

 Echinacea preparations are indicated not only for bacterial, but also for viral diseases (influenza, herpes, smallpox, poliomyelitis), for the treatment and prevention of respiratory diseases, focal pneumonia, fever, and for many chronic diseases - rheumatoid arthritis, hepatitis, nephritis, etc. They are effective. also with septic processes, with skin (eczema, psoriasis), gynecological and urological (prostatitis, cystitis) diseases. In addition, Echinacea preparations have a stimulating effect on the central nervous system, enhance sexual potency, and are also used in cases of mental depression, physical and mental exhaustion (V.K. Lavrenov, G.V. Lavrenova. Complete encyclopedia of medicinal plants. T.2 St. Petersburg, Publishing House "Neva", M., "Olma-PRESS", 1999, 816 pp.).

 Echinacea preparations are also used for prophylactic purposes at the first signs of a cold, with prolonged use of antibiotics, in the recovery of people who have been exposed to radiation or who live in areas that are unfavorable for radiation levels.

 Today, Echinacea is part of more than 200 foreign complex medical products. It is also used in the form of monopreparations, which are mainly liquid or dry extracts of all parts of a dry plant, as well as canned juice.

 In particular, drugs such as the Echinacea Herbal Drops tincture by Naturvaren Dr. Peter Theis, Germany; Echinacin liquid extract, Madaus, Germany; juice from fresh flowering Echinacea grass "Echinacea Hexal", Hexal, Germany; Echinacea juice "Immunal", Lek, Slovenia, etc.

 Also known is the domestic drug "Tincture of Echinacea purpurea", the method of preparation of which is protected by RF patent 2134584.

 However, the disadvantage of liquid drugs is the inconvenience of using and dosing compared to solid tablets or capsules. In addition, when extracting plant materials with liquid extractants or pressing (with subsequent preservation) of juice from fresh plants, a number of valuable substances contained in a natural plant are lost.

 Known domestic immunostimulating agent "Estifan" from purple coneflower and the method for its preparation according to the patent of the Russian Federation 2137490, MKI A 61 K 35/78, taken as a prototype. A medicine containing an active substance and physiologically acceptable excipients contains estifan, a dry extract from Echinacea herb, as active substance, and lactose, potato starch, methylcellulose, calcium or magnesium stearate in the following ratio of components, wt. %: estifan - 25-60, lactose - 14-49, starch - 23-27, methyl cellulose - 0.1-0.2, calcium or magnesium stearate - 0.3-0.5. A method of obtaining an immunostimulating agent from echinacea involves the extraction of crushed raw materials with a water-alcohol mixture three times, followed by concentration of the extract, evaporation under vacuum, drying, mixing the powder with excipients, moistening with a solution of methylcellulose, re-drying, granulation, dusting with calcium or magnesium stearate followed by tableting ( the essence of this technical solution is also contained in temporary pharmacopoeial articles VFS 42-2372-94 on estifan and VFS 42-2373-94 on estif tablets ana 0.2 g).

 The produced pharmacopoeial preparation contains 0.2 g of dry extract of Echinacea herb in a tablet weighing 0.5 g. The dose is 1-2 tablets 3 times a day, the course of treatment is 10-20 days.

 Known technical solution has several disadvantages.

 Since the drug is a medicine, its status implies medical prescription.

 For the purpose of tabletting, physiologically acceptable excipients are used in it, which are inert substances that do not add medicinal properties to the medicinal product.

 Upon receipt of the extract, as noted above, there is a loss of part of the substances useful to the body.

 The drug is made according to a rather complicated method, available only to pharmaceutical companies involved in obtaining dry extracts from plants.

 The objective of the present invention is to expand the range of domestic products that increase the body's defenses by stimulating the immune system.

 The result achieved when using the invention is to create a drug that meets the status of biologically active food supplements (BAA), i.e. the drug does not require medical prescription and has the most gentle healing effect on the body, which ensures the prevention of diseases caused by a decrease in immunity. The drug has a convenient, easily dosed consumer form, which provides the possibility of its administration in any environmental conditions. The manufacturing technology of the drug makes it possible to obtain tablets from the finished substance, which allows organizing its wide production by small and medium pharmaceutical enterprises that do not have special equipment for obtaining dry extracts.

 The essence of the invention lies in the fact that the proposed biologically active food supplement for the prevention of weakening of the immune system, made in tablet form and containing dry extract of Echinacea purpurea and physiologically acceptable excipients, including magnesium stearate. Dietary supplement contains fillers as a fine powder of dry herb Echinacea, ascorbic acid and microcrystalline cellulose in the following ratio of ingredients, wt. %: dry extract of grass and / or roots of Echinacea - 10.0-40.0; Echinacea dry herb powder - 20.0-70.0; ascorbic acid - 1.0-4.0; magnesium stearate - 0.3-1.0; microcrystalline cellulose - the rest is up to 100%. Supplements are made from powders of ingredients, crushed to particle sizes less than 500 microns.

 The choice of ingredients and their quantitative ratio is due to the following considerations.

 In accordance with the status of dietary supplements, the daily dose of parapharmaceuticals or, in the case of a composition, the daily dose of the active principle, parapharmaceuticals should not exceed the single therapeutic dose determined when using these substances as medicines, provided that dietary supplements are taken at least twice a day (Determining the safety and effectiveness of biologically active food additives. Guidelines. M., Federal Center for Sanitary and Epidemiological Supervision of the Ministry of Health of the Russian Federation, 1999, 87 pp.).

 The main ingredient of the proposed dietary supplement for physiological effects on the body is a dry extract of grass and / or echinacea roots (a ready-made substance of a dry extract of a plant produced by an enterprise specializing in the production of dry plant extracts is used - Harms LLC, St. Petersburg).

 Given that the recommended single therapeutic dose of dry extract of echinacea is 200-400 mg (see prototype), a single dose of the extract in dietary supplement should lie in the range from about 100 to 200 mg (20-40 wt.%) When taken 2 times per day and from 50 to 130 mg (10-26 wt.%) when taken 3 times a day. Thus, the total dosage range of the main active substance in the proposed dietary supplement should be from 10 to 40 wt.%.

 In accordance with the invention, another major ingredient of the proposed dietary supplement is a finely divided powder of dry Echinacea herb, the introduction of which into the preparation in an amount of from 20 to 70 wt.% Allows to obtain a triple effect.

 Firstly, the fine powder of a dry plant plays the role of a physiologically acceptable excipient, which makes it possible to obtain tablets of a certain mass and size. Usually, starch, sugar, microcrystalline cellulose, and others play a similar role in pharmaceutical preparations.

 Secondly, the introduction of finely divided powder of dry herb Echinacea into the preparation can enhance the healing effect of the preparation, since it contains, in contrast to inert fillers, substances useful to the body that are characteristic of a dried plant.

 Thirdly, the introduction of this powder into the preparation, which is based on the dry extract of echinacea, allows you to make up for the loss of other ingredients useful to the body that were lost in the process of liquid extraction of a dry plant or squeezing juice from a fresh plant. The dry extract of Echinacea and the powder from it are well compatible and complement each other, as they are parts of the same plant species, which eliminates the possibility of deterioration of the healing properties of the complex preparation with improper selection of plant ingredients.

 Ascorbic acid, introduced into the dietary supplement in an amount of 1.0-4.0 wt.%, Stimulates oxidative processes in the body, activates the work of various enzymes, normalizes carbohydrate metabolism, improves glucose absorption in the intestines, stimulates blood formation, and increases the body's immunity to infections.

 Magnesium stearate is introduced into the dietary supplement in an amount of 0.3-1.0 wt.% To reduce the hygroscopicity of the resulting tablets.

 In order to improve the quality of the tablets in them in an amount that provides 100% by mass, microcellulose (dietary fiber), usually used for such purposes in pharmaceutical production, is added.

 Based on experimental studies of the manufacturing process of the proposed dietary supplement, it was found that to ensure the high quality of the tablets, it is necessary to use ingredients crushed to particle sizes less than 500 microns.

 EXAMPLE 1. The mixture is prepared at the rate of: 10 wt.% (50 mg) of dry extract of grass and / or Echinacea root, 70 wt.% (350 mg) of finely divided powder of dry Echinacea grass, per 1 tablet of dietary supplement is taken, 1 wt.% (5 mg) of ascorbic acid, 0.3 wt. % (1.5 mg) of magnesium stearate and microcrystalline cellulose in an amount up to 100% (18.7 wt.% Or 93.5 mg). The mixture is thoroughly mixed, passed through a sieve with a mesh size of less than 500 microns, after which the tablets are pressed. Supplements take 1 tablet 3 times a day.

 EXAMPLE 2. The mixture is prepared at the rate of: 40 wt.% (200 mg) of dry extract of grass and / or echinacea root, 20 wt. % (100 mg) of finely divided powder of dry herb Echinacea, 4 wt.% (20 mg) of ascorbic acid, 1.0 wt.% (5.0 mg) of magnesium stearate and microcrystalline cellulose in an amount up to 100% (35 wt.% Or 175 mg). The mixture is thoroughly mixed, passed through a sieve with a mesh size of less than 500 microns, after which the tablets are pressed. Supplements take 1 tablet 2 times a day.

 Currently, the drug, which is named "STIMMUNAL", is produced by an experimental batch and is undergoing official clinical and hygienic tests in the relevant authorities of the Ministry of Health of the Russian Federation.

Claims (1)

1. A dietary supplement for the prevention of weakening of the immune system, made in tablet form and containing a dry extract of purple coneflower and physiologically acceptable excipients, moreover, it contains finely divided powder of dry coneflower herb, ascorbic acid and microcrystalline cellulose in the following ratio of ingredients, wt. %:
Dry extract of herbs and / or roots of Echinacea - 10.0 - 40.0
Echinacea dry herb powder - 20.0 - 70.0
Ascorbic acid - 1.0 - 4.0
Magnesium stearate - 0.3 - 1.0
Microcrystalline Cellulose - Up to 100
2. The additive according to claim 1 is made from powders of ingredients, crushed to particle sizes less than 500 microns.