RU2180588C1 - Biologically active food supplement for prophylaxis of depressive state - Google Patents

Abstract

FIELD: medicine. SUBSTANCE: supplement involves perforated Saint-John's-wort extract, microcellulose and magnesium stearate, Saint-John's-wort dried flowers and leaves small-dispersed powder taken in the following ratio of components, wt.-%: Saint-John's-wort dried extract, 8.0-60.0; Saint-John's-wort flowers and leaves powder, 18.0-70.0; magnesium stearate, 0.3-1.0; microcrystalline cellulose, the balance, to 100%. The supplement is made as a tableted form from component powders ground to particle size less 500 mcm. EFFECT: expanded arsenal of agents. 2 cl

Description

 The invention relates to medicine, namely to therapeutic and prophylactic agents used as antidepressants.

 Currently, various types of depression are a serious medical problem. Annually, chronic depression destroys the health of about 100 million people around the globe. For example, in the United States, the annual economic losses of Americans from depression, including the cost of medical care and temporary disability, are estimated at $ 44 billion (Katzenstein L. Zveroboj against depression. Transl. From English. M., KRON-PRESS, 1998, 213 pp. /1/).

 In modern psychiatry, synthetic antidepressants are widely used to combat depressive conditions: mono-aminoxidase inhibitors, tricyclic antidepressants, selective serotonin uptake inhibitors, etc. (Mashkovsky M.D. Medicines. T.1, Kharkov, Torsing, 1997). However, their disadvantage is the large number of side effects: palpitations, headache and dizziness, insomnia, nausea, sexual problems, constipation, agitation or depression, increased blood pressure, weight gain, aggressiveness. For some patients, the use of these synthetic antidepressants becomes a life-threatening factor / 1 /. Side effects such as drowsiness, mental, mental and motor lethargy, lethargy, lethargy, weakness, somatic discomfort, impaired attention and memory, tearfulness, conflict, neurotic disorders, drug dependence (Gindikin V.Ya. Herbs, nerves, age) are also observed. M., KRON-PRESS, 1996, 288 pp. [2]).

 In this regard, for the prevention and treatment of mild to moderate depression are increasingly used medicinal plants and drugs based on them, the use of which side effects occur much less frequently [2].

 One of these plants is St. John's wort, a widespread plant that has long been used in folk medicine in many countries.

 Hypericum herb contains a variety of biologically active compounds. The main active ingredients are photoactive condensed anthracene derivatives. Flavone compounds, essential oils, tannins, anthocyanins, saponins, carotene, nicotinic and ascorbic acids, vitamin P, ceryl alcohol, choline, traces of alkaloids, trace elements (manganese, zinc) were also found. Biflavon compounds with anti-inflammatory, anti-ulcer activity were also found (Lavrenov V.K., Lavrenova G.V. Complete Encyclopedia of Medicinal Plants. T.1, St. Petersburg, Publishing House "Neva", M., OLMA-PRESS, 1999, 736 p. / 3 /). To date, about 50 different ingredients / 1 / have been found in the leaves and flowers of St. John's wort grass.

 In Russia, the plant is widely used for a wide variety of diseases, which gave reason to call it "a cure for 99 ailments." St. John's wort is used for diseases of the gastrointestinal tract, for colitis and various diarrhea, female diseases, diseases of the liver and gall bladder, for headaches and dizziness, cystitis, bedwetting, kidney stones, bronchitis, tuberculosis, peptic ulcer and duodenal ulcer prostatitis, sciatica, hemorrhoids, furunculosis, acne, as well as a tonic for cardiovascular diseases, as a hemostatic for uterine bleeding, anti-inflammatory for angina , endocarditis, myocarditis. Grass is used for tumors of the liver and stomach, malignant skin lesions [3].

 Recently, abroad, it was found that St. John's wort herb is an excellent mild-acting antidepressant, stopping depressive states from mild depressive neurosis to depressive psychosis. Moreover, it is practically devoid of side effects (with the exception of photosensitization, which occurs in fair-skinned people). In addition to depression, St. John's wort perfectly copes with various anxiety states, insomnia, depressed, dull mood, depressing hopeless longing / 1 /. The price factor is very significant: St. John's wort is much cheaper than drugs obtained synthetically.

 It is also very convenient that, when treating depression, St. John's wort can also stop other painful manifestations - migraine, hypertension, liver, kidney (including kidney stone), lungs and bronchi. It is hypotensive, astringent, choleretic, anti-inflammatory, antimicrobial, regenerative, hemostatic, strengthens capillaries, reduces their permeability, improves venous circulation and blood supply to internal organs, stops exacerbation of hemorrhoids, improves appetite, it is recommended as an anthelmintic / 2 /.

 At present, both liquid and dry forms of St. John's wort extract are recommended in world medical practice. The most common medicinal form of St. John's wort abroad is tablets or capsules, each of which usually contains 300 mg of dry extract prepared by infusing the crushed herbs with alcohol and evaporating the extractant to obtain a powder containing a high concentration of active substances. The daily dosage of the drug is usually 900 mg (1 tablet or capsule 3 times a day). A similar drug called "Jarsin-300", first created in Germany in 1992 (the company "Lichtver Pharma"), became the first official drug for use as an antidepressant / 1 /.

 Currently, various foreign companies produce more than 20 medicines in the form of tablets and capsules containing hypericin hypericin extract standardized with St. John's wort, while the recommended single therapeutic dose of the extract is in the range from 125 to 600 mg, and the daily dose varies from 250 to 1800 mg / 1 /.

 In our country, the production of dry St. John's wort extract in the form of a substance was mastered by Harms, St. Petersburg (Sb. Manufacturers of drugs, St. Petersburg, PHARM-index, 2000, 7, 215 pp.), Information about domestic preparations from it in the form finished consumer forms are missing.

 Known drug "Negrustin" company "HEXAL", Germany, taken as a prototype (instructions for use).

 The drug is a capsule containing 425 mg of dry extract from St. John's wort, as well as about 100 mg of other components: calcium hydrogen phosphate, microcellulose, chlorophyll, gelatin, lactose, magnesium stearate, sodium dodecyl sulfate, silicon dioxide, talc, dye. The dose is 1 capsule 1-2 times a day.

 It should be noted that the prototype, like other well-known foreign drugs based on the dry extract of St. John's wort, refers to medicines whose status requires medical prescription.

 It should also be borne in mind that in the process of obtaining the extract, a number of valuable substances contained in a natural plant are lost. To compensate for these losses, multicomponent preparations are sometimes made in the form of a mixture of several medicinal plants. However, the selection of plant ingredients in this case is often ineffective, since the active substances contained in them can have the opposite effect and cause side effects. In this regard, in relation to St. John's wort, mixing it with other herbs is impractical and it is recommended to use a single-component preparation / 1, p. 203 /.

 The objective of the present invention is to expand the range of domestic drugs to combat depressive conditions, providing high efficiency for the prevention of depression of mild to moderate degree with a practical absence of side effects. The drug should have a convenient consumer form, allowing its administration in any environmental conditions.

 The result achieved when using the invention is to create a drug that meets the status of biologically active food additives (BAA), the use of which does not require medical prescription and which allow you to provide the most mild preventive effect on the body without significant side effects. The drug allows you to improve the quality of life in people prone to depression of a psychogenic nature by providing a calming effect, improving mood, relieving anxiety, restoring peace of mind, strengthening the psyche, increasing mental abilities, etc.

 The essence of the invention lies in the fact that a biologically active food supplement for the prevention of depressive conditions based on a dry extract of hypericum perforatum additionally contains finely divided powder of dried flowers and hypericum leaves, as well as magnesium stearate and microcrystalline cellulose in the ratio of ingredients, wt.%: Dry hypericum extract - 8.0-60.0; St. John's wort flowers and leaves powder - 18.0-70.0; magnesium stearate - 0.3-1.0; microcrystalline cellulose - the rest. The additive is made in tablet form from powders of ingredients, crushed to particle sizes less than 500 microns.

 The choice of ingredients and their quantitative ratio in the proposed dietary supplement 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 of parapharmaceuticals should not exceed the single therapeutic dose determined when these substances are used as medicines, provided that dietary supplements are taken at least twice a day (Safety Definition and the 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.).

 As the main ingredient of the proposed drug contains dry extract of St. John's wort. Given the data on the range of recommended single therapeutic doses of St. John's wort extract (standardized for hypericin) in drugs used in world practice, comprising 125-600 mg / 1 /, a single dose of the extract in dietary supplements should be in the range from 62.5 to 300 mg (12.5-60 wt.%) When taken 2 times a day and from 41.7 to 200 mg (8-40 wt.%) When taken 3 times a day. Therefore, the total dosage range of St. John's wort extract in dietary supplement should be from 8 to 60 wt.%.

 In accordance with the invention, another important ingredient of the proposed dietary supplement is a fine powder of dried flowers and leaves of St. John's wort, the amount of which can be 18.0-70.0 wt.% Or 90-350 mg in one tablet weighing 0.5 g.

 Introduction to the proposed preparation of dry powder of flowers and leaves of natural St. John's wort allows, firstly, to use it as a physiologically acceptable excipient, the role of which in pharmaceutical preparations is usually played by starch, sugar, microcrystalline cellulose, etc., which do not have significantly useful healing properties.

 Secondly, this technique allows you to increase the therapeutic and prophylactic effectiveness of the drug, since the filler in the form of a dry plant powder contains healing substances.

 Thirdly, the powder of hypericum flowers and leaves compensates for the loss of some other valuable substances that occur during the extraction of plant materials in order to increase the concentration of individual components by removing "excess" substances. Since St. John's wort dry extract and its herb powder are components of the same plant, i.e. "related" to each other, their mixing does not impair the properties of the drug, which sometimes occurs when other plant ingredients are introduced into complex herbal preparations.

 Based on experimental studies of the tabletting process of the proposed preparation, it was found that to ensure high quality products, the particle size of the powder of dried flowers and St. John's wort leaves introduced into the preparation should be less than 500 microns.

 In a small amount (0.3-1.0 wt.%), Magnesium stearate is introduced into the dietary supplement, which reduces the hygroscopicity of the obtained tablets (it is also known that magnesium has antidepressant properties and supports the circulatory system in a healthy state. - L. Earl. Vitamins and Minerals. M., Dialogue, p. 41).

 In order to improve the quality of the tablets, microcellulose, usually used for such purposes in pharmaceutical production, is added to them (to obtain 100 wt.%).

 Example 1. Prepare the mixture at the rate of: per tablet of the proposed dietary supplement weighing 0.5 g take 8 wt.% (40 mg) of powder of dry extract of St. John's wort, 70 wt.% (350 mg) of fine powder from dried flowers and leaves of St. John's wort, 0 , 3 wt.% Or 1.5 mg of magnesium stearate and microcrystalline cellulose in an amount providing 100 wt.% (21.7 wt.% Or 108.5 mg). The mixture is thoroughly mixed and passed through a sieve with a mesh size of less than 500 microns, after which they are pressed. The drug is prescribed in a dose of 1 tablet 3 times a day.

 Example 2. The mixture is prepared at the rate of: 60 wt.% (300 mg) of St. John's wort dry extract powder, 18 wt.% (90 mg) of fine powder from dried flowers and St. John's wort leaves, 1.0 wt.% ( 5 mg) magnesium stearate and microcrystalline cellulose - the rest (21 wt.% Or 105 mg), after which the mixture is sieved and pressed in the form of tablets. The drug is prescribed 1 tablet 2 times a day.

 Currently, normative documentation is being prepared for conducting official clinical and hygienic tests of the developed dietary supplement, which was named "OPTIMISTIN", in the relevant authorities of the Ministry of Health of the Russian Federation.

Claims (1)

1. A biologically active food supplement for the prevention of depressive conditions, containing dry extract of Hypericum perforatum, microcellulose and magnesium stearate, characterized in that it additionally contains fine powder of dried flowers and hypericum leaves with a ratio of ingredients, wt. %:
Dry hypericum extract 8.0-60.0
Hypericum powder of flowers and leaves - 18.0-70.0
Magnesium stearate - 0.3-1.0
Microcrystalline Cellulose - Up to 100
2. The additive according to claim 1, characterized in that it is made in tablet form from powders of ingredients, crushed to particle sizes less than 500 microns.