RU2473357C2 - Liquid composition improving working performance and possessing adaptogenic, wound-healing and anti-inflammatory action - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacy and concerns formulations possessing adaptogenic, anti-inflammatory and working performance improving action, and are applicable for treating gastrointestinal diseases (gastritis, gastric ulcer) and for body adaptation to the adverse conditions and improving working performance. The composition contains royal jelly, purified propolis and additionally fructose and glucose syrups, pollen extract, vitamin E, preserving agent, sweetener and water in specific proportions.

EFFECT: composition extends the spectrum of pharmacological action and bioavailability.

2 cl, 3 ex, 1 tbl

Description

The invention relates to the field of pharmacy and relates to compositions having adaptogenic, anti-inflammatory and action-enhancing effects and can be used to treat diseases of the gastrointestinal tract (gastritis, ulcer) and to adapt the body in adverse conditions and increase workability. Currently, the human body is increasingly exposed to various adverse environmental factors, chemical, radiation, stress. A large number of synthetic medicines, food additives and hygiene products are used. Many researchers are searching for tools that can increase overall resistance and the ability to adapt the body in adverse conditions.

Known means to improve the performance of athletes (application 95122037/14, 12.26.1995), including eleutherococcus extract, characterized in that it additionally contains licorice root extract dry, rosehip dry, estifan, silymar, propolis tincture and honey, and as extract of Eleutherococcus extract of Eleutherococcus dry in the following ratios of components, wt.:

Dry eleutherococcus extract 0.6 Dry licorice root extract 0.3 Dry rosehip extract 0.3 Estifan 0.3 Silimar 0.3 Propolis tincture 0.3 Natural honey Rest

Known natural multivitamin complex (Application for invention: 93048600/13, 10.20.1993) containing pollen and lactose, safflower lefthander, ascorbic acid, tocopherol acetate, propolis, calcium stearate and talc in the following ratio of components, wt .:

pollen 50-51 Safflower levzea 10 Vitamin C 3.0-3.5 α-tocopherol acetate 0.15 Propolis 2 Calcium stearate 0.92-0.95 Talc 3 Lactose Rest

Closest to the claimed is a therapeutic and prophylactic adaptogenic complex (Patent application No. 2002102631/14, 02/04/2002, publ. 10.01.2003), characterized in that it contains Schisandra fruit powder, lyophilized royal jelly milk, propolis extract, potassium iodide , iron gluconate, maltodextrin, anhydrous colloidal silica, magnesium stearate in the following ratio of components, mg per single dose:

Schisandra fruit powder 180-220 Bees' lyophilized royal jelly 9-12 Dry propolis extract 45-55 Potassium iodide 0.03-0.036 Iron gluconate 36-44 Maltodextrin 40-50 Anhydrous Colloidal Silica Magnesium stearate 3-3.8

The disadvantages of this invention include the fact that the claimed composition is characterized only by an adaptogenic effect, which is mainly provided by the extract of magnolia vine fruits in that low doses for the remaining components are prescribed for a single dose, which makes it impossible to display the beneficial properties of the remaining active substances without using all activity spectrum. In addition, this composition as an adaptogen is not indicated for children, persons suffering from hypertension and with increased sensitivity to preparations based on lemongrass.

The technical task of the invention is the creation of a highly concentrated composition having an expanded spectrum of pharmacological action, increased bioavailability due to the use of a liquid dosage form and an optimally selected ratio of pharmacologically and pharmaceutically compatible active components and their properties.

The stated technical problem is solved due to the synergistic action of the constituent ingredients. The composition includes royal jelly, propolis purified and optionally fructose and glucose syrup, pollen extract, vitamin E, preservative, sweetener and water in the following ratio in wt.% To 100%:

Royal jelly 1-40 Fructose and Glucose Syrup 0.1-22 Pollen extract 0.01-10 Propolis peeled 1-10 Vitamin E 0.01-3 Preservative 0.001-1.5 Sweetener 0.001-1.5 Water Rest

An essential distinguishing feature of the present invention is the presence of pollen in the extract, which reduces the risk of an allergic reaction and expands the spectrum of action of the proposed composition, and the liquid dosage form of the proposed composition, which improves bioavailability and reduces the onset of positive dynamics of treatment.

Instead of glucose syrup and fructose, sugar syrup, fructose syrup or glucose syrup can be used.

The composition may include flavoring.

Purified propolis can be used as a crushed powder or extract.

The water used as a solvent can be deionized, purified, injectable and of other quality that is approved for oral use.

It is preferable to carry out the production of the composition under sterile conditions (to increase the shelf life of the resulting composition (options).

For packaging the composition, it is preferable to use bottles of the minimum volume for the convenience of taking a single dose (for example, 11 ml bottles).

Cooking technology is as follows.

An example of a specific implementation No. 1

Measure the amount of water 30% of the total volume in which the substance is dissolved in the following sequence: royal jelly 1% and homogenized until completely dissolved. Then add glucose syrup 0.05% and fructose 0.05% mixed with alpha-tocopherol acetate (vitamin E) 0.01%. Then a pollen extract of 0.01% beet soaked in 10% of the amount of deionized water is introduced. Separately, purified propolis in an amount of 1% is ground into a fine powder, moistened with 10% water, a suspension is obtained and introduced into the main solution, then a preservative of 0.01% (sodium benzonate 0.005% and potassium sorbate 0.005%) is added, sweetener (stevia extract) 0.01%, thoroughly homogenized and adjusted to 100% with deionized water, mixed thoroughly, passed the mixture through a homogenizer under high pressure, filtered and poured into containers.

An example of a specific implementation No. 2

Measure the amount of purified water 10% of the total volume, in which the substance is dissolved in the following sequence: royal jelly 80% and homogenized until completely dissolved. Then add glucose syrup 11% and fructose 11%, mixed with alpha-tocopherol acetate (vitamin E) 1.0%. Then a pollen extract of 10.0% bee moistened with 10% of the purified water is introduced. Separately, purified propolis in an amount of 10% is ground into a fine powder, moistened with 10% water, a suspension is obtained, it is introduced into the main solution, then a preservative of 1.5% (sodium benzoate 0.5% and potassium sorbate 1.0%) is added, sweetener (saccharin) 1.5%, phosphorus 0.1%, chromium 0.01%, thoroughly homogenized and adjusted to 100% with purified water, mixed thoroughly, passed the mixture through a homogenizer under high pressure, filtered and poured into containers.

An example of a specific implementation No. 3

The production method is a two-phase mixing, then mixing together 2 phases of dissolved substances and then homogenization by filtration under pressure. This technique provides a homogeneous solution without precipitation, which is impossible to achieve for a similar composition obtained by conventional mixing of the ingredients. To do this, measure the amount of water injected 10% of the total volume into a reactor equipped with a stirrer, in this solvent, bee royal jelly 20% is dissolved with constant stirring and homogenized until completely dissolved.

Glucose and fructose syrup, which is an aqueous solution, are prepared in separate reactors.

In a syrup brewing kettle, when heated and continuously stirred, sugar is dissolved to obtain eighty percent sugar syrup. The resulting concentrated sugar solution is cooled to a temperature of 90 degrees and hydrochloric acid is introduced into it in the form of a ten percent solution. The acid solution is administered slowly, in small portions, with continuous stirring. Thirty minutes later, most of the sugar is hydrolyzed, after which you can neutralize the acid with an eight percent solution of sodium bicarbonate. To do this, very carefully, in small portions with vigorous stirring, the solution is introduced into pre-chilled syrup. This is done in order to avoid discoloration and clouding of the syrup as a result of the decomposition of glucose and fructose in an alkaline environment.

The resulting fructose and glucose syrup is measured in an amount of 22% of the mass fraction of the final product, fed to a reactor equipped with a paddle stirrer and a steam jacket. When heated to a temperature of no higher than 40 ° C and constantly stirring until the mass is homogeneous, successively add acetate (vitamin E), 0.1%, bee pollen extract to the syrup of alpha-tocopherol 8% (pre-prepared: soaked in 10% of the amount of water injected ) The resulting mixture under pressure is fed into a common reactor with a solution, mixing until uniform.

Purified propolis, pre-cooled to -10 ° C (the temperature of the highest brittleness of the raw material), is ground into a fine powder in a mill, the necessary amount is weighed (2% of the total weight of the finished composition), introduced into a reactor with 10% chilled water up to + 10 ° C , mix to a homogeneous suspension, which is piped into the main reactor, and preservative 0.2% (potassium sorbate 0.1%, sodium benzoate 0.05%, potassium acesulfiram 0.05%) is mixed with the main solution in the general reactor, sweetener (erythritol) 0.02%, thoroughly homogenized and adjusted to 100% with water in ektsionnoy, viscous homogeneous solution was thoroughly mixed, the mixture was passed through a homogenizer under high pressure and vacuum, passed through a filter system under vacuum, then the solution enters the dosing machine calibrated at 11 mL, filling into vials is performed while the feed stream open vials. Vials are closed automatically on the same line.

An example of a specific implementation No. 4

Measure the amount of water with deionized 20% of the total volume, in which the substances are dissolved in the following sequence: royal jelly milk 35% and homogenized until completely dissolved. Then add glucose and fructose syrup (fructose and glucose 1: 1) 20% mixed with alpha-tocopherol acetate (vitamin E) 0.1%, purified propolis 2%, preservative 0.2% (sodium benzonate 0.1% and potassium sorbate 0.1%), sweetener (sucralose) 1.5%. Then the pollen extract is introduced with 8% bee soaked in 10% of deionized water, thoroughly homogenized and brought to 100% with deionized water, mixed thoroughly, the mixture is passed through a homogenizer under high pressure, filtered and poured into containers.

Next, the solution is supplied for labeling and packaging in a shipping container. The solution in appearance is a cloudy dark liquid with a sour-sweet taste and a pleasant aromatic odor. Store in a dry, dark place at room temperature. Shelf life is 1.5 years.

The solution is recommended to take 11 ml once a day at night. There are no contraindications, with the exception of individual intolerance to the components.

An example of a specific implementation No. 5

Measure the amount of water with deionized 20% of the total volume, in which the substances are dissolved in the following sequence: royal jelly milk 35% and homogenized until completely dissolved. Then add glucose and fructose syrup (fructose and glucose 1: 1) 20% mixed with alpha-tocopherol acetate (vitamin E) 0.1%, purified propolis 2%, preservative 0.2% (sodium benzonate 0.1% and potassium sorbate 0.1%), sweetener (sodium cyclamate) 1.5%. Then pollen extract of 8% soaked in 10% of deionized water is introduced, thoroughly homogenized and adjusted to 100% with deionized water, mixed thoroughly, the mixture is passed through a homogenizer under high pressure, filtered and poured into containers.

Next, the solution is supplied for labeling and packaging in a shipping container. The solution in appearance is a cloudy dark liquid with a sour-sweet taste and a pleasant aromatic odor. Store in a dry, dark place at room temperature. Shelf life is 1.5 years.

The solution is recommended to take 11 ml once a day at night. There are no contraindications, with the exception of individual intolerance to the components.

All ingredients included are known and approved for use.

Royal jelly improves trophic tissue. It activates enzymatic metabolism, improves tissue respiration. Excites the parasympathetic division of the nervous system, increases the amount of adrenaline. Improves in general, the state of the central and peripheral nervous system, improves brain absorption of glucose, oxygen and the activity of the AT phase. Normalizes blood pressure, blood composition, bone marrow function, increases protein synthesis. It treats infertility and impotence. Stimulates the activity of the adrenal cortex, helps relieve fatigue, improves sleep, appetite, memory and working ability.

The pollen extract includes:

vitamins: A, B1, B2, B5, B6, B9 (folic acid), B12, C, P, PP, H (biotin), provitamin A (it is 20 times more than in carrots);

proteins that contain all amino acids - interchangeable and irreplaceable (not formed in the human body);

28 micro- and macrocells, including the most vital: sodium, potassium, nickel, titanium, vanadium, chromium, phosphorus, zirconium, beryllium, boron, zinc, lead, silver, arsenic, tin, gallium, strontium, barium, uranium, silicon , aluminum, magnesium, manganese, molybdenum, copper, calcium, iron, sulfur, fats, consisting of 70% of alpha-linolenic acid and 3-4% of linoleic acid, as well as saturated and unsaturated fatty acids; 6 forms of natural Sugars: fructose, glucose, stachiosis, sucrose, raffinose and pentose;

active enzymes and coenzymes: amylase, diastase, sucrose, phosphotase, cosimase, etc .;

carotenoids, bioflavonoids with immunostimulating, antioxidant, general strengthening effect; phytohormones (plant endocrinologically active substances); volatile (plant substances that can inhibit the growth of bacteria, fungi, protozoa). Due to such a diverse composition and high activity of the components, bee dust - Propolis purified - has anti-inflammatory properties. It helps to prevent, weaken and stop the development of the inflammatory response of the human body to the introduction of a foreign microorganism.

Strengthens the immune system, increasing the level of gamma globulins in the body.

The increase in bioavailability and adaptogenic action of the proposed composition compared to the prototype and beekeeping products in a pure composition was carried out on mice using generally accepted experimental methods.

The experiments were carried out on CBA mice of both sexes weighing 19-20 g. To determine the total physical endurance, a generally accepted swimming technique was used in a pool with a water temperature of 20.0 ± 0.5 ° C with a load of 5% of body weight. 3 groups of 5 mice each were created. The first group of mice was injected with a solution of the test agent intragastrically once 1 hour before testing in volumes of 0.5 and 1.0, 3.0, 5.0 ml / kg. The second group was introduced the composition of the prototype and the third group - a mixture of bee products (royal jelly, extract of pollen, purified propolis) 1 time per day 30 minutes before feeding. The total physical endurance of animals was determined by swimming the animals to complete fatigue, the criterion of which was a 10-second immersion of the animal under water. The data obtained are given in table 1. As follows from the data shown in table 1, with a single administration of the test drug in volumes of 3.0 ml / kg, an increase in overall physical endurance by 47% was noted compared with the data in mice of the control group, and in the composition of the prototype by 28% of the tested drug. In a volume of 5 ml, 37% and 26, respectively. It was also established that the severity of the adaptogenic effect of the test drug depends on the time of administration, which indicates an increase in the bioavailability of the proposed composition, the stimulating effect of the test drug is already visible 30 minutes after its single administration in the volume of 3.0 ml / kg. In 1.0 hour after drug administration, the performance of white mice increased by almost 50% and remained at this level for another 5 hours. The adaptogenic effect of the composition of the prototype after the introduction of 3.0 ml / kg appears after 1 hour, and in group 3 only after 2 hours of single use.

Thus, the obtained data indicate that the test tool has a pronounced adaptogenic effect and has increased bioavailability compared to the prototype and bee products.

To disclose the invention below presents the results of studies to study the effectiveness of the proposed tool.

Example No. 1. Patient Lazarskaya I.V. 37 years.

Complaints of severe pain in the epigastric region before eating (stop 30 minutes after eating), belching, bloating, frequent vomiting. Studies have shown the presence of gastric diameter manifestations. Fibrogastroscopy showed small expressions of the stomach.

Appointed: The use of 1 bottle (11 ml) twice a day on an empty stomach for 2 weeks.

A second examination on the third day showed the presence of positive dynamics.

Lack of belching, bloating, vomiting. Pain in the epigastric region was absent.

Repeated fibrogastroscopy showed scarring of ulcerative lesions of the stomach.

Example No. 2. Patient Silyavsky G.U. 48 years old.

Complaints of heaviness in the abdomen after eating, pain in the upper abdomen on an empty stomach or after eating, nausea, vomiting, belching, decreased appetite, symptoms are not constant, signs may appear and disappear.

An endoscopic examination of the stomach showed the presence of gastritis with low acidity.

Prescribed: Take 1 bottle (11 ml) twice a day on an empty stomach for 2 weeks

A second examination on the third day showed the presence of positive dynamics, the absence of pain, improved appetite, improved well-being.

It is recommended to continue taking the drug.

Example No. 3. Sizova L.M. 46 years old.

Condition after suffering stress and severe infection, frequent headaches, fatigue.

The drug was prescribed once a day, at night in the amount of one bottle (11 ml) for 1 week.

After repeated use on the third day, there was a positive trend: improved mood, appetite, well-being, an increase in the duration of physical activity.

Thus, the proposed composition has an adaptogenic, anti-inflammatory and performance enhancing effect and can be used to treat diseases of the gastrointestinal tract (gastritis, ulcer) and to adapt the body in adverse conditions and increase performance.

Table 1 The effect of adaptogenic agents on the overall physical endurance of white mice, depending on the volume administered Groups of animals Volume ml / kg Duration of swimming, min Experimental 1 (test tool) 0.5 15,5 Experienced 2 (test tool) 1,0 19.8 Experienced 3 (test tool) 3.0 22.0 Experienced 3 (test tool) 5,0 20.5 Experienced 4 (prototype) 0.5 15.1 Experienced 5 (prototype) 1,0 19.1 Experienced 6 (prototype) 3.0 twenty Experienced 7 (prototype) 5,0 19.7 Experimental 8 (bee products) 0.5 15.0 Experienced 9 (bee products) 1,0 15.8 Experienced 10 (bee products) 3.0 19.1 Experienced 11 (bee products) 5,0 18.8 Control 14.9

Claims (2)

1. A composition that improves performance and has an adaptogenic, wound healing, anti-inflammatory effect, containing royal jelly, propolis, characterized in that it additionally contains fructose and glucose syrup taken in equal proportions, flower pollen extract, tocopherol acetate (vitamin E), preservative , sweetener, water in the following ratio, wt.%:
royal jelly 1-40 fructose and glucose syrup 0.1-22 pollen extract 0.01-10 propolis peeled 1-10 vitamin e 0.01-3 preservative 0.001-1.5 sweetener 0.001-1.5 water rest 2. A composition that improves performance and has an adaptogenic, wound healing, anti-inflammatory effect according to claim 1, containing potassium sorbate, sodium benzoate, potassium acesulfiram, or a combination thereof as a preservative.