RU2456005C1 - Method for preparing biologically active preparation - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics, particularly a method for preparing a biologically active preparation of a male larval bee homogenate. method for preparing the biologically active preparation involving preparing the a male larval bee homogenate, mixing the prepared homogenate and an adsorbent of mixed lactose and glucose taken in appropriate proportions, grinding and drying the adsorbed homohenate with the mixing process performed by grinding the fresh homogenate and the adsorbent; grinding and drying the adsorbed homogenate are followed by granulating in a propolis spirit solution in the certain environment. The biologically active preparation prepared by the declared method containing male larval bees, propolis, the adsorbent wherein the ingredients are taken in specific proportions.

EFFECT: method provides preparing the preparation showing higher biological activity and stable properties.

3 cl, 2 tbl, 2 ex

Description

The invention relates to the field of preparation of bioenergy preparations based on beekeeping products.

Drone brood is a relatively new beekeeping product used in the preparation of dosage forms and food additives due to the biostimulating properties inherent in this product.

It is known, for example, the use of a drone brood homogenate or lyophilisate as a substance with anabolic and actoprotective effects (RU 2287334, 11/20/2006).

Known drug for the prevention and treatment of adenoma and prostatitis, containing drone brood, pollen, ascorbic acid, vitamin E, excipients (RU 2414229, 03/20/2011).

Known biologically active food supplement containing the following components (wt.%): Drone brood - 1-70, leuzea - 5-70, ascorbic acid (vitamin C) - 1-70, vitamin E - 0.05-30 and fillers - calcium stearate, talc, lactose - the rest. The additive has an effect on anabolic effects, expressed in the rapid muscle building of athletes (RU 2390270, 05.27.2010).

Medicines for the integrated activation of the body’s defenses, treatment and prevention of various diseases, containing preparations prepared on the basis of drone brood, are also described in RU 2345523, 10.27.2007, RU 2366435, 09.09.2009, RU 2372094, RU 2245155, 01.27.2005 , RU 2233666, 08/10/2004.

The activity of drugs based on natural products, including beekeeping products, largely depends on how they are prepared or how to isolate active substance from them. Recently, much attention has been paid to the development of effective methods for producing preparations containing drone brood.

A known method of preparing a biogenic stimulant, comprising 50% of the biologically active mass of drones larvae, 49.7% sodium chloride solution and 0.3% preservative, consisting in that cells with live healthy drone brood aged 18-22 days are kept in the refrigerator, then, brood cells are opened and drones of the same size, light gray in color, are selected, after which drones are crushed in a sterile laboratory mill, diluted with sterile sodium chloride solution and autoclaved at a temperature of 120 ° C and pressure uu steam atmosphere of 1.5, then adjusted weight sterile solution of sodium chloride at a concentration of 0.9% to the original volume, added preservative (phenol) and dispensed into sterile containers sealed and autoclaved (RU 2395289, 27.07.2010).

A known method is that drones larvae are frozen at a temperature, then thawed and homogenized, while a stabilizing medium using a 5% glucose solution in a ratio of 1:10 with the addition of a solution of chloroform or salicylic acid, followed by sublimation. Sublimation is carried out in a vacuum chamber at a temperature of shelf heating to 30-45 ° C. When the temperature of the preparation reaches 20-22 ° C, the temperature of the shelves is reduced to 25 ° C and drying is done within 22-24 hours (RU 2258522, 08/20/2005).

A similar method for the preparation of a biologically active preparation is known, in which, to increase the effectiveness of the agent, an organo-selenate compound, diacetophenonyl selenide, is added to the homogenate, and then a drying medium is added to the mixture of the homogenate and diacetophenonyl selenide (a sucrose-gelatin mixture containing 10% sucrose and 5% gelatin) in the ratio of homogenate and drying medium 1:10 (RU 2414919, 03/27/2011).

The methods described above are characterized by complexity in execution and instability of the properties of the target products.

Closest to the proposed method, the technical essence is a method for preparing a biologically active preparation from drones larvae, in which the wax caps of a sealed brood are cut off, the honeycomb is placed in a honey separator, up to 95% of the larvae are removed within 10-12 minutes, they are homogenized, and the adsorbent is added - a mixture of lactose and glucose, thoroughly triturated, the resulting crude adsorbed drone brood homogenate is stored at a temperature of 4-6 ° C for about 3 months before drying (V.I. Lebedev, M.A. Legovich. Harvesting drones' tide // Beekeeping, No. 3, 2003, pp. 52-54).

However, obtained in a known manner, the drug has insufficient biological activity.

The objective of the present invention is to develop a simple way to obtain a drug that provides a product with high efficiency, with stable properties while expanding the spectrum of its use.

The problem is solved by the described method of preparing a biologically active preparation, which consists in preparing a homogenate of bee drone brood larvae, mixing the prepared homogenate with an adsorbent based on a mixture of lactose and glucose taken in a mass ratio (22-25): 1, respectively, grinding and drying the adsorbed homogenate, the mixing is carried out by grinding 1 weight part of freshly prepared homogenate with 6-9 weight parts of the adsorbent, and after grinding and drying the adsorbed Nogo homogenate subjected to granulation with an alcoholic solution of propolis to a size of 1.5-2.0 mm granules with providing propolis content in the resulting preparation in an amount of 0.1-0.2 wt.%.

According to the present invention, components prepared from medicinal plants and / or their extracts, vitamins and antioxidants can be added to the prepared biologically active preparation, the preparation being carried out by co-granulation of an aqueous solution of a ground preparation containing the selected component, drone brood, adsorbent and propolis , followed by drying the resulting product at room temperature for 45-90 minutes to a moisture content not exceeding 10%.

Preferably, the preparation of a biologically active preparation is carried out to obtain the optimal ratio of components equal to (wt.%):

drone brood 7.9-8.3 propolis 0.1-0.2 adsorbent 89-92.

In the scope of the totality of the features of the claimed invention, a solution to the problem is achieved. Going beyond the stated quantitative features does not allow to obtain a high technical result for the following reasons.

The adsorbent contains a mixture of lactose and glucose at a mass ratio of (22-25): 1, since it has been experimentally established that this ratio is optimal for preserving drone brood.

Mixing the adsorbent with the homogenate of drone brood larvae is carried out by grinding 1 weight part of freshly prepared homogenate with 6-9 weight parts of the adsorbent, since this ratio is optimal for drying the finished product in a gentle manner.

Carrying out an additional granulation stage in comparison with the prototype with an alcohol solution of propolis to a granule size of 1.5-2.0 mm with a propolis content in the resulting preparation in an amount of 0.1-0.2 wt.% Allows to increase the efficiency of the target product and to stabilize its properties .

The possibility of introducing additional active components into the drug provides the possibility of expanding the spectrum of its use.

The following are examples of the preparation and use of the drug we have received, only illustrating the claimed invention, but not limiting it.

1. An example of obtaining the drug No. 1.

Preparation of source components:

A. Preparation of the adsorbent.

Glucose and lactose are dried at a temperature of + 105 ° C to constant weight in a control cabinet and mixed in a mixer-granulator at a ratio of (22-25): 1. The mixture is sieved through a vibrating screen with a mesh size of 0.02 mm.

B. Preparation of an alcoholic solution of propolis.

Prepare a 10% alcohol solution of propolis, based on 100 g of crushed propolis per 1 liter of 70% ethyl alcohol. Insist 7-10 days in a dark place. After tincture is drained, filtered.

Preparation of a working alcohol solution of propolis is carried out as follows: 300 ml of a 10% alcohol solution of propolis are mixed with 200 ml of distilled water and 500 ml of 96.4% ethyl alcohol and the resulting amount of solution is used for granulation of 40.0 kg of drone brood mixture with prepared adsorbent .

B. Preparation of adsorbed drone brood.

A drone brood homogenate is prepared at the larva collection site in an equipped mobile laboratory. Different age (9-11 daily from the day of laying the eggs), freshly selected drone brood in the comb is printed. The larvae and precubae are removed from the honeycomb with tweezers or shaken on a tray, placed in a homogenizer, thoroughly homogenized and filtered through a sieve from nylon fabrics in a chilled, clean, alcohol-treated container.

The preparation of an adsorbed drone brood is carried out immediately after preparation of the homogenate. The process of homogenization and adsorption is carried out no more than 1.5 hours. The adsorption of the drone brood is carried out by thoroughly grinding in a porcelain mortar one part of a freshly prepared homogenate with 6-9 parts of the adsorbent (by weight). Grinding is completed when the surface of the mixture acquires a brilliant hue and the resulting dense mass does not adhere to the inner surface of the porcelain mortar. Rubbing is carried out for no more than 15-20 minutes in a chilled bowl. The obtained adsorbed drone brood is weighed, crushed, passing through a sieve, laid out on cuvettes of 150 g for each cuvette with a thin layer of 2-3 mm. The cuvettes are placed in a vacuum cabinet. Drying is carried out without increasing temperature for 1.5 hours. The humidity of the drone adsorbed brood after drying does not exceed 1.8%.

G. Obtaining a granular preparation.

The dried adsorbed drone brood is placed in a granulator and granulation is carried out with a working alcohol solution of propolis, prepared as indicated in item B. After granulation, the product is sieved through a sieve with a hole diameter of about 2 mm. The granulate that has not passed through a sieve is subjected to repeated granulation. The sieved granulate is laid out in cuvettes (800-1000 g each) with a thin even layer and placed in a vacuum oven for drying. Drying is carried out at room temperature. Drying time 45-90 minutes.

As a result of numerous experiments to obtain the drug, the optimal ratio of the starting components in the obtained preparation was revealed, which amounted to (wt.%): Drone brood - 7.9-8.3; adsorbent - 89-92; propolis - 0.1-0.2.

The resulting preparation was used by us as the basis for the production of biologically active additives (BAA).

2. An example of obtaining a preparation No. 2, additionally containing active components.

Stages of preparation:

1. As a raw material for the production of dietary supplements take the product obtained as described above, as well as dry extract of rose hips and lemongrass, as well as vitamins B6 and B1. All milled raw materials are sieved on a vibrating screen through a sieve of silk fabric No. 38 or of a nylon fabric No. 43. Re-grind the components that have not passed through the specified sieves and sift them again on a vibrating sieve.

2. Prepare distilled water.

3. Sifted raw materials are placed in a mixer-granulator, mixed and granulated with distilled water. Water consumption - 400 ml per 20.0 kg of the mixture. After granulation, the mixture is sieved through a sieve with a hole diameter of about 2 mm. The granulate that has not passed through a sieve is subjected to repeated granulation.

4. The sifted granulate is laid out in ditches (800-1000 g each) with a thin even layer and placed in a vacuum oven for drying. Drying is carried out without applying temperature. The drying time is 45-90 minutes. The resulting preparation has the following composition shown in table 1.

Table 1 Name of components The number of components,% The drug according to example 1 93,613 Rosehip extract dry 6.0 Schisandra extract dry 0.35 Pyridoxine Hydrochloride (Vitamin B6) 0.02 Thiamine Chloride (Vitamin B1) 0.017 Total 100.0

The characteristics of the resulting preparation are shown in table 2.

table 2 Name of indicator Norm Humidity,%, no more 10.0 Mass fraction of decenic acids,%, not less 0,045 Schizandrin content,%, not less than 0.0035 Flavonol content,%, not less than 0.06 Vitamin B1 content,%, not less than 0.017 Vitamin B6 content,%, not less than 0.02 The content of ecdysteroids,%, not less than 0.0014

We conducted studies of the effectiveness of the drug described above and on the basis of these studies gave the following recommendations for its use.

Supplements are recommended for adults by 1 teaspoon (5.0 g) once a day in the morning during meals as a biologically active food supplement - an additional source of vitamins B6, B1, flavonols, a source of schizandrin containing ecdysteroids.

The use of 5.0 g per day provides a daily human need for vitamins B6 and B1 by 50% (1.0 mg and 0.85 mg), in schizandrine - by 35% (0.175 mg), in flavonols - by 10% (3 , 0 mg).

Especially effective is the use of the preparation No. 2 described above for various types of physical activity.

The following methods of using this drug are recommended:

1. For beginners (the transition period from a sedentary lifestyle to low-intensity exercise and gentle exercise therapy) workouts 1-2 times a week: take 5 g per day, if possible - start taking 7-10 days before the workouts, 2 months break (step aerobics, exercise bikes, aqua aerobics, dancing, shaping, Pilates, yoga, running).

2. For those who continue aerobic training of medium intensity with an average level of training - 5 g per day, a break of 1 month or a dose reduction to 2.5 g for 1 month (step aerobics, exercise bikes, aqua aerobics, dancing, shaping, Pilates , yoga, running, interval training - a combination of aerobic exercise and power load).

3. For strength training involving all muscle groups (combination of aerobic and anaerobic loads, on simulators and with weights), 5 g daily with 2 workouts per week, 7-10 g with 3 or more workouts per week for 2-3 months, a break of 1 month or a dose reduction in 1 month to 2.5 g.

4. For strength training with muscle building: it is used only during the period of maintaining weight between building cycles - 10-15 g per day for training more than 3 times a week, 5-7 g for training less than 3 times a week until the next building period. It is not used in conjunction with anabolic steroids.

5. Running, skiing, swimming, rowing, intensive physical work 5 days a week - 5 g daily for 1 month, 1 month break.

In a similar way, within the scope of the present invention, we obtained and tested other biologically active preparations based on drone brood, the composition of some of which is given below.

The drug No. 3 contains the product of example 1, namely 99.4-98.5%, vitamins C, A, E in the amount of 0.1-0.5% and antioxidants: selenopyran and dihydroquercetin in the amount of 0.5-1% The drug is intended to improve the functional state of the cardiovascular system, normalize lipid metabolism, prevent atherosclerosis, and improve the psychoemotional state of an elderly person.

The drug No. 4 contains the product of example 1, namely 98.25-88.5%, plant extracts (yohimbe) 1-10%, vitamins E, C, B1, B12 in the amount of 0.25-0.5% and antioxidants : selenopyran or dihydroquercetin in the amount of 0.1-0.5%. The drug is intended to increase libido, improve the functional state of the male reproductive system.

The drug No. 5 contains the product of example 1, namely, 97.4-88.5%, vitamins 0.1-0.5%, antioxidants 0.5-1%, plant extracts of adaptogens 1-5% and plant extracts of immunostimulants 1-5% and is intended to improve the state of the immune system, nonspecific prevention of seasonal colds, use during recovery from injuries and operations, use before planned surgical interventions.

Thus, we have developed a well reproducible and simple way to obtain effective biologically active preparations with stable properties having a wide range of uses.

Claims (3)

1. A method of preparing a biologically active preparation, comprising preparing a homogenate of bee drone brood larvae, mixing the prepared homogenate with an adsorbent based on a mixture of lactose and glucose, grinding, drying the adsorbed homogenate, characterized in that a mixture of lactose and glucose taken in bulk is used as an adsorbent the ratio of (22-25): 1, respectively, mixing is carried out by grinding 1 wt.h. freshly prepared homogenate with 6-9 parts by weight adsorbent, and after grinding and drying the adsorbed homogenate, it is subjected to granulation with an alcohol solution of propolis to a granule size of 1.5-2.0 mm, dried, ensuring the content of propolis in the resulting preparation in an amount of 0.1-0.2 wt.%. 2. The method according to claim 1, characterized in that additional components selected from the medicinal plants and / or their extracts, vitamins and antioxidants are added to the prepared preparation, the preparation being carried out by co-granulation with an aqueous or alcoholic solution of the ground preparation and an additional component, followed by drying the resulting product at room temperature for 45-90 minutes to a moisture content not exceeding 10%. 3. The biologically active preparation obtained by the method according to claim 1, including drone brood, propolis, adsorbent, in the following ratio of components equal to (wt.%):
drone brood 7.9-8.3 propolis 0.1-0.2 adsorbent 89-92