RU2232588C2 - "apilarmil" tablets based upon substances of maternal larvae of anabolic and actoprotective action - Google Patents

Abstract

FIELD: pharmaceutics, medicine.

SUBSTANCE: the present innovation deals with developing new medicinal products. Tablets contain as biologically active component: adsorbed homogenate of maternal larvae including lactose, pectin, sorbic acid, citric acid, and as additional substances: a sweetening agent, calcium stearate and an aromatizer at the following ratio of components in tablet mass/100 tbl: homogenate of maternal larvae 12.0-14.5, lactose 30.0-38.0, pectin 3.0-5.0, sorbic acid 0.1-0.4, citric acid 0.03-0.5, sweetening agent 0.05-0.5, calcium stearate 0.5-1.0, aromatizer 0.1-0.5. The method declared enables to launch wide-scale manufacturing of cheap and efficient curative product.

EFFECT: higher efficiency.

3 tbl

Description

The invention relates to the field of pharmacy and medicine and relates to the technology of solid dosage forms, namely, Apilarmil tablets.

Romania has patented a method for producing a biologically active product from drones larvae, or working bees, or queens (Pat. OSMI No. 74872/1980), which are biologically active substances for the production of biologically active food additives and cosmetics. Developed tablets based on drone larvae - the Apilarnil drug, which is effective in the treatment of mental and nervous diseases (N.V. Ilieshiu, 1983).

In Russia, the patented “Dietary supplement for obtaining regenerative cosmetics” / Pat.No.2128501. This biologically active supplement is a bee drone larvae recommended for regenerative cosmetics.

Not a single medicinal or therapeutic product has been patented containing a homogenate or lyophilisate of uterine bee larvae.

It was experimentally established that the composition and properties of the uterine larvae of bees are close to the royal jelly - apilak used in medicine (M.D. Mashkovsky, 1998). In this regard, for the prototype, we took a solid dosage form based on royal jelly - Apilaka tablets (MD Mashkovsky, 1998), containing 0.01 g of apilak for use under the tongue. This drug is recommended for use in case of malnutrition and anorexia in children, adults - in case of hypotension, eating disorders, neurotic disorders, impaired lactation in the postpartum period and other diseases.

The disadvantage of this drug is that it uses expensive raw materials.

The aim of this invention is the creation of tablets "Apilarmil" with pronounced anabolic and actoprotective effects, prepared on the basis of a natural pharmacologically active component, which is very low cost.

This goal is achieved by pressing the adsorbed homogenate of the uterine larvae with the addition of glidants, sweetener and flavoring in the following ratio of components in the tablet mass per 100 tablets, g:

Homogenate of uterine larvae 12.0-14.5

Lactose 30.0-38.0

Pectin 3.0-5.0

Sorbic acid 0.1-0.4

Citric acid 0.03-0.5

Sweetener 0.05-0.5

Calcium stearate 0.5-1.0

Flavor 0.1-0.5

The amount of excipients was selected so that 1 tablet contains 25-30 mg of dry matter of the homogenate of the uterine bee larvae, which we recommend as a 1/2 dose for an adult.

The composition of the adsorbed homogenate of the uterine bee larvae, which is part of the tablets, is the following, wt.%:

Homogenate of bee brood (uterine larvae) 25.0

Lactose 67.0

Apple Pectin 8.0

Preservatives:

Sorbic acid 0.1-0.4

Citric acid 0.03-0.5

The technological scheme for producing tablets from the adsorbed homogenate of uterine bee larvae is simple. The adsorbed uterine larva homogenate moistened with water, containing sorbic acid, lactose, pectin, citric acid, is passed through a granulator with a hole size of 3 mm. Then the obtained granulate is placed in a thermostat and dried at a temperature of 40 ° C for 2 hours. After drying, the granulate is wiped through a sieve with a hole size of 2 mm, calcium stearate, flavor, sweetener are added. Tablets are obtained by pressing granulate on a rotational tablet machine RTM-12 or another model.

An essential distinguishing feature of the claimed dosage form is the use of an practically non-toxic natural component of the uterine bee larvae as an active substance, containing a complex of biologically active substances that determine the high pharmacological activity of the dosage form. The advantages of the proposed drug are:

- low cost of production, which is associated with the use of domestic, cheap, affordable, waste raw materials, and also because of the simple and non-laborious scheme for obtaining both raw materials and dosage form;

- to simplify the production of solid dosage forms based on uterine larvae, an adsorbed homogenate is used, which is a ready-made semi-finished product for producing tablets;

- the content of the homogenate of uterine larvae in 1 tablet is 25-30 mg of dry matter, which is ^1/2 _{of the} recommended dose for an adult;

- minimal risk of side effects;

- high pharmacological activity.

A selected recipe for adsorbed uterine larva homogenate has the necessary technological properties: dosing, compressibility, which ultimately ensures the production of tablets of the required quality.

In uterine larvae, a high content of protein (up to 52% dry matter), amino acids (up to 39% dry matter), including essential (about 38% of the total amount of amino acids), nucleic acids (1.1-1.3% dry substances), enzymes (lipases, proteases, phosphatases, ureases, dehydrogenases, amylases, etc.), phospholipids (1.1-1.5%), steroid hormones (testosterone, cortisol, progesterone, etc.), carbohydrates (fructose, glucose, galactofuranose, etc.), a complex of substances of the lipid fraction, micro and macro elements, vitamins A, D, E, PP, group B and other biologically active active components.

Uterine larvae of bees contain a complex of biologically active substances, which determine a number of their pharmacological effects: immunotropic, adaptogenic, anabolic, actoprotective effect. Steroid hormones (androgenic), amino acids, enzymes, minerals, B vitamins, vitamins A, D cause anabolic effects.

The presence of a complex of biologically active substances: carbohydrates, amino acids (glycine, methionine, glutamic acid), hormones characterizes actoprotective effect, improvement of human brain activity when using drugs based on uterine larvae. In addition, the value of uterine larvae is also due to the extremely high content of vitamins A and D. This circumstance may serve as the basis for the use of uterine larvae and tablets based on them in baby food.

The whole complex of biologically active components of uterine larvae determines their immunotropic effect.

The effect of Apilarmil tablets based on the homogenate of uterine larvae on weight gain was studied on white outbred rats (females and males) weighing 50-60 g. Groups of 6 animals were isolated. For 21 days, the animals were injected once a day into the stomach through a probe aqueous solutions of tablets based on uterine larvae. Two comparison groups were administered a solution of Apilak tablets. The control group received saline. Every 3 days, the weight of the animals was determined.

As a result of the study, it was found that the Apilarmil tablets have an anabolic effect (Table 1).

To assess the actoprotective activity of the Apilarmil tablets, the open field method was used. The study of this activity of tablets based on uterine larva homogenate was carried out on white outbred rats of both sexes of 6 months of age (adults) weighing 200-250 g and 24-month-old (old) weighing 300-350 g. Animals in the first group received oral aqueous solutions of the studied the drug. The comparison groups were injected with a solution of apilak tablets, the control group received 0.5 ml of physiological saline.

We studied the effect of tablets on locomotor, orientational research activity and emotional state of animals. The test animal was placed in the center of a quadratic area measuring 80x80 cm, divided into 25 equal squares and having holes with a diameter of 3 cm. During 3 minutes of observation, the number of crossed squares (motor activity), the number of standing on the hind legs and peering into the holes were recorded (tentative research activity), the number of stereotypical movements (emotional activity) (tab. 2, 3).

As a result of the study of pharmacological activity, it was found that tablets based on uterine larvae increase the motor, tentative-research activity and emotional state of animals in relation to the control group already on the 4th day from the start of the study. In groups of animals that were injected with the studied substances, a weakening of emotional activity was observed.

Thus, the conducted experimental studies have shown that Apilarmil tablets have anabolic, actoprotective effect and can be offered both as general tonic, anabolic and auxiliary agents in pediatric and geriatric practice.

The use of the claimed composition of the tablets will allow to organize the mass production of domestic inexpensive and effective therapeutic agents.

Claims (1)

Tablets with anabolic and actoprotective effects, characterized in that as a biologically active component they contain an adsorbed homogenate of uterine larvae, including lactose, pectin, sorbic acid, citric acid, and as auxiliary substances - sweetener, calcium stearate and flavor in the following ratio of components in tablet mass per 100 tablets, g: Homogenate of uterine larvae 12.0-14.5 Lactose 30.0-38.0 Pectin 3.0-5.0 Sorbic acid 0.1-0.4 Citric acid 0.03-0.5 Sweetener 0.05-0.5 Calcium stearate 0.5-1.0 Flavor 0.1-0.5