RU2288727C1 - Medicinal formulation of gel-base pantohematogen and method for its preparing - Google Patents

Abstract

FIELD: chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to a pantohematogen-base medicinal formulation for external using that comprises the following components, wt.-%: dry pantohematogen, 0.01-6; polymeric gel-forming composition, 0.1-20, and water, the balance. Proposed medicinal formulation provides using pantohematogen an aqueous solution without addition of alcohol and therefore it can be used in cases wherein alcohol-containing formulations are contraindicative - in burns of different degree, small skin damages and others and can be used in treatment of patients showing intolerance to alcohol-containing preparations. Method for preparing the pantohematogen medicinal formulation for external using involves preparing "dry" pantohematogen aqueous solution in the ratio limits pantohematogen : water = (1:50)-(1:200) by weight and solution is kept under normal conditions for 1 h and filtered. Additionally an aqueous solution of rare-linked polymer is prepared in the ratio = (1:10)-(1:200) and an aqueous solution of neutralizing agent in the amount necessary for providing slightly alkaline medium of final solution. In the volume ratio of pantohematogen aqueous solution and rare-linked polymer in the ranges = (3:1)-(1:10) components are mixed and stirred to obtain the homogenous solution. Then neutralizing agent aqueous solution is added to a mixture and stirred to obtain homogenous solution with slightly alkaline reaction (pH = 6-8). The advantage of proposed technology in preparing the medicinal formulation involves its simplicity and providing prolonged fitness period.

EFFECT: improved preparing method.

6 cl, 1 ex

Description

The invention relates to medicine, namely to the technology for the production of medicines, and can be used in pharmacology for the preparation of preparations based on dry blood of antler deer - pantogematogen "dry" for external use. The preferred field of application of the new dosage form is the treatment of diseases where alcohol-containing forms are contraindicated for burns of varying degrees, the presence of minor skin lesions, etc., and the treatment of persons with intolerance to alcohol-containing drugs.

In oriental medicine, antlers - dried young non-ossified antler antlers (red deer, red deer, sika deer and red deer) are widely used in the treatment of anemia, nervous exhaustion, general weakening of the body after infectious diseases, cardiovascular failure, wound healing, etc. . In Russia, pantocrine (alcoholic extract of antlers), developed back in the 20s of the 20th century, gained the greatest popularity. In the 60s of the last century, analogues of pantocrine were made: Rantarin, Velcornin, etc. In the Chinese Pharmacopoeia of the 16th century, covering medical knowledge for 4 thousand years, a special section is devoted to non-ossified deer antlers - antlers (lu-rong), ossified deer antlers - Antler (jio) and his blood (shue). The main healing property of antlers is blood. Antlers that have lost blood do not have a therapeutic effect on the human body.

It is known that from the defibrinated blood of antler deer taken during the period of antler cutting using conventional hematogen production technology, a psychostimulant called Pantogematogen is made (Patent RU No. 20088008).

It is also known that it has a nootropic and adaptogenic effect, and a method for producing it from donor blood of Altai deer (similarly, you can get dry blood of other antler deer). In this way dry dehydrated blood of maral was obtained - pantogematogen "dry", which turned out to be an effective tool in the treatment of various somatic diseases (patent RU No. 2130314). Preparations based on dry dehydrated blood of antler deer belong to the group of adaptogens and have a multivalent effect on the human body. They are used in various forms: "dry" - in the form of tablets, capsules and "liquid" - in the form of freshly prepared bath solutions, microcurrent physiotherapy, microclyster, etc.

For the prototype of the invention adopted "Dosage form pantohematogen on a gel basis" (patent RU No. 2200564). This external dosage form includes pantohematogen and an aqueous medium. The aqueous medium contains a polymer gelling composition. Pantohematogen is introduced in the form of a water-alcohol solution containing 8-14% ethyl alcohol, in the following ratio of components, wt.%:

- pantogematogen "dry" in the form of a 3% aqueous alcohol solution - 5-35;

- polymer gelling composition - 0.5-15;

- water - the rest.

The production technology of the dosage form of the prototype is as follows. First, an aqueous-alcoholic solution is prepared in the usual manner by adding ethyl alcohol to distilled water. The strength of the water-alcohol solution is set from 8 to 14 °. Then, a weighed sample of pantogematogen "dry" is added to the solution container at the rate of 3 g of substance per 100 g of solution and continuous mixing is carried out for 40-60 minutes. Insoluble sediment is removed by centrifugation at rotational speeds of the order of 4000 rpm. As a result of centrifugation, a dark brown opalescent transparent liquid is obtained. Next, prepare a polymer gelling composition. For this, the components: a polymer gelling agent, for example, a rare crosslinked polymer of acrylic acid and / or polyvinylpyrrolidone, carbomer, glycerin and / or propylene glycol, preservatives: nipagin (methylparaben) and nipazole (propylparaben) are mixed with distilled water. The neutralizing agent triethanolamine is added in an amount providing a slightly alkaline environment (pH = 6-8). For swelling, the composition is allowed to stand and homogenized on standard equipment used in the pharmaceutical industry. In the prepared polymer gel-forming composition, an appropriate amount of an aqueous-alcoholic solution of the “dry” pantomatogen prepared according to the described procedure is introduced, mixed, and the homogenization process is repeated. The resulting pantohematogen gel is packaged in a container and sealed in a known manner.

The disadvantage of this dosage form is the presence of a water-alcohol solution containing 8-14% ethyl alcohol, a long and complicated technology for its preparation. The use of alcohol violates the natural basis of pantogematogen "dry" and thereby affects the healing properties of the dosage form.

Description of the invention

The objective of the invention is to develop a method for producing a dosage form based on pantogematogen "dry" with the maximum possible preservation of its known and yet unknown natural properties, i.e. with a minimal effect of preservatives on its natural composition (without the use of alcohol in the technology for the production of dosage forms).

A method of obtaining pantogematogen "dry" - dry dehydrated blood from donated blood of Altai maral is known (see analogue of the invention - patent RU No. 2130314).

The technical result of the invention is the simplification of the technology, providing a highly effective dosage form for external use in the form of a gel, which is based on the pantogematogen "dry", an increase in shelf life up to 2 years without compromising its medicinal properties and reducing the cost of its production.

The objective of the invention is solved and the technical result is achieved in that the dosage form of pantogematogen for external use includes pantogematogen "dry", an aqueous medium, a polymer gel-forming composition. To prepare the pantogematogen dosage form, an “dry” pantogematogen aqueous solution is prepared within the pantogematogen-water ratio: 1 / 50-1 / 200 by weight (pantogematogen, wt.%: 2-0.5). Under normal conditions, withstand the solution, and then filter it. Additionally, an aqueous solution of a rare crosslinked polymer, for example acrylic acid, is prepared by dissolving it in water in a ratio of 1/10 to 1/200 (polymer, wt.%: 10-0.5). The ratio of the volumes of an aqueous solution of pantohematogen and a rare crosslinked polymer should be in the range: 3 / 1-1 / 10.

Additionally, an aqueous solution of a neutralizing agent, for example, triethanolamine, is prepared in an amount necessary to provide a slightly alkaline medium in the final solution (pH = 6-8).

An aqueous solution of a rare crosslinked polymer is mixed with a filtered aqueous solution of pantohematogen. The resulting mixture was stirred for 5-10 minutes to obtain a homogeneous solution. An aqueous solution of a neutralizing agent is added to this solution with vigorous stirring, after which the solutions are mixed for 5-10 minutes until a homogeneous solution is obtained. The reaction of the resulting solution should be slightly alkaline (pH = 6-8).

Using this technology, a new dosage form based on pantogematogen for external use is obtained, which includes pantogematogen "dry", water and a polymer gel-forming composition. Pantohematogen "dry" in the dosage form is introduced in the form of an aqueous solution with a ratio by weight of pantohematogen / water: 1 / 50-1 / 200. The components have the following proportions, wt.%:

pantogematogen "dry" - 0.01-6%;

polymer gelling composition - 0.1-20%;

water is the rest.

Common features of the invention and prototype are: pantohematogen, water and a polymer gelling composition.

The developed dosage form has a number of significant advantages over the known forms, in particular:

1) the proposed tool is applicable where alcohol-containing forms are contraindicated - for burns of varying degrees, in the presence of minor skin lesions, etc .;

2) the proposed tool does not cause any inflammatory reactions;

3) the proposed tool can be used in the treatment of persons with intolerance to alcohol-containing drugs.

The practical use of aqueous solutions of dry pantohematogen, made by known technologies, showed that the storage time of the diluted product is limited to several hours, after which the irreversible processes of decomposition of the proteins that make up the pantohematogen begin, with the appearance of a sharp specific smell of decomposing proteins.

Ethyl alcohol is used as a preservative in the prototype of the invention. In an aqueous-alcoholic solution of pantohematogen, the shelf life of the finished product is 2 years.

In the proposed method for producing a gel composition, a long shelf life of the finished product is achieved due to the fact that an aqueous pantohematogen solution is placed inside three-dimensional cells formed during the reaction of the neutralizing agent with a rare crosslinked polymer when the polymer is crosslinked to form a spatial "framework" of the polymer. The resulting spatial framework of the "walls" of the polymer during storage protects the pantogematogen solution inside it from oxidation and, accordingly, from further decomposition. Due to this, the shelf life of the finished product is increased to 2 years. For external use (massage, rubbing, etc.), the polymer skeleton is destroyed and an aqueous solution of pantohematogen enters the skin, which penetrates the body through the pores of the skin and has a therapeutic effect.

An aqueous solution of pantogematogen "dry" is the closest to the living blood of antler deer with the preservation of its natural properties, in contrast to the water-alcohol form. The new dosage form increases bioavailability. Moreover, it can be applied in a new field, for example, in dermatology, in particularly sensitive areas of the body, post-burn rehabilitation, etc. This makes the final product more valuable to use.

The proposed technology makes it much easier and faster to achieve complete homogenization of the final product, which saves time and material costs. A distinctive feature of this technology is the process of mixing an aqueous solution of pantohematogen with an aqueous solution of polyacrylic acid in a slightly acidic environment, and not in a slightly alkaline one. Since polyacrylic acid is a weak acid, it is practically not dissociated in water. Its molecular chains represent an agglomerate with a very low swelling ability. In a slightly alkaline medium, negative ions - COOH groups, due to electrostatic repulsion, change their configuration from globular to a state of free conformation, which is accompanied by a significant increase in viscosity.

At the stage of mixing an aqueous solution of pantohematogen with an aqueous solution of polyacrylic acid, an increase in viscosity is an undesirable process. It is more technologically advanced at the beginning to mix pantogematogen and polymer solutions, after which adjust the pH of the medium to slightly alkaline by adding a neutralizing agent and thus increase the viscosity of the final product.

The invention allows:

- use without adding alcohol an aqueous solution of pantogematogen "dry", which leads to a significant improvement in the quality of the final product and increase the effectiveness of therapeutic and prophylactic agents and shelf life;

- get an improved homogeneous gel composition due to the uniform distribution throughout the volume of the active substance;

- to simplify the manufacturing process of the dosage form of pantogematogen "dry" on a gel basis, which reduces the costs of the manufacturer.

An example of the practical implementation of the therapeutic form of pantohematogen

The medicinal form of pantogematogen “dry” in aqueous solution possesses the best therapeutic properties in the following ratios of components (wt.%)

- pantogematogen "dry" - 0.5;

- polymer gelling composition - 5;

- water - the rest.

The aqueous solution of pantogematogen "dry" has a ratio by weight of pantogematogen / water: 1/100. Under normal conditions, the solution is kept for at least an hour, after which it is filtered. Additionally, an aqueous solution of a rare cross-linked polymer, acrylic acid, is prepared by dissolving it in water in a ratio of 1/20. The ratio of the volumes of an aqueous solution of pantohematogen and a rare crosslinked polymer is 1/2.

Additionally, an aqueous solution of a neutralizing agent, triethanolamine, is prepared in an amount that provides an alkaline medium with pH = 7 in the final solution.

An aqueous solution of a rare crosslinked polymer is mixed with a filtered aqueous solution of pantohematogen. The resulting mixture was stirred for 10 minutes until a homogeneous solution was obtained. An aqueous solution of a neutralizing agent is added to this solution with vigorous stirring, after which the solutions are mixed for 10 minutes until a homogeneous solution is obtained. The reaction of the resulting solution becomes slightly alkaline (pH = 7).

The effect of the new pantogematogen dosage form was tested in the treatment of thermal burns of the skin and athlete's bruises. External use of this dosage form (application to a burned place, rubbing and massage) for thermal burns of the skin of the 2nd "a" degree led to a reduction in the acute stage, early epithelization of the damaged skin surface. At the kickboxing competition, a new dosage form was applied to an athlete with multiple bruises of the face, expressed by pain, and massage movements. Within 15 minutes there was a marked improvement - the swelling decreased, the pain went away, this allowed the athlete to continue the performance.

Claims (6)

1. Dosage form based on pantogematogen for external use, including pantogematogen, water and a polymer gel-forming composition, characterized in that pantogematogen "dry" is introduced in the form of an aqueous solution with a ratio of pantogematogen / water by weight: 1 / 50-1 / 200 in the following the ratio of components, wt.%: Pantohematogen "dry"  0.01-6% Polymer gelling composition  0.1-20% Water  Rest 2. The dosage form according to claim 1, characterized in that the polymer gelling composition has a composition, wt.%: Polymer Gelling Agent - Rare Crosslinked acrylic acid polymer and / or polyvinylpyrrolidone  1-6 Carbomer  2.1-7.5 Glycerin and / or propylene glycol  2-60 Preservatives nipagin and nipazole  0.05-0.4 Triethanolamine  To a pH of 6-8 Water  Rest 3. The dosage form according to claim 1 or 2, characterized in that it further comprises an aromatherapy component in an amount of 0.2-2 wt.%. 4. The dosage form according to claim 1 or 2, characterized in that the aromatherapy component is at least one essential oil of natural origin. 5. A method for producing a dosage form of a pathogen according to claim 1 for external use, based on the preparation of a solution of pantogematogen "dry" and an aqueous solution of a polymer gel-forming composition and mixing thereof, characterized in that an aqueous solution of pantogematogen "dry" is prepared within a weight ratio of pantogematogen / water: 1 / 50-1 / 200, the solution is kept under normal conditions, after which it is filtered, an aqueous solution of a rare cross-linked polymer is additionally prepared in a ratio of 1/10 to 1/200 and an aqueous solution of neutralizing a enta in the amount necessary to provide a slightly alkaline medium in the final solution, with the ratio of the volumes of the pantogematogen aqueous solution and the rare crosslinked polymer in the range: 3 / 1-1 / 10 they are mixed and mixed until a homogeneous solution is obtained, an aqueous solution of a neutralizing agent is added to this solution and mix to obtain a homogeneous solution with a slightly alkaline reaction (pH = 6-8). 6. A method of obtaining a dosage form of a pathogen according to claim 5, characterized in that the polymer gelling composition has a composition, wt.%: Polymer Gelling Agent - Rare Crosslinked acrylic acid polymer and / or polyvinylpyrrolidone  1-6 Carbomer  2.1-7.5 Glycerin and / or propylene glycol  2-60 Preservatives nipagin and nipazole  0.05-0.4 Triethanolamine  To a pH of 6-8 Water  Rest