RU2740284C1 - Hygienic tampon impregnating agent, having antimicrobial activity, and phytotampone producing method having antimicrobial activity - Google Patents

Abstract

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to pharmaceutical industry, namely to an agent for impregnating a hygienic tampon and a method for producing a hygienic tampon. Hygienic tampon impregnation agent having antimicrobial activity is a water-alcohol extraction obtained by ethanol extraction of the vegetable raw material mixture, including common Saint-John's wort, sickle-weed herb, common persicaria herb and wild apple tree leaves taken in certain amounts. Method for producing a hygienic tampon involves holding a hygienic tampon in the impregnating agent described above, followed by drying to constant weight.

EFFECT: above described agent and method enable to preserve biologically active substances from impregnating agent in tampon during its manufacturing and provide maximum extraction of active substances when using a tampon, which enables to apply a tampon for preventing and treating gynaecological diseases related to growth of pathogenic microorganisms in vagina.

2 cl, 2 dwg, 2 tbl, 1 ex

Description

The technical field to which the invention relates

The group of inventions relates to the field of medicine, the pharmaceutical industry, namely to compositions based on plant raw materials for therapeutic and prophylactic hygienic tampons and methods of making therapeutic and prophylactic tampons with antibacterial activity and preventive action against the development of bacterial vaginosis and ensuring the restoration of the physiological level of vaginal acidity ...

State of the art

From the prior art, various tampons and methods for their manufacture are known, which ensure the hygienic needs of the user and have improved technological characteristics (for example, patent RU2433809). However, these products do not contain therapeutic and prophylactic ingredients.

Known antibacterial filler for a feminine sanitary napkin or tampon, a method for its production and use (Patent RU2286800). The filler contains 1% chitosan hydrochloride hydrogel, which includes metronidazole and dioxidine. However, the use of this filler suggests the need for self-dosing when applied to a tampon or sanitary napkin, which can lead to an incorrect dosage of metronidazole and dioxidine, as a result of which the formation of resistance of certain strains of anaerobic bacteria to these agents is possible, as well as the occurrence of relapses against the background of successful treatment, which , according to the literature, are possible within eight months in 75-80% of patients (MV Mazurkevich, TA Firsova, MV Dukhanina. Pathogenetic correction of vaginal dysbiosis. Pharm-sintez.ru). In addition, allergic reactions to the ingredients declared in the product are possible.

Also known is an antibacterial composition for local treatment of bacterial vaginosis (Patent RU2236851), which is a 3.5% chitosan-ascorbate gel containing metronidazole at a dose of 2 mg in 1 ml.

However, this agent has a high viscosity, which makes it technically difficult to introduce this composition into a sanitary napkin or tampon. It should also be noted the possible drug intolerance to metronidazole and allergic reactions in some patients (Malashenkova T.E. Pharmacoepidemiology of drug allergy in the Stavropol Territory. Abstract of the thesis for the competition for the academician of medical sciences Volgograd 2008).

Known therapeutic agent for application to a tampon, which is used as a citrate buffer pair with a pH of 3.9-4.2, as well as a method of treating bacterial vaginosis using this agent (Patent RU2113183). At the same time, a biopolymer resorbable sponge, in which a buffer pair is impregnated, is fixed at the end of the tampon.

The disadvantage of this solution is the imperfection and inconvenience of using a tampon with a therapeutic agent, which provides for fixing a sponge impregnated with a buffer pair at the end of the tampon, while the method of fixing the sponge is not indicated.

Closest to the proposed invention is a method for making a therapeutic and prophylactic tampon and a composition for a tampon (Patent RU2682643), including angelica root, nettle leaf, fresh sea buckthorn fruits, oregano herb, motherwort herb, coriander fruits, water extract of dandelion root, water extract of root marshmallow, licorice syrup, borneol, taken in a certain amount. The collection of herbs is pressed and placed in a gauze casing to form a ball with a diameter of 10-15 mm. The top of the gauze ball is tied with a thread, which, when the tampon is inserted into the vagina, remains outside and is designed for further comfortable removal.

The disadvantage of this solution is the use of a composition of crushed raw materials, which is placed in a gauze shell for direct administration, while the plant powder can injure the mucous membrane. In addition, licorice syrup is added to the composition, the composition of which includes sugar syrup, which can contribute to microbial contamination of the proposed tampon.

The technical problem solved by the group of inventions is the need to expand the arsenal of hygienic tampons, which have a prophylactic antimicrobial effect, in particular, preventing the development of bacterial vaginosis, based on plant materials.

Disclosure of the essence of the invention

The technical result of the group of inventions is the development of a means for impregnating a feminine hygienic tampon based on plant materials with antibacterial activity, as well as a method for making phytotampon using this means, which allows preserving biologically active substances from the impregnating agent in a tampon during its manufacture and ensuring maximum extraction of active substances when using a tampon, which makes it possible to use it for the prevention and treatment of gynecological diseases associated with the growth of pathogenic microorganisms in the vagina. In addition, a tampon made in accordance with the proposed method is easy to use, does not require self-dosing of the drug or fixing additional agents (sponges) soaked in a medicinal solution on it, has a uniform therapeutic effect on the mucous membranes and skin of the female genital organs.

The technical result is achieved by creating a means for impregnating a hygienic tampon with antimicrobial activity, which is an aqueous-alcoholic extract obtained by extraction with 40% ethanol of a mixture of plant raw materials, including St. John's wort grass, peppermint grass, knotweed grass and crushed apple leaves to the size of particles passing through a sieve with a diameter of 1-3 mm, with a raw material: extractant ratio of 1: 5, while a mixture of plant raw materials is used with the following ratio of components, wt. %:

St. John's wort herb 20-40; knotweed herb 20-40; mountaineer grass 20-40; forest apple leaves 20-40.

The technical result is also achieved by creating a method for producing a hygienic tampon with antimicrobial activity, according to which the hygienic tampon is kept in the above-mentioned impregnating agent for at least 10 minutes, followed by its drying to constant weight.

Optimally selected components of the impregnating agent ensure the suppression of bacterial gynecological infections, and restore the physiological level of vaginal acidity. The method is simple in the implementation of obtaining the final product, which has a pronounced antimicrobial effect and allows you to combine the hygienic properties of the product and its antimicrobial activity, in contrast to tampons impregnated with medical and hygienic means, which are used, for example, a citrate buffer pair with a pH value 3.9-4.2.

Of the proposed types of raw materials for obtaining the extraction, three (St. John's wort, herb of Pepper's Wort and Herb) are pharmacopoeial (FS.2.5.0015.15 St. John's wort; GF 11, v.2, art.58. Herb of highlander; GF 11, v.2 Article 57. The herb of the mountaineer (A.S. Chistyakova. Pharmacognostic study of the herb of the knotweed. Abstract of the thesis of Ph.D. 2017; A.A. Gudkova Pharmacognostic study of representatives of the genus mountaineer, as a promising source of drugs Abstract of the thesis in Ph.D. 2020) Leaves of the forest apple (Malus sylvestris Mill) contain a variety of biologically active substances, including phenolic derivatives and flavonoids, and have long been used as an anti-inflammatory agent (N.V. Nesterova, Samylina IA Study of the qualitative composition and quality indicators of the leaves of the apple tree forest and home // Journal "Health and Education in the XXI century", 2015, No. 4, v. 17, pp. 251-258).

The pharmacological activity of plant objects is largely due to the content of flavonoids and phenolcarboxylic acids, which provide anti-inflammatory and antimicrobial effects, the presence of which in extracts from raw materials is confirmed by the form of a specific UV spectrum. To assess the completeness of the extraction of active substances when using tampons obtained by the proposed method, extraction into distilled water was carried out, followed by evaluation of the obtained UV spectra.

Brief Description of Drawings

The invention is illustrated by illustrations, where FIG. 1 shows the UV spectrum of an aqueous-alcoholic extract from a mixture of St. John's wort, herb of Knotweed, herb of Knotweed, apple leaves, Fig. 2 - UV spectrum of extraction from tampons impregnated with the proposed product.

Implementation of the invention

The proposed method for producing hygienic phytotampon is as follows.

Pre-dried herb St. John's wort, herb of mountaineer, herb of knotweed and apple leaves, taken in a ratio of 20 to 40 wt% of each component crushed to a particle size passing through a sieve with a diameter of 1-3 mm, and then mixed. The resulting mixture is poured with 40% ethyl alcohol in a ratio of 1: 5 (at a ratio of raw materials in parts by weight and extractant in parts by volume) and infused for 2-3 days at room temperature, then filtered, the residue is squeezed out on a press and attached to the hood. Hygienic tampons of industrial production are kept for at least 10 minutes (for example, 10 - 20 minutes) in the resulting extract, and then dried at a temperature of 30-35 ° C to constant weight. As tampons, any gynecological female tampons known from the prior art, with or without an applicator, made of an absorbent material, for example, rayon fiber, cotton or a combination thereof, of any degree of absorbency (without a shell) can be used. Tampons can be used daily during the inflammatory process and / or during the menstrual cycle, with tampons changing every 5-6 hours.

Table 1 shows examples of the compositions of the feedstock for obtaining water-alcohol extraction.

Table 1.

Components Number of components, g Composition 1 Composition 2 Composition 3 Composition 4 Composition 5 St. John's wort herb 5 5 5 ten 6.25 knotweed herb 5 5 ten 5 6.25 mountaineer grass 5 ten 5 5 6.25 apple leaves ten 5 5 5
6.25

An example of a specific implementation

About 25 g of the prepared dried raw material - St. John's wort herb, Pepper's wort herb, Knotweed herb, apple leaves (weight of each component 6.25 g (exact weight)) was crushed to a particle size passing through a sieve with a diameter of 2 mm, and then mixed. This mixture of plant powders was poured with 40% ethyl alcohol in a ratio of 1: 5 and infused for 48 hours, after which it was filtered, the residue was squeezed out on a press and attached to a hood.

Industrial swabs made of cotton or viscose fiber (GOST R 53224-2016; GOST 10546-80) were placed in the resulting extract for 10 minutes, after which they were dried in an isothermal oven at 30 ° C for 60 minutes. To assess the transition of biologically active substances from the obtained extract to the tampon, a comparison of UV spectra obtained for the initial aqueous-alcoholic extracts from a mixture of 4 raw materials was carried out: St. John's wort herb, Knotweed herb, Knotweed grass, apple leaves (Fig. 1) and spectra of extracts obtained by immersing pre-treated extract and dried swabs in distilled water (Fig. 2), to compare the identity of the obtained spectra and to prove the release of biologically active substances from the soaked swab into a humid environment.

As can be seen from Fig. 1 and Fig. 2, the coincidence of the absorption maxima indicates the identity of the composition of the substances extracted from the tampon and the substances included in the initial extraction. When analyzing the qualitative composition of flavonoids and phenolcarboxylic acids by TLC, we used Sorbfil-P-A-UV-254 plates, the solvent system n-butanol-acetic acid-water (4: 1: 2). The front of the passage of solvents is about 13 cm.To detect the zones of adsorption corresponding to flavonoids and phenolcarboxylic acids, observation was carried out in UV light (365 nm) before and after treatment with a 3% alcohol solution of aluminum chloride with keeping the chromatograms for 2-3 minutes in an oven at a temperature 100 ° C. During the analysis, standard samples were used - rutin, hyperoside, gallic and caffeic acids. Flavonoid compounds were detected by their own fluorescence under UV light (light yellow to brownish adsorption zones). After the chromatograms were developed with a 3% alcohol solution of aluminum chloride and heated in an oven, the fluorescence of the zones increased and the zones of flavonoid nature acquired a yellow-green color. In UV light, the absorption zones of phenolcarboxylic acids were blue in color. On the chromatograms of the initial aqueous-alcoholic extract from four types of raw materials - St. John's wort, herb of peppermint, grass of the mountaineer, apple leaves, as well as extraction from a tampon, 18 adsorption zones were found, of which 13 corresponded in color to substances of a flavonoid nature, and 5-phenolcarboxylic acids. According to the Rf values and comparison with the values of standard samples, the following were identified: hyperoside (Rf -0.33), rutin (Rf-0.49), gallic (Rf-0.44) and caffeic (Rf-0.28) acids. The composition of the substances found on the chromatograms of the initial extraction and extraction into the aqueous medium from the swab soaked in the initial extraction coincided.

When studying the antimicrobial activity of the obtained tampon, we used a method based on the properties of biologically active substances to diffuse into agar contaminated with test cultures of microorganisms and suppress the growth of the latter. (a guide to microbiological and virological research methods under the editorship of Birger M.O. - M.: Medicine 1982, pp. 172-177). For the analysis, we used pure cultures of microorganisms (table 2), pre-cultivated on meat-peptone agar (MPA) at a temperature of 37 ° C for 24 hours. A standard bacterial suspension was prepared in a sterilized 0.9% sodium chloride solution. For this, the test culture was introduced with a bacteriological loop into a sterilized vial with sterile saline and the concentration of microorganisms was adjusted to a value of 0.5 units of the McFarland turbidity standard. MPA was melted, cooled to 56 ° C, and poured into Petri dishes. The studied suspensions of microorganisms were introduced on the frozen agar using an automatic pipette under sterile conditions. After uniform distribution of microorganisms, the plates were incubated at room temperature for 15-20 minutes. Then, wells were formed, into which the studied samples of the initial extraction from a mixture of four types of raw materials and the extraction obtained from the tampon were introduced. Samples were incubated at 37 ° C for 16 hours. The results were accounted for by the absence of bacterial growth around the wells with extracts by measuring the diameter of the zone around the well in millimeters. The analysis results are presented in Table 2.

Table 2. Diameter of zones of growth inhibition of test cultures of microorganisms by the investigated extracts

Test cultures of microorganisms Diameter of growth inhibition zone of test cultures of microorganisms, mm Combined extract from St. John's wort, Knotweed, Knotweed, and Crabapple leaves Water extraction from test swabs Bacillus anthracoides - 1. 31 ± 1 15 ± 2 Bacillus subtilis L2 27 ± 1 13 ± 1 Echerisch ia coli 675 28 ± 1 15 ± 1 Salmonella galenarum 26 ± 1 12 ± 1 Staphylococcus aureus (209) 31 ± 2.5 16 ± 1 Staphylococcus aureus (Tupe) 30 ± 1.5 14 ± 1 Staphylococcus epidermidis Wood - 46 31 ± 1 14 ± 1 Proteus vulgaris 28 ± 1 13 ± 1

From the data in Table 2, it follows that the studied extract has a pronounced antimicrobial effect against all the microorganisms presented, as well as a moderate antimicrobial effect of the water extract from the tampons treated with the specified mixture.

Studies of extracts with a different quantitative content of the original plant components (table 1) were also carried out, which also showed antibacterial activity and the maximum release of biologically active substances from the tampon, which shows the significance of the indicated intervals of the values of the signs.

As you know, facultative anaerobic microorganisms, such as Echerichia coli, are the causative agents of at least 23.4% of cases of bacterial vaginosis (NN Volodin, VM Korshunov. Bacterial vaginosis. Women's health. In the world of drugs, 2000, No. 2, pp. 23-28), which allows considering the proposed tampons not only as a prophylactic, but also as a therapeutic agent. It is also known that anaerobic bacteria responsible for the production of primary amines cause a significant increase in the pH of the vaginal discharge, which normally does not exceed 4.5. The pH value of the water extract from the tampon is 3.6-3.8, that is, it is in the acidic region, due to the content of phenol carboxylic acids in the plant objects used to obtain the extract for impregnating the tampon, including gallic and caffeic acids by TLC , which has a beneficial effect on the mucous membrane and helps to restore the physiological level of vaginal acidity.

Claims (3)

1. Means for impregnating a hygienic tampon, which has antimicrobial activity, which is a water-alcohol extract obtained by extraction with 40% ethanol of a mixture of plant raw materials, including St. John's wort grass, pepper knotweed grass, knotweed grass and apple tree leaves, crushed to particle size, passing through a sieve with a diameter of 1-3 mm, with a ratio of raw materials: extractant 1: 5, while the mixture of plant materials is used with the following ratio of components, wt. %: St. John's wort herb 20-40 knotweed herb 20-40 mountaineer grass 20-40 forest apple leaves 20-40 2. A method of obtaining a hygienic tampon having antimicrobial activity, comprising keeping the hygienic tampon in an impregnating agent according to claim 1 for at least 10 minutes, followed by drying it to constant weight.

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