Vol 72, No 7 (2023)

The article presents the specifics of the development and production of microtablets in experiment. Microtablets, or mini-tablets, are tablets with a diameter of 1 to 4 millimeters. Tablets up to 4 mm in diameter are rarely distinguished as a separate type in the regulatory documentation. However, they have a number of advantages. The small size of individual particles allows the usage of microtablets in cases of violation of the swallowing process. The great variability in dosing allows in theory the use of this form in personalized medicine. With the help of microtablets it is possible to achieve a reliable physical separation of active pharmaceutical ingredients in combined preparations. However, their dimensions also require attention to the technological process.

The small size of the matrix orifices affects the requirements for the physical and technological properties of the tableting mass and for the settings of the tablet press, necessary to achieve mass uniformity and dosing of this type of tablets. For small orifices in the tablet press matrix, the effect of powder suction due to the movement of the lower punch plays an important role, depending on the fractional composition of the tableting mass and the speed of rotation of the press rotor.

Also, the production process involves the use of specialized tooling of various types of design for a tablet press.

Microtablets, like tablets of regular diameter, can provide modified release of drugs, however, due to their size, both their technology and dissolution in the organism must be taken into account. The article also mentions the features of quality control of tablets of this type, and critically important technological parameters.

Introduction. The samples of the Agastache rugosa (Fisch.et Mey.) Kuntze, cultivated in the conditions of the taiga zone of Western Siberia were study.

Objective: determination of diagnostic microscopic (anatomical) signs of cultivated Agastache rugosa.

Material and methods. Air-dry raw material of the Agastache rugosa, during the period of mass flowering and fruiting in 2021 were collected. The study of the anatomical structure, preparation and enlightenment of drugs was carried out in accordance with generally accepted methods. Leaf petioles and stems were fixed in 70% ethanol. Cross sections from each part of the stem (lower, middle, upper) were studied. The anatomical structure of the leaves was studied on the middle and terminal parts of the leaf, the epidermis of the petals upper and lower from the surface. All samples were studied in 5-fold repetition.

Results. Specific features have been established: strongly winding lower leaf epidermis with characteristic thickened cell walls; 8-, rarely 6-cellular essential oil glands located in crypts; simple 1–4-celled and multicellular trichomes with a smooth or warty surface; capitate trichomes unicellular and bicellular on a unicellular, less often on a two-celled leg in leaves, flowers, petioles, less often in stems; papillary outgrowths of the epidermis of the stem, leaf, flowers. For the first time, receptacles, crystals of calcium oxalate in the form of drusen were found in the leaves, idioblast in the flowers, and an accumulation of small warty club-shaped bulbs. It has been established that in the leaves there are two types of stomata it is diacytic and anomocytic, in flowers it is only diacytic type.

Conclusion. These specific data are important from the point of view of fundamental and practical interest, obtaining new data and diagnosing raw materials.

Introduction. White poplar (Populus alba L.) as a promising source of raw materials containing phenolic compounds is of interest for expanding the raw material base of medicinal plant materials with antimicrobial activity. It is known that the leaves of the white poplar contain flavonoids, for example, rutin, phenylpropanoids (p-coumaric acid, caffeic acid), simple phenols (salicin) and other compounds.

From the point of view of standardization of this raw material, flavonoids are of interest.

The aim of the present study is to develop a technique for quantifying of the total flavonoids in the leaves of white poplar (Populus alba L.).

Material and methods. The research material was the leaves of the white poplar harvested in 2022 in the Samara region (near the village of Alekseevka).

Differential spectrophotometry was used as a method of investigation, held according with Pharmacopoeial monograph 1.2.1.1.0003.15 «Spectrophotometry in ultraviolet and visible spectrum». Spectral characteristics of water-ethanolic extraction was marked on spectrophotometer Specord 40 (Analytik Jena AG, Germany) in cuvette with layer thickness 10 mm.

Results. There was developed the methods for the quantitative determination of the total flavonoids in leaves of white poplar. We used the differential spectrophotometry method with the state standard sample of rutin at an analytical wavelength of 410 nm. The content of total flavonoids in the plant raw material is varied from of 1,30±0,04 % to 2,19±0,05 % (calculated on rutin). The error of a single determination with a confidence level of 95% is ±5,22%.

Conclusion. As a result of the conducted research, the expediency of assessing the quality of raw materials Populus alba leaves by the content of the total flavonoids in canculated on rutin was justified.

The validation evaluation of the developed methodology was carried out according to the indicators of specificity, linearity in accordance with the State Pharm of the Russian Federation of the XIV edition. Based on the results of the validation evaluation of the experimental results, we can conclude about the suitability of using this technique for quantifying of the total flavonoids calculated on rutin.

The obtained research results can be used in the development of regulatory documentation for a promising type of raw material Populus alba leaves for introduction into the State Pharmacopoeia of the Russian Federation.

Introduction. The development of a dosage form is always associated with the need to resolve issues related not only to the bioavailability and stability of the drug, but also to creating comfortable conditions for administration, including acceptable organoleptic characteristics, which is especially important in geriatrics and pediatric practice. It is syrup as a dosage form that is a special pharmaceutical product; it contains medicinal substances and a complex of excipients that correct its organoleptic properties. The purpose of this study is to develop technology and evaluate the pharmacological activity of medicinal syrup with piracetam.

Material and methods. To obtain the syrup, piracetam substance, mint and valerian tinctures were used. When determining the density of the syrup, generally accepted methods were used. The quality of the resulting medicinal syrup and the quantitative determination of piracetam were assessed by reverse-phase high-performance liquid chromatography (HPLC). To assess the pharmacological activity of the resulting syrup, a series of behavioral tests were carried out on 30 male white laboratory rats (body weight 352.3±58.9 g), divided into 3 groups of 10 animals each. Statistical processing of the results was performed using the GraphPad Prism 5.0 program. The correspondence of the distribution of analyzed values to the normal distribution was assessed using the Kolmogorov-Smirnov and Shapiro–Wilk tests. The statistical significance of intergroup differences was assessed using one-way analysis of variance (ANOVA) with Newman–Keuls post-test.

Results. A medicinal syrup with piricetam was obtained, which also contains tinctures of valerian and mint. The syrup was standardized according to density. The content of piracetam in the resulting syrup was quantitatively determined. The pharmacological activity of the resulting medicinal syrup was assessed.

Conclusion. The resulting medicinal syrup meets the requirements of the ND in terms of density. The results obtained from assessing the pharmacological activity suggest that the study drug piracetam in syrup dosage form, due to the introduction of additional active ingredients into the composition, has additional anxiolytic properties not associated with muscle relaxant effects, which makes further study of the developed dosage form promising.

Introduction. High importance of enteral nutrition food products (ENP) as a means of providing nutritional support to patients of various profiles, it makes it relevant to form an idea of the current state of consumption of this type of product in medical organizations of the North-Western Federal District (NWFD).

Objective: to study the state and trends of ensuring the needs of medical organizations in PET, including the sources of covering this need.

Material and methods. The sources of information were data on contracts concluded for 2016–2021, posted in the unified information system in the field of procurement, and data from the Unified Register of Certificates of State Registration of Products.

Results. In the structure of general purchases of ENP by medical organizations of the North-Western Federal District for 2016–2021, 43% were products for siping (oral) use, 20% – intended for administration through a tube, 36% – for mixed intake. Mixtures with a liquid form of release and with a standard functional purpose prevail. The share of specialized (metabolic-oriented) mixtures for the entire period under review was 30%. The growth rates of purchases of standard ENP outpaced the general dynamics of specialized mixtures, with the exception of ENP for diabetic patients and those suffering from respiratory insufficiency, which can be associated with the COVID-19 epidemic. In 2021, the volume of purchases of ENP amounted to 673.6 thousand units, twice exceeding the level of 2016. 85% of the need for ENP was met at the expense of products of foreign origin, 15% – Russian. More than a third of the supplied ENP are products of B.Braun (Germany).

Conclusion. Reducing risks while ensuring the need for nutritional support for patients within the framework of medical care necessitates overcoming import dependence in the supply of ENP.

Introduction. The global and rapid spread of COVID-19 has had a huge impact on all healthcare sectors around the world and has expanded the existing understanding of the nature of the course of this disease, which is reflected in domestic and foreign publications.

Objective: to study the acute toxicity, antiviral and antithrombotic activity of an anticoronavirus agent based on curcutzinc, allthrombosepin and ascorbic acid.

Material and methods. The study of acute toxicity was carried out according to the generally accepted method. The study of the antiviral (cytoprotective) activity of the preparation was carried out according to the ability of the drug to stabilize erythrocyte membranes under conditions of osmotic hemolysis. The study of the antithrombotic activity of the preparation was carried out on a shock lung model, namely, generalized adrenaline-collagen thrombosis.

Results. The data obtained indicate the presence of significant antiviral (cytoprotective), antithrombotic activity in the test preparation. At the same time, the antiviral effect significantly exceeds the reference drug, and the antithrombotic effect is comparable to the reference drug. There was also an average lethal dose LD₅₀ = 6000 (4285,7-8400,0) mg/kg of the drug, and it was found that the drug belongs to the fifth class of toxicity – «Practically non-toxic».

Conclusion. The studied anticoronavirus agent has a significant antiviral (cytoprotective), antithrombotic activity. Also, the high safety of the test preparation was established, since the drug belongs to the fifth class of toxicity – «Practically non-toxic».