Introduction. The active pharmaceutical substance of the tablets is vitamin D3 (cholecalciferol), therefore, quantitative analysis methods are being developed to determine it. The methodology given in the general pharmacopoeia article of the OFS was taken as a basis.1.2.3.0017.15 "Methods of quantitative determination of vitamins" of the State Pharmacopoeia of the Russian Federation XV edition. This article proposes a quantitative analysis of vitamin D3 using the method of high-performance liquid chromatography (HPLC). Goal. Development and validation of a methodology for the quantitative determination of the active pharmaceutical substance vitamin D3 in tablets. Material and methods. To develop and validate a method for the quantitative determination of vitamin D3 in tablets, a high-performance liquid chromatography method was used: chromatograph Chromosome A02 (Chromosome Engineering, Russia) equipped with an ECD2000 UV detector (ECOM, Czech Republic), a column Luna C18(2) 150×4.6 mm was used for separation. The analysis and validation characteristics were performed in accordance with the requirements of the State Pharmacopoeia of the Russian Federation XV edition. Results. It was found that during HPLC analysis, the average content of cholecalciferol in the drug was 126.2±3 micrograms/ml (100.9% of the declared value; the relative error of determination was ±2.38%). A validation assessment of the proposed technique was carried out in terms of specificity, linearity, precision (level of convergence), which confirmed its suitability for authenticating and quantifying cholecalciferol in a medicinal product. Conclusion. The results obtained indicate the possibility of using the method of high-performance liquid chromatography in the isocratic mode for the quantitative determination of the active pharmaceutical substance vitamin D3 in tablets coated with an intestinal soluble shell for the treatment and prevention of vitamin D-dependent nosologies.

In a traditional drug delivery system, it is difficult to achieve precise control of the drug release rate and the drug release site. Poly-D,L-lactide-co-glycolide is one of the most frequently studied biodegradable polymeric drug carriers for drug delivery to target organs. Biodegradable polymers must have good biocompatibility. Targeted delivery of drugs obtained using modern technologies can provide a new therapeutic strategy for more localized treatment of diseases, potentially provide systemic delivery of drugs, reduce the dose of the administered drug and its possible side effects on the patient. In the experiment, we obtained microparticles based on cinnarizine with poly-D,L-lactide-co-glycolide using the co-precipitation method. The physicochemical characteristics of microparticles are of key importance for understanding their properties for further use in pharmaceuticals, since they can have different effects on the target organ due to their unique properties. The study of the dispersed composition of the obtained samples of cinnarizine microparticles based on poly-D,L-lactide-co-glycolide was carried out using photon correlation spectroscopy on a Photocor-Complex installation (Antek-97, Russia). The size and shape of microparticles explain their ability to penetrate blood vessels, tissues and target cells of target organs. The purpose of this work was to determine the effect of various cryoprotectants on the size and shape of cinnarizine microparticles at different ratios to poly-D,L-lactide-co-glycolide. Under experimental conditions, a cryoprotector was selected. As a result of the tests, it was determined that the nature of the cryoprotector affects the size and shape of the resulting particles - the optimal ratio of cinnarizine and poly-D,L-lactide-co-glycolide is 1:3, which produces microparticles 104 nm in size, spherical in shape, having a uniform distribution in the sample.

Abstract: Alfredia drooping is a source of vegetable raw materials with cerebroprotective, antioxidant and antiradical effects. We obtained a dry polyfraction extract from the lower, petiolate leaves of Alfredia. The purpose of the research is to develop a technology of water-soluble granules based on a polyfraction extract of Alfredia drooping dry for the preparation of a drink. We used polyextract from the leaves of alfredia drooping and water-soluble excipients: maltodextrin DE 12-19, starch sodium glycolate, sodium chloride and sucrose, ethyl alcohol 95% as objects of research. The wet granulation method was used to produce pellets. The technology of the granules consisted in the fact that all the components of the granules (humidity no more than 2%) were mixed, moistened with 95% ethyl alcohol and granulated by pressing through the mesh (holes 2 mm). The granules was dried at a temperature no higher than 30°C to a residual humidity of no more than 2%. The granules were then re-granulated and sieved through a sieve (2 mm holes).In the course of research, the product was evaluated according to the indicators "granulation ability", "disintegration", "uniformity of dosing", "dissolution", "taste". The composition of granules with alfredia polyextract was determined as a result of experiments: polyextract: maltodextrin: sugar: calcium glycerophosphate: starch sodium glycolate: sodium chloride in the ratio 1,41:0,8:1,2:0,16:0,16:0,13 g, respectively. The obtained granules have withstood all tests according to the indicators provided for by GF 14 of the edition: "description", "size of granules", "loss in mass during drying", "disintegration", "uniformity of mass", "microbiological purity". The shelf life for granules with Alfredia extract can be set for a duration of 18 months.

Abstract. This article is a literature review that describes the prospects for the use of poly-D,L-lactide-co-glycolide (PLGA) in pharmacy as a material for the development of nano-delivery agents for therapeutic agents. The aim of the review is to summarize information about modern drug delivery systems based on PLGA. Results. Biodegradable polymers play an important role in the development of the modern pharmaceutical industry and allow solving the problems of targeted delivery and controlled release of medicinal substances. Due to their exceptional properties, microparticles based on these polymers can protect drug molecules from instant degradation in vivo, while providing a customizable release rate and profile, and maximize their pharmacological effects by reducing their side effects. PLGA is considered one of the most successfully synthesized biodegradable polymers. For the creation of polymer nanostructures, PLGA has attracted attention due to its key controllable properties. It is biocompatible and biodegradable to non-toxic endogenous compounds. PLGA microparticle production methods are well-defined and easy to replicate in laboratory and industrial environments. The use of PLGA as a basis for nanoparticles, followed by surface modification, makes it possible to achieve such positive changes as an increase in the bioavailability of substances, leveling of unwanted side effects, the possibility of targeted drug delivery to target organs, maintaining a constant plasma concentration, and reducing the number of injections. The potential of PLGA nanoparticles for targeted and controlled delivery of various micro- and macromolecules, including drugs, peptides, proteins, monoclonal antibodies, growth factors and DNA, etc., has been widely studied. The field of application of these nanoparticles includes a wide range of pathologies, which is especially important in therapy oncological, cardiovascular, cerebrovascular and other diseases. The development and implementation of PLGA-based delivery nanostructures, providing targeted, prolonged release of therapeutic agents, will allow solving urgent problems of pharmacy and medicine. Conclusions. Based on the analysis of the literature data carried out by the authors, the prospects for the use of PLGA for the development of nanosystems for drug delivery are shown.

In the course of this study, the expediency of using oil adjuvants as part of an antiviral vaccine was established. The choice of excipients is justified. It was found that as auxiliary substances, the most optimal are TEA, lecithin, oleic acid, mannitol. Stable compositions were obtained using TOTAL oils and base oil. A technology for producing oil adjuvant compositions has been developed. The stability of vaccine preparations with the use of oil adjuvant compositions has been studied. The oil adjuvant is convenient in the production process, as it forms a fairly stable emulsion, the vaccine is freely injected. It was found that the most advantageous physical and technological properties for practical use were the vaccine samples with a volume ratio of antigen and adjuvant 40:60.

The main objective of the planned experiment is to obtain a stabilized nanoemulsion of vitamin D3, followed by obtaining nanocapsules of vitamin D3 with a high biological potential, as well as to analyze the spatial (dimensional) characteristics, to study the stability and stability of the resulting product. In the presented study, the physicochemical and technological properties of the vitamin D substance were studied and the optimal ultradispersion mode was selected. The composition is experimentally established and a technology for obtaining laboratory samples of nanocapsules is proposed. The shape and size of the obtained nanocapsules with vitamin D were studied. Based on the developed experimental model, the optimal composition of nanocapsules was obtained. The quantitative content of vitamin D3 in the analyzed sample of nanocapsules was 76.9% with a holding time of 2.0 min. The results of studying the stability and stability of vitamin D nanocapsules proved their stability for 12 months. The developed vitamin D nanocapsules are a way of modifying the vitamin D substance for the subsequent production of tablets with improved biopharmaceutical properties. The selection of the composition of excipients based on the prediction of their properties, as well as the technology for producing nanocapsules, allows to increase the duration of the therapeutic effect while simultaneously reducing the maximum concentration of the drug in the body. The optimal composition of solubilizers for achieving a more complete, rapid and targeted dissolution of the active substance in a given part of the intestine has been experimentally confirmed. The aim of the study is to obtain a quality drug with improved properties such as adequate bioavailability, safety, low toxicity, no side effects and controlled release.

The long-term pharmacological action of cinnarizine nanoparticles based on biodegradable poly(D,L-lactide-co-glycolide) (PLGA) was studied using adult male Wistar rats (240 – 260 g). The reference drug was cinnarizine substance at a dose of 5.6 mg/kg. Changes in the cerebral hemodynamics were studied by ultrasound dopplerography, measured as the level of cerebral blood flow recorded over time intervals of 2, 4, 6, 8, 10, and 12 h and characterized by indicators of systolic linear and volumetric velocities of cerebral hemodynamics in terms of the Pourcelot and Gosling indices. The study revealed prolongation of the cinnarizine effect for 12 h, which favorably distinguished the developed PLGA dosage form from other drugs available on the pharmaceutical market, which is likely to mitigate side effects of the parent drug.

A search for new anticonvulsants led to a series of 2-(4-oxo-2-thioxo-1,4-dihydro-3(2H)-quinazolinyl)- acetamides that were synthesized by reacting (4-oxo-2-thioxo-1,4-dihydro-3(2H)-quinazolinyl)acetic acid with the appropriate amines in the presence of N,N′-carbonyldiimidazole. The tested compounds showed weak and moderate anticonvulsant effects in a pentylenetetrazole-induced seizure model in mice. Several features of the structure—activity relationships are discussed.

An assay method for the excipients (sucrose, phosphatidylcholine, and cholesterol) of liposomal medicinal formulations of the phthalocyanine photosensitizer lipophthalocyan by TLC with chromatodensitometry was validated. Coefficients of standard residual deviation for establishment of linearity were 3.48 for sucrose, 1.69 for phosphatidylcholine, and 1.36 for cholesterol. The coefficients of variation for determination of similarity and intermediate precision were less than 5%. The method was shown to be reliable over a wide range of conditions for the suitability of the system.

С целью поиска новых противосудорожных субстанций синтезирован ряд 2-(4-оксо-2-тиоксо-1H-хиназолин-3-ил)ацетамидов взаимодействием 4-оксо-2-тиоксо-1,4-дигидрохиназолин-3(2H)-ил)уксусной кислоты с соответствующими аминами в присутствии N,N’-карбонилдиимидазола. На модели пентилентетразоловых судорог у мышей исследуемые вещества показали слабый и умеренный противосудорожный эффект. Обсуждены некоторые закономерности «структура — активность».

The Shilajit was prepared according to different technologies, depending on the extraction stages, the purification method and the drying method, after which the content of the ballast substances was determined in the obtained samples.For the obtained samples, complete elemental analysis was performed on the S8 Tiger Wave X-ray fluorescence spectrometer.In the course of the experiment, the dependence of the content of ballast silicon (Si) and aluminum (Al) substances was revealed depending on the extraction stages, the purification method, and the drying method.As a result of the research, the optimum technological regime was chosen, observance of which of the Shilajit will be the minimum content of ballast substances.

— Therapeutic sulphide silt mud from Tambukan lake has been formed for a long period of time. Balneological value of silt mud from that specific lake is high because of high level of ferrous sulphides and water-soluble salts in it’s content, including recognized as therapeutically active bromine and boric acid; high concentration of lipids and carotenoids, which have anti-inflammatory, anti-bacteria, immune stimulating and bio stimulating effects. Goal: development of the method for stimulation of the peloid extract obtaining process from the Tambukan mud by an ultrasound-assisted extraction with further determination of biologically active substance using a spectrophotometric method. The research is based on formerly known and patented methods, offered by Kh.G.Karagulov. The method is reasonable, allows to extract carotenoid in full. The disadvantage of it is the energy-demanding and the usage of an organic solvent. As the object of the research a deep seated mud sample from the Tambukan lake was taken. After an ultrasound-assisted extraction there was obtained an oily extract from the mud sample. Quantitative content estimation was held out using a spectrophotometric method in visible region of absorption. The ability to optimize the process of peloid extraction from the Tambukan mud by the ultrasound-assisted extraction has been proven. Offered method for extraction and determination of carotenoid amount in Tambukan mud is less resource- and energy-demanding. Alongside with that it provides best possible carotenoid amount in the outcome. Effective and less expensive method to obtain peloid from Tambukan mud has been developed. The research results point out that the level of carotenoids in Tambukan silt mud has been reduced resulting in serious reduction of therapeutic effect. in

Валидирована методика количественного определения вспомогательных компонентов (сахарозы, фосфатидилхолина и холестерина), входящих в состав липосомальной лекарственной формы фотосенсибилизатора из группы фталоцианинов — липофталоцина — методом ТСХ с хроматоденситометрией. Коэффициент стандартного остаточного отклонения при установлении линейности составил для сахарозы 3,48, фосфатидилхолина — 1,69, холестерина — 1,36. Коэффициент вариации при определении сходимости и промежуточной прецизионности составил меньше 5 %. Надежность метода установлена в широком диапазоне различных условий пригодности системы.

BACKGROUND:The urgent tasks of experimental balneology are to design and investigate of the action of native mineral waters (MW) enriched with essential trace elements in order to improve their therapeutic and prophylactic effects.OBJECTIVE:To investigate the mechanisms of direct action of the cycle intake of Essentuki MWs modified with selenium (Essentuki Novaya - MW1, Essentuki No. 4 - MW2) on healthy animals.MATERIAL AND METHODS:According to the experimental conditions, 102 male albino rats were divided into 7 groups using a simple randomization method. Group 1 (n=15) received only drinking water (DW) (a control group); Group 2 (n=13) used native MW1; Group 3 (n=13) took native MW2; Group 4 (n=15) had MW1 with selenium (MW1Se1 - 3 mcg/kg); Group 5 (n=15) received MW1Se2; Group 6 (n=15) had MW2Se1 - 300 mcg/kg; and Group 7 (n=16) used MW2Se2.RESULTS:After cycle drinking, the body weight of the animals in the experimental groups did not significantly differ from that in the control group and was determined within the normal species range. X-ray densitometry showed that the body fat composition in the rats was lower than the control values only after MW1Se1, MW1Se2, and MW2Se1 cycles. The rat lipid spectrum in different groups displayed differences: the atherogenic index was low after MW1, MW1Se1, and MW1Se2 cycles. The blood glucose levels increased in the rats after drinking native MWs (F=2.7; p=0.01). After selenium-modified MW cycles, the blood glucose levels corresponded to the control values. The blood of experimental and control animals showed no differences in bone mineral density (BMD), levels of hormones (insulin, thyroxine, dehydroepiandrosterone (DHEA) and end products of protein metabolism. Selenium-modified Essentuki No. 4 changed the orientation of functional relationships from negative to positive ones between glucose and BMD.CONCLUSION:The findings suggest that cycle drinking with native and selenium-enriched Essentuki MWs differently affect the animals. The Essentuki Novaya MW (MW1, MW1Se1, and MW1Se2) drinking cycles predominantly affected in reducing blood atherogenic lipids. The volume of an animal fat component was lower after selenium-modified Essentuki Novaya and Essentuki No. 4 water (MW1Se1, MW1Se2, and MW2Se1) cycles. A direct relationship between DHEA and BMD was found in animals after using the selenium-enriched Essentuki No. 4 cycle.

The article is devoted to the anniversary of Professor Eleonora Fedorovna Stepanova – a bright representative of the Russian intelligentsia: a talented lecturer, an inventor, an author of numerous books, an internationally recognized scholar!

Data on the biological and physiological role of vitamin D3 have changed significantly over the past 30 years. Itbecame known about its significant impact on fertility of both men and women. We have studied the current data onpharmacological effects and optimal doses, the range of dosage forms of vitamin D3. The analysis showed that the composition of drugs of vitamin D3, permitted for use in the Russian Federation, include: cholecalciferol, alfacalcidol, paricalcitol, calcitriol. Only three drugs of foreign production contain a medical dose of vitamin D for women: Akvadetrim,Vigantol, D3-droplet, therefore, the development of domestic drug is relevant. Only 50 % of the oral dose of vitamin D3is absorbed in metabolic disorders. We have confirmed the need to create a new solid dosage form of vitamin D3 with aconcentration of cholecalciferol of at least 3000 IU. For its production we suggest using the cyclodextrin and mannitol(Parteck HPB and Parteck M, “Merck KGaA”, Germany). They can ensure the stability of the drug in the body and itsgood digestibility. Vitamin D3 tablets, coated with an intestinal-soluble shell will be convenient for use, stable duringstorage, provide the necessary pharmacological effect. Such dosage form can be an alternative to the already knownimported drugs