The characteristics of the excipients as components of gels for oral administration have been considered in the article. The properties of gelatinizing, sweetening and preservation agents have been described. The compositions of the commercially available on the Russian market medical products and dietary supplements in the form of gels for oral administration have been analyzed.

The process of desorption of vinpocetine on the surface of crystalline silicon and silicon oxide in various media has been studied by molecular dynamics modeling. The desorption of vinpocetine in water has been established both from the surface of silicon and from the surface of silicon oxide. The character of the desorption of vinpocetine from silicon and silicon oxide at pH 6.8 and pH 7 differs insignificantly (within the error of the simulation results). The desorption of vinpocetine in acidic medium (pH 2) from silicon and silicon oxide occurs more efficiently and at a higher rate, compared to pH 6.8 and pH 7.

A new bifunctional ointment with chondroitin sulfate and celecoxib on a hydrophilic base was developed. The optimum conditions of the technology and technological properties of the ointment were determined. The techniques for quantitativecontrol of active components in a bifunctional ointment are developed. Quantitative determination of chondroitin sulfate in an ointment was conducted by turbidimetric titration. A relative error of determination with confidence probability P=95% is not more than 2,01%. Quantitative determination of celecoxib was conducted by spectrophotometry. A relative error of determination with confidence probability P=95% is not more than 3,22%.

The review is about on polymers used as embol for vascular occlusion. Existing and developed means for embolization vascular were considered. Particular attention is paid to polymers and compositions on their basis, which it is capable of forming gel structures suitable for occluding vessels.

The article describes the main requirements for ophthalmic gels and presents the study of the rheological properties of ophthalmic gels, registered in the Russian Federation: Korneregel®, Solcoseryl®, Vidisic®, Ophtagel®, Oftan-Timogel®, Systein gel®. The parameters of rheological measurements conducted for ophthalmic gels are substantiated. On the basis of the results obtained, optimum rheological characteristics are suggested, which can be recommended for use in the development of ophthalmic gels.

The paper discusses the possibility of reducing the concentration of ethanol in the preparation of calendula tincture. Sample quality research conducted depending on the concentration used extractant. It found that the use as the extractant ethanol concentration of 40% and 20% in the preparation of infusions showed better quantitative results in terms of quantity as compared with recognized calendula tincture made 70% ethanol, but use as ethyl alcohol extractant concentrations less than 40% doesn’t guarantee the receipt of tinctures with a certain microbiological purity. These studies can be used in the pharmaceutical industry to obtain infusions with lower alcohol content.

The article discusses the usage of ion-exchange resins (IOSs) as excipients and pharmaceutical substances. The main functions of IOSs as excipients are: taste masking, disintegration of tablets, stabilization of substances, modified release, etc. Were described the examples of IOSs usage in oral, ophthalmic, nasal, transdermal dosage forms. Good technological properties: solid, liquid, application.

In the present work critical importance and benefits of Super Refined excipients for drug stability, integrity and safety are described. It was shown, that impurities can disrupt API and cause cell irritation. It was proved, that chromatographically purified excipients are fundamental to develop efficient, stable and reliable pharmaceutical formulations.

A convenient method for analyzing the content of vitamins A, D₃ and E in premixes has been developed (the tests were carried out using the example of the premixes «Mauervit» and «randvitam») using ultra HPLC. The necessary changes of the procedure have been made in comparison with the ones presented previously in GOST R 50928-96 due to the presence in the premix components hampering analysis (in particular, Tween 80). The developed procedure has been tested in terms of specificity, accuracy and precision. In addition, the possibility of using a simpler procedure for the analysis of vitamins extract, used as raw material for premix production, has been demonstrated.

A procedure for the simantenous determination of aminotriazole, triazolopyrimidinone and nirotriazolopyrimidinone was developed using the HPLC method with UV detection. To achieve the best chromatographic characteristics, it is proposed to use a column with a grafted aminophase Zorbax NH2 (Agilent Technologies, USA). The possibility of applying the developed methodology for the technological control of the second stage of the drug «Triazid» preparation is established following the results of the validation.

The developed method for the quantitative determination of phenibut in tablet drugs is based on the dansylation reaction in an alkaline medium (pH 9.18). The reaction results in the formation of a fluorescent derivative with λ_em=505 nm and λ_ex=335 nm. Optimal conditions were selected to complete the reaction: temperature and time of thermostatting (40 °C and 15 min), molar ratio of phenibut and dansyl chloride (1:1.4). The method was validated in parameters of specificity, linearity, precision and accuracy. A plot of fluorescence intensity versus concentration of phenibut over the range of 800-1200 ng/ml is described by the regression equation y =0.1003x+1.4685 ( r =0.9999). The limit of detection and limit of quantification were 29.55 и 89.54 ng/ml respectively.

Application of luminescent reagents for detection of toxicants including warfare agents, pesticides and their degradation products and precursors has been systematically reviewed. Methods of organophosphorus toxicants and products of their destruction (OP) detection based on lanthanide luminescent complexes (primarily Eu³⁺) have the similar sensitivity as the most advanced instrumental chromatographic and biochemical assays with detection level in the range of several ppts that allows to determine supertoxicants at the safety requirements concentration levels and at appropriate analysis duration from a few seconds to 10 minutes. High selectivity of toxicants identification is achieved by means of imprinted materials, modified cyclodextrins and luminescent sensor arrays. This is the basis for development of new technologies for trace analysis of toxicants and their decomposition products, including possible technology of luminescent contrast agents’ application to increase sensitivity of spectroscopic methods and remote determination of toxicants on the ground. Further possibilities to develop next generation materials for protective gear, equipment and multifunctional contact surfaces providing visualization and identification of toxicants and simultaneous catalytic self-decontamination is discussed. Relationship between technologies for improving safety and security at the crossroads of analytical chemistry of warfare agents, criminalistics, chemical safety and pharmaceutics has been demonstrated.

Currently, the key problem in the field of drug provision for the population of the Russian Federation is the lack of affordable and high-quality domestic drugs for the treatment of diseases associated with violations of fat and carbohydrate metabolism. At the same time, highly developed countries have increased interest to drugs based on natural compounds. Authors set the task to assess the prospects of the drugs’ market that based on natural compounds to correct violations of fat and carbohydrate metabolism and the chances of Russia in this market, including on the basis of the analysis of the distribution of patent documents in obtaining biologically active substances in three ways: biosynthesis, chemical synthesis, isolation from natural compounds.

Coumarins (also known as 2Н-1-benzopyran-2-one or 2H-chromen-2-one), in contrast to other groups of heterocyclic compounds, are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti-inflammation, anti-HIV, anticoagulant, anti-bacterial, analgesic, comparative immune-modulation. Recently, coumarins have attracted intense research interest in various fields of science. Of great interest is the possibility that many substances from this class of heterocyclic compounds could be a source of the development of highly active drugs for the therapy of several diseases. Many of these agents are combined (hybrid) molecules, which are designed through concept of molecular hybridization and have shown multiple pharmacological activities. This review will focus on recent advances in the molecular and cellular mechanisms of the action of the combined coumarin derivatives involved in the relationship between the«structure and activity» ((SAR) of these highly interesting heterocyclic compounds.

The reaction of benzonitrile with some arylamines was studied. It was found that the structure of arylamines affects the yield of N-arylbenzamidines and the possibility of their obtainment, which was confirmed by quantum-chemical calculations. The reaction of benzonitrile with arylamines is thermodynamically controlled. Maximal yield of product was obtained at t=180°C. The structure of synthesized compounds was proved by means of modern physicochemical methods of analysis: NMR ¹Н-, ¹³С-, ¹⁵N-spectroscopy, X-ray diffraction analysis (RSА).

The acid hydrolysis of amide of carboxyethyl alginic acid was studied. The influence of reaction’s temperature, characteristics of mother amide and presence of nitrous acid in the reacting mass to the results of the reaction.

The possibility and prospects of carrying out the chlorination step in the scheme for the synthesis of bendamustine hydrochloride were investigated. The advantages and prospects of the process in the flow microreactor are shown. The conditions for conducting the process in the flow microreactor under which the chlorination reaction proceeds with a lower content of by-products and a higher yield are chosen.

The article presents data on the development of a technique for determination of intrinsic viscosity of injectable drug with chondroitin sodium sulfate. A 0.2 M solution of sodium chloride was use as a solvent to eliminate polyelectrolyte swelling. The calculated viscosity of the test solutions was determinate in the concentration range of chondroitin sulfate 4.5-20 mg /ml. The value of the intrinsic viscosity, determined for each of the tested preparations, was in the range 0.03-0.042 m³/kg.

The paper contains the data on the development of quality control sample (QCS) for determination of specific activity of heterologous anti-rabies immunoglobulin in neutralization test on white mice. Given are the results on QCS attestation in reference to international standard samples of human immunoglobulin against rabies. The quality control sample is put on the register of QCSs approved for application in experimental-production subdivisions and in the department of biological and technical control. It is deployed for final quality control of anti-rabies immunoglobulin preparation in commercial batches.

Is necessary to ensure thorough purification of the target proteins, since the presence of host cell proteins (HCP) from CHO cells in the final product is fraught with a number of negative consequences. Thus, it is has to reduce the contamination of HCP to minimum levels. A comparison of the immunoenzymatic assays of the second and third generations of Cygnus technologies for the quantification of host cell proteins (CHO) in a monoclonal antibody adalimumab was done. It was found that a kit of the 2nd generation does not show the true level of the host cell proteins, underestimating the result. In this connection, it becomes necessary to confirm the validity of the method for determining the total quantity of host cell proteins (CHO) by a set of 3rd generation in adalimumab substance according to the following analytical characteristics: system suitability test, specificity, limit of detection, limit of quantitation, hook capacity, precision.

Microbiological studies conducted the effectiveness of surfaces decontamination by using potassium iodide submicron aerosol, made by the device Generator of sea air «Aeroiodine». We used bacteria of the genus Staphylococcus as the test cultures. The effectiveness of decontamination was 35±5%.

The development of new and improvement of existing methods for determining antioxidant activity is an urgent task of pharmacy, cosmetic and food industries. In the present work, the systematization and analysis of methods for determining antioxidant activity have been carried out, which have found the widest application and are described in the domestic literature. The most widely used electro-chemical and spectrophotometric methods of analysis. Today there is no method that would give complete information about the state and interactions of complex systems in which antioxidants are formed and enter into the reaction. There is also no single term that would determine the antioxidant properties of the compound. All existing methods for determining antioxidant activity suffer from one or other of the following drawbacks. It should be noted the objective impossibility of existence is not that of a single method, but even the possibility of comparing the results obtained by different methods. Therefore, each researcher, based on his goals and capabilities, chooses the ready, creates a new one, modifies an already known method, or often resorts to the study of the antioxidant activity of the studied object using a set of different methods.

Efficacy of non-equilibrium low-temperature plasma treatment for reducing microbial contamination of medicinal plant raw materials (chamomile flowers and peppermint leaves) was studied. Decontamination of plant raw materials was carried out at experimentally defined conditions: exposure time - 5.0 min, glow discharge frequency - 1.76 MHz, working pressure - 0.1 Pa, working gas of plasma - argon. It was found that spore-forming bacteria count after treatment under these conditions decreases by 2 orders of magnitude, yeast and mould count decreases by 3 orders of magnitude.

The article presents the results of a study of technological parameters (specific mass, bulk, mass, volume mass, porosity, quantity cavities between particles, free volume of layer of raw materials and coefficient of absorption of solvents) and individual the numerical indicators of the quality [moisture, ash residue (total and insoluble in 10% solution of hydrochloric acid ), chopped raw materials foreign materials] of the herb of aristolochia clematitis. The content of extractive substances was determined. The obtained data will be used in the development of the project of a pharmacopeia article on the herb of Aristolochia clematitis and in the technological process in the production of extraction preparations.

The analysis of component composition of the Schizandra chinensis has been carried out. Fruits (Fructus Schisandre) and seeds (Semina Schisandre) of Schisandra Chinese serve as medicinal plant raw materials. The chromatography analysis of component composition of alcoholic tincture of fructus of the Schizandra chinensis and of alcoholic tincture of semina of the Schizandra chinensis has been carried. The existence of major and minor components has been established by the results of chromatography analysis made with Agilent Technologies device. Qualitative and quantitative distinction between galenicals has been revealed with the help of ChemStationE 02.00 software and library for Mass Spectrometry NIST-05. In galenicals terpenoids, phenylpropanoids, threternenal saponins, carbohydrates, lignans, aminoacids and furanocumarins have been detected. As a result of the analysis of tincture of fruits Schisandra сhinese were detected 36 substances belonging to different classes: alcohols, acids, sugars, ketones, anthracene derivatives, terpenes, ethers and other compounds. The relative percentage of each component was calculated taking into account unidentified peaks. According to the results of the study, it's possible to draw a conclusion about the chemical heterogeneity of the essential oil of Shizandra сhinesis' seeds. The following groups of biologically active substances were found in the essential oil from the Shizandra сhinesis' seeds: terpenoids, phenylpropanoids, triterpene saponins, glycosides, carbohydrates, lignans, amino acids and furanocoumarins.

In vitro antimicrobial activity of infusion (1:10) from the combination plant medicinal product «Lorpoliphyt», infusions (1:10) the individual components of combination and model infusion, made from infusions (1:10) of the individual components of the combination plant medicinal product, taken in proportion to the parts of the collection, against gram-positive and gram-negative microorganisms were studied. The presence of bactericidal and bacteriostatic action against Staphylococcus aureus ATCC 6538-P and Escherichia coli ATCC 25922 was revealed. The antimicrobial activity of all tested infusions (1:10) against Candida albicans ATCC 10231 was not found.

Descriptions of mathematical models using for drug dissolution studying from modified-release systems (zero-order kinetic, first-order kinetic, Weibull model, Hixon - Crowell model, Higuchi model, Baker - Lonsdale model, Hopfenberg model, Gompertz model, Korsmeyer - Peppas model, Peppas - Sahlin model) were presented in the article. Results of ibuprofen release from carbomer matrix tablets were processed using Higuchi and Korsmeyer - Peppas models.

The results of the study of the wound healing activity of the drug «GMDP lyophilizate for solution for injection» are presented in the model of infected skin and soft tissue wound in rats in order to confirm the benefits of combined therapy of infected wounds with an antibiotic and the immunotherapeutic agent being tested in comparison with monotherapy with an antibiotic. The study used macroscopic, planimetric and histological methods. The advantages of the proposed combined therapy for the speed and completeness of wound cleansing and closure, including the intensity of epithelialization, the formation of granulation tissue, as well as the quality of granulation tissue, the degree of reduction of inflammatory changes, and lysis of the scabies are statistically reliable. In the control (intact) group the area of wounds decreased on average with speed 14,0±4,1 mm²/day, while in the «GMDP lyophilizate + Ceftriaxone» group this value was 25,1±4,7 mm²/day (significant difference from the control, p=0,0096).

In this work the intestinal permeability of phospazide in vitro was investigated using Caco-2 cell model in apical-basolateral (A-B) and basolateral-apical (B-A) directions as well as with the option of adding of P-glycoprotein (Pgp) inhibitor cyclosporine A. The following standard substances were used: ranitidine and propranolol. Papp values of test and standard substances were obtained. The obtained data were compared with the values (A) log P for the test and standard substances. According the results of this study, the phosphatide presumably has a low intestinal permeability in terms of BCS. The affinity of phosphazide for the efflux transporter Pgp was demonstrated.

The effect of a new drug - selective activator of Ca-dependent NO-synthase on the processes of hemostasis in norm and type 2 diabetes in laboratory animals is shown in this paper.

In the present paper some immunological effects on T- and B-cell immunity of a new drug Vitanam - selective activator of Ca-dependent NO-synthase were shown on the animal model.

Allergenic and genotoxic effects of the medical device «Resorbable collagen material "COLLOST® gel» were studied in laboratory animals. It was shown than immediate-type hypersensitivity reaction is not detected in mice by the cutaneous anaphylaxis test after once weekly sensitization during 30 days. Conjunctival test revealed no hypersensitivity to medical device in guinea pigs after three times sensitization for every 48 hours. Guinea pig maximization test did not reveal any skin-sensitizing effect of the medical device. Bone marrow chromosome aberration test did not detect genotoxic effects of the medical device.

Clinical study report is one of the main documents during the drug development. The preparation of the clinical study report requires knowledge of Russian and foreign legislation, awareness of guidelines and recommendatioins issued by the professional associations as well as the effective process management. This article provides an overview of the current Russian and international regulatory documents and recommendations of professional organizations on the content and structure of the clinical study report, and describes an example of an algorithm for preparing the report from the earliest stages (data processing) to writing the final report with interpretation of study results.

The article presents information on the use of the IDEF0 standard in process visualization pharmaceutical development analytical stage.

The received results show that the greatest (79%) share of plant-based drugs is presented by the domestic manufacturers. The greatest contribution (more than 13%) in structure of import supply is made by the European manufacturing enterprises. Germany (6.86%) is leading among them. The presentation of botanical drugs (31.54%) is the most frequent. One can’t help paying attention to the fraction of substances (7.67%) and semi-finished products (10.17%) in structure of import supply. The latter the indicates the dependence of domestic manufacturers on supply of raw materials from abroad. It is important to notice the share (19.87%) of medicines for digestive tract diseases and metabolic disorders treatment.

Global medicine spending will reach nearly $1.12 trillion by 2022 on an invoice price basis, up nearly $370 billion from the 2016 estimated spending level. Current trends are based on disruptive technologies including gene-editing, precision medicines and digital technologies, Big Data etc. The characteristics of biopharmaceutical innovation have also evolved over the past two decades, with increases in the share of cancer treatment launch, orphan indications.

In this article the current state of the legal regulations in Russian Federation for pharmacovigilance has been analyzed. The lack of legal regulations of a lot of aspects of holding concrete actions by pharmacists in pharmacies, necessary for further implementation of pharmacovigilance, has been shown. Our functional model of the conducting activities in pharmacies for implementation of pharmacovigilance has been presented. Necessity of presence of the standard operating procedures in pharmacies regulating an order of conducting activities for implementation of pharmacovigilance has been revealed.

The results of present work show that the largest (52%) share of drugs for etiotropic therapy of pneumonia in pediatrics is represented by foreign manufacturers. Asian countries (India (38,45%) and China (6,46%) bring the most contribution into the structure of import. Drugs in form of powders and lyophilizates (43,20%), tablets (36,66%), and injections (11,72%) have the largest specific weight on market. The fraction of substances (83,75%) in the structure of import supply indicates the dependence of local manufacturers on raw material from abroad. The presentation of beta-lactam antibiotics (drugs - 45,70%, pharmaceutical substances - 36,98%) is most frequent. It's important to notice that only 50% of drugs for pneumonia therapy may be allowed to use for children under 3 years. The monitoring of side effects in pediatrics results (meronem, cephtriaxon, ciprofloxacin and cephtazidim) shows high probability of developing of adverse effects from digestive and nervous systems.

At present, there is a tendency in Russia to switch domestic manufacturers of drugs from the system of purchases of chemical products to own production of active pharmaceutical ingredients. The article reviews the current state of production of active pharmaceutical substances in the Russian Federation. The historical milestones in the production of pharmaceutical substances in the Soviet Union and the current situation of this market are considered. In addition, it provides an overview of the current international practices of quality control of active pharmaceutical ingredients and formulated assumption about the future state of the purchase market of API in countries with a low level of the control system. The authors analyze the structure and price indicators of the Russian API market.

The paper presents information on how the Sumerians, doctors of Egypt, Ancient Greece and the Roman Empire treated their patients two thousand years or more ago. An attempt is made to analyze the assortments of medicines and technological methods used by physicians of different states and cultures. It is established that they had many similarities and consisted of representatives of the vegetable and animal kingdoms, as well as the world of minerals. The technology of preparation of medicines consisted of simple operations, which, however, improved over time. Most of the medicines used by ancient doctors have lost their meaning, although some of them are still valid today.