The article analyzes and systematizes approaches to justification of drug formulation technology, depending on the API`s biopharmaceutical classification system (BCS). The solubility and absorption inherent to BCS are the most important characteristic of pharmaceutical substances and should be the factor of rational justification of formulations and technologies for safe medicines. Article shows the overview of modern biopharmaceutical technology for improving the characteristics of API, which are belongs to different classes of BCS. Were shown that during the development of dosage forms with poorly soluble APIs is better to use technology solubility enhancement, for substances of IIIrd and IVth classes - needs to increase absorption. Article describes the design of dosage form of successful medicinal products.

The possibility of formation of paracetamol of orthorhombic modification by the method of calorimetry is studied. The studies include technological experiments, optical microscopy, differential scanning calorimetry, X-ray diffraction and IR spectroscopy. It is found that in the result of temperature cycling the crystals of paracetamol are modified in the crystals of orthorhombic syngony. Microphotographs, X-ray diffraction patterns, differential scanning spectroscopy curves and absorption spectra are presented.

The article is about the study of the characteristic properties of a microemulsion composition for insulin transdermal therapeutic system (TTS). The type of microemulsion "water in oil" was determined and its stability was investigated. Instrumental methods have been used to evaluate parameters such as refractive index, viscosity and particle size. The conditions for the release of insulin from the microemulsion have been found, which make it possible to ensure the release of the hormone into a volume more than 95% of the claimed amount. In vitro study hormone diffusion from TDS containing a microemulsion with insulin through the native rabbit skin was ~1 U/h. It corresponds to hormone rate secretion by the pancreas of a healthy person.

This review is about nonsteroidal anti-inflammatory drugs and different approaches to development of pharmaceutical forms for controlled nonsteroidal anti-inflammatory drug release. Natural and synthetic biocompatible polymers used as drug carriers were considered. Different methods used for production of polymeric microparticles and formulations of nonsteroidal anti-inflammatory agents based on them were discussed. Characterization of microparticles with encapsulated nonsteroidal anti-inflammatory agents was given.

Experimental data on the development of composition and technology of oro-dispersible tablets with azithromycin. There is shown the study of sweet taste of the tablets masses, the production of tablets on the basis of their granulates. Antimicrobial properties of the tablet granulates are investigated for studying of the antibiotic stability, when azithromycin is used in wet granulation tableting technology. Identifies the main technological characteristics of the granulates, the tablets are produced by compression and indicators of quality are studied.

Medicated chewing gum (MCG) are an alternative to solid dosage forms for oral use. In the Pharmacopoeia of the United States submitted an article on chewing gum of nicotine. A monograph of this drug form is available in Belarusian and European Pharmacopoeias. The article presents the analysis of the literature on the use MCG as delivery system of drugs, excipients for the manufacture of MCG, as well as the schemes for the production of medicinal chewing gum and tests of their quality.

Currently, one of the promising methods of taking medications are instant formulations (in particular, medicinal films), which have a number of advantages over traditional dosage forms. In addition, the classification of rapidly dissolving films and their application are considered, and an assortment of transmucosal dosage forms is presented.

Ketoprofen is a medicinal substance that has not lost its relevance in modern medicine and pharmacy. The article describes the aspects of its application. The prospects of creating new dosage forms containing ketoprofen are considered. The possibility of creating effervescent dosage forms containing solid dispersions of ketoprofen is described.

The process of the synthesis of silicon-containing glycerol derivatives of Si(С₃H₇O₃)₄ ∙ 6С₃Н₈O₃ 
composition was optimized on the example of creation of the experimental industrial technology of the drug substance «Silativit» production. The main criterion of optimization was reducing a time and energy expenditure on carrying out the synthesis, representing heterophase reaction of alcoholysis of initial alkoxysilane by polyol. Optimization was performed on such indicators of process as temperature condition, the mode of removal of an easily volatile product of reaction, the mode of mixture of reactionary weight and type of the used mixing device.

The article describes the approaches to classification and separation of groups of excipients in oral suspensions of both domestic and foreign authors. A number of existing classifications of excipients for oral suspensions are presented. The analysis of formulations of oral suspensions that are registered on the pharmaceutical market of Russia to assess the range of excipients the most relevant at the present time. Evaluations of the frequency of use of specific excipients are carried out and, if possible, the concentrations used.

The article presents the results of studying the rheological characteristics of dental preparations in the form of gels registered in the Russian Federation: Dentamet®, Kamistad®, Calgel®, Metragyl-Denta® and Holisal®. The parameters of rheological measurements conducted for dental soft medicinal forms are substantiated. On the basis of the results obtained, optimum rheological characteristics are suggested, which can be recommended for use in the development of dental gels.

The possibility of applying sedimentation, centrifuge, and filtration techniques for concentration of F. tularensis 15 NIIEG suspensions obtained after submerged cultivation has been evaluated. It is established that realization of tangential ultrafiltration as part of technological process of live tularemia vaccine production is of distinct advantage. Characteristics of Francisella tularensis 15 NIIEG concentrate stored under different temperature/time-dependent conditions have also been studies. It is demonstrated that it is practical to preserve them at 4 °C within ≤6 days.

The article presents an overview of the main methods for producing liposomal medications, such as convectional and acoustic methods, high pressure method, detergent dissolution and removal method and the vapor method with phase inversion. The problems of hydrophobic technology of antioxidant pharmaceuticals (low solubility and chemical stability of such drug) and the advantages of liposomes to deliver them are reported. It is established that the most promising technology of producing liposomes containing drugs with antioxidant effects is a thin film hydration method with further sonication.

The article presents data on the development of a technique of photometric determination of ferric chloride (III) as a hemostatic tool, through the formation of salicylates iron. The developed method was validated for following validation characteristics: specificity, linearity, accuracy. The results of the study the main validation characteristics of the method meet the acceptance criteria. The technique is intended for definition of iron in the painted solutions of medicines in the range of 0,04-0,07 g/ml. Relative error of measurement of 0,83%.

Method of simultaneous determination of aminotriazole and triazolopyrimidinone using HPLC with UV-detection was developed. For best chromatographic performance Zorbax NH₂ amino phase column (Agilent Technologies, USA) was selected. The applicability of the developed method for providing technological control of the 1st stage of «Triazide» production was approved according to the results of validation procedure.

It was established that chromatographic column with amide sorbent (XBridge Amide) could be applied to the analysis of Pt (II) coordination compounds. The compounds could be analyzed by both reversed-phase chromatography [mobile phase: MeCN - Н₂О (2:98)] and hydrophilic interaction liquid chromatography [mobile phase: MeCN - Н₂О (90:10)]. The analytes were better resolved for hydrophilic interaction liquid chromatography. The properties of the amide columns differed substantially for analysis of Pt (II) coordination compounds using mobile phases with more 80% MeCN. Sorption of the Pt compounds to the amide columns at high MeCN contents was due to specific coordination interactions between the Pt atom and sorbent amides.

The possibility of using the infrared spectra of the diffuse reflection in the near and medium field of standardization and optimization of the technological process of tablet forms of aliphatic amino acids: butyric, β-alanine, γ-aminobutyric acid. Shown near infrared informative to normalize the moisture content of a substance in the stages of the process, as well as in the finished dosage form. The paper analyzed the descriptiveness of the infrared spectra with respect to the tablet form of gamma-aminobutyric acid, glycine. The spectral data to differentiate the homologous amino acids: γ-aminobutyric, beta-aminopropanoic, and glycine.

The article is a review of publications on the quantitative determination of polysorbates in pharmaceuticals. The author touches upon the structure and properties of polysorbates. The question of the use of polysorbates in the production of drugs is considered. Approaches and methods for quantitative determination of polysorbates are evaluated, their advantages and disadvantages are indicated.

Anthelmintic, insecticidal activities and influence on hemostasis of aroylhydrazides 1,4-dicarboxylic acids were investigated. Anthelmintic activity was investigated for 8 compounds, including three substances showed effect that exceed effect of the standard (Pyrantelum). Insecticidal activity was investigated for 4 hydrazides 1,4-dicarboxylic acids, all compounds are inactive. Compounds that were tested for hemostasis do not possess anticoagulant activity. They are characterized by a hemostatic effect which is lower than activity of Etamsylate.

The results of an experimental study of the effect of structure of substituting groups and pH value on the partition coefficients in biphasic systems of n-octanol and water for a number of 2,5-substituted 6-hydroxypyrimidine-4-(3H)-ones are presented.

Medicines based on opioid analgesics are the basic means of pharmacotherapy of severe pain at present. Approaches to increase efficacy and safety of complex opioid analgesia are described and classified based on analysis of medicinal and veterinary analgesics acting on different CNS biotargets. Principles of creation multitargeted fixed-dose combinations (FDC) and some schemes of multimodal analgesia are demonstrated by the example of opioid combinations with ligands of alpha-2 adrenergic receptors, antagonists of excitatory amino acid receptors, GABA ligands, their derivatives and analogues, cannabinoids, monoamines reuptake inhibitors and opiate receptor antagonists. Importance of multitargeted substances in general including codrug approach for facilitating of drug delivery and bioactivity enhancement were demonstrated. Development of opioid formulations with low level of dependency and tolerance and also principles to protect opioid formulations against non-medical use were described. Methodology of multitargeted analgesia is one of the drivers in drug development on the background of low progress in the development of new effective molecules for relief of severe and moderate pain. The greatest interest is development of FDC with drug potentiation and efficacy at low doses. It allows creating wide variety of analgesics formulations.

The method of obtaining new heterocyclic compound - chloride 2-[(1Z)-1-(3,5-diphenyl-1,3,4-thiadiazol-2(3H)-ilidene)methyl]-3,5-diphenyl-1,3,4-thiadiazol-3-Ia was developed. Its structure was proved by physicochemical methods of identification of organic compounds: ¹Н- and ¹³С-NMR-, IR-spectrometry, mass spectrometry. Antifungal activity was defined against С. albicans, T. rubrum, T. mentagrophytes, F. proliferatum, S. brevicaulis . It was shown that this compound has potent antifungal activity and can potentially be used in medicine as antimicrobial with fungicidal action.

Methods of synthesis of 7 warfarin derivatives from which three are combined has been developed. Their structural features, physicochemical properties of synthesized compounds by modern and spectral methods (IR, NMR spectroscopy) were determined. Their anticoagulant activity in vivo were studied by determining prothrombin time (PT). The most pronounced activity was possessed by substances AZ-5 (conjugate warfarin with a fragment of the substance diumancal, 41,2±2,3 s) and AZ-9 (diumancal, 45,18±4,85 s), comparable with the reference drug warfarin (37,4±2,8 s).

The article presents the chemical composition of medicinal plants the mixture of the multivitamin raw material. The methods of identification biologically active compounds, depending on their nature, such as the qualitative of the reaction, thin layer chromatography, high performance liquid chromatography are considered. Methods of quantitative definition as separate components of a metabolom of folia Urticae and fructus Sorbi, and total content of biologically active connections are given.

Extracts from rhizomes of ginger (Zingiber officinale) are widely used in the production of biologically active additives and in the food industry. In addition to essential oils and phenolic compounds, ginger is also rich in amino acids. To identify the amino acid profile, a qualitative and quantitative analysis of the rhizomes of ginger was carried out. As a result of the experiments, the following amino acids were identified by thin-layer chromatography: arginine, histidine, glutamic acid, isoleucine, valine, proline, leucine, methionine. By means of spectrophotometric analysis, the number of amino acids was determined to be 10.22%. The relative error of the single definition with a confidence probability of 95% is 1.89%. Thus, we can conclude that further research and improvement of approaches to standardization of rhizomes of ginger, as well as the creation of new dosage forms based on it.

In present review the actual and most widely used physical and chemical methods for testing antioxidative activity of herbal raw material and it`s conversion products in pharmacy, perfumery and food industry are discussed and systematized.

The article presents results of study of Bupleurum aureum grass dry extract using experimental models of acute gastric ulcer in rats and formalin-induced limb swelling in mice. A significant stomach-protective effect and dose-dependent anti-inflammatory effect of the extract were found. The results show that Bupleurum aureum grass dry extract is a promisinig candidate for development of therapeutic agents for prevention and treatment of a wide range of diseases.

Coumarins, known as 2Н-1-benzopyran-2-one (or 2H-chromen-2-one), are present in remarkable amounts in plants, also have been detected in microorganisms and animal sources. The structural diversity found in this family of compounds led to the division into different categories, from simple coumarins to many other kinds of polycyclic coumarins, which possess extremely important pharmacological activity. This paper presents the results of a full analysis of domestic and foreign literature in the field of research on the combined covalent derivatives 2H-1-benzopyran-2-one of natural origin. It is shown that at the present time, researchers are paying extraordinary attention to this class of compounds, based on the many points of view and actively expand the area of their practical application, especially in the prevention and treatment of diseases of the cardiovascular and immune systems.

The development of new antinociceptive agents and new approaches to pain relief based on potent non-narcotic analgesics is one of the most in demand and urgent directions of modern pharmacology. This work substantiates the choice of the clinically most relevant representative of non-narcotic analgesics from the α₂-adrenoreceptor agonist class - dexmedetomidine, which acts at low doses and demonstrates high therapeutic index for various modes of administration. An analgesic efficacy of dexmedetomidine in single intranasal administration of the original experimental pharmaceutical formulation was evaluated in models of acute thermal and visceral pain in laboratory animals (female outbred white mice). A pronounced dose-dependent analgesic effect of the dexmedetomidine preparation in the 10 and 50 μg/kg dosage was revealed in the test models of visceral pain. The analgesic effect of dexmedetomidine was accompanied by a dose-dependent sedative (but not anesthetic) effect in mice, with peak at 30 minutes for intranasal administration of 50 μg/kg of drug. In the doses used, dexmedetomidine did not exert any acute toxic effects in mice.

Study of the anti-arrhythmic influence of the new organic synthesis’s products was the purpose of an actual research. Such characteristics of these compounds as acute toxicity, anti-arrhythmic and pro-arrhythmic activity were studied. The mostly strongly marked effect was discovered while using M-0 and M-18. These compounds showed the highest anti-arrhythmic activity and the lowest toxicity. It was also discovered that M-18 compound is less dangerous than M-0 one due to absence of the certainly expressed spill-over effect of an arrhythmogenic action.

This article describes main methods of preventing degradation of chemically unstable drugs and their metabolites in biological fluids during storage after collection from patients. It is necessary for accurate quantitative determination of these compounds.

The main goal of preclinical studiesis the development of effective, high-quality and safe drugs. The task of preclinical studiesis to obtain exhaustive information, reliable and reproducible results. The article presents an overview of modern normative documents regulating the quality of preclinical studies, focuses attentionon the most important information in these documents and gives recommendations to specialists. A careful and reasonable application of the rules, guidelines and implementation of requirements of regulatory documents by experts involved in the process of drug development, allow to obtain reliable, complete and qualitative results of preclinical studies. This is extremely important both for planning and conducting subsequent clinical trials, and for evaluation of the desirability of continuing the project of development.

The analysis of educational institutions’ material and technical base, that implement applied research and development in the field of innovative medicines, was released. The directions for intensification and internationalization of such centers of innovative drugs development were offered, one of these directions is the establishment of Network Center for pharmaceutics of BRICS countries. The formation of this center will bring together leading universities and research institutions of the BRICS countries in the preparation of highly qualified personnel for the pharmaceutical industry, as well as to develop the scientific and technical BRICS cooperation in the field of drug development.

The matter presents a statistical evaluation of results obtained from GMP inspections of foreign pharmaceutical manufacturers held by Russian GMP-inspectorate in the year 2016. Overview and analysis of critical discovered non-conformities and their possible causes are given.

In this research is carried out the review of the Russian pharmaceutical market and the comparative characteristic of medicines of group of inhibitors of a proton pomp. Data on production, registration and sales of this group of medicines are provided during 2007-2016.

Integrity of records or data integrity is the most «hot» requirement when assessing documentation systems for compliance with Good Manufacturing Practice (GMP). It's in the center of focus of attention during inspections of pharmaceutical companies. This article is the first of a series of articles devoted to this topic. In it explains the reasons for the importance of preserving the integrity of records and provides examples of identified deviations.

This article is devoted to the history of the system of registration of medicines in Russian Federation. The article describes the main stages of formation of the legislative basis of regulation of circulation of medicines in the Russian Federation, highlights the key provisions of the Agreement on common principles and rules of circulation of medicines within the Eurasian economic Union.

The tendencies of development of the pharmaceutical ingredients production at the turn of the XX century in Russia were analysed. During this period, the production of pharmaceutical ingredients turned into a state of deep crisis. The reason for crisis were the sharp decrease of production volumes, production capacities and the level of their load, the practical termination of R&D in creation and introduction of new domestic original drugs. The macroeconomic and industry-specific causes of this crisis were identified. Since market mechanisms at the turn of the XX and XXI centuries in Russia were not able to ensure the withdrawal of the development and production of pharmaceutical ingredients from the crisis, therefore, government support measures that were provided for by the Federal Target Program «Development of the pharmaceutical and medical industry of the Russian Federation for the period Until 2020 and a further perspective» and are implemented in the process of its effectuation.

This article provides the overview of the Russian Pharmacopoeia (RPh) XIX - early XX century. There are the review of the RPh I-VI general pharmacopoeia articles and their systematization in accordance with the modern classification of dosage forms. The study of the highly potent drugs regulation of the manufacture and storage are shown. Additionally, these paper describers the approaches to the industrial production regulation after its appearance.