The study is devoted to novel manufacturing method of preparation of polymeric microparticles, loaded by naltrexone base, in flow through regime. Special module construction was developed for providing emulsification in continuous regime. Focusing on production of polymeric microparticles with characteristics, compatible with characteristics of the pharmaceutical Vivitrol and its native analogue, parameters of encapsulation process were defined. An ability of prepared microparticles to prolonged drug release during 28 days was demonstrated.

The technology of obtaining samples of ointments of nifedipine on the emulsion and hydrophilic bases using the method of solid dispersions is developed. The quality of the obtained soft medicinal forms was evaluated. The effectiveness of the proposed technology for the preparation of nifedipine ointments has been proved, which makes it possible to increase the pharmaceutical availability of the water-soluble test substance, providing better release by increasing its solubility and dissolution rate.

A composition and a technological scheme for the preparation of the combined dragees, containing isoniazid and ofloxacin, were developed. The parameters of the quality of the developed dragees, were studied. The shelf life of the dragee with isoniazid and ofloxacin has been established, when stored 2 years, in glass-massed banks with a screw mouth closed with plastic caps in a dry, dark place at a temperature of 20-25 °C.

Information on the toxicological and pharmacological characteristics of the main excipients used in the formulation of torasemide (sodium croscarmellose, microcrystalline cellulose, magnesium stearate, pregelatinized corn starch, silica, mannitol) is presented in the article.

The aerodynamic properties of the developed generic product Salbutamol metered dose inhaler 100 μg/dose and Salbutamol-Teva metered dose inhaler 100 μg/dose using apparatuses A, C, D and E in accordance with the general article 2.9.18 of the European Pharmacopoeia have been studied. In vitro equivalence of the generic product and the comparator with regard to such aerodynamic characteristics as the fine particle dose, the particle size distribution, the relative amount of salbutamol passed through the apparatus stages, the mass median aerodynamic diameter (MMAD), and the geometric standard deviation (GSD) has been shown. It is shown that the device A is useful for testing of the respirable fraction, and the apparatuses D and E are suitable for the assessment of the particle size distribution, MMAD and GSD.

The article is devoted to main approaches to the development of the professional standard «Specialist for quality control and testing of nanostructured pharmaceutical products». The structure of the Professional Standard Project is described, as well as the description of the labor functions and competences of the specialists.

This work reflects the description of the developed professional standard «Specialist in the preparation and operation of equipment for the production of nanostructured pharmaceuticals». Formulations of the generalized labor functions are resulted, the benefit of development of the given standard, both in relation to experts, and in relation to employers is shown.

The article is devoted to main approaches to the requirements formation to specialist-researcher in the field of nanostructured pharmaceuticals. The structure of the Professional Standard Project «Specialist-researcher for the development of the nanostructured pharmaceuticals formulation» is described, as well as the description of the labor functions and competences of the specialists.

The article describes a method for quantitative determination of aminocaproic acid in a multi-component hemostatic medical agent having the local effect. The analysis uses the method of direct spectrophotometry with the wavelength of 568 nm. Based on the results of the study, the main validation characteristics of the method meet the eligibility criteria according to the general pharmaceutical article «Validation of analytical methods» from the XIII edition of the State Pharmacopoeia. The analytical area of the procedure was 0.04-0.06 g/ml. The technique can be reproduced in laboratories with the confidence level P=95%, the correctness of the measurement was 1.36%.

In the human body, coenzyme Q₁₀ is in the oxidized and reduced forms and can be found in every organ. The review describes modern HPLC methods of coenzyme Q₁₀ analysis using electrochemical, spectrophotometric and mass spectrometric detectors. In the article we present information on sampling, preparation of biomaterial for analysis and preservation of coenzyme Q₁₀ stability in biomaterial. It is carried out a comparative analysis of the determination methodologies for the oxidized and reduced forms of coenzyme Q₁₀ by its sensitivity and selectivity.

A sensitive and developed the validation method for quantification by using the chromatograph for Etoricoxib. The method was validated in terms of specificity, linearity, accuracy, precision and analytical range. The results of validation method and approbation at selected sites are given. It was shown than main validation characteristics meet the requirements. Using the HPLC method the dispersion was 0,253%. The analytical range of method is 25-85 µg/ml for HPLC.

A new approach to the robustness investigation of HPLC/UPLC methods that includes use of risk analysis is offered. It allows reliable justification of the choice as well as omission of certain factors at study of the robustness of HPLC/UPLC methods. The risk level of factors is determined using a special matrix and a table to assess the сriticality of the factor and the рrobability of its critical impact on responses. It is emphasized that the exclusion of any factor associated with the chromatographic system from investigation of robustness at validation of a concrete method has to be reliably justified - with the use of a risk analysis including consideration of the features of chromatograms and theoretical arguments. For the factors that often have the high and average level of risk, we provide and discuss the guide values for the limits of the factor change based on our own experience and literary data. We also suggest the guide values for permissible limits of the responses variation as well as an example of assessment of robustness of the method for determining impurities using risk analysis and «оne-factor-at-a-time» method. Recommendations are made to study of the robustness of HPLC/UPLC methods.

Anthelmintic, insecticidal, anticoagulant, hemostatic activities of monosubstituted amides of phthalic acid were investigated. Insecticidal, anthelmintic and antico-agulant activities for investigated monosubstituted amides of phthalic and tetrachlorophthalic acids were not discovered. Amides of tetrachlorophthalic acid are characterized by a hemostatic effect. Hemostatic effect of one compound in 1.5 times exceeds the effect of Etamsylate.

Algorithm of selection of compounds and formulations for development of multi-purpose CNS targeted medicinal products for emergency field and civil therapy is justified on the example of potent analgesics. Key criteria and quantitative parameters for selection of substances and dosage forms are singled out. The advantages of strong synthetic opioids vs traditionally used morphine, its derivatives and analogues are demonstrated. Advantages of multi-target formulations are shown. Choice of transmucosal dosage forms of analgesics, antiemetics and antidotes for urgent therapy is substantiated. Approaches to development of universal pharmacological platform for creating drugs acting on CNS are proposed. The current situation in the field of potent analgesics and other limited use medicines in the Russian Federation is described, problems are noted and possible solutions are suggested.

Functional diagnostics method (scintigraphy), connected with injection of radioactive isotopes with further getting of 2-D image by emitting radiation detection, is widely used in medicine. Scintigraphic visualization of infections and inflammation with ⁶⁸Ga-citrate is powerful diagnostic instrument for patients with inflammation or infection disease. ⁶⁸Ga is short-lived positron emitting radionuclide (half-life time is 67,6 min, positron energy is 2,92 MeV). Such characteristics allowed to get better images of other radiopharmaceuticals with ⁶⁸Ga. Benefits of the drugs, mechanism of mother radionuclide fission is described in the article, as well as equipment for ⁶⁸Ga-citrate synthesis with all the technological processes. Obtained ⁶⁸Ga-citrate is suitable for positron emission tomography diagnostics for infection disease and inflammation detection in clinical practice.

As a result of the studies was shown that the relative ratios of isomers by integration in DMSO-d₆: (S, R)-warfarin – (S, S)-warfarin – open chain warfarin are 70%: 28%: 2%; in СDCl3 are 45%: 40%: 15%. In the IR spectra of warfarin specific absorption bands are observed in the regions 3271–3277 cm^-1, 1681–1682 cm^-1, 1103–1076 cm^-1, corresponding to:νOH, νCH=CH: ν_as C–O–C. The molecular peak of warfarin after silylation has m/z 380 corresponding to the mass of trimethylsilyl-warfarin. Thus, the possibility of using IR, NMR spectroscopy and chromatography-mass spectrometry to confirm the authenticity of warfarin derivatives has been demonstrated.

Morphological and physico-chemical properties of erythrocytes encapsulated by terpenoindol alkaloids (TIA) by nephelometry and osmotic resistance of erythrocytes in a medium with low concentrations of sodium chloride have been studied. Changes in the morphological and physico-chemical parameters of TIA-loaded erythrocyte carriers and freshly isolated erythrocytes have been studied. It was found that during the process of encapsulation of TIA by a modified hypotonic swelling method, the morphological and physicochemical parameters of erythrocytes change insignificantly in comparison with the control.

The paper considers the requirements to the production of pharmaceutical substances and the current trends in the toxicity assessment of the preparations obtained. The results of research of the use cell cultures for test bioactive substances, including cholera toxin are given. Evaluated are the advantages of in vitro methods application, in particular, continuous cell lines at some stages of cholera chemical vaccine manufacturing.

The contents of natural radionuclides in camomile and of germanium element in some herbs and ginseng of different origin were determined by mass spectrometry and inductively coupled plasma atomic emission spectrometry. A substantial divergence with the available literature data is found. The necessity to form a domestic database for the complete microelement composition of herbal plant raw materials is substantiated.

Drug form of paracetamol formed on the basis of molecular crystals of rhombic modification was studied. The studies included technological experiments, optical microscopy, differential scanning calorimetry, X-ray diffraction and IR spectroscopy. It is found that drug forms of paracetamol, synthesized by calorimetric method, together with enlarged solubility possess remarkable sensibility to temperature and mechanic grinding. It is presented X-ray patterns, IR spectra and curves of differential scanning calorimetry.

This article shows the results of a study of pharmaceutical equivalence of atorvastatin generics using Dissolution test. A significant difference in the intensity of atorvastatin release from tablets from different manufacturers has been established. From 10 to 97% of atorvastatin was released from tablets of different manufacturers by the 15th minute of the test. In the similitude of the dissolution profiles, 6 generics out of 13 studied were pharmaceutically equivalent to the reference drug in doses 10 mg and 20 mg. It is shown that the inclusion of disintegrants and solubilizers in the formulation leads to an increase in the release rate of the active pharmaceutical substance from the dosage form.

A study of the toxic properties of the drug cabazitaxel was carried out on outbred rats with intravenous administration. The toxicity was assessed with a single and repeated weekly administration of the drug. It was noted that the toxic and lethal effects were delayed. In an acute experiment, the mean lethal dose was calculated, which for animals of both sexes was 4.2 mg/kg. With repeated administration, the maximum tolerated dose was 1.5 mg/kg, lethal - 2.5 mg/kg. The clinical picture of intoxication was characterized by depressed behavior, decreased response to external stimuli and tonus of skeletal muscles, tachypnea and diarrhea. A decrease in feed intake and body weight of animals was detected. Target organs of toxic effect of cabazitaxel: gastrointestinal tract, liver, bone marrow, reproductive system of male rats.

The biological activity of a number of N'-arylbenzenecarbоximidohydrazide hydrohalides in vitro against Staphylococcus aureus, Bacillus cereus, Escherichia coli and Candida albicans and Aspergillus brasiliensis fungi, as well as anti-inflammatory and analgesic activities in vivo has been studied. N'-(4-nitrophenyl)benzenecarboximidohydrazide hydrochloride (3c) exhibits marked antimicrobial activity against St. aureus, 4-nitro-N'-phenylbenzenecarboximidohydrazide hydrochloride (3b) is effective against C. albicans and A. brasiliensis fungi. Acute toxicity of the obtained compounds for mice with intragastric administration was 1000 to 2000 mg/kg and intraperitoneal administration was 200 to 400 mg/kg. 4-nitro-N'-phenylbenzenecarboximidohydrazide hydrochloride (3b) has anti-inflammatory and analgesic activities that do not exceed that of the reference preparations.

The success of developing new drugs largely depends on the methodology of preclinical research. For developing cerebroprotective drugs, there are many experimental models with different complexity. In this review the most used stroke models are described and characterized, model procedures briefly described, own research experience in utilizing some model methods in establishing efficacy of drugs is also described.

The definition of safety, tolerability and efficacy of drugs is largely related with the results of clinical trials (CTs). Currently, phase I studies, pharmacokinetics and bioequivalence, conducted with the participation of healthy volunteers, are one of the main ways to registering drugs in our country and in the world. Despite this, the question of perception by the subjects of these types of studies remains open to this day. The purpose of this work was to analyze the formation and priorities of the motivational determinant by evaluating the experience of participation of healthy volunteers in CTs. During the study, the factors influencing the decision to participate in bioequivalence studies were analyzed.

Soporific substances of the third generation - Z-preparations: Zaleplon (Andante), Zopiclone (Imovane) and Zolpidem (Ivadal) - are widely used in medicine for the treatment of insomnia. Despite a number of advantages over of barbiturate derivatives and 1,4-benzodiazepine, the identified preparations are toxic. Poisoning incidents, including fatalities, are described. To diagnose intoxications by these medicines and other purposes (for monitoring the concentration of these medicines in the blood, studying pharmacokinetics, evaluating drug interactions, optimizing treatment control), the development of methods for defining Z-preparations in biological objects becomes important, that is currently developed insufficient. Therefore, the purpose of this work is to study and analyze the specialized literature on the chemical, physico-chemical, pharmacological properties, methods of analysis of investigated substances, methods of extraction, purification, methods of identification and quantification while studying the biological objects.

The results of a comparative analysis of the nomenclature of the assortment of nasal sprays in the pharmaceutical markets of the Russian Federation and the USA are presented. The assortment of nasal sprays of the Russian pharmaceutical market is represented by 122 trade names, 30 international non-proprietary names, 14 pharmacotherapeutic groups, 11 ATX groups, and 21 producer countries. In the US pharmaceutical market, nasal sprays are represented by 12 ATC groups, among which the largest group is R01A Decongestants. There are 4 directions for development of nasal sprays for the domestic pharmaceutical industry: 1) development of sprays, which are presented in the US pharmaceutical market; 2) development of sprays, which are absent in domestic and foreign pharmaceutical markets; 3) development of sprays, which are represented by other dosage forms; 4) development of pharmaceutical production sprays.

The scope of certification of the quality management system is extended to research activities at the St. Petersburg Chemical and Pharmaceutical Academy. This allowed to to create more universal and effective system of organizing educational and research activities at the Academy when the integration of the process model mentioned and existing in the academy occurred. Based on this experience, management plans to confirm the compliance of activities of one of the structural units with GLP requirements. The authors demonstrated the feasibility of implementing a quality management system in accordance with the ISO 9001 standards as a strategic platform for preparing for the certification of preclinical research for compliance with the requirements of good laboratory practice (GLP).