Vol 5, No 6 (2017)

The low-molecular synthetic drugs, used for the treatment of tuberculosis nowadays, are highly toxic and do not have the ability to selectively penetrate into phagocytes; besides, they are quickly removed from the body without providing a prolonged action. To solve the existing problem, modern methods of modifying the properties of biologically active compounds by joint synthesis of antibiotic with high-molecular compounds, by incorporating antituberculosis drugs into the carrier polymers have been applied. These methods have made it possible to purposefully change their physical-chemical and medical-biological properties.The aim of the work is to evaluate the technological properties of the substance of the combined anti-tuberculosis drug “Biomayrin” and to work out its drug product.Materials and methods. The object of the study was the substance of the original medicinal preparation “Biomayrin”, obtained on the basis of high molecular compounds, and synthetic antituberculosis drugs by the molecular design method.Results and discussion. The results of the comparative analysis of technological properties of the biomayrin substance and the prepared capsular masses with the addition of various antifriction agents are shown in the article. The introduction of antifriction agents greatly improved the technological properties of the substance. As a result, the angle of the natural slope decreased from 42.7° to 31–39°, and the fl owability increased to 2.6–3.6 g/s.Conclusion. Thus, the infl uence of various antifriction agents on the technological properties of the substance of the anti-tuberculosis drug “Biomayrin” was investigated, which allowed to work out the optimal composition of the drug product.

In their structure pyrimidin-4-one derivatives are similar to the endogenous nitrogen bases. This makes it possible to predict a wide range of pharmacological activities characteristic for them. The compounds of this series exhibit neurotropic, immunotropic, actoprotective, hypotensive, antihypoxic, anti-infl ammatory and antioxidant activity. Within this framework, the search for and creation of highly effective and safe anti-infl ammatory drugs in the series of N-arylpyrimidin-4(1H)-one is of great current interest.The aim of the work is to carry out predictive studies and targeted synthesis of N-substituted derivatives of pyrimidine-4(1H)-one with anti-infl ammatory activity, as well as toconfi rm the validity of their molecular construction by the results of pharmacological tests.Materials and methods. The research was carried out using the logical-structural approach and information technologies. The computer analysis of biological activity was carried out by the PASS program. Synthesis of the target compounds was carried out using a modifi ed procedure. The structure of the synthesized compounds was confi rmed by 1H NMR, IR and UV spectroscopy. The investigation of the anti-infl ammatory effect of the synthesized compounds was carried out on the model of acute aseptic infl ammation. The synthesized substances were injected intraperitoneally, the magnitude of the edema was the criterion for evaluating the anti-infl ammatory activity.Results and discussion. In the course of the research on the basis of the logico-structural approach, hydroxyphenyl and alkyl derivatives of pyrimidin-4(1H)-one with anti-infl ammatory properties were validated. A preliminary analysis of the pharmacological properties of the predicted structures was carried out using the PASS program and the most promising compounds were selected. To synthesize the tolyl and hydroxyphenyl derivatives of pyrimidin-4(1H)-one, a modifi ed procedure was used. Its essence consists in the use of catalytic amounts of dimethylsulfoxide in order to increase the nucleophilicity of the amine component of the reaction. In order to confi rm the reliability and expediency of the molecular construction, the antiexudative activity of the target compounds was studied.Conclusion. The results of pharmacological studies indicate the prospect of searching for and creating new biologically active compounds having anti-infl ammatory activity among the tolyl and hydroxyphenyl derivatives of pyrimidin-4(1H)-one.

Nowadays studying plant objects in the framework of environmental monitoring to improve the quality of herbal remedies is a very important area of research.The aim of the work is to determine the elemental composition and assessment of environmental cleanliness of rosemary shoots (Rosmarinus offi cinalis L.), introduced in Botanical garden of Pyatigorsk medical-pharmaceutical Institute (PMPI), Pyatigorsk (Russia).Materials and methods. An experimental study was performed at the Central research laboratories spectral analysis (“Kavkazgeolsyemka”) on diffraction spectrograph DFS-8-1 by evaporation from a crater of the carbon electrode. Photometric measurement of spectrograms was performed using the Atlas of spectral lines and spectra of standards with an accuracy of not more than 2% in terms of ash.Results and discussion. For the fi rst time there were 25 elements identifi ed in rosemary shoots introduced in the North Caucasus. The prevailing macro elements were K, Ca, Mg, Na, P and the trace elements were Al, Si and Fe. The toxic elements As, Cd, Hg, Bi, Sb were not detected in the rosemary shoots. Rosemary does not accumulate heavy metals or they are present in trace amounts.Conclusion. The absence of heavy metals or their low content in rosemary shoots can be explained prosperous environmental conditions of Pyatigorsk Botanical garden. The use of rosemary shoots as a source of natural compounds of primary and secondary synthesis and minerals, are involved in the regulation of life processes. This underlines the therapeutic importance of the raw materials and the possibility of creating drugs of combined action on the basis of rosemary for the treatment and prevention of pathologies associated with disorders of mineral metabolism.