Vol 24, No 9 (2021)

Relevance. Individual natural compounds are promising basic structures for the production of semi-synthetic drugs with predictable activities. Carotenoids are characterized by the lability of the main pharmacophore, lipophilicity, and the presence of geometric isomers. Biocatalysts make it possible to solve synthesis problems associated with the physicochemical and structural features of natural compounds, in particular, carotenoids. The aim of the study is to demonstrate the possibility of using biocatalysis in pharmaceutical synthesis by the example of obtaining lutein esters. Material and methods. The synthesis of esters was carried out in a non-aqueous medium at a temperature of 37 °C in the presence of the catalyst Novozyme 435. The structure of the esters was confirmed by 1H NMR and mass spectrometry. Results. Six new esters of lutein and benzoic, 4-methylbenzoic, phenylglycolic, 2-hydroxybenzoic, nicotinic acids and ibuprofen were synthesized, and their structure was confirmed. Conclusion. Using the example of obtaining new lutein compounds, the prospect of using biocatalysis in pharmaceutical synthesis and the fundamental possibility of obtaining esters of natural individual compounds and medicinal substances are shown.

In order to standardize the raw materials of garden strawberries, we have developed a method for quantifying the amount of flavonoids in terms of rutin. The article presents the results of validation of the method of quantitative determination of the amount of flavonoids in terms of rutin in strawberry leaves to prove the guarantee of accuracy and reliability of the results of the analysis of raw materials and its subsequent application in the quality assurance system of research. Purpose. Validation of the method of quantitative determination of the amount of flavonoids in terms of rutin in strawberry leaves using the method of differential spectrophotometry. Material and methods. Validation of the method was performed on a combined sample of strawberry leaves. Validation parameters were determined using SF-2000 and SHIMADZU UV-1800 spectrophotometers. Results. Linearity was determined at five levels of concentration. The correlation coefficient was 0.9997, which indicates a linear relationship between the values of the optical density and the content of the sum of flavonoids in the extracts. The repeatability of the technique was determined in tenfold repetition under identical conditions within a short period of time. The intra-laboratory reproducibility of the technique was determined on three samples of three-fold repetition. Interlaboratory reproducibility of the technique was performed on three samples in three-fold repetition in two laboratories. The results of the determination confirm the precision of the method in the conditions of intra-laboratory and inter-laboratory reproducibility, since the relative standard deviation did not exceed 15%. The correctness of the method was established by adding the required amount of standard routine to the extraction. The results of the analysis showed that the analysis error is within the error of a single definition and does not exceed 2.24%. As a result of the conducted studies, the validation characteristics of the method for quantifying the amount of flavonoids in terms of rutin in the leaves of strawberry garden were established: linearity, precision (repeatability, reproducibility) and correctness. Conclusions. The developed method of spectrophotometric determination of the amount of flavonoids in terms of rutin in strawberry leaves is valid, does not require expensive reagents, is accurate, reproducible and accessible, which makes it possible to use it for a reliable assessment of the quality of raw materials.

UV spectroscopy is used in pharmaceutical analysis to determine the quality of pharmaceutical substances and preparations as a versatile and sensitive method that allows to analyze small quantities of drugs, including in a single dose, as well as perform the analysis automatically and in a short time. Raman spectroscopy which is not inferior in its capabilities to UV spectroscopy is characterized as an express and non-destructive method. Purpose of the study. To assess the possibility of using total spectra for the development of an express and economical method for the determination of the quality of industrial drugs of complex composition using Raman spectra and integral intensity. Material and methods. The objects of research were the substances of paracetamol Hebei Jiheng batch № 1606107, Daru Phash batch № 309547, Anqiu Luan batch № 1730144, Zhejiang Kanglite batch № 7602925; Solpadein fast soluble tablets, Solpadein fast film-coated tablets, Migrenol, Migrenium; model mixtures that reproduce the composition of the tablets under study and contain 80120% of active substances from the nominal amount. Certified and calibrated equipment was used, the validation assessment was carried out in accordance with the recommendations of Russian Pharmacopoeia (14 edition). Results. By the example of paracetamol substances from different manufacturers, the stability and reproducibility of the Raman spectra was shown, the absence of the influence of the analysis duration on the position of the characteristic signals of the Raman spectrum was established. On the model two-component mixtures and some commercially available tablets containing paracetamol the possibility of assessing the quality by means of the integral intensity of the total UV absorption spectrum was studied. Conclusions. The validation assessment showed that the Raman spectra and the integrated intensity of the total UV spectra are stable and reproducible indicators that can be used as an additional characteristic for an alternative rapid assessment of the quality of pharmaceutical substances and two-component preparations. They may be recommended as methods for the implementation of stepwise control of pharmaceutical production.

According to the WHO, more than 80% of people suffer from eye diseases. In the modern world, combined diseases of glaucoma and myopia are most often found. In this regard, the creation of combined drugs for the treatment of this disease is an urgent task. The aim of the work is to identify the most effective components of the ocular dosage form for the treatment and prevention of glaucoma complicated by myopia. The analysis of the pharmaceutical market of the Russian Federation of drugs of antiglaucoma, as well as anti-bacterial action is carried out. It is shown that betaxolol hydrochloride occupies a leading position in the market (39%). It is able to reduce intraocular pressure by reducing the production of intraocular fluid, while there is some improvement in the outflow of watery moisture. Taurine occupies the leading position among the antimiopathic drugs (35%). Its therapeutic effect is based on metabolic mechanisms, namely, participation in the normalization of the functions of cell membranes, in maintaining the electrolyte composition of the cytoplasm in relation to potassium, calcium, activation of energy and metabolic processes.