Аналіз критеріїв транспортної логістики пасажирських перевезень

В тезах проаналізовано основні чинники, які характеризують особливості транспортної логістики міських пасажирських перевезеньIn abstracts of the main factors that characterize the features of logistics urban passenger transportatio

HPLC METHOD DEVELOPMENT FOR THE ANALYSIS OF BISOPROLOL IN COMBINED DOSAGE FORM CONTAINING BISOPROLOL AND ENALAPRIL AND IN VITRO DISSOLUTION STUDIED

Objective: A simple, rapid and reproducible HPLC method was developed for the determination of bisoprolol in experimental combined dosage forms containing bisoprolol and enalapril and for drug dissolution studies. Methods: A C18 column (Hi Qsil C18, 5 μm, 4.6х250 mm) and a mobile phase methanol: phosphate buffer solution (65:35, v/v) mixture were used for separation and quantification. Analyses were run at a flow rate of 1.0 ml/min and at ambient temperature. The injection volume was 300 μL and the ultraviolet detector was set at 225 nm. The method was validated as per ICH guidelines. Results: Under these conditions, bisoprolol was eluted at 4.75 min. Total run time was shorter than 6 min. A linear relationship between the concentration and the area of ​​chromatographic peaks of bisoprolol in the range of 0.625 mg/ml-5.000 mg/ml (3.750 mg/ml at pH 1.2) has been established. In the medium with pH 1.2 release of bisoprolol from tablets in 5 min is 38.42%, and after 15 min-85.51%, in medium with pH 4.5 the release of bisoprolol from tablets in 5 min makes 59.78%, and after 15 min-103.71%; in a medium with pH 6.8, the release of bisoprolol from tablets in 5 min is 61.29%, and after 15 min-85.90%. Conclusion: The developed method was applied successfully for quality control assay of bisoprolol in experimental tablets and in vitro dissolution studies

Cardioprotective Activity of Some 2-Arylimino-1,3-Thiazole Derivatives

The article presents the synthesis of 2-arylimino-4-methyl-2,3-dihydro-1,3-thiazoles via Hantzsch reaction of thioureas and 3-chloropentane-2,4-dione or ethyl 2-chloro-3-oxobutanoate. The structure of synthesized compounds was confirmed by LCMS, 1H, and 13C NMR spectra. Cardioprotective activity of synthesized thiazole derivatives were studied in vitro on the isolated rings of the thoracic aorta of laboratory rats. Based on pharmacological studies, the tested compounds possessed a moderate to high cardioprotective effect. A prospective 1-[2-(4-methoxyphenylimino)-4-methyl-3-(4-methylpiperazine-1-yl)-2,3-dihydro-1,3-thiazole-5-yl] ethan-1-one hydrochloride 4c was identified. The mentioned compound has delayed the development of constrictor responses of isolated rings of the thoracic rat aorta and exceeds the activity of L-carnitine by 18.2% and meldonium by 12.9%. The compound 4c may be proposed as a potential cardioprotective agent for in-depth pharmacological studies

QSAR-analysis of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one’s derivatives as potential antioxidants

Aim. The aim of study was to determine of the parameters of the molecular structure of new 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one derivatives and QSAR-analysis. The latter can be considered as the theoretical basis for de novo design of new potential antioxidants. Materials and methods. 14 new derivatives of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl] propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one were involved in the study and their antioxidant activities were evaluated. Hyper-Chem 7.59 and BuildQSAR software were used for calculation of molecular descriptors and building the QSAR-models. Results. The calculation of number of molecular descriptors (electronic, steric, geometric, energy) was carried out for the tested compounds: 14 derivatives of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl] propyl) -2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one. For QSAR analysis, the compounds studied were divided into a training and test sample. The correlations between the antioxidant activity level and abovementioned molecular descriptors were shown in multivariate linear QSAR-model: Activity = ∑хіаі + bі, where xi – molecular descriptor. Based on the analysis of the obtained QSAR-models, it was found that antioxidant activity increases with decreasing of the area, molecular volume, lipophilicity, polarisation and increasing the magnitude of the dipole moment. The increase in the energy of the bonds, the energy of inter-nuclear interactions, the energy of the lower vacant molecular orbit and the reduction of the energy of hydration and energy of the higher vacant molecular orbitals also results in an increase in the antioxidant activity. The greatest effect of effective charges on atoms on the antioxidant activity was detected: the increase in the charge value on the morpholine cycle Oxygen and the decrease in the charge size on the Sulphur atom of the thiazole ring and the Oxygen atom of the acetyl group. QSAR models with better statistics were selected. QSAR models obtained are characterised by high predictive ability, determined both by internal and external validation and can be used for virtual screening of the antioxidant activity of substances of this class of compounds. Conclusions. 1). The study of the structure–activity relationships for 1-[2-(R-phenylimino)-4-methyl-3-(3- [morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one derivatives were carried out. 2). QSAR analysis revealed the following: polarisation, dipole moment, lipophilicity, energy parameters as well as the size of the molecule and its branching possessed the most significant effect on antioxidant activity; the antioxidant activities of the compounds were increased with the increase in their hydrophilic and reductive properties; the molecules with small volume and surface area showed the higher level of antioxidant activity. 3). Obtained QSAR models are proposed for antioxidant activity prediction within the above-mentioned row of compounds and can be considered as a theoretical basis for de novo design of new potential antioxidants

HPLC method for simultaneous determination of impurities and degradation products in Cardiazol

Aim. The aim of study was to develop a simple and accurate procedure that could be applied for the determination of impurities and degradation products in cardiazol. Materials and methods. Separation in samples was carried out with Acquity H-class UPLC system (Waters, Milford, USA) equipped with Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm) (Waters, Milford, USA). Xevo TQD triple quadrupole mass spectrometer detector (Waters Millford, USA) was used to obtain MS/MS data. Mobile phase A: 0.1% solution of trifluoroacetic acid R in water R; Mobile phase B: acetonitrile R. Samples were chromatographed in gradient mode (Table 1). Flow rate of the mobile phase: 1 ml / min. Column temperature: 30 °С. Detection: at 240 nm wavelength. Injection volume: 10 μl. Results. The retention time of the main substance is about 18.5 minutes. The order of the peak, the retention times and relative retention times: impurity B (12.04, 0.65); impurity А (18.5; 0.98); Cardiazol (18.87; 1.00). The LOD and LOQ values obtained were in the range of 30 ng/mL to 100 ng/mL and 80 ng/mL to 310 ng/mL respectively (with respect to sample concentration of 2 mg/ ml). Linearity was established in the range of LOQ level to 0.2% having regression coefficients in the range of 0.9996 to 0.9999. The change in the temperature of the column affects the degree of separation of cardiazol and the impurity A, and thus, with a decrease of 5 ° C, the degree of separation is (1.06), while with increasing this index (3.43). When changing the flow rate of the mobile phase, the degree of separation changes in the following order, with a decrease to 0.9 ml / min separation (1.90), with an increase in speed to 1.1 ml / min (2.45). When the number of mobile phase B decreases by 5%, the degree of separation varies by (2.65), with an increase of 5% (1.82). In comparison with the chromatogram of the tested solution, the substance is not resistant to the action of peroxide, alkaline and acid decomposition

Кластерна політика інноваційного розвитку національної економіки: інтеграційний та інфраструктурний аспекти

В монографії розглянуто теоретико-концептуальні, методологічні та практичні аспекти іннова- ційного розвитку національних економік на основі кластерного підходу. На підставі узагальнення світового та європейського досвіду доводиться стратегічна роль кластерних структур для економіч- ного зростання та забезпечення конкурентоспроможності національних економік на глобальному рівні. Розглянуто особливості формування кластерної політики країн ЄС в умовах розвитку мереже- вої та інтелектуальної економіки, визначені проблеми та перспективи розвитку кластерів в Україні та запропоновані певні критеріальні вимоги до формування українських кластерних об’єднань згідно з кращими практиками ЄС. Запропонована концептуально-методологічна модель оціню- вання синергетичних ефектів кластерних структур. Проаналізовано інноваційні та інституаційні передумови формування та розвитку кластерних структур в Україні з урахуванням економічної політики кластеризації Європейського Союзу. На основі сегментного аналізу галузевих кластерних ініціатив в Україні запропонована кластерна модель структурної трансформації та конкурентного розвитку стратегічно важливих для економіки країни галузей. На основі дослідження стану та перспектив розвитку регіональних кластерів, розроблено рекомендації щодо використання клас- терного підходу при формуванні регіональної політики, зокрема, в українському Причорномор’ї та в Одеській області. Розроблено комплекс заходів щодо формування та розвитку транспортно-ло- гістичних кластерів, які належать до кластерів інфраструктурного типу та мають першочергове значення для розвитку національної економіки. Надані рекомендації щодо побудови ефективної системи доставки на основі кластеризації міської території. Запропонована еколого-інноваційна модель кластерної взаємодії транспорту та промисловості в умовах інформаційної економіки. Призначається для науковців, викладачів, студентів економічних спеціальностей, підприємців, представників органів державної та регіональної влади та інших зацікавлених осіб.The monograph deals with theoretical and conceptual, methodological and practical aspects of innovative development of national economies based on the cluster approach. Based on the generalisation of the world and European experience, the strategic role of cluster structures for economic growth and ensuring the competitiveness of national economies at the global level is proven. The features of cluster policy formation of the EU countries in the conditions of the network and intellectual economy develop- ment are considered. The problems and prospects of clusters development in Ukraine are defined. Specific criteria for the formation of Ukrainian cluster associations accord- ing to the best EU practices are proposed. A conceptual and methodological model for evaluating the synergetic effects of cluster structures is proposed. The innovative and institutional prerequisites for the formation and development of cluster structures in Ukraine, taking into account the economic policy of the European Union’s clustering, are analysed. Based on the segmental analysis of industry clusters initiatives in Ukraine, a cluster model of structural transformation and competitive development of strategi- cally important industries for the country’s economy is proposed. Based on the study of state and prospects of regional clusters’ development, developed recommendations for the use of the cluster approach in the formation of regional policy, in particular, in the Ukrainian black sea region and the Odesa region. A set of measures developed for the formation and development of transport and logistics clusters, which are related to infrastructure-type clusters and are of primary importance for the development of the national economy. Recommendations for building an effective delivery system based on clustering of the city territory are given. An ecological and innovative model of clus- ter interaction between transport and industry in the information economy is proposed. This monograph is for scientists, teachers, students of economic specialities, entre- preneurs, state and regional authorities’ representatives and other interested persons