INFLUENCE OF A PULSE MAGNETIC FIELD OF HIGH VOLTAGE ON THE INDICATORS OF ANTI-AGGREGATION ACTIVITY OF THE CHEMICAL SUBSTANCE AND THE PREPARED PHARMACY PREPARATION PENTOXYPLIN

It was found that the pharmaceutical preparation of pentoxifylline, treated with a pulsed magnetic field (PMF), changes the antiaggregatory properties.The pharmaceutical preparation contains the pure substance of pentoxifylline and a number of excipients. To understand the mechanism of changes in the antiaggregatory activity of a pharmaceutical preparation, the goal was to further investigate the effect of PMF parameters on its chemically pure substance.PMF processing was carried out on the «MIU Bio» installation with a single exposure at a field strength in the range (0.48–1.17) 106 A/m at discharge circuit frequencies (8–50) 103 Hz.Experiments have shown that the effect of PMF on the pure substance of pentoxifylline did not cause significant changes in its antiaggregatory activity. This result made it possible to get one step closer to understanding the mechanism of the effect of PMF on a given drug. Apparently, the reason for the change in the biological effectiveness of the pharmaceutical pentoxifylline treated with PMF lies in the effect of impurities, which will be the focus of further research.

CHANGE IN THE ACTIVITY OF PENTOXYPLIN UNDER THE ACTION OF A PULSE MAGNETIC FIELD DEPENDING ON THE DRUG COMPOSITION

According to the results of the study, it was found that irradiation of the tabletted preparation of pentoxifylline leads to an increase in its antiaggregatory activity. The aim of this work is to study the effect of a pulsed magnetic field of high intensity on the antiaggregatory activity of the pure substance of petoxifylline. When exposed to a pulsed magnetic field on the pure substance of pentoxifylline (without the presence of excipients), changes in the antiaggregatory activity of the drug were not detected. Irradiation with a pulsed magnetic field was carried out on an MIU-15 setup at various magnetic field strengths with single-turn and multi-turn inductors with the number of pulses n = 1. The authors put forward a hypothesis that excipients in a tabletted medicinal product affect the change in biological activity after exposure to the drug by a pulsed magnetic field of high intensity. The study of the pure substance of pentoxifylline for antiaggregatory activity was carried out on an AT-02 platelet aggregation analyzer. Control samples of the medicinal product were not exposed to the magnetic field. It is assumed that the presence of excipients in the tablet form of pentoxifylline after exposure to a pulsed magnetic field can cause a change in the conformation of the drug molecule. In addition, a transition from one conformation to another is possible due to abrupt changes in properties, i.e. when exposed to a high-intensity magnetic field. An antiplatelet agent with excipients, being in a magnetic field, goes into a more active state, after which it retains it for some time, in which an increase in pharmacological activity is manifested.

Antiaggregatory activity of new 1-ethylxanthine cyclohexylammonium salt in vitro

Aim. To study the biochemical effect on hemostasis of a new cyclohexilammonium salt of 2-[1-ethyl-3-methyl-7(dioxotiethanyl-3)xantinyl-8-thio]acetic acid in vitro. Methods. Thromboelastography was performed using the citrate blood samples of healthy male donors. Global hemostatic effect, fibrinogen and platelet function, fibrinolysis and clot strength, and stability were analyzed at thromboelastography. The impact of firstly synthesized xantine derivative and pentoxifylline on the functional activity of platelets in vitro was studied using a laser analyzer of platelet aggregation. Adenosine diphosphate, collagen, epinephrine and ristocetin induced clotting were registered. General clotting characteristics, maximal aggregation values, maximal aggregation speed, mean platelet aggregate size, activity of platelet-derived factor 3, level of platelet-derived factor 4 were measured. Release of platelet-derived factors 3 and 4 at platelet aggregation were assessed after adenosinediphosphate-induced aggregation and centrifugation. Results. Cyclohexylammonium salt of 2-[1-ethyl-3-methyl-7-(dioxotiethanyl-3)xantinyl-8-thio]acetic acid in vitro showed antiaggregatory activity that exceeds such of pentoxifylline. It has been revealed that the second platelet aggregation wave, that is induced by small dose of adenosinediphosphate, is absent in the presence of the new cyclohexylammonium salt, lag-period in collagen-induced platelet aggregation elongates, and availability and release of platelet-derived factors 3 and 4 decreases. Conclusion. The research findings show potentially high antiaggregatory activity of 2-[1-ethyl-3-methyl-7-(dioxotiethanyl-3)xantinyl-8-thio]acetic acid cyclohexylammonium salt as an inhibitor of platelet release reaction.

Effect of Heating on Onion (Allium cepa L.) Antiplatelet Activity and Pungency Sensory Perception

Onion, in its raw form, is recognized as an antiplatelet agent that may contribute to the prevention of cardiovascular disease. In raw onions, the content of pyruvate, is significantly correlated with antiplatelet activity (AA) and the sensory perception of pungency. However, onion is generally cooked before consumption. Herein, we examine the effect of heating — using different boiling intensities — on the in vitro antiaggregatory activity (IVAA), the pyruvate concentration and the flavor (pungency) of crushed-onion samples. In general, heating is detrimental for onion AA. Boiling for 3 min has no significant effect on platelet aggregation, as compared to raw onion. Heating for 46 min completely suppresses IVAA, whereas samples boiled for > 20 min have pro-aggregatory effects. Significant differences in AA are found between the blood donors. Pyruvate content is not reduced after 30 min boiling. Pungency ratings decrease with the intensity of the heat treatment. Strong significant positive correlations are found between IVAA and pungency, but not between pyruvate and the former two variables. Our results suggest that: (i) in order to obtain the maximum health benefits onions should be eaten raw or moderately cooked, (ii) extensive heating may result in pro-aggregatory effects, (iii) pyruvate is not a good indicator of AA in cooked onions, (iv) the decrease in IVAA and pungency during onion cooking may be due to degradation of sulfur compounds (e.g. thiosulfinates) which are, likely, less tolerant than pyruvate to the high temperatures.