Abstract
The aimof the work was a comparative experimental study of the effect of oral administration of Pentoxifylline microparticles based on PLGA, and “standard” Pentoxifylline, on the ADP-induced platelet aggregation process in rats.Materials and methods.Pentoxifylline substance (100 mg/kg) was used as a reference drug, and PLGA-based Pentoxifylline microparticles with an average dynamic radius of 175.4 nт were used as the object in study. In the experiment, male Wistar rats (m = 300–330 g), the same age group (9 months) were used. They were divided into 3 groups, each of 6 animals. The antiplatelet activity was assessed by determining the degree and rate of platelet aggregation in 1, 3, 5, 8 and 24 hours after a single oral administration of the reference drug and the object under study. Adenosine diphosphate (ADP) at the concentration of 5 μM was used as an aggregation inducer. The aggregation process was recorded using a two-channel laser platelet aggregation analyzer ALAT-2, wavelength of 0.785 μm. by determining the average conventional size of the aggregates.Results.The experiment has proved the following: PLGA-based Pentoxifylline microparticles are more effective at reducing the possibility of platelets to aggregate within 24 hours of the investigation (more than 40%) conventional to the control group value. Besides, it should be noted that according to the effectiveness of the pharmacological action during AD-induced platelet aggregation, the microparticles are commensurate with the standard sample - Pentoxifylline. The action of the microparticle object under study lasts for 24 hours, while the effect of the reference drug is over after 3 hours and then the indicators of the reference group do not differ from those of the control onel.Conclusion.When administered per os, PLGA-based Pentoxifylline microparticles prolong the pharmacological effect significantly – up to 24 hours.
Highlights
Цель – сравнительное экспериментальное изучение влияния перорального введения микрочастиц пентоксифиллина на основе PLGA и «стандартного» пентоксифиллина, на процесс АДФ-индуцированной агрегации тромбоцитов крыс.
Целью исследования явилось изучение влияния перорального введения микрочастиц пентоксифиллина на основе поли-DL-лактид-ко-гликолида на АДФ- индуцированный процесс агрегации в сравнении с пентоксифиллином.
Таблица 1 – Действие микрочастиц пентоксифиллина на основе поли-DL-лактид-ко-гликолида и стандартного образца пентоксифиллина при пероральном введении в дозе 100 мг/кг на процесс АДФ-индуцированной агрегации тромбоцитов
Summary
Цель – сравнительное экспериментальное изучение влияния перорального введения микрочастиц пентоксифиллина на основе PLGA и «стандартного» пентоксифиллина, на процесс АДФ-индуцированной агрегации тромбоцитов крыс. Целью исследования явилось изучение влияния перорального введения микрочастиц пентоксифиллина на основе поли-DL-лактид-ко-гликолида на АДФ- индуцированный процесс агрегации в сравнении с пентоксифиллином. Таблица 1 – Действие микрочастиц пентоксифиллина на основе поли-DL-лактид-ко-гликолида и стандартного образца пентоксифиллина при пероральном введении в дозе 100 мг/кг на процесс АДФ-индуцированной агрегации тромбоцитов После однократного внутрижелудочного введения пентоксифиллина (в дозировке 100 мг/кг), степень АДФ-индуцированной агрегации тромбоцитов в стандартизованной плазме через 1 ч введения составила 23,9±1,9 усл.
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