Abstract
The aim - to establish the main pharmacokinetic parameters of 11-deoxyimisoprostol after intragastric administration. Materials and methods. The experiments were performed on 410 white outbred rats - females weighing 180-220 g. 11-deoxymysoprostol was administered to rats intragastrally at a dose of 2.0 mg/kg. Blood and organs were taken for examination at 6, 12, 15, 30 minutes and hourly for 12 hours after administration. After these intervals, the concentration of the drug in the blood and tissue homogenates of laboratory animals was determined, and in the urine - every hour during the day. Chromatographic separation was carried out using a liquid chromatograph (Shimadzu, Japan LC-20 PROMI- NENCE with a diode - array detector SPD-20A).Results. 11-deoxyimisoprostol is rapidly absorbed from the gastrointestinal tract. The maximum (6.625 μg/ml) of the compound in the blood plasma is reached 15 minutes after intragastric administration. When this occurs, a simultaneous in - crease in the concentration of the metabolite - 11-deoxyimisoprostolic acid. The maximum concentration (23.547 µg/ml) of the metabolite in the blood plasma is reached 30 minutes after the administration of 11-deoxyimisoprostol. 11-deoxyimisoprostol is intensively distributed throughout the organs and tissues, while the compound has the highest affinity for myometrium and liver. The smallest quantities of the test substance were found in the lungs, the brain, and the omentum. The active metabolite of 11-deoxyimisoprostol is intensively distributed in organs and tissues, while in the greatest amounts it was detected in the myometrium and the liver and kidneys. The smallest quantities of the test substance were found in the lungs, the brain, and the omentum. In the urine, 11-deoxyimisoprostolic acid is determined during the first days of the study, with a maximum clearance of 6-8 hours after administration.Conclusion. 11-deoxyimisoprostol has a short half - life after intragastric administration (T1/2=0,550 h), which indicates the absence of cumulative properties. The nature of the pharmacokinetic curve is monoexponential.
Highlights
ВВЕдЕНиЕ Важным разделом создания новых лекарственных средств является изучение экспериментальной фармакокинетики
Знание фармакокинетических свойств позволяет обосновать выбор путей и методов их введения, выявить ткани, в которые они проникают наиболее интенсивно и/или в которых удерживаются наиболее длительно, установить основные пути элиминации фармакологического средства
Анализируя полученные данные, можно сделать заключение о том, что 11-ДМП имеет небольшой период полувыведения (T =0,550 ч) при внутрижелудочном введении, что свидетельствует об отсутствии кумулятивных свойств
Summary
ВВЕдЕНиЕ Важным разделом создания новых лекарственных средств является изучение экспериментальной фармакокинетики. Исследуемое вещество 11-дезоксимизопростол (11-ДМП) – этиловый эфир (±)-11,15-дидезоксирис. Цель исследования – установить основные фармакокинетические параметры 11-ДМП при внутрижелудочном введении. Взятие крови и органов для исследования производилось через 6, 12, 15, 30 мин и ежечасно в течение 12 ч после введения, мочу лабораторных животных собирали каждый час в течение суток.
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