PHARMACOKINETICS OF THE NEW CEREBROPETECTOR FERRUM BIS(CITRATO)GERMANATE AT THE STAGE OF ITS DISTRIBUTION TO THE ORGANS IN CLOSED HEAD INJURY

V. Lukianchuk, T. Bukhtiarova, I. Seifullina, E. Polishchuk, O. E. Martsinko, H. A. Topolnytska
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引用次数: 2

Abstract

Background. Previous studies showed that new coordinate compound Cerebrogerm (ferrum bis(citrato)germanate) is a promising cerebroprotector. Objective of the study is a comparative analysis of the central stage of the pharmacokinetics of Cerebrogerm as well as its distribution in vital organs in cases of closed head injury. Methods. On the experimental original model of closed brain injury in rats the parameters of the central stage of Cerebrogerm pharmacokinetics: the distribution in brain, liver, kidneys, were studied. Results. It is established that, in cases of closed head injury Cerebrogerm reaches maximum concentration first in the brain (in 3.75 h), then in the kidneys (in 3.92 h), and finally in the liver (in 4.17 h). In this case, the magnitude of the Cmax of the coordinating compound of germanium that is being investigated in different biosubstrates of the rats with closed head injury may be presented in descending order as follows: brain (7.95 mg/L) > liver (6.22 mg/L) > kidneys (1.79 mg/L). Conclusions. The compound Cerebrogerm studied easily gets through the blood-brain barrier and meets the present requirements for cerebroprotectors and antihypoxants. The attained results allow noting that in the early post-traumatic period of closed head injury, the blood circulation in the kidneys does not change and cannot modify the absorption-elimination processes of xenobiotics. It has been also established that Cerebrogerm is distributed faster in the examined organs in cases of closed head injury. The highest concentration of the drug is present in the brain and the smallest one – in the kidneys.
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新型脑保护剂二(柠檬酸)锗酸铁在闭合性颅脑损伤器官分布阶段的药代动力学
背景。研究表明,新的配位化合物脑胚芽铁(柠檬酸铁)是一种很有前途的脑保护剂。本研究的目的是比较分析闭合性颅脑损伤患者脑胚药代动力学的中心阶段及其在重要脏器中的分布。方法。在闭合性脑损伤大鼠实验原始模型上,研究了大鼠脑、肝、肾中央期药代动力学参数的分布。结果。证实,在封闭的头部受伤的情况下Cerebrogerm达到最大浓度首先在大脑(3.75小时),然后在肾脏(3.92小时),最后在肝脏(4.17小时)。在这种情况下,大小的Cmax协调的锗化合物正在调查在不同biosubstrates的老鼠在封闭的头部受伤可能按降序显示如下:大脑(7.95 mg / L) >肝脏(6.22 mg / L) >肾脏(1.79 mg / L)。结论。所研究的复方脑芽易通过血脑屏障,满足目前对脑保护剂和抗氧剂的要求。所获得的结果允许注意到,在闭合性头部损伤的早期创伤后时期,肾脏的血液循环不会改变,也不能改变异种抗生素的吸收-消除过程。在闭合性颅脑损伤病例中,脑芽在被检查器官中的分布速度更快。这种药物在大脑中浓度最高,在肾脏中浓度最低。
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