大鼠静脉注射墨西多脂质体乳剂和水溶液后药动学参数的比较研究。

IF 0.7 4区 医学 Q4 MEDICINE, RESEARCH & EXPERIMENTAL Bulletin of Experimental Biology and Medicine Pub Date : 2025-01-01 Epub Date: 2025-02-13 DOI:10.1007/s10517-025-06331-z
V S Shindyaikina, A V Siprov, V I Inchina, I A Gololobova, V I Shlyapkina, O A Kulikov
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引用次数: 0

摘要

比较了50 mg/kg剂量的美西多脂质体乳剂和美西多水溶液在大鼠体内静脉注射后的药动学参数。用高效液相色谱法测定给药后30、60、120、240 min、24和48 h血浆和肺、肝、肾、睾丸和卵巢匀浆中墨西多的浓度。与水溶液相比,墨西多尔脂质体迅速从体循环中消失(给药后4小时血浆浓度下降5倍),主要被肝脏和肺部吸收并保留较长时间:24小时后,墨西多尔脂质体在肝脏中的浓度超过其水溶性形式的14.2倍,在肺部的浓度超过63%。在睾丸中,注射后4小时内,墨西多尔脂质体浓度超过其水溶性形式:1小时后4倍,4小时后2倍,而在卵巢组织中,脂质体和水溶性形式的浓度相同。在性腺组织中,墨西多的水溶性形式比其脂质体形式保留的时间更长。
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Comparative Assessment of Pharmacokinetic Parameters of Mexidol after Intravenous Administration of Liposomal Emulsion and Aqueous Solution to Rats.

We compared the pharmacokinetic parameters of liposomal emulsion and aqueous solution of Mexidol after intravenous injection to rats at a dose of 50 mg/kg. The concentrations of Mexidol in blood plasma and homogenates of the lungs, liver, kidneys, testes, and ovaries were measured 30, 60, 120, 240 min, 24 and 48 h after administration by HPLC. The liposomal Mexidol in contrast to its aqueous solution quickly disappeared from systemic circulation (a 5-fold decrease in plasma concentration was noted as soon as 4 h after administration) and was predominantly absorbed and retained for a longer period by the liver and lungs: after 24 h, the concentration of liposomal Mexidol exceeded that of its water-soluble form by 14.2 times in the liver and by 63% in the lungs. In the testes, the concentration of liposomal Mexidol exceeded that of its water-soluble form during the first 4 h postinjection: by 4 times after 1 h and by 2 times after 4 h, whereas in the ovarian tissues, the same concentrations were observed after administration of liposomal and water-soluble forms. In the gonadal tissues, the water-soluble form of Mexidol was retained longer than its liposomal form.

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来源期刊
Bulletin of Experimental Biology and Medicine
Bulletin of Experimental Biology and Medicine 医学-医学:研究与实验
CiteScore
1.50
自引率
14.30%
发文量
265
审稿时长
2 months
期刊介绍: Bulletin of Experimental Biology and Medicine presents original peer reviewed research papers and brief reports on priority new research results in physiology, biochemistry, biophysics, pharmacology, immunology, microbiology, genetics, oncology, etc. Novel trends in science are covered in new sections of the journal - Biogerontology and Human Ecology - that first appeared in 2005. World scientific interest in stem cells prompted inclusion into Bulletin of Experimental Biology and Medicine a quarterly scientific journal Cell Technologies in Biology and Medicine (a new Russian Academy of Medical Sciences publication since 2005). It publishes only original papers from the leading research institutions on molecular biology of stem and progenitor cells, stem cell as the basis of gene therapy, molecular language of cell-to-cell communication, cytokines, chemokines, growth and other factors, pilot projects on clinical use of stem and progenitor cells. The Russian Volume Year is published in English from April.
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