单次吸入给药后 C57BL/6Y 小鼠血清和肺组织中 Leutragin 肽类药物的药代动力学比较研究

N. S. Ogneva, M. S. Nesterov, D. Khvostov, Y. Fokin, V. Karkischenko
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摘要

本文介绍了一种新型吸入式抗炎六肽药物(注册名为 "Leutragin")的药代动力学研究。病毒性肺炎的严重病程与细胞因子炎症级联反应(即细胞因子风暴)直接相关。这项研究涉及对 C57BL/6Y 系小鼠单次吸入剂量为 150 毫克/千克的 Leutragin 后的肺组织和血清进行调查。在血清和肺中达到最大浓度(Tmax)所需的时间分别为 30 分钟和 10 分钟。肺中的最大浓度(Cmax)为 358.5 纳克/克,比血液中的最大浓度(53.84 纳克/克)高出六倍多。研究发现,吸入给药后,Leutragin 会迅速从体内排出,血清和肺中的药物半衰期(t1/2el)为 25.8 至 38.9 分钟。
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Comparative Pharmacokinetics Study of the Leutragin Peptide Drug in Blood Serum and Lung Tissue in C57BL/6Y Mice after Single Inhalation Administration
This paper presents a study into the pharmacokinetics of a new inhaled anti-inflammatory hexapeptide, registered as “Leutragin”. This drug is used as a new treatment approach for viral pneumonias, whose severe course is directly related to the cytokine inflammatory cascade referred to as a cytokine storm. The study involved investigation of lung tissue and serum after a single inhalation administration of Leutragin to mice of the C57BL/6Y line at a dose of 150 mg/kg. The time required to reach the maximum concentration (Tmax) of Leutragin in serum and lung was 30 min and 10 min, respectively. The maximum concentration (Cmax) in lung was 358.5 ng/g, which exceeded the concentration maximum for blood (53.84 ng/g) by over six times. It was found that, after inhalation administration, Leutragin is rather rapidly eliminated from the body with the half-life of the drug (t1/2el) from blood serum and lungs ranging from 25.8 to 38.9 min.
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