在实验中对亲水性基质上的嘧啶类药物软制剂的渗透和抗炎活性进行比较评估

A. G. Izmailov, S. V. Dobrokvashin, S. G. Izmailov, E. Lukoyanychev, Andrey Yu. Zharinov
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引用次数: 0

摘要

背景:尽管人们一直在寻找用于局部预防手术感染的新药物,但术后软组织伤口的化脓性炎症并发症问题至今仍然存在。目的:通过实验研究所开发的含喜树碱软膏成分左旋氧氟沙星与知名软膏二氧甲基四氢嘧啶+氯霉素(左旋美可)的渗透活性和抗炎特性。材料与方法:在 60 只近亲繁殖的雄性 Wistar 大鼠身上对药膏的抗炎特性进行了活体研究,这些大鼠分为三组,每组 20 只。第一组为对照组。第二组使用左旋美可软膏,第三组使用左旋氧可软膏。在体外实验中,与已知药物相比,对实验性软膏成分左旋氧氟沙星的渗透活性进行了评估。为了评估软膏的抗炎活性,使用了角叉菜胶诱导的大鼠爪水肿模型。采用 Mann-Whitney U 检验来分析各组动物出现研究结果频率的差异。结果:渗透活性显示,浸泡在药膏中的湿巾吸收了以下数量的对比剂(Me [Q1; Q3]):左旋美可 - 28.2 (26.4; 31.3) ml;左旋氧可 - 41.8 (39.5; 43.4) ml (p=0.001)。在注射角叉菜胶 3 小时和 5 小时后,软膏形式的抗炎活性表现为抑制大鼠爪子的肿胀。在使用左旋咪唑软膏时,从 3 小时开始,随着角叉菜胶的引入,液体流出量为 1.8±0.19 毫升。在使用左旋咪唑软膏的情况下,从 3 个小时开始使用卡拉胶时,流出的液体量为 1.57±0.16 毫升(p=0.013)。结论:体外实验表明,左旋西可软膏具有更长的渗透活性;体内实验数据表明,与左旋美可软膏相比,使用开发的左旋西可软膏在最初的 2-3 小时内通过减少移位液体量对软组织炎症过程有积极影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comparative assessment of the osmotic and anti-inflammatory activity of soft dosage forms of pyrimidine drugs on hydrophilic bases in an experiment
BACKGROUND: Despite the constant search for new medications for local prevention of surgical infection, the problem of purulent-inflammatory complications from postoperative soft tissue wounds remains relevant to this day. AIM: To experimentally study the osmotic activity and anti-inflammatory properties of the developed xymedone-containing ointment composition levoxycol in comparison with the well-known ointment dioxomethyltetrahydropyrimidine + chloramphenicol (levomekol). MATERIAL AND METHODS: The anti-inflammatory properties of the ointments were studied in vivo on 60 outbred male Wistar rats, which were divided into three groups, 20 animals each. The first group served as control. In the second group of animals, levomekol ointment was used, in the third group — levoxycol. An assessment of the osmotic activity of the experimental ointment composition levoxycol in comparison with a known drug was carried out in an in vitro experiment. To evaluate the anti-inflammatory activity of ointments, a model of carrageenan-induced edema of rat paws was used. To analyze differences in the frequency of the studied outcomes in groups of animals, the Mann–Whitney U test was used. RESULTS: Osmotic activity showed that wipes soaked in ointment forms absorbed the following amount of contrast (Me [Q1; Q3]): levomekol — 28.2 (26.4; 31.3) ml; levoxycol — 41.8 (39.5; 43.4) ml (p=0.001). The anti-inflammatory activity of the ointment forms manifested itself in the form of suppression of swelling of the rats' paws at 3 and 5 hours after the injection of carrageenan. When using the ointment form of levomekol, the volume of displaced liquid with the introduction of carrageenan, starting from 3 hours, was 1.8±0.19 ml. When using the ointment form of levoxicol, the amount of displaced liquid when carrageenan was administered, starting from 3 hours, was 1.57±0.16 ml (p=0.013). CONCLUSION: In vitro experiments have shown that the ointment form of levoxicol has a longer osmotic activity; experimental data in vivo indicated that the use of the developed ointment form of levoxicol, in contrast to the ointment form of levomekol, has a positive effect on the course of inflammatory processes in soft tissues in the first 2–3 hours by reducing the volume of displaced fluid.
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