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Evaluation of combined famotidine with quercetin for the treatment of peptic ulcer: in vivo animal study

机译:法莫替丁与槲皮素联合治疗消化性溃疡的评估:体内动物研究

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Abstract: The aim of this work was to prepare a combined drug dosage form of famotidine (FAM) and quercetin (QRT) to augment treatment of gastric ulcer. FAM was prepared as freeze-dried floating alginate beads using ion gelation method and then coated with Eudragit RL100 to sustain FAM release. QRT was prepared as solid dispersion with polyvinyl pyrrolidone K30 to improve its solubility. Photo images and scanning electron microscope images of the prepared beads were carried out to detect floating behavior and to reveal surface and core shape of the prepared beads. Anti-ulcerogenic effect and histopathological examination of gastric tissues were carried out to investigate the effect of the combined drug formulation compared with commercial FAM tablets and FAM beads. Gastric glutathione (GSH), superoxide dismutase, catalase, tissue myeloperoxidase, and lipid peroxidation enzyme activities and levels in rat stomach tissues were also determined. Results revealed that spherical beads were formed with an average diameter of 1.64±0.33 mm. They floated immediately with no lag time before floating, and remained buoyant throughout the test period. Treatment with a combination of FAM beads plus QRT showed the absence of any signs of inflammation or hemorrhage, and significantly prevented the indomethacin-induced decrease in GSH levels (P<0.05) with regain of normal GSH gastric tissue levels. Also, there was a significant difference in the decrease of malondialdehyde level compared to FAM commercial tablets or beads alone (P<0.05). The combined formula significantly improved the myeloperoxidase level compared to both the disease control group and commercial FAM tablet-treated group (P<0.05). Formulation of FAM as floating beads in combination with solid dispersion of QRT improved the anti-ulcer activity compared to commercially available tablets, which reveals a promising application for treatment of peptic ulcer.
机译:摘要:这项工作的目的是制备法莫替丁(FAM)和槲皮素(QRT)的组合药物剂型,以增强对胃溃疡的治疗。使用离子凝胶法将FAM制成冻干的浮游藻酸盐珠,然后用Eudragit RL100包被以维持FAM释放。 QRT与聚乙烯吡咯烷酮K30制备为固体分散体,以提高其溶解度。进行制备的珠子的照片图像和扫描电子显微镜图像以检测漂浮行为并揭示制备的珠子的表面和核心形状。进行了胃组织的抗溃疡作用和组织病理学检查,以研究联合药物制剂与市售FAM片剂和FAM珠相比的作用。还测定了大鼠胃组织中的谷胱甘肽(GSH),超氧化物歧化酶,过氧化氢酶,组织髓过氧化物酶和脂质过氧化酶的活性和水平。结果显示形成球形珠,其平均直径为1.64±0.33mm。它们立即漂浮,漂浮之前没有滞后时间,并且在整个测试期间保持漂浮状态。 FAM珠加QRT联合治疗显示没有任何炎症或出血迹象,并显着阻止了消炎痛诱导的GSH水平下降(P <0.05),并恢复了正常的GSH胃组织水平。而且,与单独使用FAM的商业片剂或微珠相比,丙二醛水平的下降也有显着差异(P <0.05)。与疾病对照组和市售FAM片剂治疗组相比,联合配方明显改善了髓过氧化物酶水平(P <0.05)。与市售片剂相比,将FAM配制为浮珠并结合QRT的固体分散剂可改善抗溃疡活性,这揭示了在治疗消化性溃疡方面的应用前景广阔。

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