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

被引:27
作者
Abourehab, Mohammed A. S. [1 ,2 ]
Khaled, Khaled A. [1 ]
Sarhan, Hatem A. A. [1 ]
Ahmed, Osama A. A. [1 ,3 ]
机构
[1] Menia Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Al Minya, Egypt
[2] Umm Al Qura Univ, Fac Pharm, Dept Pharmaceut, Mecca, Saudi Arabia
[3] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Jeddah 21589, Saudi Arabia
关键词
anti-ulcerogenic effect; biochemical studies; floating beads; histopathological examination; INDUCED GASTRIC-ULCER; H-2-RECEPTOR ANTAGONISTS; ANTIOXIDANT ACTIVITY; LIPID-PEROXIDATION; MUCOSAL INJURY; RATS; INDOMETHACIN; ACID; INHIBITION; METRONIDAZOLE;
D O I
10.2147/DDDT.S81109
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:2159 / 2169
页数:11
相关论文
共 56 条
[1]  
Ahmed O.A.A., 2013, Int. J. Pharm. Pharmaceut. Sci., V5, P1
[2]   Design and Optimization of Self-Nanoemulsifying Delivery System to Enhance Quercetin Hepatoprotective Activity in Paracetamol-Induced Hepatotoxicity [J].
Ahmed, Osama A. A. ;
Badr-Eldin, Shaimaa M. ;
Tawfik, Mona K. ;
Ahmed, Tarek A. ;
El-Say, Khalid M. ;
Badr, Jihan M. .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2014, 103 (02) :602-612
[3]   Strawberry Polyphenols Attenuate Ethanol-Induced Gastric Lesions in Rats by Activation of Antioxidant Enzymes and Attenuation of MDA Increase [J].
Alvarez-Suarez, Jose M. ;
Dekanski, Dragana ;
Ristic, Slavica ;
Radonjic, Nevena V. ;
Petronijevic, Natasa D. ;
Giampieri, Francesca ;
Astolfi, Paola ;
Gonzalez-Paramas, Ana M. ;
Santos-Buelga, Celestino ;
Tulipani, Sara ;
Quiles, Jose L. ;
Mezzetti, Bruno ;
Battino, Maurizio .
PLOS ONE, 2011, 6 (10)
[4]   The role of antioxidant activity of Phyllanthus emblica fruits on prevention from indomethacin induced gastric ulcer [J].
Bandyopadhyay, SK ;
Pakrashi, SC ;
Pakrashi, A .
JOURNAL OF ETHNOPHARMACOLOGY, 2000, 70 (02) :171-176
[5]   The inhibition of gastric mucosal lesion, oxidative stress and neutrophil-infiltration in rats by the lichen constituent diffractaic acid [J].
Bayir, Y. ;
OdabaSoglu, F. ;
Cakir, A. ;
Aslan, A. ;
Suleyman, H. ;
Halici, M. ;
Kazaz, C. .
PHYTOMEDICINE, 2006, 13 (08) :584-590
[6]   Protective Effect of Mirtazapine on Indomethacin-Induced Ulcer in Rats and Its Relationship with Oxidant and Antioxidant Parameters [J].
Bilici, Mehmet ;
Ozturk, Cengiz ;
Dursun, Hakan ;
Albayrak, Fatih ;
Saglam, Mustafa Bahadir ;
Uyanik, Abdullah ;
Gulaboglu, Mine ;
Tekin, Salim Basol .
DIGESTIVE DISEASES AND SCIENCES, 2009, 54 (09) :1868-1875
[7]  
Bombardier C, 2002, AM J CARDIOL, V89, p3D
[8]   In vitro effect of quercetin on human gastric carcinoma: Targeting cancer cells death and MDR [J].
Borska, Sylwia ;
Chmielewska, Magdalena ;
Wysocka, Teresa ;
Drag-Zalesinska, Malgorzata ;
Zabel, Maciej ;
Dziegiel, Piotr .
FOOD AND CHEMICAL TOXICOLOGY, 2012, 50 (09) :3375-3383
[9]   Antimicrobial activity of flavonoids [J].
Cushnie, TPT ;
Lamb, AJ .
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2005, 26 (05) :343-356
[10]  
de Groot H, 1998, FUND CLIN PHARMACOL, V12, P249