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

Abourehab MA, Khaled KA, Sarhan HA, Ahmed OA - Drug Des Devel Ther (2015)

Bottom Line: QRT was prepared as solid dispersion with polyvinyl pyrrolidone K30 to improve its solubility.Also, there was a significant difference in the decrease of malondialdehyde level compared to FAM commercial tablets or beads alone (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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt ; Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia.

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.

No MeSH data available.


Related in: MedlinePlus

Histological evaluation of stomach tissues from indomethacin-induced ulcer model in rats of hematoxylin and eosin staining of gastric mucosa (magnification ×100).Notes: (A) Normal control; (B) disease control group; (C) commercial FAM; (D) FAM beads; (E) FAM beads plus QRT–PVP.Abbreviations: FAM, famotidine; PVP, polyvinyl pyrrolidone; QRT, quercetin.
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f5-dddt-9-2159: Histological evaluation of stomach tissues from indomethacin-induced ulcer model in rats of hematoxylin and eosin staining of gastric mucosa (magnification ×100).Notes: (A) Normal control; (B) disease control group; (C) commercial FAM; (D) FAM beads; (E) FAM beads plus QRT–PVP.Abbreviations: FAM, famotidine; PVP, polyvinyl pyrrolidone; QRT, quercetin.

Mentions: Histopathological examination was carried out to confirm the morphological changes in stomach tissues in the studied animal groups. Figure 5 shows the histopathological effect of different treatments on indomethacin-induced ulcer model. Stomach histology of control normal rats shows normal microscopic architecture with normal glands, without any signs of abnormalities. The parietal cells located in the upper half of gastric glands with eccentric nuclei and pale eosinophilic vacuoles in the cytoplasm (Figure 5A). On the other hand, the figure reveals a severe inflammatory reaction, manifested by submucosal edema with local mononuclear leucocytic infiltration (mainly lymphocytes and few eosinophils) in the lamina propria, muscularis mucosa, and submucosal layers of the stomach tissue for the indomethacin-treated control group (2). The submucosal blood vessels were congested and the muscular coat was hypertrophied and partially hyalinized. These observations revealed the acute phase of ulcer and a severe inflammatory reaction (Figure 5B). The stomach tissue of group 3, receiving the commercial FAM tablets, showed moderate inflammatory reaction (Figure 5C). The reaction severity was milder in case of animals receiving the beads (Figure 5D), who showed moderate amounts of leucocytic inflammatory cell infiltration in the submucosal layer and muscularis mucosa. Animals in group 5, receiving the beads formula plus the QRT–PVP (Figure 5E), were the best-preserved group in terms of morphological integrity. It showed a uniform epithelial and glandular structure and arrangement, and good tissue architecture. Only minor leucocytic inflammatory cells were encountered in tissue sections.


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

Abourehab MA, Khaled KA, Sarhan HA, Ahmed OA - Drug Des Devel Ther (2015)

Histological evaluation of stomach tissues from indomethacin-induced ulcer model in rats of hematoxylin and eosin staining of gastric mucosa (magnification ×100).Notes: (A) Normal control; (B) disease control group; (C) commercial FAM; (D) FAM beads; (E) FAM beads plus QRT–PVP.Abbreviations: FAM, famotidine; PVP, polyvinyl pyrrolidone; QRT, quercetin.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4403742&req=5

f5-dddt-9-2159: Histological evaluation of stomach tissues from indomethacin-induced ulcer model in rats of hematoxylin and eosin staining of gastric mucosa (magnification ×100).Notes: (A) Normal control; (B) disease control group; (C) commercial FAM; (D) FAM beads; (E) FAM beads plus QRT–PVP.Abbreviations: FAM, famotidine; PVP, polyvinyl pyrrolidone; QRT, quercetin.
Mentions: Histopathological examination was carried out to confirm the morphological changes in stomach tissues in the studied animal groups. Figure 5 shows the histopathological effect of different treatments on indomethacin-induced ulcer model. Stomach histology of control normal rats shows normal microscopic architecture with normal glands, without any signs of abnormalities. The parietal cells located in the upper half of gastric glands with eccentric nuclei and pale eosinophilic vacuoles in the cytoplasm (Figure 5A). On the other hand, the figure reveals a severe inflammatory reaction, manifested by submucosal edema with local mononuclear leucocytic infiltration (mainly lymphocytes and few eosinophils) in the lamina propria, muscularis mucosa, and submucosal layers of the stomach tissue for the indomethacin-treated control group (2). The submucosal blood vessels were congested and the muscular coat was hypertrophied and partially hyalinized. These observations revealed the acute phase of ulcer and a severe inflammatory reaction (Figure 5B). The stomach tissue of group 3, receiving the commercial FAM tablets, showed moderate inflammatory reaction (Figure 5C). The reaction severity was milder in case of animals receiving the beads (Figure 5D), who showed moderate amounts of leucocytic inflammatory cell infiltration in the submucosal layer and muscularis mucosa. Animals in group 5, receiving the beads formula plus the QRT–PVP (Figure 5E), were the best-preserved group in terms of morphological integrity. It showed a uniform epithelial and glandular structure and arrangement, and good tissue architecture. Only minor leucocytic inflammatory cells were encountered in tissue sections.

Bottom Line: QRT was prepared as solid dispersion with polyvinyl pyrrolidone K30 to improve its solubility.Also, there was a significant difference in the decrease of malondialdehyde level compared to FAM commercial tablets or beads alone (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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt ; Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia.

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.

No MeSH data available.


Related in: MedlinePlus