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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

Gross appearance of the gastric mucosa in stomachs of indomethacin-induced models.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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f3-dddt-9-2159: Gross appearance of the gastric mucosa in stomachs of indomethacin-induced models.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: Macroscopic examination of the investigated rat stomachs is shown in Figure 3. The normal control group (1) stomachs (Figure 3A) revealed normal mucosa, no inflammation, and no hemorrhage or patches of hyperemia. On the other hand, the diseased rats group (2) showed marked severe injuries in the gastric mucosa (Figure 3B). Oral administration of indomethacin (50 mg/kg) produced severe hemorrhagic lesions predominantly on glandular mucosa segment of the stomach and few or none in the antrum. Dark reddish patches of ulcers covered the majority of the stomach body, and there were numerous ulcer patches with different forms and sizes within the stomach mucosa. There was remarkable hyperemia in the stomach mucosa. Upon treating the animals with crushed commercial FAM tablets (Figure 3C), the stomachs showed significantly lower numbers of ulcers. They showed moderate mucosal injuries compared to those of ulcerated control rats, and ulcers appeared as discontinuous lesions in the gastric mucosa; no perforation was noticed in all treated animal groups. While treatment with FAM beads (Figure 3D) showed milder ulceration reaction, few small lesions appeared in the gastric mucosa and produced more prominent inhibition effect when compared with the commercial FAM tablets treatment group. On the other hand, treatment with a combination of beads formula plus QRT–PVP coprecipitate (Figure 3E) showed a nearly normal stomach appearance, as minor ulceration was observed in addition to the absence of any sign of inflammation or hemorrhage. Animals of treated groups were healthy and showed nearly normal activity during the experiment.


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)

Gross appearance of the gastric mucosa in stomachs of indomethacin-induced models.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

f3-dddt-9-2159: Gross appearance of the gastric mucosa in stomachs of indomethacin-induced models.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: Macroscopic examination of the investigated rat stomachs is shown in Figure 3. The normal control group (1) stomachs (Figure 3A) revealed normal mucosa, no inflammation, and no hemorrhage or patches of hyperemia. On the other hand, the diseased rats group (2) showed marked severe injuries in the gastric mucosa (Figure 3B). Oral administration of indomethacin (50 mg/kg) produced severe hemorrhagic lesions predominantly on glandular mucosa segment of the stomach and few or none in the antrum. Dark reddish patches of ulcers covered the majority of the stomach body, and there were numerous ulcer patches with different forms and sizes within the stomach mucosa. There was remarkable hyperemia in the stomach mucosa. Upon treating the animals with crushed commercial FAM tablets (Figure 3C), the stomachs showed significantly lower numbers of ulcers. They showed moderate mucosal injuries compared to those of ulcerated control rats, and ulcers appeared as discontinuous lesions in the gastric mucosa; no perforation was noticed in all treated animal groups. While treatment with FAM beads (Figure 3D) showed milder ulceration reaction, few small lesions appeared in the gastric mucosa and produced more prominent inhibition effect when compared with the commercial FAM tablets treatment group. On the other hand, treatment with a combination of beads formula plus QRT–PVP coprecipitate (Figure 3E) showed a nearly normal stomach appearance, as minor ulceration was observed in addition to the absence of any sign of inflammation or hemorrhage. Animals of treated groups were healthy and showed nearly normal activity during the experiment.

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