Inhibition of Ethanol-Induced Gastric Mucosal Damage by Carvedilol in Male Wistar Albino Rats: Possible Biochemical Changes

Al-Rejaie, Salim S.

doi:10.3923/ijp.2009.146.154

Cited by 10 publications

(5 citation statements)

References 37 publications

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“…It has previously reported that acute exposure of ethanol leads to the increase in stomach weight and stomach coefficient, which was due to haemorrhage, oedema, necrosis and inflammation. 39 Moreover, no significant change in the body weight was observed, which might be due to the acute exposure of ethanol. In the present study, a significant decrease in gastric juice pH was observed in per se ethanol-exposed stomach in comparison to control stomach and pre-administration of tBHQ at both the doses and omeprazole 20 mg/kg significantly increased the pH in comparison to per se ulcer group.…”

Section: Discussionmentioning

confidence: 92%

Ethanol-induced gastric ulcer in rats and intervention of tert-butylhydroquinone: Involvement of Nrf2/HO-1 signalling pathway

2019

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Gastric ulcer (GU) is the most common health concern that occurs due to alcohol consumption, smoking and physiological stress. Ethanol-induced GU in animal model resembles the pathophysiology of human ulcer. The present study was designed to investigate the cytoprotective and anti-inflammatory properties of tert-butylhydroquinone (tBHQ), a nuclear factor erythroid 2-related factor 2 (Nrf2) activator, against gastric mucosal damage induced by acute exposure of ethanol (5 ml/kg). The intervention of tBHQ (25 and 50 mg/kg, per os (po)) and omeprazole (20 mg/kg, po) was done for 10 consecutive days. Omeprazole was chosen as a standard drug because it is prescribed for the treatment of GU. Pretreatment of tBHQ decreased gastric mucosal lesion, ulcer index, apoptotic cells and lipid peroxidation level induced by ethanol. Furthermore, the intervention of tBHQ increased gastric mucosa integrity, pH, reduced glutathione, collagen and mucus-producing goblet cells. Intervention of tBHQ increased the expression of antioxidant markers such as Nrf2, haeme oxygenase-1 and catalase and decreased the expressions of inflammatory markers such as nuclear factor kappa-light-chain-enhancer of activated B cells and cyclooxygenase-2. The cytoprotective potential of tBHQ against gastric mucosal damage might be due to its ability to enhance cellular antioxidants and anti-inflammatory responses.

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Section: Discussionmentioning

confidence: 92%

Ethanol-induced gastric ulcer in rats and intervention of tert-butylhydroquinone: Involvement of Nrf2/HO-1 signalling pathway

2019

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“…Microscopic reactive, reparative or degenerative changes seen in the mucosal layer were scored as follows: (1) mucosal congestion, (2) mucosal hemorrhage, (3) glandular disarray/degeneration, (4) mucosal erosions, (5) ulcer formation, (6) active inflammation, (7) submucosal edema, and (8) muscularis layer degeneration. The severity of histopathological changes was expressed according to scale of Rejaie (2009).…”

Section: Histopathological Assessmentmentioning

confidence: 99%

Possible biochemical effects following inhibition of ethanol-induced gastric mucosa damage byGymnema sylvestrein male Wistar albino rats

Al‐Rejaie

Abuohashish²,

Ahmed

et al. 2012

Pharmaceutical Biology

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“…Under these hypochlorhydric conditions, high variations in gastric acidity could result in inter‐ and intra‐subject variability in the dissolution and absorption profiles of drugs (Tenero et al, ), possibly leading to inconsistent clinical outcomes. Previous studies in healthy elderly patients also demonstrated that increasing gastric pH with H 2 receptor antagonists reduced the absorption of weakly basic drugs (Al‐Rajaie, ).…”

Section: Introductionmentioning

confidence: 85%

Amorphous solid dispersions of carvedilol along with pH‐modifiers improved pharmacokinetic properties under hypochlorhydoria

Halder

Tabata

Seto

et al. 2018

Biopharm & Drug Disp

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Carvedilol (CAR) belongs to biopharmaceutics classification system class-II drugs, with poor aqueous solubility and pH-dependent solubility. The present study aimed to develop a novel amorphous solid dispersion (ASD) of CAR with acidic counter ions for pH modifications in microenvironment to improve the pharmacokinetic properties under hypochlorhydric conditions. CAR-ASD was prepared by freeze-drying in combination with counter ions and hydroxypropyl cellulose, and their physicochemical properties including dissolution behavior, storage stability, and photostability were characterized. Pharmacokinetic studies were carried out after oral administration of CAR samples in both normal and omeprazole-treated (30 mg/kg, p.o.) rats as a hypochlorhydria model. Among the tested six counter ions, citric acid (CA) was found to be a preferable pH-modifier of CAR with respect to the dissolution profile and photostability (both potency and colorimetric evaluation). In CAR-ASD formulation with 50% loading of CA (CAR-ASD/CA50), amorphization of CAR was observed during the preparation process. After the oral administration of crystalline CAR in rats under hypochlorhydric condition, there was a 34.4% reduction in the systemic exposure of CAR compared with that in normal rats. However, orally-dosed CAR-ASD/CA50 resulted in limited alterations of pharmacokinetic behavior between normal and omeprazole-treated rats. From these findings, addition of CA as pH-modifier in CAR-ASD might provide consistent pharmacokinetic behavior of CAR even under hypochlorhydric conditions.

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Inhibition of Ethanol-Induced Gastric Mucosal Damage by Carvedilol in Male Wistar Albino Rats: Possible Biochemical Changes

Cited by 10 publications

References 37 publications

Ethanol-induced gastric ulcer in rats and intervention of tert-butylhydroquinone: Involvement of Nrf2/HO-1 signalling pathway

Ethanol-induced gastric ulcer in rats and intervention of tert-butylhydroquinone: Involvement of Nrf2/HO-1 signalling pathway

Possible biochemical effects following inhibition of ethanol-induced gastric mucosa damage byGymnema sylvestrein male Wistar albino rats

Amorphous solid dispersions of carvedilol along with pH‐modifiers improved pharmacokinetic properties under hypochlorhydoria

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