Comparative gastric ulcerogenic effects of meseclazone, 5-chlorosalicylic acid and other nonsteroidal anti-inflammatory drugs following acute and repeated oral administration to rats

Diamantis, W.; Melton, John; Sofia, R. D.; Ciofalo, Vincent B.

doi:10.1016/0041-008x(80)90340-3

Cited by 17 publications

(6 citation statements)

References 8 publications

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“…The methods used to evaluate lesions were based on previously reported procedures used to assess GI ulcerogenic effects of NSAIDs in rats. 16 Intestinal toxicity was evaluated by a person blind to the identity of the treatment group and was measured as the relationship between the weight of the damaged areas and the total weight of the small intestine (Table I, column 3). In the cecum, ulcerous lesions were assessed by measuring their larger length in mm.…”

Section: Evaluation Of Intestinal Lesionsmentioning

confidence: 99%

Intestinal Ulcerogenic Effect of S(+)‐Ketoprofen in the Rat

Cabré¹,

Fernández²,

Zapatero³

et al. 1998

The Journal of Clinical Pharma

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Nonsteroidal antiinflammatory drugs (NSAIDs) inhibit prostaglandin synthesis in the gastrointestinal mucosa, which can lead not only to stomach ulcers but also ulcers in the small and large intestines. Ulcers of the small intestine are less common than those of the stomach, but intestinal lesions are more life threatening. Although the R(-)-enantiomers of the arylpropionic acid (APA) class of NSAIDs are assumed to lack the toxic effects of cyclooxygenase inhibition, they may contribute to the ulcerogenicity of racemates. We have examined the intestinal ulcerogenic effects of single oral doses of S(+)-ketoprofen compared with racemic ketoprofen in the small intestine and cecum of rats. The toxicity in the small intestine was measured as the weight ratio between portions of intestine showing lesions and the total weight of the tissue. Toxicity in the cecum was evaluated by measuring the size of the ulcers. S(+)-ketoprofen had no significant ulcerogenic effect at 10 or 20 mg/kg. However, racemic ketoprofen was clearly ulcerogenic in the small intestine and cecum at the 40 mg dose. R(-)-ketoprofen at 20 mg/kg does not show any effect in the cecum and only limited ulcerogenesis in the small intestine: The latter effect may be the result of racemic inversion. Therefore, the ulcerogenic action of racemic ketoprofen can be interpreted as a synergism between S(+)- and R(-)-ketoprofen. The mechanism of this synergism is not well understood but may be a general feature of APA NSAIDs.

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Section: Evaluation Of Intestinal Lesionsmentioning

confidence: 99%

Intestinal Ulcerogenic Effect of S(+)‐Ketoprofen in the Rat

Cabré¹,

Fernández²,

Zapatero³

et al. 1998

The Journal of Clinical Pharma

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“…The gastric irritation is mainly due to the free carboxylic acid group in the chemical formula [3]. Due to its short plasma half life of 1-3 h following oral dosing and the gastric irritation, ibuprofen is an ideal candidate for preparing prolonged or controlled release drug products [3][4][5][6][7][8][9][10][11]. Since the property of reswelling is susceptible to the environmental pH, the incorporation of acid-sensitive drugs into the beads protects them from the gastric juice [12].…”

Section: Introductionmentioning

confidence: 99%

Modified Chitosan‐Clay Nanocomposite as a Drug Delivery System Intercalation and In Vitro Release of Ibuprofen

Abdeen

Salahuddin

2013

Journal of Chemistry

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The present paper focused on the intercalation of ibuprofen into sodium montmorillonite, chitosan, and chitosan montmorillonite nanocomposites as a sustained release drug carrier. The compounds were characterized by X-ray diffraction (XRD), infrared spectroscopy (IR), thermogravimetric analysis (TGA), and transmission electron microscopy (TEM). The basal spacing of montmorillonite increased from 9.6Å to 19.6Å indicating the intercalation of modified chitosan and ibuprofen between lamellar layers. UV spectroscopy was employed to monitor the in vitro drug release processes in both pH 5.4 and 7.8 solutions. The results revealed that ibuprofen was released from MMT, CS, and Mod-CS/MMT steadily and was pH dependent.

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“…We also included 5-chlorosalicylic acid in this study since it is the main and active metabolite of meseclozone. 22 Of relevance are recent literature reports on the synthesis of bismuth(III) complexes derived from ciprofloxacin 23 and norfloxacin 24 which show good antibacterial activity against Escherichia coli, Klebsiella pneumoniae, Bacillus pumilus, Staphylococcus aureus and Staphylococcus epidermidis. More recently it is claimed that a 1 : 1 bismuth(III) complex derived from diclofenac, synthesised in situ from bismuth subcitrate and the Na salt of diclofenac, displayed an unusual increase in ulcerogenic activity in rats in comparison to the Na diclofenac salt itself, though the actual composition of the claimed 1 : 1 'bismuth diclofenac' complex is not established.…”

Section: Introductionmentioning

confidence: 99%

Bismuth(iii) complexes derived from non-steroidal anti-inflammatory drugs and their activity against Helicobacter pylori

et al. 2010

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The formation of bismuth(III) complexes of carboxylates and benzoates derived from the 1 : 3 reaction of BiPh(3) with the common non-steroidal anti-inflammatory drugs (NSAIDs) ketoprofen, naproxen, ibuprofen, mefenamic acid, diflunisal, 5-chlorosalicylic acid, fenbufen, sulindac, tolfenamic acid and flufenamic acid, has been achieved using both solvent-free and solvent-mediated methods. The thermochemical profiles of the solvent-free reactions were studied using DSC-TGA. All reactions produced the tris-substituted complexes of general formula [BiL(3)](n), with the complexes derived from ketoprofen and sulindac having an additional single bismuth bound H(2)O molecule in the inner coordination sphere. The complexes are stable in air over a period of six months, do not undergo significant decomposition when suspended overnight in water, but decompose in 1 M HCl solution to release the free acid form of the NSAID. All ten complexes show excellent in vitro activity against Helicobacter pylori with MIC values of > or = 6.25 microg mL(-1).

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Comparative gastric ulcerogenic effects of meseclazone, 5-chlorosalicylic acid and other nonsteroidal anti-inflammatory drugs following acute and repeated oral administration to rats

Cited by 17 publications

References 8 publications

Intestinal Ulcerogenic Effect of S(+)‐Ketoprofen in the Rat

Intestinal Ulcerogenic Effect of S(+)‐Ketoprofen in the Rat

Modified Chitosan‐Clay Nanocomposite as a Drug Delivery System Intercalation and In Vitro Release of Ibuprofen

Bismuth(iii) complexes derived from non-steroidal anti-inflammatory drugs and their activity against Helicobacter pylori

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