In this study, we have evaluated the efficacy of dosmalfate, a new flavonoid derivative compound, for the prevention and treatment of experimental colitis. To induce colitis, BALB/c mice received 5% dextran sulphate sodium (DSS) in their drinking water continuously for 7 days. Colitis was quantified by a clinical damage score, colon length, weight loss, stool consistency and rectal bleeding. Inflammatory response was assessed by neutrophil infiltration, determined by histology and myeloperoxidase (MPO) activity. Interleukin (IL)-1 beta, prostaglandins (PG)E(2) and (PG)D(2) concentrations in colonic tissue, histological and histochemical analysis of the lesions were also measured. Dosmalfate (400-800 mg/kg body weight, p.o.) ameliorated severe colitis reduced the degree of inflammation through reduction of neutrophil infiltration and IL-1 beta levels. (PG)E(2) and (PG)D(2) synthesis were significantly reduced in colitis control group and treatment with dosmalfate abolished the decrease in PG synthesis in colon mucosa. We conclude that dosmalfate is protective in acute DSS-induced colitis. The beneficial effects seem to be related to a decrease of neutrophil infiltration, absence of up-regulation of IL-1 beta and increase of PG production in colon mucosa.

01 Jan 2003·European Journal of PharmacologyQ3 · MEDICINE

Effects of dosmalfate, a new cytoprotective agent, on acute and chronic trinitrobenzene sulphonic acid-induced colitis in rats

Q3 · MEDICINE

Article

Author: Isabel Villegas ; Carmen La Casa ; Catalina Alarcón de la Lastra ; Aurelio Orjales

Activated neutrophils and proinflammatory cytokines, such as tumor necrosis factor-alpha (TNF-alpha) are clearly involved in the pathogenesis of bowel disease. Increased expression of epidermal growth factor-receptor (EGF receptor) has been reported for the colon mucosa surrounding areas of ulceration, suggesting a pivotal role in mucosal defence and repair. In this study, we examined the effects of dosmalfate, a new flavonoid derivative compound (diosmin heptakis) with antioxidant and cytoprotective properties, on acute and chronic experimental trinitrobenzene sulphonic acid (TNBS)-induced colitis in rats. The inflammation response was assessed by neutrophil infiltration as evaluated by histology and myeloperoxidase activity. Mucosal TNF-alpha production and histological analysis of the lesions was also carried out. In addition, we studied the expression of the EGF receptor inmunohistochemically during the healing of TNBS-induced chronic colitis. A 2-day treatment with 400 or 800 mg/kg of dosmalfate ameliorated the colon damage score and the incidence of adhesions. It also significantly (P<0.05) decreased myeloperoxidase activity and colonic mucosal production of TNF-alpha. Chronic treatment (14 days) with 800 mg/kg/day of dosmalfate also had significant protective effects on TNBS-induced colitis which were reflected by significant attenuation (P<0.05) of the damage score while the inflammatory indicators were not improved. The chronic beneficial effect of dosmalfate was apparently related to the enhancement of EGF receptor expression. These findings confirm the protective effects of dosmalfate in acute and chronic experimental colitis.

Shipin Yu Yaopin

Determination of related substances of dosmalfate by HPLC

Author: Ma, Yu-zhen ; Zhang, Guang-zhou ; Zhao, Ren-yong ; Zhang, Dai-zhou

An RP-HPLC method for the determination of the related substances of dosmalfate was established.The separation was performed with ODS C18 column.Glacial acetic acid 0.4 mL and triethylamine 1.6 mL was dissolved with 400 mL water, adjusting pH to 7.5 with phosphoric acid.The mobile phase consisted of this solution-methanol (72: 28).The detection wavelength was set at 330 nm.In this chromatog. system, the related substances had a good separation and a good linear relation over the determination concentrationThis method is simple, accurate and applicable for the determination of related substances of dosmalfate.

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Indication	Country/Location	Organization	Date
Ulcer	Spain	Faes Farma SA	20 Jun 2000
Peptic Ulcer	Spain	Faes Farma SA	01 May 1999
Poisoning	Spain	Faes Farma SA	01 May 1999

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Duodenal Ulcer	Preclinical	Portugal	Faes Farma SA	-
Stomach Ulcer	Preclinical	Portugal	Faes Farma SA	-
Ulcer	Preclinical	France	Faes Farma SA	-

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