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 Anti-allergy anti-inflammatory composition

Details
Inventors: Singh, Amarjit; Jain, Rajesh;
Assignee: Panacea Biotec Limited (New Delhi, IN)
Primary Examiner: Geist; Gary
Assistant Examiner: White; Everett
Attorney, Agent or Firm: Oblon, Spivak, McClelland, Maier & Neustadt, P.C.

A novel composition of Nimesulide and salts thereof and Cetrizine possessing antileukotriene, antihistaminic, antiallergic and antiinflammatory action is disclosed. The composition is useful in the cure of allergic disorders such as rhinitis, bronchitis, asthama, urticaria and the like.

DETAILED DESCRIPTION OF THE INVENTION The following unique features of Nimesulide may prove to be quite beneficial in all allergic disorders.
1) Nimesulide is a potent stabilizer of mast cells and basophils.
Thus, it prevents the release of histamine, proteases, TNF-a, Prostaglandins, leukotrienes, PAF and other cytokines from activated mast cells.
2) Nimesulide indirectly blunts the eosinophil deluge in asthmatic attacks because of its mast cell and basophil stabilizing property.
Mast cells and basophils release an eosinophil chemotactic factor that causes eosinophils to migrate towards inflamed allergic tissue.
Nimesulide is also reported to inhibit chemotaxis and synthesis of platelet activating factor and leukotrienes by human eosinophils.
3) Nimesulide potently inhibits the phosphodiesterase type IV in human polymorphonuclear leukocytes.
The resultant increase in cAMP accounts for a marked decrease in chemotaxis, degranulation and free radical generation.
PDE-IV inhibitors are finding a place as anti-asthmatic drugs.
4) Nimesulide inhibits the neutrophil respiratory burst and hence the release of free radicals, cytokines, eicosanoids, prostaglandins etc.
5) Nimesulide is a potent anti-oxidant.
Hence it prevents tissue injury at sites of inflammation by maintaining natural host protective systems.
Second generation Histamine (H,receptor) antagonist (e.
g.
cetirizine, fexofenadine, acrivastine, astemizole, loratidine etc.
) are the drugs of choice in the treatment of allergic rhinitis as they are long acting and are free from sedative and anticholinergic effects.
In addition, second generation anti-histamines have the following unusual and potentially beneficial properties.
1) These non-sedative anti-histamines have demonstrated dose-related protection against histamine induced bronchoconstriction.
2) These have been shown to protect against exercise, ultrasonic nebulized distilled water and cold air induced bronchoconstriction.
3) These produce modest but statistically significant acute bronchodilation in mild to moderate asthma



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