Introduction to Mesalamine: 1) Physicochemical properties Name: - Mesalamine Chemical name:- 5-amino-2-hydroxybenzoic acid Chemical formula:- C7H7NO3 Molecular Weight:-

153.1354 gm/mol Chemical structure:-

Description:- Light tan to pink colored , needle-shaped crystals Solubility:- It is slightly soluble in water (1mg/ml), soluble in dilute HCL and dilute alkali hydroxides. Slightly soluble in dehydrated alcohol, Acetone & methyl alcohol. Practically insoluble in chloroform , ether, butyl alcohol, ethyl acetate, n-hexane, methylene chloride & propylene alcohol. The aqueous solubility of mesalamine has been reported to be 0.844mg/ml at 250c & 1.41mg/ml at 370c. Storage conditions:- Preserve in tight , light resistant container, Melting range:- 283 0C Loss On Drying:- Not more than 0.5 % Related Substance:Heavy Metals:- 0.002% 2) Category:- Anti inflammatory Agents 3) Pharmacology: Mesalazine (INN, BAN), also known as Mesalamine (USAN) or 5aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract (Crohn's disease) and mild to moderate ulcerative colitis. Mesalazine is a bowel-specific aminosalicylate drug that is metabolized in the gut and has its predominant actions there, thereby having fewer systemic side effects. As a derivative of

salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism. Although the mechanism of action of mesalazine is not fully understood, it appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalazine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon. 2.2.4 Pharmacokinetic: Absorption 20 to 30% absorbed following oral administration. 10 to 35% absorbed from the colon (rectal suppository) - extent of absorption is determined by the length of time the drug is retained in the colon. Distribution

Metabolism Rapidly and extensively metabolized, mainly to N-acetyl-5-ASA (Ac-5-ASA) in the intestinal mucosal wall and the liver. Ac-5-ASA is further acetylated (deactivated) in at least 2 sites, the colonic epithelium and the liver. Indications And Usage: For the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. It is indicated for the maintenance of remission of ulcerative colitis in patients who are intolerant of sulfasalazine. Contraindications:Hypersensitivity to salicylates. Interactions:The co-administration of salicylates and low molecular weight heparins or heparinoids may result in an increased risk of bleeding (i.e., hematomas) following neuraxial anesthesia. Salicylates should be discontinued prior to the initiation of a low molecular weight heparin or heparinoid. If this is not possible, it is recommended to monitor patients closely for bleeding.

Increased prothrombin time in patients taking concomitant warfarin has been reported. Market formulation: Asacol Asacolitin Canasa Claversal Fisalamine Lixacol Mesasal Pentasa Rowasa Salofalk

References: Analytical Profiles of Drug Substances and Excipients, Volume 25 By Harry G. Brittain Drug bank Usp monograph of mesalamine