Mesalamine SR Pellets / Granules

Ulcerative colitis and other inflammatory diseases cause excessive production of bio-chemicals, for example, prostaglandins, that produce inflammation in the colon. Prostaglandins are produced by the enzymes, cyclooxygenase and lipoxygenase. These enzymes are over-active in individuals with ulcerative colitis. Mesalamine may work by blocking the activity of cyclooxygenase and lipoxygenase, thereby, reducing the production of prostaglandins. Reduced production of prostaglandins decreases inflammation in the colon and the symptoms associated with ulcerative colitis. Available forms of mesalamine differ in their route of administration and how often they are administered.

Mesalamine is used to treat ulcerative colitis (a condition which causes swelling and sores in the lining of the colon and rectum). Mesalamine is in a class of medications called anti-inflammatory agents. It works by stopping the body from producing a certain substance that may cause inflammation.

The mechanism of action of mesalamine appears to be local to the intestinal mucosa rather than systemic. Mucosal production of arachidonic acid metabolites (prostanoids, leukotrienes and hydroxyeicosatetraenoic acids) is increased in patients with ulcerative colitis, and Mesalamine diminishes inflammation by blocking production of arachidonic acid metabolites.

Mesalamine comes as a Delayed-release tablet (releases the medication in the intestine where its effects are needed),

Delayed-release capsule (releases the medication in the intestine where its effects are needed),

Controlled-release capsule (releases the medication throughout the digestive system),

Extended-release capsule (long-acting).

Suppositories:

For the treatment of active ulcerative proctitis and ulcerative colitis

Adults: 500 mg twice daily. Alternatively, 1000 mg once daily at bedtime may be used.

The type of Medication to be taken is depending on how the symptoms are controlled.

The type and formulation of therapy recommended for patients with ulcerative colitis (UC) is dependent on both the location of the disease and the degree of severity. In some patients, the inflammation is limited to the rectum only (distal), but other affected individuals have colonic disease that extends along the length of much of the colon (extensive). Topical (rectal) therapy is the starting point for patients with disease limited to the left colon, with oral therapy added on in patients with more extensive disease. For active distal (rectum and sigmoid colon) disease, the US and European professional bodies recommend topical therapy with mesalamine. Oral mesalamine is necessary for patients with disease extending beyond the left colon. Using topical and oral mesalamine together is more effective than either alone in these patients.

Mesalamine suppositories or enemas are recommended for maintenance of remission in patients with proclitic. Oral 5-aminosalicylic acid (5-ASA) formulations will be required for patients with more extensive disease.

MKPPL have different formulations of 5-ASA medications, which can be differentiated based on their means of release of mesalamine until it reaches the colon. Since there is an ascending pH gradient from the proximal to the distal intestinal tract (low pH in the stomach and upper small bowel; higher pH in the distal small bowel and colon), some delivery systems have an enteric coating that dissolves when the pH rises above a certain threshold. Eudragit S polymer is a pH-sensitive polymer that disintegrates at a pH >7, allowing the drug to be released in the terminal ileum or cecum. By contrast, Eudragit^® L resin breaks down at a pH ≥6, thus releasing the active drug throughout the jejunum, terminal ileum and colon.

Another formulation of MKPPL Mesalamine ER Pellets formulation that has a pH-independent delivery mechanism. This formulation consists of mesalamine microgranules coated in a moisture-sensitive ethyl cellulose semi-permeable membrane, which allows it to be released in a pH-independent fashion, beginning in the duodenum and continuing throughout the intestinal tract.

Mesalmaine ER Pellets have dissolution time of 8 hours and are released as per the USP Monograph.

The pharmaceutical formulation of sachet comprising a total dosage amount of mesalamine consisting of 0.5g, 1.0g., 1.5g., 2g, 3g, 4g and 5g.