In the pharmaceutical industry, Aminosalicylates (also known as 5-ASAs) are a specialized class of anti-inflammatory drugs used as the primary treatment for Inflammatory Bowel Disease (IBD), particularly Ulcerative Colitis.
As a pharmacist and manufacturer, I view these molecules as “topical” agents for the gut—they are designed to reach the colon to reduce inflammation directly on the intestinal lining rather than acting systemically.
Primary Examples of Aminosalicylates
| Generic Name | Common Brand Names | Primary Delivery Site |
| Mesalamine (5-ASA) | Asacol, Pentasa, Mezavant | Small intestine and/or colon (formulation dependent) |
| Sulfasalazine | Salazopyrin, Azulfidine | Primarily the Colon (requires bacterial activation) |
| Balsalazide | Colazal, Giazo | Primarily the Colon |
| Olsalazine | Dipentum | Primarily the Colon |
Technical Breakdown by Formulation
The challenge with these drugs is preventing them from being absorbed in the stomach. At your WHO-GMP facility in Mumbai, manufacturing these requires advanced “Site-Specific Delivery” technologies:
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Mesalamine (Mesalazine): This is the “pure” form of 5-ASA. It is available in various coatings (pH-dependent or time-release) to ensure it dissolves exactly where the inflammation is located.
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Sulfasalazine: This is a “prodrug.” It consists of 5-ASA linked to a sulfapyridine molecule. It remains inactive until it reaches the colon, where bacteria break the link to release the medicine. Note: The sulfapyridine part causes most of the side effects.
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Balsalazide & Olsalazine: These are newer prodrugs that use a different carrier or two 5-ASA molecules linked together, designed to reduce the side effects seen with Sulfasalazine.
Mechanism: Local Anti-Inflammatory Action
Unlike systemic steroids, 5-ASAs work locally on the gut wall:
Leukotriene Inhibition: They block the production of leukotrienes (chemicals that attract inflammatory cells to the gut).
Prostaglandin Synthesis: They interfere with the cyclooxygenase (COX) pathway in the gut lining to reduce swelling and mucus production.
Antioxidant Effect: They act as “scavengers” to neutralize free radicals that damage the intestinal tissue during a flare-up.
The Pharmacist’s “Technical Warning”
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The “Sulfa” Allergy: Patients allergic to sulfa drugs cannot take Sulfasalazine. They should be switched to pure Mesalamine.
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Renal Monitoring: Although they act locally, a small amount is absorbed. Long-term use requires periodic Kidney Function Tests (KFTs) to monitor for interstitial nephritis.
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The “Tablet Integrity” Rule: Patients must be told not to crush or chew extended-release or enteric-coated tablets, as this destroys the site-specific delivery mechanism.
The Manufacturer’s Perspective: Technical & Export
From a production and B2B standpoint at your facility in Mumbai:
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The “Pellet” USP: On your marketplace, highlight if you offer Mesalamine Pellets or Delayed-Release Granules. These provide more uniform distribution in the colon than traditional tablets.
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Export Potential: These are high-value, “chronic use” drugs. International buyers in the Middle East and Africa look for reliable WHO-GMP sources for Mesalamine because the brand names are often prohibitively expensive.
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Dossier Support: We provide full CTD/eCTD Dossiers for various delivery forms (Tablets, Suppositories, and Enemas) to support your firm’s registration in international GI tenders.