Description

Esomeprazole Enteric Coated Pellets is a pharmaceutical formulation of the proton pump inhibitor (PPI) drug, esomeprazole. The active ingredient, esomeprazole, is an acid-labile compound, meaning it is quickly degraded by the highly acidic environment of the stomach. To prevent this degradation and ensure the drug reaches its site of action, it is manufactured as tiny pellets (micro-pellets or granules) that are coated with a special enteric coating.

This coating is designed to resist dissolution in the acidic stomach environment. The pellets remain intact as they pass through the stomach and only dissolve in the more alkaline environment of the small intestine, where the drug can be safely absorbed into the bloodstream. These pellets are then typically filled into capsules or compressed into tablets.

Indications

Esomeprazole enteric coated pellets are indicated for the same range of acid-related conditions as other formulations of esomeprazole. The use of this specific formulation is to ensure the drug’s stability and effectiveness. Key indications include:

• Gastroesophageal Reflux Disease (GERD): For the treatment of GERD symptoms like heartburn and acid regurgitation, and for the healing and long-term maintenance of erosive esophagitis.

• Healing of Stomach and Duodenal Ulcers: Used to treat and prevent ulcers, particularly those caused by the long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) or an infection with Helicobacter pylori (H. pylori).

• Zollinger-Ellison Syndrome: For the long-term treatment of this pathological hypersecretory condition.

Mechanism of Action

The mechanism of action of esomeprazole enteric coated pellets is a combination of the drug’s pharmacological effect and its unique delivery system.

1. Enteric-Coating for Protection: The enteric coating is the first crucial step in the drug’s mechanism. It protects the acid-sensitive esomeprazole from degradation in the stomach. The coating is a pH-sensitive polymer that remains undissolved below a pH of approximately 5.5.
2. Absorption in the Small Intestine: Once the pellets leave the stomach and enter the small intestine, where the pH is higher, the enteric coating dissolves, releasing the esomeprazole. The drug is then absorbed into the bloodstream.

3. Targeting the Proton Pump: The absorbed esomeprazole is an inactive prodrug. It travels through the bloodstream and accumulates in the highly acidic secretory canaliculi of the gastric parietal cells.
4. Activation and Irreversible Inhibition: In this acidic environment, esomeprazole is converted into its active form, a sulfenamide. This active form then irreversibly binds to the H+/K+-ATPase enzyme, which is the “proton pump” responsible for the final step of gastric acid secretion.

5. Cessation of Acid Production: By permanently inactivating the proton pump, esomeprazole effectively blocks both basal (resting) and stimulated acid secretion. Because the binding is irreversible, acid production is suppressed until the parietal cells synthesize new proton pumps, which ensures a sustained and powerful acid-suppressing effect.