Description

Dexlansoprazole Dual Delayed Release Pellets is a specific pharmaceutical formulation of the proton pump inhibitor (PPI) dexlansoprazole. The term “Eq: Dexlansoprazole” means that the pellets contain an amount of the drug equivalent to the stated dosage of dexlansoprazole. This formulation is characterized by its unique dual delayed-release delivery system. The pellets are engineered with two different enteric coatings, each designed to dissolve at a different pH level. This allows for two separate releases of the drug in the small intestine, providing a sustained therapeutic effect.

Indications

This specific formulation of dexlansoprazole is used to treat a range of acid-related conditions. Its primary indications include:

• Healing of Erosive Esophagitis (EE): It is used for the short-term healing of all grades of EE, which is damage to the esophageal lining caused by gastroesophageal reflux disease (GERD).

• Maintenance of Healed EE: It is also used for the long-term maintenance of healed EE. The dual-release mechanism helps to provide a consistent level of acid suppression, which is crucial for preventing a relapse.
• Symptomatic Non-Erosive GERD: It is used for the treatment of heartburn and other symptoms of GERD in patients who do not have erosive esophagitis. The dual-release system can be particularly beneficial for patients with nocturnal or breakthrough symptoms.

Mechanism of Action

The mechanism of action of dexlansoprazole dual delayed release pellets is a combination of the drug’s inherent pharmacological effect and its unique delivery system.

1. Inhibition of the Proton Pump:
   • Dexlansoprazole is a prodrug that is absorbed into the bloodstream from the small intestine.
   • It then travels to the gastric parietal cells, where it is converted to its active form in the acidic environment of the secretory canaliculi.
   • The activated form of dexlansoprazole irreversibly binds to the H+/K+-ATPase enzyme, also known as the “proton pump.”

• • This pump is responsible for the final step of gastric acid secretion. By permanently inactivating it, the drug effectively blocks both basal and stimulated acid production.

2. Dual Delayed-Release Delivery:
   • This is the unique aspect of the formulation. The pellets within the capsule have two different coatings:
     • First Release: A portion of the pellets has a coating that dissolves at a relatively high pH, allowing for a rapid initial release of the drug in the proximal small intestine. This provides a quick onset of acid suppression.
     • Second Release: The remaining pellets have a coating that requires a lower pH to dissolve, resulting in a second, later release of the drug in the distal small intestine, approximately 4 to 5 hours after the first release.
   • This two-stage release system creates two distinct peaks of drug concentration in the plasma. This provides a longer duration of effective acid suppression over a 24-hour period, helping to manage symptoms throughout the day and night and improve healing rates.