Stability of Esomeprazole Capsule Contents After In Vitro Suspension in Common Soft Foods and Beverages

David A. Johnson, M.D., FACP, FACG, Albert C. Roach, Pharm.D., FACG, Anders S. Carlsson, M.Sc., Anders A.S. Karlsson, Ph.D., Dan E. Behr, Ph.D.

Disclosures

Pharmacotherapy. 2003;23(6) 

In This Article

Discussion

Because nearly 4% of patients receiving proton pump inhibitors prefer or require a delivery route other than swallowing an intact oral capsule or tablet, there is a need for alternate delivery systems. Previous studies have demonstrated that the contents of an esomeprazole, lansoprazole, or omeprazole capsule can be mixed with small amounts of applesauce before ingestion, with an expectation of good bioavailability.[10,11,12] Likewise, administration of proton pump inhibitors through feeding tubes or intravenously is feasible but restricted to certain subsets of the patient population.[8,13,14,15]

Suspension of a proton pump inhibitor in a beverage or soft food would be another practical method for providing gastric acid suppression. In our study, esomeprazole enteric-coated pellets from an opened capsule were more than 98% stable when suspended in a small volume (~100 ml) of tap water, cultured milk, yogurt, orange juice, or apple juice. Clinical trial data show that esomeprazole 40 mg once/day provides higher healing rates and improved symptom relief than omeprazole 20 mg or lansoprazole 30 mg in patients with reflux-associated erosive esophagitis.[3,4,16] Thus, the ability to administer esomeprazole in a beverage represents an attractive option for some patients.

The enteric coating of the pellets protects esomeprazole from the acidic gastric milieu and effectively preserves its integrity until digestion in the small intestine. The stability of esomeprazole enteric-coated pellets was not affected by suspension in any of the beverages or soft foods tested, except milk. The decreased stability of the pellets in milk, which has a high buffering capacity, may have been due in part to its near-neutral pH (6.7), which caused dissolution of the enteric-coated polymer of the pellet, with release of its contents and rapid degradation after acid exposure. There is no evidence that this phenomenon would occur when swallowing an intact capsule with liquid.

Water also has a high pH, but it lacks buffering capacity. Therefore, after small amounts of the acidic enteric-coated polymer pellets were suspended in water, the pH decreased rapidly and protected the pellets from dissolution. Other factors, such as ionic strength, fat content, and enzyme activity, also may contribute to the stability differences observed between milk and the other beverages or soft foods.

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