Rabeprazole sodium delayed-release multiparticulates: Effect of enteric coating layers on product performance

Abstract

Rabeprazole sodium is one of the most effective proton pump inhibitors (PPIs) used in antiulcer therapy. Like most other PPIs, owing to its acid-labile nature, the drug is formulated as enteric-coated dosage form. Conventional means of producing delayed release multiparticulate dosage forms of PPIs require large quantities of enteric polymer coatings. In the present study, in order to better evaluate the effect of polymeric coating on product performance, the pellet core structure and composition was kept constant. Four different enteric-coating formulations and designs were evaluated. Enteric-coated drug multiparticulates prepared with single polymeric coatings (acrylic or cellulosic) were compared with two different polymeric layer coatings to evaluate the effectiveness of latter coatings in more effectively producing a better rabeprazole sodium delayed-release pellet product. The pH-dependent, enteric acrylic, and cellulosic polymers were used either alone, in combination, or applied one over the other to impart delayed-release properties to the core drug pellets. It was demonstrated that dual delayed-release coating with two different enteric polymers—an inner acrylic coating followed by an outer cellulosic coating—yields the best product that provides all the desired physicochemical and drug dissolution characteristics.

pH- and ion-sensitive polymers for drug delivery

“…There are several launched products containing enteric polymers for protecting acid-liable drugs. Coating of beads containing rabeprazole with Eudragit L or HPMC-P has been shown to suppress drug release at acidic pH without compromising the release at neutral pH [6]. Further, enteric capsules could preserve the integrity of tenatoprazole until the drug reached the small intestine [35] and were able to obtain almost 2.5 times higher C max of blood drug levels compared with free drug solution after oral administration to dogs [36].…”

“…Higher efficacy of drugs can be achieved through improving water solubility of drugs [1-3], restricting drug release in a site-specific manner [4,5], or preventing undesired drug degradation in the stomach or during blood circulation [6,7]. DDS formulation can also promote drug safety by reducing systemic side effects [8,9], preventing drug release at stomach and subsequent gastric damage [10], and preventing drug distribution into normal tissues [11-13].…”

Development and evaluation of diltiazem hydrochloride controlled-release pellets by fluid bed coating process

“…Also, resistance to external factors such as moisture, air, and light is the most advantageous property of these dosage forms. [1234]…”

Pharmacokinetics of rabeprazole granules versus tablets, and the effect of food on the pharmacokinetics of rabeprazole granules in healthy adults—cross‐study comparison

“…It is marketed globally as enteric‐coated 10 mg and 20 mg tablets . Rabeprazole, like other PPIs, is acid‐labile, and is enteric‐coated to prevent degradation in the gastric environment . Enteric‐coating allows the tablets to be released in the small intestine where the drug is absorbed …”

“…Enteric‐coated granules have several advantages over enteric‐coated tablets, including rapid emptying in the small intestine; faster drug dissolution and absorption; and quicker onset of action. Rapid emptying into the small intestine enables better protection against degradation in the gastric acid …”