Review article: similarities and differences among delayed‐release proton‐pump inhibitor formulations

Abstract

SUMMARYProton-pump inhibitors are acid-labile, and require an enteric coating to protect them from degradation in the stomach when given orally. However, this leads to delayed absorption and onset of action of the protonpump inhibitor.This article aims to review the similarities and differences between the various formulations of delayed release proton-pump inhibitors. Delayed-release omeprazole and delayed-release lansoprazole have been suspended in sodium bicarbonate for tube administration; however, for omeprazole, absorption is further impaired and antisecretory effects are disappointing. Although such formulations may be more convenient for clinical use in certain patient groups, absorption of the proton-pump inhibitor is still influenced by residual enteric coating. There are few differences among the currently available delayed-release proton-pump inhibitors with respect to their pharmacodynamic effects during chronic administration. There are minor formulation-based pharmacokinetic differences among these agents, primarily reflected in their bioavailability following the first few doses.Differences in bioavailability may explain slight differences in the rate of onset of maximal antisecretory effect. However, minor pharmacodynamic and pharmacokinetic differences are not associated with meaningful differences in clinical outcomes.

Potential Options to Optimize Therapy of Gastroesophageal Reflux Disease with Proton Pump Inhibitors

“…Indeed, esomeprazole 20 mg/day exerts a superior intragastric pH control (pH ≥4) compared to the same dose of omeprazole at 8, 12, and 16 h in patients with GERD [59]. As a consequence, esomeprazole has a superior bioavailability compared to omeprazole, reaching a value of 90% (the highest value among PPIs) with 40 mg/day [7, 63, 64]. Furthermore, this dose has the most prominent antisecretory effect compared to other standard doses of PPIs, since it is able to maintain intragastric pH ≥4 for at least 14 h in a day [59], as observed at day 5 of treatment (fig.…”

“…The current challenge in GERD is to optimize the therapy by adopting cost-effective strategies for uncomplicated forms of the disease with mild symptoms (e.g. the on-demand approach) [5, 6], for moderate/severe erosive esophagitis or NERD refractory to conventional PPI doses [7]. Thus, two strategies are to be implemented in clinical practice, e.g.…”

Acid Suppression Therapy: Where Do We Go from Here?

“…1 = Inert core; 2 = lansoprazole layer; 3 = undercoating layer -improves stability in high humidity; 4 = fi rst enteric-coating layer -improves stability of lansoprazole; 5 = second enteric-coating layer -prevents breakage of the enteric coats during tablet compression; 6 = third enteric-coating layer -neutralizes taste of microgranule; 7 = overcoating layer -improves tablet hardness (from Baldi and Malfertheiner [156] 23 ing of the granules disintegrates and a suspension formed. Due to the impaired absorption of omeprazole from this extemporary preparation [154] , a lower than expected antisecretory effect can be predicted.…”

“…In addition, when this formulation is dispersed in water, it provides a less expensive alternative to intravenous PPIs for patients with nasogastric or gastric tubes in ICU or long-term care settings [153] . Some studies (reviewed by Horn and Howden [154] ) have evaluated PPI absorption from intact nonen-capsulated omeprazole or lansoprazole as well as their suspension in sodium bicarbonate (8.4%) solution. Although, with exception of the so-called simplifi ed omeprazole suspension (SOS) whose bioavailability was impaired, the other 'extemporary' formulations allowed a proper PPI absorption, predisintegrated lansoprazole ODT would represent the most appropriate choice for administration via nasogastric or gastrostomy tube.…”

Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations

“…The enteric delayed-release dosage form of LPZ has been reported to be unable 4030 alai and lin to efficiently suppress nocturnal acid secretion in the event of gastroesophageal reflux disease. 6,7 Nocturnal acid breakthrough frequently occurs in patients with gastroesophageal reflux disease during the first half of the sleeping period, and affects sleep quality and daytime functioning. Eudragit ® RS100 and poly(lactic-co-glycolic acid) (PLGA) polymers have been used as drug carriers.…”