Review article: dual delayed release formulation of dexlansoprazole MR, a novel approach to overcome the limitations of conventional single release proton pump inhibitor therapy

Abstract

SUMMARY BackgroundProton pump inhibitors (PPIs) provide the most effective pharmacotherapy for treating acid-related disorders. However, PPIs do not completely control acid over 24 h with once-daily dosing.

Guidelines for the Diagnosis and Management of Gastroesophageal Reflux Disease

“…Dexlansoprazole is a dual delayed release PPI released in 2009. Comparative trials of dexlansoprazole compared only with lansoprazole 30 mg demonstrated superior control in esophageal pH values in one trial, and the convenience of being able to dose the drug any time of the day regardless of food intake ( 61 ). Superiority to lansoprazole in healing of erosive esophagitis was demonstrated in one trial, with non-inferiority in another study ( 62 ).…”

Pharmacological and Safety Profile of Dexlansoprazole: A New Proton Pump Inhibitor – Implications for Treatment of Gastroesophageal Reflux Disease in the Asia Pacific Region

“…In addition, as the drug release is pH dependent, dose dumping has not been observed with dexlansoprazole, and there have been no clinically troubling findings for laboratory values, vital signs, or gastric biopsy results. 15 The safety profile of dexlansoprazole 30-90 mg has been shown to be similar to that of lansoprazole. 50 Analysis of pooled data from six phase III randomized controlled trials and a 12-month safety study involved 4270 patients receiving dexlansoprazole 30, 60, or 90 mg, lansoprazole 30 mg, or placebo.…”

“…9 The effects of PPIs tend to diminish during the 24-hour period enabling resumption of gastric acid secretion by uninhibited, restored, or new proton pumps towards the end of the 24-hour dosing interval (if given once daily). 15 Due to the lack of complete efficacy of PPIs during the 24-hour period, some patients report taking twice-daily therapy, which may be prescribed by their clinician or may be self-medicated. 9 In the USA, approximately 30% of PPI prescriptions are twice daily or on-demand (22.2% and 6.8%, respectively).…”

“…14 Suppression of gastric acid secretion by PPIs is at its greatest when proton pumps are the most active. 15 PPIs are the most effective therapy for patients with GERD. 10 PPIs are also given in conjunction with non-steroidal anti-inflammatory drugs for patients with risk factors for upper gastrointestinal bleeding, 14 and for acid suppression in the regimen for Helicobacter pylori eradication.…”

“…18 The active ingredient in a PPI must be present in high concentrations when the proton pumps are stimulated before and during a meal. 15 As PPIs are acid labile, they need protection from degradation in the stomach by enteric coating or buffering. 19 PPIs are rapidly absorbed and subsequently eliminated, leading to a short plasma half-life and ultimately restricting their administration to before meals to achieve their full effect.…”