The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open‐label crossover study

Proton pump inhibitors (PPIs) effectively block gastric acid secretion and are the treatment of choice for heartburn. PPIs differ, however, in onset of action and bioavailability. In this single‐center, open‐label, three‐way crossover study, onset of action of immediate‐release omeprazole 20 mg/sodium bicarbonate 1100 mg (IR‐OME) and delayed‐release (DR) lansoprazole 15 mg was evaluated in 63 healthy fasting adults. Subjects were randomized to once daily IR‐OME, or DR‐lansoprazole, or no treatment for 7 days. The primary efficacy endpoint was the earliest time where a statistically significant difference was observed between IR‐OME and DR‐lansoprazole in median intragastric pH scores for three consecutive 5‐min intervals on day 7. Secondary endpoints compared effects of active treatments on days 1 and 7 (e.g., time to sustained inhibition, percentage of time with pH >4). A significant difference in median intragastric pH favoring IR‐OME was observed on day 7 starting at the 10‐ to 15‐min interval postdosing (P = 0.024) and sustaining through the 115‐ to 120‐min interval (P = 0.017). On day 1, IR‐OME achieved sustained inhibition of intragastric acidity significantly faster than DR‐lansoprazole. IR‐OME maintained pH >4 significantly longer than DR‐lansoprazole over a 24‐h period (P = 0.007) on day 7. Overall, results of this study demonstrate IR‐OME is safe and well tolerated and that treatment with IR‐OME results in significantly faster onset of action and better gastric acid suppression at steady state than DR‐lansoprazole.

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“…; Shin et al. ) as the objective measurement of pH is not known to be prone to placebo effect or subject rating bias.…”

Section: Methodsmentioning

confidence: 99%

A randomized, crossover pharmacodynamic study of immediate‐release omeprazole/sodium bicarbonate and delayed‐release lansoprazole in healthy adult volunteers

Pratha

McGraw

Tobin³

2016

Pharmacology Res & Perspec

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“…[28][29][30] Accordingly, ilaprazole is expected to have a longer duration of action and less NAB compared to other PPIs. 31,32 But we found that GERD symptoms, 24-hour mean gastric pH, nocturnal mean gastric pH, frequency and duration of NAB, were comparable between the ilaprazole and omeprazole groups. The only significant difference was occurrence of lesser number of NAB episodes in the ilaprazole group.…”

Section: Discussionmentioning

confidence: 68%

Esophageal Acidification During Nocturnal Acid-breakthrough with Ilaprazole Versus Omeprazole in Gastroesophageal Reflux Disease

Karyampudi

Ghoshal

Singh

et al. 2017

J Neurogastroenterol Motil

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Background/AimsThough nocturnal acid-breakthrough (NAB) is common in gastroesophageal reflux disease (GERD) patients, its clinical importance results from esophageal acidification, which has been shown to be uncommon. Ilaprazole, a long-acting proton pump inhibitor, may cause NAB infrequently. Accordingly, we studied prospectively, (1) frequency and degree of esophageal acidification during NAB, and (2) frequency and severity of NAB while on ilaprazole versus omeprazole. MethodsFifty-eight consecutive patients with GERD on once daily ilaprazole, 10 mg (n = 28) or omeprazole, 20 mg (n = 30) for > one month underwent 24-hour impedance-pH monitoring prospectively. NAB was defined as intra-gastric pH < 4 for > one hour during night, and esophageal acidification as pH < 4 for any duration. Nocturnal symptoms (heartburn, regurgitation, and chest pain) were also recorded. Results Of ConclusionsThough NAB was common while patients were on a proton pump inhibitor, esophageal acidification was uncommon. Frequency and severity of NAB were comparable among patients on ilaprazole and omeprazole, except for the lesser number of NABs with ilaprazole.

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“…13 Thus, many physicians from this study also opine that almost half of the patients of APD could be the potential candidates for longer acting PPIs for better symptomatic control. Expert opinion by Bartoli et al highlights that, ilaprazole (10 mg) is better than conventional PPIs like pantoprazole, rabeprazole etc.…”

Section: Discussionmentioning

confidence: 76%

Prescribing pattern of proton pump inhibitors in the management of acid peptic disorders, focus on ilaprazole

Mayabhate

2016

Int J Basic Clin Pharmacol

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INTRODUCTIONAcid peptic disorders (APDs) are a collective term that includes many conditions such as peptic ulcer disease, GERD and Gastritis. Acid peptic disorders are the result of distinctive, but overlapping pathogenic mechanisms leading to either excessive acid secretion or diminished mucosal defense. The prevalence of gastroesophageal reflux disease (GERD) in India is likely to be between 8% and 19%, which is comparable to GERD prevalence rates published in western countries.2 Peptic ulcer disease (PUD) tends to have a chronic remitting course with imperfect correlation between symptoms and the presence of an ulcer. Each year PUD affects 4 million people around the world. A recent study by Dutta AK et al showed a time trends in epidemiology of peptic ulcer disease in India and observed the frequencies of 2.9% for duodenal ulcer and 2.7% gastric ulcer from 1988 to 2008. The causes of APD include H. Pylori infection, over use of NSAIDS, smoking and alcohol consumption and it is also linked with stress and dietary factors such as spicy and oily food. The increase in incidence of APD in the current scenario can be linked to the present stressful lifestyles. Patients commonly present with nausea, heartburn, dysphagia and abdominal pain. If left ABSTRACT Background: Acid peptic disorders (APDs) result from characteristic but overlapping pathogenic mechanisms that involve acid effects on diminished mucosal defense. Proton pump inhibitors (PPIs) have become a mainstay in the APDs. This survey was aimed to determine the usage profile of different proton pump inhibitors and overall physicians' opinion about the clinical experience with newer PPI, ilaprazole. Methods: This survey was based on the clinical experience of 107 randomly selected physicians on an aggregate patient basis in the management of acidpeptic disorders from different parts of India. A data report form (DRF) comprising of various questions was answered by these physicians. The responding physicians answered the DRF of patients who suffered from acidpeptic disorders and were eligible for PPI therapy. A minimum of 50 patients per physician were evaluated in this survey. Results: The commonly encountered APD in physicians' clinical practice were gastroesophageal reflux disorder (GERD) followed by non-ulcer disease. 58.88% physicians highlighted the prevalence of night time symptoms of APD reported by the patients. About 1/4th physicians were of the opinion that longacting PPIs would be the preferred to offer 24 hour control of gastric acid secretion thereby controlling the nocturnal symptoms. 63.73% of physicians reported significantly better symptomatic relief with once daily dose of ilaprazole than existing PPIs. Conclusions: This survey highlights the lack of 24 hour acid control in APDs with use of conventional PPIs leading to variety of symptoms, especially at night, seriously hampering the sleep quality. Ilaprazole displays important advantages in the clinical settings, with regard to better probability of extending the inhibition of acid secret...

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The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open‐label crossover study

Abstract: SUMMARY BackgroundIlaprazole, a proton pump inhibitor (PPI) currently in clinical use, may provide improved acid suppression vs. other PPIs.

Cited by 29 publications

References 17 publications

A randomized, crossover pharmacodynamic study of immediate‐release omeprazole/sodium bicarbonate and delayed‐release lansoprazole in healthy adult volunteers

A randomized, crossover pharmacodynamic study of immediate‐release omeprazole/sodium bicarbonate and delayed‐release lansoprazole in healthy adult volunteers

Esophageal Acidification During Nocturnal Acid-breakthrough with Ilaprazole Versus Omeprazole in Gastroesophageal Reflux Disease

Prescribing pattern of proton pump inhibitors in the management of acid peptic disorders, focus on ilaprazole

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