A new esomeprazole packet (sachet) formulation for suspension: in vitro characteristics and comparative pharmacokinetics versus intact capsules/tablets in healthy volunteers

Bladh, Nina; Blychert, Eva; Johansson, Karin; Backlund, Anna; Lundin, Christina; Niazi, Mohammad; Pettersson, Gunilla; Fjellman, Mia

doi:10.1016/j.clinthera.2007.03.014

Cited by 24 publications

(9 citation statements)

References 11 publications

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“…The mean plasma concentration-time curves for dexlansoprazole and esomeprazole in our study were generally similar to that reported in the literature 2,13–15. Following administration of a single dose of dexlansoprazole modified-release 60 mg, the mean plasma concentration-time curve displayed two peaks at approximately 2 and 5 hours postdose, which are representative of the dual delayed-release characteristics of the dexlansoprazole modified-release capsule; in addition, plasma concentrations were generally detectable throughout the 24-hour postdose interval.…”

Section: Resultssupporting

confidence: 90%

Comparator pH study to evaluate the single-dose pharmacodynamics of dual delayed-release dexlansoprazole 60 mg and delayed-release esomeprazole 40 mg

Kukulka¹,

Eisenberg²,

Nudurupati³

2011

CEG

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Background:This paper describes a Phase 1, single-center, randomized, open-label, two-period crossover study which compared the pharmacodynamic effects of single doses of dexlansoprazole modified-release 60 mg and esomeprazole 40 mg on 24-hour intragastric pH in healthy adult subjects.Methods:Forty-four subjects aged 20–54 years were randomized in a 1:1 ratio to two sequence groups defining the order in which they received dexlansoprazole and esomeprazole in periods 1 and 2. Primary pharmacodynamic end points over 24 hours postdose were percentage of time with intragastric pH > 4 and mean pH, and secondary pharmacodynamic end points were percentage of time intragastric pH > 4, and mean pH at 0–12 hours, and at >12–24 hours postdose. Each drug was given after an overnight fast and one hour before breakfast. Continuous pH recording began immediately before dosing through to 24 hours postdose.Results:At 0–24 hours postdose, the mean percentage of time with pH > 4 for dexlansoprazole and esomeprazole was 58% and 48%, respectively; the difference was statistically significant (P = 0.003). The average of mean pH values at 0–24 hours postdose for dexlansoprazole and esomeprazole were 4.3 and 3.7, respectively; the difference was statistically significant (P < 0.001). At >12–24 hours postdose, mean percentage of time with pH > 4 and average of mean pH were greater for dexlansoprazole (60% and 4.5, respectively) compared with esomeprazole (42% and 3.5, respectively); the difference was statistically significant (P < 0.001 for both intervals). At 0–12 hours postdose, the difference in dexlansoprazole and esomeprazole values for the pharmacodynamic end points was not statistically significant.Conclusion:For the entire 24-hour postdose period, predominantly resulting from the >12–24-hour postdose interval, the average intragastric pH following a single dose of dexlansoprazole 60 mg was higher compared with that observed following a single dose of esomeprazole 40 mg, and the difference was statistically significant.

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Section: Resultssupporting

confidence: 90%

Comparator pH study to evaluate the single-dose pharmacodynamics of dual delayed-release dexlansoprazole 60 mg and delayed-release esomeprazole 40 mg

Kukulka¹,

Eisenberg²,

Nudurupati³

2011

CEG

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“…However, esomeprazole levels increase in patients with severe hepatic impairment. 21 Esomeprazole is available as a tablet, capsule, and oral suspension, with similar absorption for all three, 22,23 as well as for intravenous usage. 24 Esomeprazole has a low potential for interaction with other drugs, 14 but may interact with inducers or inhibitors of CYP2C19 and CYP3A4, such as voriconazole and clarithromycin, which can double esomeprazole systemic exposure.…”

Section: Metabolism and Pharmacokinetic Profilementioning

confidence: 99%

Section: Mechanism Of Action Metabolism and Pharmacokinetic Profilementioning

confidence: 99%

Gastric Acid-Related Diseases: Focus on Esomeprazole

Al-Judaıbı¹,

Chande²,

Sultan

et al. 2010

Clinical Medicine Insights: Therapeutics

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Esomeprazole (S-omeprazole) is a single optical enantiomer proton-pump inhibitor (PPI) approved for the management of gastro-oesophageal reflux disease, the prevention and treatment of Non-Steroidal Anti-Inflammatory Drugs (NSAID) associated gastric ulcer disease, treatment of duodenal ulcer disease associated with Helicobacter pylori infection, and the treatment of Zollinger-Ellison syndrome. Esomeprazole has been shown to be safe and effective during pregnancy and was introduced to the market in 2001. PPI therapy may interact with clopidogrel by cytocrome 2C19. Clopidogrel is a prodrug which is partially activated by cytochrome 2C19 and esomeprazole is a competitive inhibitor of 2C19. Esomeprazole is more effective than other PPIs in controlling esophageal and gastric pH, but efficacy in symptom relief is less clear.

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“…The C max of sachet formulation was 2.84 being closer to the capsule (3.16) and tablet (2.98) formulation. [7] Gastro-esophageal reflux disease (GERD) is a very common problem faced by patients which was treated by prescribing esomeprazole in combination with domperidone by the physicians. To minimize the number of tablets, and for long term therapy, a fixed dose combination (FDC) capsule was developed with no pharmacokinetic profile.…”

Section: Introductionmentioning

confidence: 99%

An Overview on Formulations and Their Evaluation of Esomeparozle – A Proton Pump Inhibitor

Haq¹,

Ailaboyina²,

Tirunagari³

2019

IRJPS

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Esomeprazole, a proton pump inhibitor (PPI) is known to be widely used due to its properties and reduced side effects. There have been many publications in the literature concerning the various formulations with respect to treating various other diseases in combination with other drugs such as antibiotics. Therefore, it was found necessary to present a collective data on the various formulations. The present review is focused on briefing the literature on the formulations of esomeprazole which can be helpful to get further innovative ideas to develop new formulations with increased efficacy.

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A new esomeprazole packet (sachet) formulation for suspension: in vitro characteristics and comparative pharmacokinetics versus intact capsules/tablets in healthy volunteers

Cited by 24 publications

References 11 publications

Comparator pH study to evaluate the single-dose pharmacodynamics of dual delayed-release dexlansoprazole 60 mg and delayed-release esomeprazole 40 mg

Comparator pH study to evaluate the single-dose pharmacodynamics of dual delayed-release dexlansoprazole 60 mg and delayed-release esomeprazole 40 mg

Gastric Acid-Related Diseases: Focus on Esomeprazole

An Overview on Formulations and Their Evaluation of Esomeparozle – A Proton Pump Inhibitor

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