Related Experiment Videos
Relative bioavailability of different oral sustained release oxprenolol tablets
S E Leucuta1, M Follidis, R Capalneanu
1University of Medicine and Pharmacy, Faculty of Pharmacy, Cluj-Napoca, Romania.
European Journal of Drug Metabolism and Pharmacokinetics
|September 2, 1998
Summary
This study evaluated oxprenolol oral dosage forms for bioequivalence. Megaloporous tablets were bioequivalent to Slow-Trasicor, while floating tablets showed varied absorption based on food intake.
Area of Science:
- Pharmacology
- Pharmaceutical Sciences
- Clinical Pharmacy
Background:
- Oxprenolol is a beta-blocker used to manage cardiovascular conditions.
- Assessing the bioequivalence of different oral dosage forms is crucial for therapeutic efficacy and patient safety.
- Various sustained-release and rapid-release formulations of oxprenolol hydrochloride were developed.
Purpose of the Study:
- To determine the bioequivalence of novel oxprenolol hydrochloride oral dosage forms compared to reference products.
- To evaluate the pharmacokinetic profiles and bioavailability of different oxprenolol formulations.
- To assess the impact of food on the absorption of floating slow-release oxprenolol tablets.
Main Methods:
- A triple crossover study involving two groups of 12 healthy volunteers each.
- Administration of single 160 mg doses of oxprenolol hydrochloride in various formulations (megaloporous, hydrophil matrix, Slow-Trasicor, floating, rapid release).
- Serum oxprenolol concentrations were quantified using gas chromatography, followed by pharmacokinetic analysis and statistical evaluation (paired Student's t test).
Main Results:
- Megaloporous oxprenolol tablets demonstrated bioequivalence with the reference product Slow-Trasicor.
- Hydrophil matrix tablets exhibited moderate sustained-release properties.
- Floating slow-release tablets showed significantly enhanced oxprenolol absorption when administered with food, leading to non-bioequivalence with unfed floating tablets and rapid-release tablets. However, fasting floating tablets were bioequivalent to Slow-Trasicor when taken with food.
Conclusions:
- Megaloporous system tablets are bioequivalent to Slow-Trasicor, offering a viable alternative sustained-release formulation.
- The absorption of floating slow-release oxprenolol tablets is significantly influenced by food intake.
- Further investigation into the optimal administration conditions for floating oxprenolol tablets is warranted to ensure consistent therapeutic outcomes.