Abstract
1 Plasma concentrations of oxprenolol have been measured in six healthy volunteers following single-dose oral administration of the drug in conventional and Oros dosage forms in fasting and postprandial states.
2 After the Oros system, plasma concentrations reached peaks in most subjects at 3-8 h after dosing and were approximately 25% of those achieved with the conventional tablet. Plasma concentrations were well sustained for at least 24 h. A secondary peak occurred consistently at 12 h, possibly reflecting a transient change in clearance and/or distribution of the drug following the evening meal.
3 With each formulation, plasma drug concentration profiles following administration in the fasting state did not differ significantly from those obtained when the drug was given postprandially.
4 Drug absorption in vivo corresponded reasonably closely with in vitro drug release from the Oros system.
Keywords: oxprenolol, food, plasma concentration
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- BRANDT J. L., CASTLEMAN L., RUSKIN H. D., GREENWALD J., KELLY J. J., Jr The effect of oral protein and glucose feeding of splanchnic blood flow and oxygen utilization in normal and cirrhotic subjects. J Clin Invest. 1955 Jul;34(7 Pt 1):1017–1025. doi: 10.1172/JCI103151. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Dawes C. P., Kendall M. J., Welling P. G. Bioavailability of conventional and slow-release oxprenolol in fasted and nonfasted individuals. Br J Clin Pharmacol. 1979 Mar;7(3):299–302. doi: 10.1111/j.1365-2125.1979.tb00936.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Degen P. H., Riess W. Simplified method for the determination of oxprenolol and other beta-receptor-blocking agents in biological fluids by gas-liquid chromatography. J Chromatogr. 1976 Jun 9;121(1):72–75. doi: 10.1016/s0021-9673(00)82299-2. [DOI] [PubMed] [Google Scholar]
- George C. F., Blackwell E. W., Davies D. S. Metabolism of isoprenaline in the intestine. J Pharm Pharmacol. 1974 Apr;26(4):265–267. doi: 10.1111/j.2042-7158.1974.tb09268.x. [DOI] [PubMed] [Google Scholar]
- Kahela P., Anttila M., Tikkanen R., Sundquist H. Effect of food, food constituents and fluid volume on the bioavailability of sotalol. Acta Pharmacol Toxicol (Copenh) 1979 Jan;44(1):7–12. doi: 10.1111/j.1600-0773.1979.tb02288.x. [DOI] [PubMed] [Google Scholar]
- Mason W. D., Winer N. Pharmacokinetics of oxprenolol in normal subjects. Clin Pharmacol Ther. 1976 Oct;20(4):401–412. doi: 10.1002/cpt1976204401. [DOI] [PubMed] [Google Scholar]
- McLean A. J., Isbister C., Bobik A., Dudley F. J. Reduction of first-pass hepatic clearance of propranolol by food. Clin Pharmacol Ther. 1981 Jul;30(1):31–34. doi: 10.1038/clpt.1981.123. [DOI] [PubMed] [Google Scholar]
- Melander A., Danielson K., Scherstén B., Wåhlin E. Enhancement of the bioavailability of propranolol and metoprolol by food. Clin Pharmacol Ther. 1977 Jul;22(1):108–112. doi: 10.1002/cpt1977221108. [DOI] [PubMed] [Google Scholar]
- Melander A. Influence of food on the bioavailability of drugs. Clin Pharmacokinet. 1978 Sep-Oct;3(5):337–351. doi: 10.2165/00003088-197803050-00001. [DOI] [PubMed] [Google Scholar]
- Vaughan D. P., Dennis M. Mathematical basis of point-area deconvolution method for determining in vivo input functions. J Pharm Sci. 1978 May;67(5):663–665. doi: 10.1002/jps.2600670524. [DOI] [PubMed] [Google Scholar]
- Walle T., Fagan T. C., Walle U. K., Oexmann M. J., Conradi E. C., Gaffney T. E. Food-induced increase in propranolol bioavailability--relationship to protein and effects on metabolites. Clin Pharmacol Ther. 1981 Dec;30(6):790–795. doi: 10.1038/clpt.1981.239. [DOI] [PubMed] [Google Scholar]