Abstract
1 Oxprenolol was administered in single doses by mouth to healthy volunteers either in a polymer-matrix slow-release formulation (Slow Trasicor®) or in osmotic drug-delivery systems (oxprenolol Oros). Plasma oxprenolol concentrations and heart rates after exercise were measured.
2 Plasma concentrations of the drug were maximal at 3 h but negligible at 24 h after administration of Slow Trasicor. Following ingestion of the Oros systems measurable concentrations were maintained throughout 24 h.
3 Significant reduction of exercise-induced tachycardia persisted for 24 h after administration of oxprenolol Oros. With Slow Trasicor heart rate responses had returned to baseline values by this time.
4 The osmotic drug-delivery systems appear to sustain significant β-adrenoceptor blockade for 24 h after a single oral dose.
Keywords: oxprenolol, Oros, dosage, form, plasma, concentrations, β-adrenoceptor, blockade
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