Single-dose pharmacokinetic and pharmacodynamic comparison of polymer-matrix (Slow Trasicor) and Oros dosage forms of oxprenolol in healthy volunteers.
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. 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. 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. The osmotic drug-delivery systems appear to sustain significant beta-adrenoceptor blockade for 24 h after a single oral dose.
D000328:Adult; D003692:Delayed-Action Preparations; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008297:Male; D010096:Oxprenolol / Q000008:administration & dosage / Q000378:metabolism* / Q000494:pharmacology; D005082:Physical Exertion
D003692:Delayed-Action Preparations; D010096:Oxprenolol