Paper
Design of a new multiple-unit controlled-release formulation of metoprolol — Metoprolol CR
Published Jan 1, 1988 ·
European Journal of Clinical Pharmacology
68
Citations
3
Influential Citations
Abstract
A new controlled-release (CR) formulation of the β_1-selective adrenoceptor antagonist metoprolol^1 has been developed, aiming at an even 24-h pharmacological effect. In order to achieve this, using a once-daily dose, factors such as absorption characteristics, physicochemical properties, and technological aspects had to be considered. The new formulation, called metoprolol CR, is a disintegrating tablet consisting of several hundred coated pellets of metoprolol succinate, each pellet being its own CR delivery unit.In vitro testing and in vivo studies in healthy volunteers show that the new CR formulation gives continuous delivery of metoprolol throughout the day, resulting in smooth plasma concentration profiles, without peaks and troughs. The release of the drug is independent of pH and other physiological variables, such as food intake, which do not seem to alter the biopharmaceutical properties of the formulation.
The new controlled-release formulation of metoprolol CR provides continuous, smooth, and independent drug delivery throughout the day, independent of pH and physiological variables.
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