Abstract
Metoprolol, a β 1-adrenergic blocker, was formulated into a number of sustained-release formulations. Some of these were prepared by a spray-drying technique specially developed by us to produce homogeneous spherical microparticles, 5–20 μm, which could then be compressed into tablets. The application of this technique, which is usually employed in the food industry, to pharmaceuticals provides an innovative means of formulating slow-release drugs, specially for highly water-soluble compounds. Our formulations were compared with a commercially available product, Lopresor Divitab (Ciba-Geigy) and with “nonfonnulated” metoprolol in in vitro and in vivo (dogs) tests. The kinetics of the rate of release in simulated gastrointestinal juices of the active ingredient from the sustained-release formulations were found to fit best to the Hixon-Crowell equation. Statistical treatment of the pharmacokinetic data obtained in the in vivo tests showed that there were no significant differences between our products and the commercially available formulation. These encouraging results open the way for the possible testing of our formulations on human volunteers.
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