DEMONSTRATION OF THE IMPORTANCE OF BIPHASIC OLEIC-ACID DELIVERY FOR ENHANCING THE BIOAVAILABILITY OF PROPRANOLOL IN HEALTHY-VOLUNTEERS

Two studies involving six healthy volunteers were carried out to asses s the importance of biphasic rapid and sustained release of oleic acid in enhancing the bioavailability of propranolol using the HALO(TM) dr ug delivery system. The results of the first study showed that mean Cm ax and AUC values for propranolol were increased by at least 300% usin g biphasic HALO(TM)-propranolol capsules compared with Half Inderal(R) LA, both containing an 80mg dose of propranolol. In the second study no significant differences in propranolol bioavailability were observe d between monophasic enteric-coated capsules containing only the susta ined release component of the HALO(TM) delivery system and Half Indera l(R) LA, when an equivalent 8Omg dose of propranolol was administered. The use of improved enteric-coating procedures increased propranolol bioavailability compared with previous studies using biphasic HALOT(TM )-propranolol capsules. The possible explanations for the effectivenes s of biphasic rapid and sustained delivery of oleic acid for enhancing the bioavailability of propranolol are discussed.