Comparative steady state bioavailability of conventional and controlled-release formulations of albuterol

✍ Scribed by Mark L. Powell; Miryam Weisberger; Yvonne Dowdy; Richard Gural; Samson Symchowicz; Dr James E. Patrick

• Publisher: John Wiley and Sons
• Year: 1987
• Tongue: English
• Weight: 386 KB
• Volume: 8
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510080506

✦ Synopsis

A new controlled-release (CR) dosage formulation of albuterol has been developed which is suitable for twice-a-day dosing. The present study was conducted in twelve healthy adult male volunteers to compare the steady state plasma levels obtained following repeated administration of a 4mg C R tablet (q12h) compared to a 2mg conventional table (q6h) for 5 consecutive days. The mean steady state plasma level-time curves for both the C R and conventional tablet treatments were comparable over time and reproducible. There were no significant differences in the A U C or C,,, values between the two treatments. The mean 48-h A U C values were 240.7 and 231.3 h X ng ml-' for the conventional and C R tablets, respectively, while the corresponding C,,, values ranged from 5.3 to 6.8 ng ml-' and 5.4 to 6.5 ng ml-I. There were no significant differences in Cmi, values except for one 12-h (day 4) value. C,,, values ranged from 3.8 to 4.3 ng ml-' and 3.0 to 4.8 ng ml-' for the conventional and C R tablets, respectively. The data show that the 4mg albuterol C R tablet (q12h) is bioequivalent to a 2mg conventional albuterol tablet (q6h). The C R tablet formulation will offer the advantage of increased patient compliance; additionally, the CR formulation may prove to be especially beneficial in the treatment of nocturnal asthma.