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

Abstract

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 4 mg CR tablet (q12h) compared to a 2 mg conventional table (q6h) for 5 consecutive days. The mean steady state plasma level-time curves for both the CR and conventional tablet treatments were comparable over time and reproducible. There were no significant differences in the AUC or Cmax values between the two treatments. The mean 48-h AUC values were 240.7 and 231.3 h X ng ml-1 for the conventional and CR tablets, respectively, while the corresponding Cmax values ranged from 5.3 to 6.8 ng ml-1 and 5.4 to 6.5 ng ml-1. There were no significant differences in Cmin values except for one 12-h (day 4) value. Cmin values ranged from 3.8 to 4.3 ng ml-1 and 3.0 to 4.8 ng ml-1 for the conventional and CR tablets, respectively. The data show that the 4 mg albuterol CR tablet (q12h) is bioequivalent to a 2 mg conventional albuterol tablet (q6h). The CR 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.