Relative bioavailability of a controlled‐release albuterol formulation for twice‐daily use

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Abstract
A two‐way‐crossover bioavailability study was completed with 15 healthy male volunteers to evaluate the relative bioavailability of an orally administered controlled‐release (CR) formulation of albuterol as compared to the immediate‐release (IR) formulation of albuterol. The CR formulation of albuterol used in this study was based mechanistically on the elementary osmotic pump.1 Each subject received one 8 mg CR tablet every 12 h for 8 consecutive days and one 4 mg IR tablet every 6 h for 8 consecutive days, with 7 days separating each phase. During day 8 of dosing, hourly blood samples (0–12 h) were collected after the morning dose and three additional samples were obtained 16, 20 and 24 h following this dose. Plasma concentrations were measured using a gas chromatography‐mass spectrometry procedure. No statistically significant differences were observed in mean steady‐state values for Cmax AUC(0–12 h) and peak‐to‐trough fluctuations (PTF) in comparing the two dosage formulations. Mean steady state Tmax values were 2.6 and 6.0 h for the TR and CR formulations, respectively. It was concluded that twice daily administration of the controlled‐release formulation of albuterol provides an alternative to four times daily administration of conventional (immediate‐release) albuterol tablets.

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