Multiple‐Dose Albuterol Kinetics

Abstract
Albuterol a beta‐adrenergic agonist bronchodilator, was studied in 12 healthy male volunteers to evaluate the steady‐state pharmacokinetics following oral administration of 4‐mg tablets, given every six hours for five days. The kinetics of albuterol were best described by a two‐compartment open model with first‐order absorption kinetics. Steady‐state plasma levels were predictable from the kinetic data and were reached by the third day of dosing (ninth and tenth dose). Small accumulation ratios of approximately two were seen based on area under the plasma concentration‐time curve and maximal and minimal concentration data. The elimination phase half‐life was determined to be 6.5 hours, which is similar to the values reported following single‐dose administration.