Comparative bioavailability and pharmacokinetics of three formulations of albuterol.
Albuterol sulfate, alpha'[[1,1-dimethyl)amino]methyl]-4-hydroxy-1,3-benzenedimethanol sulfate, is a relatively selective beta-2-adrenergic bronchodilator used for the relief of bronchospasm. The bioavailability of two 4-mg tablet formulations, differing in their inactive excipients, and a syrup formulation, was evaluated. The three dosage forms were orally administered to 12 normal male volunteers in a randomized three-way crossover study. Plasma samples were collected at frequent time points through 12 h and analyzed for albuterol content by a specific GC-MS method. The drug was rapidly absorbed from all three formulations. Maximum drug concentrations were comparable for the three formulations and were obtained between 1.8-2.0 h. The areas under the plasma concentration-time curves were 68-78 h X ng/mL. The drug elimination phase half-live (t1/2 beta) ranged from 4.8 to 5.5 h. Analysis of the data showed that the bioavailability of albuterol from a tablet formulation is equivalent to that from a solution.
D000284:Administration, Oral; D000328:Adult; D000420:Albuterol / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D001682:Biological Availability; D002133:Calcium Sulfate; D002626:Chemistry, Pharmaceutical; D005079:Excipients; D006801:Humans; D007700:Kinetics; D007785:Lactose; D008297:Male; D012996:Solutions; D013607:Tablets; D013810:Therapeutic Equivalency
D005079:Excipients; D012996:Solutions; D013607:Tablets; D007785:Lactose; D000420:Albuterol; D002133:Calcium Sulfate