Single dose and steady-state pharmacokinetics of 4 mg and 8 mg oral salbutamol controlled-release in patients with bronchial asthma

Eur J Clin Pharmacol. 1989;37(1):49-52. doi: 10.1007/BF00609424.

Abstract

Fifteen patients with asthma were given salbutamol controlled-release (SCR) 4 mg or 8 mg twice daily for seven days, in a randomised double-blind cross-over design. Plasma salbutamol levels were measured after the first and fifteenth doses for a 12 h period following drug ingestion. At steady-state the geometric mean values for Cmax were 8.2 ng/ml for 4 mg, and 16.1 ng/ml for 8 mg. Median tmax values were 300 and 240 min respectively. The geometric mean AUC (0-12) were 4507 ng.min.ml-1 and 8980 ng.min/ml. Peak to trough fluctuation ratios were 0.577 and 0.572. There were no significant differences between 4 mg or 8 mg formulations, for any of the parameters measured, after appropriate corrections for dose. The concentration-time profiles at steady-state showed little fluctuation in plasma salbutamol levels over the twelve hour dosing interval. These results show that 4 mg and 8 mg formulations of SCR provide smooth plasma profiles at steady-state with a twice daily dosing regime.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Albuterol / administration & dosage
  • Albuterol / pharmacokinetics*
  • Albuterol / therapeutic use
  • Asthma / drug therapy*
  • Asthma / physiopathology
  • Delayed-Action Preparations
  • Double-Blind Method
  • Female
  • Forced Expiratory Volume
  • Humans
  • Male
  • Middle Aged
  • Randomized Controlled Trials as Topic
  • Time Factors

Substances

  • Delayed-Action Preparations
  • Albuterol