Temporal Variations in Trough Serum Theophylline Concentrations at Steady State

• Published in: Journal of pharmaceutical sciences 1980-03, Vol.69 (3), p.358-359
• Main Authors: Lesko, L.J., Brousseau, D., Canada, A.T., Eastwood, G.
• Format: Article
• Language: English
• Subjects: Adult; Aminophylline - metabolism; Bronchodilators-theophylline; Bronchodilators—theophylline, trough serum concentrations at steady state, temporal variations; Delayed-Action Preparations; Female; Humans; Kinetics; Male; Pharmacokinetics-theophylline; Pharmacokinetics—theophylline, trough serum concentrations at steady state, temporal variations; temporal variations; Theophylline - administration & dosage; Theophylline - blood; Theophylline-trough serum concentrations at steady state; Theophylline—trough serum concentrations at steady state, temporal variations; Time Factors; trough serum concentrations at steady state
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.2600690332

Temporal variations in serum theophylline concentrations were observed in 14 healthy volunteers receiving multiple doses of theophylline. After repeated oral doses (6.9–18.2mg/kg/day) of theophylline as either a nonalcoholic aminophylline solution or a controlled-release capsule, trough theophylline levels at steady state were significantly higher (p < 0.05) in the morning than in the afternoon or evening. With the solution, the mean (±SE) trough serum level at 7am was 11.1 ± 0.9 μg/ml, and at 1pm it was 9.6 ± 0.8 μg/ml. With the capsule, the mean (±SE) trough serum level at 8am was 13.8 ± 0.9 μg/ml, and at 8pm it was 10.7 ± 0.9 μg/ml. Temporal variations in serum theophylline concentrations have not been reported previously and may be important in therapeutic monitoring.