Pharmacokinetics and relative Bioavailability of Oral Theophylline Capsules

The oral bioavailability of liquid-filled theophylline capsules relative to a nonalcoholic aminophylline solution was determined in normal volunteers. In addition, theophylline absorption and elimination kinetics were reexamined. There were no statistically significant differences between the bioava...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1979-11, Vol.68 (11), p.1392-1394
Main Authors: Lesko, L.J., Walker, D., Brousseau, D.R., Canada, A.T., Eastwood, G.
Format: Article
Language:English
Subjects:
Adult
bioavailability
Bioavailability-theophylline
Bioavailability—theophylline, various oral dosage forms
Biological Availability
capsule compared to liquid
Capsules
Female
Humans
Kinetics
Male
Muscle relaxants (smooth muscle)-theophylline
Muscle relaxants (smooth muscle)—theophylline, oral dosage forms, pharmacokinetics, bioavailability, capsule compared to liquid
oral dosage forms
pharmacokinetics
Theophylline - administration & dosage
Theophylline - blood
Theophylline - metabolism
Theophylline-oral dosage forms
Theophylline—oral dosage forms, pharmacokinetics, bioavailability, capsule compared to liquid
various oral dosage forms
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Summary:The oral bioavailability of liquid-filled theophylline capsules relative to a nonalcoholic aminophylline solution was determined in normal volunteers. In addition, theophylline absorption and elimination kinetics were reexamined. There were no statistically significant differences between the bioavailability of capsules and liquid as measured by the area under the curve (AUC) from time 0 -→ ∞ (p > 0.05). The bioavailability parameters of Cmax, tmax, and AUC were determined from actual serum theophylline concentration-time data and from a nonlinear least-squares fit of the serum concentration-time data. Theophylline absorption from the capsules was noticeably faster than from the liquid in most subjects, although the differences in absorption rates were not significantly different (p > 0.05). The determined apparent volume of distribution, elimination half-life, and plasma clearance of theophylline were similar to values reported by other investigators. Marked inter- and intraindividual variations in the elimination half-life were noted.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600681114