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The rise and fall of serum theophylline concentration: a comparison of sustained‐release formulations in volunteers with rapid theophylline clearance.
Author(s) -
Mucklow JC,
Kuhn S.
Publication year - 1985
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1985.tb05116.x
Subject(s) - theophylline , pharmacology , medicine , metabolic clearance rate , pharmacokinetics , serum concentration , chemistry , endocrinology
The pharmacokinetics of four sustained‐release formulations of theophylline have been examined after single doses (Nuelin SA, Phyllocontin, Slo‐phyllin and Theo‐Dur) and at steady‐state (Phyllocontin, Theo‐Dur) in six healthy adult volunteers, selected because they all eliminated theophylline rapidly after an intravenous dose of aminophylline. After a single dose of Theo‐Dur, the peak concentration of theophylline was smaller and occurred later than after single doses of Nuelin SA, Phyllocontin and Slo‐phyllin, suggesting that absorption occurs over a longer period. The systemic availability of theophylline was virtually complete after all four formulations. After repeated 12‐hourly dosing to steady‐state, and adjustment of dose to achieve trough concentrations of between 5 and 10 mg l‐1 (28‐55 mumol l‐1), theophylline concentration fluctuated to a significantly greater extent within a dose interval when the subjects were taking Phyllocontin than when they were taking Theo‐Dur.