Absorption of theophylline from enteric coated and sustained release formulations in fasted and non-fasted subjects

✍ Scribed by Mohamed A. Osman; Rajni B. Patel; David S. Irwin; Peter G. Welling

• Publisher: John Wiley and Sons
• Year: 1983
• Tongue: English
• Weight: 466 KB
• Volume: 4
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510040109

✦ Synopsis

The influence of prior food ingestion, and also of varying fluid volumes, on plasma theophylline levels was examined following single oral doses of two sustained-release formulations, Theobidm (260 mg) and Theo-Dur@ (200 mg) and one partially entericcoated formulation, Choledyl@ (128 mg), to 9 healthy volunteers.

Prior food ingestion tended to delay the absorption of theophylline from all formulations to a small extent. This effect was observed only at early sampling times, and plasma dru profiles were similar for all treatments within a particular formulation.

sustained-release formulations, with mean C,,, values of 5 -5 7 pg ml-(Theobid@) and 2.8-3.2 pgml-(Theo-Dur@) occurring at 53-9.1 h after dosing. Choledyl@ gave rise to a longer absorption lag time than the other formulations but was subsequently absorbed at a faster rate yielding mean C,,, values of 3.2-3.5 pgml-at 2.8-4.1 h.

The intersubject variability in theophylline plasma levels, and also in most pharmacokinetic parameter values, was generally less following Theo-Dur@ compared to the other formulations.

Theobid 8 and Theo-Dur@ gave rise to plasma profiles that were characteristic of KEY WORDS Theophylline pharmacokinetics Plasma levels Food Bioavailability