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Comparative pharmacokinetic analysis of a novel sustained-release dosage form of theophylline in humans

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Summary

The pharmacokinetics and relative bioavailability of theophylline from a new sustained-release formulation (Theotard®) and from a standard sustained-release formulation (Theo-Dur®) were compared in 6 healthy, adult, male volunteers. After a single oral dose of 300 mg Theotard, a mean maximal plasma concentration (Cbmax of 3.49±1.05 mg/l was obtained after 8 h (tmax). After an identical dose of Theo-Dur, a peak plasma concentration of 4.68±1.33 mg/l was obtained after 6.33 h. The mean relative bioavailability of theophylline from Theotard was 1.02±0.16 relative to that of Theo-Dur. In 5 of the volunteers the Theotard formulation exhibited a more prolonged and uniform absorption rate and yielded more sustained plasma levels.

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Raz, I., Bialer, M., Salame, K. et al. Comparative pharmacokinetic analysis of a novel sustained-release dosage form of theophylline in humans. Eur J Clin Pharmacol 26, 401–403 (1984). https://doi.org/10.1007/BF00548775

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