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Comparison of the in vitro dissolution properties and in vivo steady-state pharmacokinetics of two sustained-release theophylline preparations

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Abstract

The sustained-release properties and relative bioavailability of Theolin® Retard and Pharphylline® Retard were studied in eight healthy adults after treatment for five days with twice daily 450 mg, respectively 425 mg. During the day-time dosing interval on the fourth and fifth day theophylline plasma concentrations were assayed by HPLC. After intake of Theolin® Retard, minimum theophylline plasma concentrations were significantly higher, fluctuations in theophylline plasma concentrations were significantly smaller andt 75 (the period within a dosing interval during which the plasma concentration exceeds 75% of the maximal concentration) was significantly longer than after Pharphylline® Retard. Maximal concentrations and AUC values were not significantly different. For both products the plasma concentration time-curves on day 5 were significantly lower than on day 4.In vitro dissolution tests confirmed the more sustained release of theophylline from Theolin® Retard. These results indicate an equal extent of absorption from the two products but better sustained-release properties for Theolin® Retard.

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Authors and Affiliations

  1. Department of Analytical Chemistry and Toxicology, State University of Groningen, Ant. Deusinglaan 2, 9713, AW Groningen, the Netherlands

    J. H. G. Jonkman

  2. Department of Biopharmaceutics and Clinical Pharmacology, Pharma Bio-Research International BV, P.O. Box 147, 9400, AC Assen, the Netherlands

    W. J. V. Van Der Boon & G. Grasmeijer

Authors
  1. J. H. G. Jonkman
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  2. W. J. V. Van Der Boon
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  3. G. Grasmeijer
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Jonkman, J.H.G., Van Der Boon, W.J.V. & Grasmeijer, G. Comparison of the in vitro dissolution properties and in vivo steady-state pharmacokinetics of two sustained-release theophylline preparations. Pharmaceutisch Weekblad Scientific Edition 10, 17–21 (1988). https://doi.org/10.1007/BF01966430

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  • DOI: https://doi.org/10.1007/BF01966430

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