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Pharmaceutisch Weekblad

, Volume 10, Issue 1, pp 17–21 | Cite as

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

  • J. H. G. Jonkman
  • W. J. V. Van Der Boon
  • G. Grasmeijer
Original Articles

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 andt75 (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.

Key words

Bioavailability Dissolution rate Drug evaluation Pharmacokinetics Side effects Tablets, sustained release Theophylline 

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Copyright information

© Bohn, Scheltema & Holkema 1988

Authors and Affiliations

  • J. H. G. Jonkman
    • 1
  • W. J. V. Van Der Boon
    • 2
  • G. Grasmeijer
    • 2
  1. 1.Department of Analytical Chemistry and ToxicologyState University of GroningenAW Groningenthe Netherlands
  2. 2.Department of Biopharmaceutics and Clinical PharmacologyPharma Bio-Research International BVAC Assenthe Netherlands

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