Comparative pharmacokinetic evaluation of sustained-release theophylline formulations in dogs and humans

Ziad Hussein, Meir Bialer*, Michael Friedman, Itamar Raz

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

19 Scopus citations

Abstract

Several new sustained-release formulations of theophylline were developed and their sustained-release performance was evaluated in a comparative pharmacokinetic analysis. These new formulations, Theo-Dur, Theotrim and aminophylline were administered to 5 dogs and 6 healthy volunteers. Plasma levels of theophylline were determined by an HPLC assay. The absorption profiles of the various formulations were analyzed pharmacokinetically, using the Wagner-Nelson procedure. Two new formulations, Theotrim and Theo-Dur demonstrated very good sustained-release performance in humans and dogs. One formulation (T-2-A) showed incomplete absorption in both species, and its bioavailability relative to aminophylline was about 65% in humans and 78% in dogs. These results were also confirmed by the Wagner-Nelson Procedure. In this study the dog was found to be a good animal model as far as the rate and extent of absorption of the various tested theophylline formulations were concerned; the dog may be useful in primary screening of new formulations from this series.

Original languageEnglish
Pages (from-to)97-102
Number of pages6
JournalInternational Journal of Pharmaceutics
Volume37
Issue number1-2
DOIs
StatePublished - Jun 1987
Externally publishedYes

Keywords

  • Animal model
  • Pharmacokinetics
  • Sustained-release dosage form
  • Theophylline

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