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Pharmaceutisch Weekblad

, Volume 13, Issue 2, pp 83–90 | Cite as

Direct high pressure liquid chromatographic analysis and preliminary pharmacokinetics of enantiomers of oxazepam and temazepam with their corresponding glucuronide conjugates

  • T. B. Vree
  • A. M. Baars
  • E. W. Wuis
Articles

Abstract

Three high pressure liquid chromatographic systems for the separation of oxazepam, temazepam and their glucuronides (system A), the separation of theirR,S glucuronide diastereomers (system B) and the chiral separation of the parent drugs (system C) are described. Preliminary pharmacokinetics ofR,S-oxazepam andR,S-temazepam in a human volunteer reveal that the protein binding of the glucuronides is lower than that of the parent drugs, but that there is no difference in protein binding between theR-oxazepam/temazepam andS-oxazepam/temazepam and their corresponding glucuronides. TheS-glucuronide is the main metabolite formed and excreted by man. The plasma ratioR/S-glucuronide is 1∶1 for both oxazepam and temazepam. The renal clearances ofR-temazepam, andS-temazepam are similar, and those ofR-oxazepam andS-oxazepam tend to be different.

Keywords

Chromatography, high pressure liquid Enantiomers Glucuronates Oxazepam Pharmacokinetics Protein binding Temazepam 

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Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1991

Authors and Affiliations

  • T. B. Vree
    • 1
  • A. M. Baars
    • 1
  • E. W. Wuis
    • 1
  1. 1.Department of Clinical PharmacyUniversity Hospital NijmegenHB Nijmegenthe Netherlands

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