Pharmacokinetics of oxatomide given percutaneously to healthy volunteers

Biopharm Drug Dispos. 1992 Oct;13(7):495-502. doi: 10.1002/bdd.2510130703.

Abstract

The percutaneous absorption of oxatomide gel at 5 per cent concentration was studied after single and repeated administration (85 mg b.i.d.) in six male and six female healthy volunteers, aged 25.7 +/- 0.8 years (mean +/- SEM) weighing 64.4 +/- 4.5 kg and the results compared with those obtained following a single oral dose (30 mg). The measurement of oxatomide was by means of a new sensitive and specific HPLC assay with limits of detection of 0.2 ng ml-1 in plasma and 1.0 ng ml-1 in urine. Poor percutaneous absorption was confirmed by the peak plasma concentrations which were 5.03 +/- 0.79 ng ml-1 following application of the gel for 7 days and 10.08 +/- 1.29 ng ml-1 following oral administration; the corresponding amounts of unchanged oxatomide recovered from 24 h urine collections were 1.42 +/- 0.39 micrograms and 3.93 +/- 0.92 micrograms.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Cutaneous
  • Administration, Oral
  • Adult
  • Drug Administration Schedule
  • Female
  • Gels
  • Histamine H1 Antagonists / administration & dosage
  • Histamine H1 Antagonists / blood
  • Histamine H1 Antagonists / pharmacokinetics*
  • Humans
  • Male
  • Piperazines / administration & dosage
  • Piperazines / blood
  • Piperazines / pharmacokinetics*
  • Reference Standards
  • Reproducibility of Results
  • Skin Absorption

Substances

  • Gels
  • Histamine H1 Antagonists
  • Piperazines
  • oxatomide