Comparison of oxycodone pharmacokinetics after buccal and sublingual administration in children

Clin Pharmacokinet. 2006;45(7):745-54. doi: 10.2165/00003088-200645070-00009.

Abstract

Objective: We evaluated and compared the pharmacokinetics of two oral administration routes of oxycodone parenteral liquid (10 mg/mL)--single buccal and sublingual administration--in 30 generally healthy awake children, aged 6-91 months.

Methods: Two groups of children undergoing inpatient surgery were enrolled. In a randomised fashion, children received a single dose of oxycodone 0.2 mg/kg buccally (n = 15) or sublingually (n = 15). Regular blood samples were collected for up to 12 hours, and plasma was analysed for oxycodone, oxymorphone and noroxycodone using gas chromatography-mass spectrometry.

Results: Bioavailability was similar after administration at the two instillation sites. The area under the plasma concentration-time curve from time zero extrapolated to infinity (AUCinfinity) was 2400-8000 ng x min/mL (median 4200 ng x min/mL) in the buccal group and 2700-7900 ng x min/mL (median 5500 ng x min/mL) in the sublingual group. After buccal administration, maximum plasma concentration (Cmax) was 5.4-39 ng/mL (16 ng/mL) after buccal and 5.5-42 ng/mL (22 ng/mL) after sublingual administration. Twelve of the 15 children in both groups reached the oxycodone analgesic concentration of 12 ng/mL, which was sustained for 43-209 minutes (median 160 minutes) in the children with buccal oxycodone and for 32-262 minutes (median 175 minutes) in the children with sublingual oxycodone. The terminal elimination half-lives were closely similar in the two groups: 104-251 minutes (median 140 minutes) in the buccal group and 110-190 minutes (150 minutes) in the sublingual group.

Conclusion: The results of this study show that in young children the absorption of oxycodone is similar after buccal and sublingual instillation.

Publication types

  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Buccal
  • Administration, Sublingual
  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / blood
  • Analgesics, Opioid / pharmacokinetics*
  • Area Under Curve
  • Child
  • Child, Preschool
  • Female
  • Gas Chromatography-Mass Spectrometry
  • Half-Life
  • Humans
  • Indicators and Reagents
  • Infant
  • Male
  • Morphinans / blood
  • Oxycodone / administration & dosage
  • Oxycodone / blood
  • Oxycodone / pharmacokinetics*
  • Oxymorphone / blood

Substances

  • Analgesics, Opioid
  • Indicators and Reagents
  • Morphinans
  • noroxycodone
  • Oxymorphone
  • Oxycodone