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Comparison of oxycodone pharmacokinetics after buccal and sublingual administration in children
Hannu Kokki1, Ilpo Rasanen, Merja Lasalmi
1Department of Anaesthesiology and Intensive Care, Kuopio University Hospital, Kuopio, Finland. hannu.kokki@kuh.fi
Insights
Buccal and sublingual administration of oxycodone showed similar absorption in young children. This study compared the pharmacokinetics of these two oral routes for effective pain management in pediatric patients.
Area of Science:
- Pharmacology
- Pediatric Anesthesiology
- Pharmacokinetics
Background:
- Oxycodone is a common analgesic used in pediatric patients.
- Understanding optimal administration routes is crucial for effective pain management.
- Buccal and sublingual routes offer potential for rapid absorption.
Purpose of the Study:
- To compare the pharmacokinetics of buccal versus sublingual administration of oxycodone in children.
- To evaluate the absorption, distribution, and elimination of oxycodone via these two oral routes.
- To determine if one route offers superior bioavailability or faster onset of action.
Main Methods:
- Thirty generally healthy children (6-91 months) undergoing surgery were enrolled.
- Participants were randomized to receive a single dose of oxycodone (0.2 mg/kg) buccally or sublingually.
- Plasma samples were collected for 12 hours and analyzed for oxycodone and its metabolites using gas chromatography-mass spectrometry.
Main Results:
- Bioavailability was comparable between buccal and sublingual administration sites.
- Median area under the plasma concentration-time curve (AUCinfinity) was 4200 ng x min/mL (buccal) vs. 5500 ng x min/mL (sublingual).
- Median time to reach analgesic concentration (12 ng/mL) was 160 minutes (buccal) vs. 175 minutes (sublingual), with similar terminal elimination half-lives.
Conclusions:
- Buccal and sublingual administration of oxycodone result in similar pharmacokinetic profiles in young children.
- Both routes provide comparable absorption and achieve therapeutic analgesic concentrations.
- These findings support the use of either buccal or sublingual administration for effective oxycodone delivery in pediatric patients.
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.
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