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Pharmacokinetics of oxycodone after intravenous, buccal, intramuscular and gastric administration in children
Hannu Kokki1, Ilpo Rasanen, Matti Reinikainen
1Department of Anaesthesiology and Intensive Care, Kuopio University Hospital, Kuopio, Finland. hannu.kokki@kuh.fi
Insights
Pharmacokinetics of intravenous oxycodone in children are similar to adults. Intramuscular administration offers consistent absorption, while buccal and gastric routes show significant variability in pediatric patients.
Area of Science:
- Pediatric pharmacology
- Pain management
- Drug absorption and distribution
Background:
- Oxycodone is a widely used analgesic.
- Understanding its pharmacokinetic profile in children is crucial for safe and effective pain management.
- Parenteral liquid formulations offer flexibility in administration, but route-specific data in pediatric populations is limited.
Purpose of the Study:
- To evaluate and compare the pharmacokinetics of oxycodone parenteral liquid (10 mg/mL) across four different administration routes in children.
- To assess single intravenous, intramuscular, buccal, and gastric administration of oxycodone.
- To determine the bioavailability and absorption characteristics of each route in pediatric patients.
Main Methods:
- A study involving 40 generally healthy children aged 6-93 months undergoing inpatient surgery.
- Administration of a single dose of oxycodone (0.1 mg/kg) via intravenous, intramuscular, buccal, or gastric routes post-anesthesia induction.
- Serial blood sample collection for up to 12 hours, with plasma oxycodone levels quantified using gas chromatography-mass spectrometry.
Main Results:
- Intravenous administration yielded the highest peak drug concentration (mean 82 µg/L).
- Intramuscular administration showed relatively constant absorption (bioavailability 0.68), while buccal (bioavailability 0.55) and gastric (bioavailability 0.37) routes exhibited large interindividual variations in absorption rate and extent.
- Terminal elimination half-lives were similar across all four administration routes, ranging from 73 to 246 minutes.
Conclusions:
- The pharmacokinetics of intravenous oxycodone in children aged 6-93 months closely resemble those reported in adults.
- Intramuscular administration of oxycodone in children provides predictable drug absorption.
- Buccal and gastric administration routes in pediatric patients are associated with significant interindividual variability in drug absorption, necessitating careful consideration in clinical practice.
Objective:
To evaluate the pharmacokinetics of four administration routes of oxycodone parenteral liquid (10 mg/mL), single intravenous and intramuscular injections and buccal and gastric administration, in children.
Patients And Participants:
Forty generally healthy children, aged 6-93 months, undergoing inpatient surgery.
Methods:
After induction of anaesthesia, children received a single dose of oxycodone 0.1 mg/kg intravenously (n = 9), intramuscularly (n = 10), buccally (n = 11) or via an orogastric tube into the stomach (n = 10). Regular blood samples were collected up to 12 hours, and plasma was analysed for oxycodone using gas chromatography-mass spectrometry (limit of quantification 1 microg/L).
Results:
The peak drug concentration observed was 57-110 (mean 82) microg/L after intravenous administration, 23-54 (34) microg/L after intramuscular administration, 3.9-14 (9.8) microg/L after buccal administration and 1.7-15 (9.2) microg/L after gastric administration. The time to peak concentration was 2-30 (16) minutes in the intramuscular group, 30-480 (221) minutes in the buccal group and 60-360 (193) minutes in the gastric group. The terminal elimination half-lives were closely similar in the four groups: 124-208 (163) minutes in the intravenous group, 162-227 (150) minutes in the intramuscular group, 73-234 (150) minutes in the buccal group and 80-246 (147) minutes in the gastric group. Area under the concentration-time curve (AUC) was 5037-8954 (6612) microg x min/L in the intravenous group, 3084-5524 (4473) microg x min/L in the intramuscular group, 1444-5560 (3658) microg x min/L in the buccal group and 692-3843 (2436) microg x min/L in the gastric group. The estimated bioavailability (AUC/mean intravenous AUC) of intramuscular oxycodone was 0.47-0.84 (0.68), that of buccal oxycodone 0.22-0.84 (0.55) and that of gastric oxycodone 0.10-0.58 (0.37).
Conclusion:
The pharmacokinetics of intravenous oxycodone in children aged 6-93 months are fairly similar to those reported in adults. Intramuscular administration provides relatively constant drug absorption, but after buccal and gastric administration the interindividual variation in the rate and extent of absorption is large.
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