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Stereoselective disposition of ibuprofen enantiomers in infants
E Rey1, A Pariente-Khayat, L Gouyet
1Département de Pharmacologie Périnatale et Pédiatrique, Hôpital Saint-Vincent de Paul, Paris, France.
Insights
Infant pharmacokinetics of ibuprofen show similar half-lives for both enantiomers. However, lower plasma concentrations of the active S(+)-ibuprofen suggest higher infant dosages may be needed.
Area of Science:
- Pharmacology
- Pediatric Medicine
- Drug Metabolism
Background:
- Ibuprofen is a common nonsteroidal anti-inflammatory drug (NSAID) used for pain and inflammation.
- Understanding the pharmacokinetic differences between ibuprofen enantiomers is crucial for optimizing pediatric dosing.
- Infant drug metabolism can differ significantly from adults, necessitating specific pharmacokinetic studies.
Purpose of the Study:
- To investigate the pharmacokinetic profiles of S(+) and R(-) ibuprofen enantiomers in infants.
- To compare the enantiomer-specific pharmacokinetics of ibuprofen in an infant population.
- To determine if current ibuprofen dosing regimens are adequate for infants based on enantiomer-specific concentrations.
Main Methods:
- Oral administration of a single racemic ibuprofen dose (7.6 mg/kg) to 11 infants.
- Measurement of plasma concentrations of S(+) and R(-) ibuprofen enantiomers over time.
- Calculation of pharmacokinetic parameters including half-life and area under the concentration-time curve (AUC).
Main Results:
- Mean half-life for S(+)-ibuprofen was 1.6 ± 0.5 hours; for R(-)-ibuprofen, it was 1.5 ± 0.5 hours.
- Mean AUC for S(+)-ibuprofen was 31.5 ± 14.3 mg·h/L; for R(-)-ibuprofen, it was 36.6 ± 13.8 mg·h/L.
- Plasma concentrations of the active S(+)-enantiomer were lower in infants compared to adult data.
Conclusions:
- The pharmacokinetics of ibuprofen enantiomers in infants show comparable elimination rates.
- Lower plasma levels of S(+)-ibuprofen in infants suggest potential underdosing compared to adults.
- Further studies are warranted to establish optimal ibuprofen dosage regimens for pediatric populations.
Abstract:
The pharmacokinetics of the enantiomers of ibuprofen were investigated after oral administration of a single 7.6 +/- 0.3 mg kg-1 dose of the racemate in 11 infants. Mean (+/- s.d.) half-lives were 1.6 +/- 0.5 h for S(+) and 1.5 +/- 0.5 h for R(-) and mean (+/- s.d.) AUC values were 31.5 +/- 14.3 mg l-1 h for S(+) and 36.6 +/- 13.8 mg l-1 h for R(-). Since plasma concentrations of the active S(+)-isomer were lower than those reported in adults, a higher dosage might be required in infants.