Pharmacokinetics of ketoprofen following oral and intramuscular administration in young children

• Published in: European journal of clinical pharmacology 2001-11, Vol.57 (9), p.643-647
• Main Authors: KOKKI, Hannu, TUOMILEHTO, Henri, KARVINEN, Marko
• Format: Article
• Language: English
• Subjects: Administration, Oral; Analgesics; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Area Under Curve; Biological and medical sciences; Child; Child, Preschool; Children & youth; Chromatography, High Pressure Liquid; Drug therapy; Female; Humans; Infant; Injections, Intramuscular; Ketoprofen - administration & dosage; Ketoprofen - pharmacokinetics; Male; Medical sciences; Metabolism; Neuropharmacology; Pharmacology. Drug treatments; Prospective Studies; Time Factors
• ISSN: 0031-6970; 1432-1041
• DOI: 10.1007/s002280100339

The pharmacokinetics of ketoprofen following intramuscular injection or oral tablet was determined in children aged 10-69 months. Ten children received a single intramuscular injection of 1 mg kg(-1) ketoprofen. Six children, weight 12-17 kg, received a 12.5-mg ketoprofen tablet and four children, weight 18-23 kg, received a 25-mg tablet. Venous blood samples were collected at 15 min and 30 min and 1, 2, 4, 6 and 8 h following drug dosing. Plasma ketoprofen levels were measured using a validated high-performance liquid chromatography method. The maximal plasma concentration of ketoprofen ranged between 3.6 microg ml(-1) and 7.4 microg ml(-1) in the intramuscular group and, following a dose normalisation, between 2.8 microg ml(-1) and 8.2 microg ml(-1) in the tablet group (dose normalised for 1 mg kg(-1)). The rate and extent of absorption of ketoprofen were comparable after intramuscular and oral administration. The relative bioavailability of oral ketoprofen was about 100% of the intramuscular administration. The extrapolated area under the plasma concentration-time curve (AUC0-infinity) ranged between 8.8 microg ml(-1) h and 14.6 microg ml(-1) h in the intramuscular group and between 8.7 microg ml(-1) h and 14.1 microg ml(-1) h in the tablet group (dose-normalised AUC0-infinity). The terminal half-life was comparable in both study groups, ranging between 0.8 h and 2.2 h in the intramuscular group and between 0.9 h and 2.1 h in the tablet group. According to the pharmacokinetic properties determined in this study, there is no justification for using intramuscular administration in awake children.