Pharmacokinetics, safety, and tolerability of a rapid infusion of i.v. ibuprofen in healthy adults

• Published in: American journal of health-system pharmacy 2011-01, Vol.68 (1), p.47-51
• Main Authors: Pavliv, Leo, Voss, Bryan, Rock, Amy
• Format: Article
• Language: English
• Subjects: Administration, Oral; Adult; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - adverse effects; Anti-Inflammatory Agents, Non-Steroidal - blood; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Cross-Over Studies; Dosage and administration; Double-Blind Method; Drug tolerance; Female; Gas Chromatography-Mass Spectrometry; Half-Life; Humans; Ibuprofen; Ibuprofen - administration & dosage; Ibuprofen - adverse effects; Ibuprofen - blood; Ibuprofen - pharmacokinetics; Infusions, Intravenous; Male; Pharmacokinetics
• ISSN: 1079-2082; 1535-2900
• DOI: 10.2146/ajhp100120

The pharmacokinetics, safety, and tolerability of a rapid infusion of i.v. ibuprofen in healthy adults were evaluated. Methods In this randomized, double-blind, placebo-controlled, single-dose, crossover study, 12 healthy subjects age 18-65 years were randomized to receive a single dose of either 800 mg i.v. ibuprofen (infused over five to seven minutes) concomitantly with an oral placebo or 800 mg oral ibuprofen with concomitant i.v. placebo (0.9% sodium chloride injection). After a six-day washout period, subjects received the treatment not previously received. Blood samples were taken 1 hour before each dose of study medication was administered and throughout the 12 hours thereafter. Plasma ibuprofen concentrations were determined using validated liquid chromatography-tandem mass spectrometry methods. The frequency and severity of treatment-emergent adverse effects were monitored throughout the study. The maximum plasma concentration (C(max)) of i.v. ibuprofen was approximately twice that of oral ibuprofen, and the (t(max)) of i.v. ibuprofen was 0.11 hour, compared with 1.5 hours for oral ibuprofen. However, the elimination half-life of i.v. and oral ibuprofen did not differ, both of which were approximately 2 hours. Oral ibuprofen was 100% bioavailable; therefore, the area under the concentration-time curve did not differ between i.v. and oral ibuprofen. In addition, i.v. ibuprofen infused over five to seven minutes did not differ in terms of safety or tolerability when compared with oral ibuprofen. I.V. ibuprofen, when administered over five to seven minutes in healthy subjects, achieved a higher C(max) and a more-rapid t(max) than did oral ibuprofen and was found to be safe and well tolerated.