Pharmacokinetic Properties of Intravenous Ibuprofen in Healthy Chinese Volunteers

Abstract

Background and objectives: No pharmacokinetic data of intravenous ibuprofen were available in a Chinese population and the published information remained inadequate. The present study aimed to investigate the pharmacokinetic properties of intravenous ibuprofen in healthy Chinese volunteers after single- and multiple-dose administration.

Methods: Twelve subjects received single doses of 200, 400, and 800 mg intravenous ibuprofen, respectively, and multiple doses of 400 mg intravenous ibuprofen, four times per day (every 6 h) till the morning of the sixth day in each study period.

Results: After single doses of 200, 400 and 800 mg and multiple doses of 400 mg intravenous ibuprofen, the main pharmacokinetic parameters obtained were: maximum plasma concentration (C _max) 23.05 ± 2.96, 41.90 ± 3.22, 76.06 ± 8.70, and 49.53 ± 3.92 μg/ml, respectively, which were achieved immediately at the end of the infusion; area under the plasma concentration-time curve from time zero to the time of last quantifiable concentration (AUC_0-t ) 49.82 ± 10.92, 88.79 ± 12.43, 152.34 ± 25.23, and 106.68 ± 18.94 µg·h/mL, respectively; AUC from time zero to infinity (AUC_0-∞) 51.91 ± 10.67, 91.46 ± 12.06, 155.04 ± 25.70, and 108.58 ± 19.49 µg·h/ml, respectively; half-life (t _½) 1.87 ± 0.30, 1.93 ± 0.24, 2.02 ± 0.38, and 1.74 ± 0.26 h, respectively. The accumulation index (AI) was 1.22 ± 0.17 after multiple doses. The most obvious accumulation was observed in males; other parameters revealed no significant differences.

Conclusions: Similar pharmacokinetic properties of intravenous ibuprofen in healthy Chinese volunteers were observed to those reported in a Caucasian population. Multiple doses of intravenous ibuprofen every 6 h caused slight accumulation. Except for the AI, sex did not affect the pharmacokinetics of intravenous ibuprofen. CHICTR.

Org identifier: ChiCTR-IIR-15007347.