Yali Shen1, Feng Nan2, Mei Li2, Maozhi Liang2, Ying Wang2, Zhihui Chen2, Zhu Luo3. 1. Department of Abdominal Oncology, Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China. 2. GCP Center/Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China. 3. GCP Center/Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China. luozhu720@163.com.
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 (AUC0-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 (AUC0-∞) 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.
RCT Entities:
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 (AUC0-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 (AUC0-∞) 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.
Authors: Elena García-Martín; Carmen Martínez; Beatriz Tabarés; Jesús Frías; José A G Agúndez Journal: Clin Pharmacol Ther Date: 2004-08 Impact factor: 6.875