Pharmacokinetic and Bioequivalence Studies of Ibuprofen Suspension after a Single-dose Administration in Healthy Chinese Volunteers

Abstract

Objective:

The aim of this study was to assessed the pharmacokinetic and bioequivalence of 2 formulations of ibuprofen suspension.

Method:

20 healthy volunteers were enrolled into this random, single-dose, 2-way crossover, open-label, single-centre, pharmacokinetic study. After overnight fasting, 2 formulations (test and reference) of ibuprofen (400 mg ibuprofen/20 mL suspension) were administered as a single dose on 2 treatment days separated by a 7-day washout period. After dosing, blood samples were drawn for a period of 12 h. The plasma samples were analyzed for the presence of ibuprofen by HPLC with ultraviolet detection. Pharmacokinetic parameters were determined from plasma concentrations for both formulations.

Results:

The main pharmacokinetics parameters of test and reference were as follows: t_1/2 was (1.94±0.38) h and (1.95±0.28) h; C_max was (33.41±7.83) μg · mL^− 1 and (31.08±9.30) μg · mL^− 1; AUC_0–12 was (91.44±19.26) μg · mL⁻¹ · h and (84.75±24.45) μg · mL⁻¹ · h; AUC_0–∞ was (92.82±19.94) μg · mL⁻¹ · h and (85.97±24.99) μg · mL⁻¹ · h; median Tmax was 0.5 h (range, 0.25, 2) and 0.5 h (range, 0.25, 1.5). The 90% confidence intervals of the test/reference treatment ratios for C_max, AUC_0–12 and AUC_0–∞ were observed to be within the predetermined acceptable interval of 80–125%.

Conclusion:

This single-dose study in healthy Chinese fasted volunteers was shown that the ibuprofen test and reference met the requirement of the State Food and Drug Administration, and the test and reference were bioequivalent.

Key word

ibuprofen - bioequivalence study - pharmacokinetics - HPLC

• References

• 1 Lee E, Williams K, Day R et al. Stereoselective disposition of ibuprofen enantiomers in man. Br J Clin Pharmacol 2004; 58: 759-764
• 2 Evans AM, Nation RL, Sansom LN et al. Stereoselective plasma protein binding of ibuprofen enantiomers. Eur J Clin Pharmacol 1989; 36: 283-290
• 3 Vane JR, Botting RM. Mechanism of action of anti-inflammatory drugs. Scand J Rheumatol Suppl 1996; 102: 9-21
• 4 Hersh E, Moore P, Ross G. Over-the-counter analgesics and antipyretics: a critical assessment. Clin Ther 2000; 22: 500-548
• 5 Department of Health . The British Pharmacopoeia. 99^th ed. London, UK: Stationery Office Books; 1999
• 6 Al-Talla ZA, Akrawi SH, Tolley LT et al. Bioequivalence assessment of two formulations of ibuprofen. Drug Design, Development and erapy 2011; 5: 427-433
• 7 Peng W, Meiling Q, Lihe L et al. Determination of ibuprofen in dog plasma by liquid chromatography and application in pharmacokinetic studies of an ibuprofen prodrug in dogs. Journal of Pharmaceutical and Biomedical Analysis 2005; 38: 714-719
• 8 Yunhao Z, Yuqin H, Yanning H. Pharmacokinetic and Bioequivalence of Ibuprofen Soft Capsules in Healthy Volunteers. Journal of Medical Theory and Practice 2009; 22: 144-146
• 9 Zhen D, Chunlian T, Yan S et al. Pharmacokinetics and bioequivalence of ibuprofen granules. Pharmaceutical Care and Research 2009; 436-439
• 10 Ludan B, Li Y, Yunzhen G et al. Bioavailability of ibuprofen soft capsules in healthy volunteers. Chinese journal of new drug 2006; 2062-2064
• 11 Bramlage P, Goldis A. Bioequivalence study of three ibuprofen formulations after single dose administration in healthy volunteers. BMC Pharmacology 2008; 1-9