Comparative Pharmacokinetics and Safety Studies of Dexibuprofen Injection and a Branded Product Ibuprofen Injection in Healthy Chinese Volunteers.

Abstract

Ibuprofen, a nonsteroidal anti-inflammatory drug, is considered a safe and effective analgesic for treating different types of pain and joint disorders. Dexibuprofen, S-(+)-ibuprofen, is the single pharmacologically active enantiomer of ibuprofen. It is more potent than the racemic formulation of ibuprofen in terms of analgesic and anti-inflammatory properties and causes less acute gastric damage. For the first time, in the present single-dose, randomized, open-label, 2-period crossover study, the safety and pharmacokinetic (PK) characteristics of a single-dose dexibuprofen injection (0.2 g) were evaluated in healthy Chinese subjects and compared with the PK characteristics of a 0.2-g ibuprofen injection. Five consecutive men and women were randomly administered a single dose of the 0.2-g ibuprofen or 0.2-g dexibuprofen injection after fasting in every period during the 5-day interval. Then, plasma samples were collected for liquid chromatography-tandem mass spectrometric analysis. WinNonlin software was used for calculating the PK parameters. The geometric mean ratios of the 0.2-g dexibuprofen injection/ibuprofen injection for maximal plasma concentration, area under the plasma concentration-time curve (AUC) from time 0 to the last quantifiable time point, and AUC from time 0 to infinity were 184.6%, 136.9%, and 134.4%, respectively. The dexibuprofen plasma exposure of the 0.15-g dexibuprofen injection was comparable to that of the 0.2-g ibuprofen injection, calculated using AUC from time 0 to infinity.

• Authors: Wenyan Hua, Wenjia Zhou, Mei Su, Quanying Zhang, Shunlin Zong, Meng Wang
• Journal: Clinical pharmacology in drug development (Clin Pharmacol Drug Dev) Vol. 12 Issue 9 Pg. 881-887 (09 2023) ISSN: 2160-7648 [Electronic] United States
• PMID: 37140399 (Publication Type: Comparative Study, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
• Copyright: © 2023, The American College of Clinical Pharmacology.

Chemical References

• Anti-Inflammatory Agents, Non-Steroidal
• Cyclooxygenase Inhibitors
• dexibuprofen
• Ibuprofen

Topics

• Female
• Humans
• Male
• Anti-Inflammatory Agents, Non-Steroidal (administration & dosage, adverse effects, pharmacokinetics)
• Cross-Over Studies
• Cyclooxygenase Inhibitors (administration & dosage, adverse effects, therapeutic use)
• East Asian People
• Ibuprofen (administration & dosage, adverse effects, analogs & derivatives, therapeutic use)
• Volunteers
• Healthy Volunteers
• Injections