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

Abstract

AbstractIbuprofen, 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.