Preliminary pharmacokinetic study of ibuprofen enantiomers after administration of a new oral formulation (ibuprofen arginine) to healthy male volunteers.

  title={Preliminary pharmacokinetic study of ibuprofen enantiomers after administration of a new oral formulation (ibuprofen arginine) to healthy male volunteers.},
  author={Gianfranco Fornasini and Nunzia Ceppi Monti and Giandomenico Brogin and M Gallina and M. Eandi and Stefano Persiani and Massimo Bani and Carlo Della Pepa and Gian Paolo Zara and Margherita Strolin Benedetti},
  volume={9 3},
The pharmacokinetics of ibuprofen enantiomers were investigated in a crossover study in which seven healthy male volunteers received single oral doses of 800 mg racemic ibuprofen as a soluble granular formulation (sachet) containing L-arginine (designated trade name: Spedifen), 400 mg (-)R-ibuprofen arginine or 400 mg (+)S-ibuprofen arginine. Plasma levels of both enantiomers were monitored up to 480 minutes after drug intake using an enantioselective analytical method (HPLC with ultraviolet… Expand
Simultaneous fitting of R- and S-ibuprofen plasma concentrations after oral administration of the racemate.
Ibuprofen formulations were bioequivalent and may serve as a basis for future pharmacokinetic/pharmacodynamic calculations after administration of racemic ib uprofen. Expand
Pharmacokinetics of ibuprofen enantiomers in rats after intravenous and oral administration of ibuprofen arginate.
The pharmacokinetics of ib uprofen enantiomers were studied in rats after intravenous and oral administration of ibuprofen arginate by means of a chiral HPLC method and it could be concluded that the pharmacological actions might be similar when ibUprofenArginate was given orally and intravenously, except some differences in the onset of action. Expand
A comparative study of the pharmacokinetics of ibuprofen arginate versus dexibuprofen in healthy volunteers
Ibuprofen arginate approaches maximum concentrations of S(+)-ib uprofen faster and higher than dexibupro Fenox, and demonstrates a 45% higher maximum concentration (Cmax), and a time to peak concentration (Tmax) 2 h sooner. Expand
Pharmacokinetic-Pharmacodynamic Modelling of the Antipyretic Effect of Two Oral Formulations of Ibuprofen
Because of the indirect nature of the effect exerted by ibuprofen, the implications of differences found in the plasma drug concentration profiles between suspension and effervescent granules are less apparent in the therapeutic response. Expand
Stereoselective pharmacokinetics of ibuprofen and its lysinate from suppositories in rabbits.
  • F. Główka
  • Chemistry, Medicine
  • International journal of pharmaceutics
  • 2000
Studies were performed on the effect of ibuprofen racemate ionisation extent on the pharmacokinetics of its enantiomers following administration in suppositories to rabbits and AUC was markedly higher following administration of suppositories containing IBP than following suppositories with IBPL. Expand
Clinical Pharmacokinetics of Ibuprofen
  • N. Davies
  • Chemistry, Medicine
  • Clinical pharmacokinetics
  • 1998
A relationship between ibuprofen plasma concentrations and analgesic and antipyretic effects has been elucidated and a proposed site of action for nonsteroidal anti-inflammatory drugs is proposed. Expand
Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen.
The regulatory acceptance of achiral bioanalytical methods for ibuprofen bioequivalence studies is justified because the sum of both enantiomers is more discriminative than the chiral methods where only the eutomer is used for regulatory decisions. Expand
Influence of CYP2C8 and CYP2C9 polymorphisms on pharmacokinetic and pharmacodynamic parameters of racemic and enantiomeric forms of ibuprofen in healthy volunteers.
This study suggest an impaired metabolism of racemic, S-ibuprofen and R-ib uprofen in CYP2C9*3; an increased R-IBuproen metabolism in CYC2C8*3 volunteers; and fewer adverse events in CYp2C 8*3 Volunteers; that correlates with a decreased expression of iNOS. Expand
Enantioselective analysis of ibuprofen enantiomers in mice plasma and tissues by high-performance liquid chromatography with fluorescence detection: Application to a pharmacokinetic study.
A direct fluorometric high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of ibuprofen enantiomers in mouse plasma and tissues using liquid-liquid extraction and 4-tertbutylphenoxyacetic acid as an internal standard and successfully applied to a pharmacokinetic study. Expand
Comparison of gastric endoscopic lesions and tolerability to ibuprofen and ibuprofen-arginate in healthy subjects.
The aim was to compare gastric endoscopic lesions, in addition to tolerability, in healthy volunteers treated with ibuprofen or ib uprofen-arginate in humans, to demonstrate clinically significant differences. Expand


Human pharmacokinetics of ibuprofen enantiomers following different doses and formulations: intestinal chiral inversion.
The influences of absorption rate and dosage size on the pharmacokinetics of ibuprofen (IB) enantiomers were studied and it was found that in humans, the chiral inversion of IB is not influenced by the dosage size but is enhanced by prolongation of the residence time in the intestine. Expand
Variability in the stereoselective disposition of ibuprofen in patients with rheumatoid arthritis.
Interindividual variation in the pharmacokinetics of (S)-ibuprofen following administration of the racemate was similar to that following theadministration of the single isomer suggesting that chiral inversion is not a major factor contributing to variability in the disposition of this drug. Expand
Isomeric inversion of ibuprofen (R)-enantiomer in humans.
In vivo metabolism of ibuprofen to its carboxy metabolite was not stereoselective, and both (S)-(+)- and (R)-(-)-enantiomers of the intact drug were transformed independently in vivo to the major metabolites. Expand
Lack of presystemic inversion of (R)‐ to (S)‐ibuprofen in humans
The bioavailability of both enantiomers of ibuprofen is complete and no evidence of significant presystemic inversion is found. Expand
Update on Ibuprofen: Review Article
  • M. Busson
  • Medicine
  • The Journal of international medical research
  • 1986
Non-steroidal anti-inflammatory drugs (NSAIDs) have become the principal mode of therapy for rheumatic diseases and their use has continued to increase despite concern expressed recently regardingExpand
The metabolic chiral inversion and dispositional enantioselectivity of the 2-arylpropionic acids and their biological consequences.
The biological consequences of the metabolic chiral inversion and enantioselective disposition of the 2-arylpropionates have been summarized in terms of their implications for the development and use of safer and more effective drugs of this class. Expand
Enzymatic inversion at saturated carbon: nature and mechanism of the inversion of R(-) p-iso-butyl hydratropic acid.
A detailed enzymatic pathway for this optical inversion in which the existence of an R-aryl propionic acid isomerase system is postulated is proposed, making understandable the bioequivalence of a variety of (S) and (R) isomers of non-steroidal anti-inflammatory agents. Expand