Clinical Pharmacokinetics of Ibuprofen

@article{Davies1998ClinicalPO,
  title={Clinical Pharmacokinetics of Ibuprofen},
  author={Neal M. Davies},
  journal={Clinical Pharmacokinetics},
  year={1998},
  volume={34},
  pages={101-154}
}
  • N. Davies
  • Published 1 February 1998
  • Medicine, Biology, Chemistry
  • Clinical Pharmacokinetics
Ibuprofen is a chiral nonsteroidal anti-inflammatory drug (NSAID) of the 2 arylpropionic acid (2-APA) class. A common structural feature of 2-APA NSAIDs is a sp3-hybridised tetrahedral chiral carbon atom within the propionic acid side chain moiety with the S-(+)-enantiomer possessing most of the beneficial anti-inflammatory activity. Ibuprofen demonstrates marked stereoselectivity in its pharmacokinetics. Substantial unidirectional inversion of the R-(−) to the S-(+) enantiomer occurs and thus… 
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254 Citations
Highly Influential Citations
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Background Citations
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Methods Citations
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Results Citations
5

254 Citations

Stereoselectivity of ibuprofen metabolism and pharmacokinetics following the administration of the racemate to healthy volunteers
TLDR
The stereoselective metabolism and pharmacokinetics of the enantiomers of ibuprofen have been investigated following the oral administration of the racemic drug to 12 healthy volunteers and analysis of the stereochemical composition of the urinary excretion products indicated that 68% of the dose of (R) -ib uprofen had undergone chiral inversion.
Pharmacokinetic interaction of ibuprofen enantiomers in rabbits
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The enantiomeric interaction in the pharmacokinetic behaviour of ibuprofen after racemic administration is considered to be a result of an alteration in the metabolic or excretion phase (or both) rather than stereoselective protein binding in the systemic distribution.
Clinical Pharmacokinetics of Oxaprozin
  • N. Davies
  • Biology, Medicine
    Clinical pharmacokinetics
  • 1998
TLDR
After administration of multiple doses, the apparent oral clearance and volume of distribution of total oxaprozin increased while those of the unbound drug decreased significantly, and patients with renal impairment demonstrate an increase in unbound plasma concentrations of oxAProzin.
Solubility of ( ± )-Ibuprofen and S ( + )-Ibuprofen in the Presence of Cosolvents and Cyclodextrins
TLDR
Of the two compounds studied, higher equilibrium solubilities were observed for SIB as compared with racIB, and the solubilization process is discussed in terms of solvent polarity and differential solid-state structure of racIB and SIB.
Sila-Ibuprofen.
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The synthesis, characterization, biological activity and toxicology of sila-ibuprofen, a silicon derivative of the most common non-steroidal anti-inflammatory drug, is reported and the understanding of the mechanism of action of the inhibition process is improved.
Comparative study of anti-inflammatory, ulcerogenic and cytotoxic activities of racemate and S-ibuprofen
TLDR
The present findings suggest that the S-enantiomer of ibuprofen could be considered a therapeutic alternative to minimize gastrointestinal side effects, since the chiral inversion of R(-)-ib uprofen to S(+)-ibuprofeno did not result in an improved anti-inflammatory response.
Chiral pharmacokinetics and inversion of enantiomers of a new quinoxaline topoisomerase IIbeta poison in the rat.
TLDR
XK469 (NSC 697887; (+/-)-2-[4-(7-chloro-2-quinoxaliny)oxy]phenoxy propionic acid), an analog of the herbicide Assure, which possesses antitumor activity, has recently been found to be the first topoisomerase IIbeta poison.
Pharmacokinetic Drug Interaction Study of Bazedoxifene and Ibuprofen
TLDR
The lack of interaction between bazedoxifene and ibuprofen suggests that they may be coadministered without dose adjustment, and the increase in bazedxifene plasma concentrations when combined with ib uprofen versus bazed oxifene alone is unlikely to be clinically significant.
Stereoconfiguration of antiallergic and immunologic drugs.
  • L. Bielory, A. Leonov
  • Medicine, Biology
    Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
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Rectal Administration of Ibuprofen: Comparison of Enema and Suppository Form.
TLDR
The pharmacokinetic parameters of rectal administration of ibuprofen between enema and suppository form were compared in order to provide evidence for the faster absorption rates of ib uprofen enema to provide faster onset of analgesic and antipyretic benefit.
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