The Pharmacokinetics of Ibuprofen in Humans and Animals

Jamali, Fakhreddin; Brocks, Dion R.

doi:10.1002/9781118743614.ch4

Cited by 8 publications

(3 citation statements)

References 140 publications

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“…The EFs in influents confirmed that minimal enantioselectivity occurs for this drug, administered as racemate, during human metabolism [33]. Regarding naproxen, it is administered as an enantiomerically pure formulation of (S)-naproxen due to the known hepatotoxicity of (R)-naproxen and, similar to ketoprofen, minor chiral inversion occurs during human metabolism.…”

Section: Determination Of Profen Content and Enantiomeric Fraction Inmentioning

confidence: 61%

Enantioselective determination of representative profens in wastewater by a single-step sample treatment and chiral liquid chromatography–tandem mass spectrometry

Caballo

Sicilia

Rubio

2015

Talanta

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Section: Determination Of Profen Content and Enantiomeric Fraction Inmentioning

confidence: 61%

Enantioselective determination of representative profens in wastewater by a single-step sample treatment and chiral liquid chromatography–tandem mass spectrometry

Caballo

Sicilia

Rubio

2015

Talanta

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“…23 Jamali and Brocks suggested that the administration of racemic IBP to individuals after dental surgery reduced the chiral inversion of (R)-IBP. 28 Evidence supporting this proposition was derived from the alteration in the enantioselective ratio of the drug in the bloodstream. Prior to the surgical procedure, the mean plasma AUC value for (S)-IBP exceeded that of (R)-IBP.…”

Section: Stereoselective Pharmacokinetics Of (R)-and (S)-ibpmentioning

confidence: 99%

Enantioselective separation and determination of ibuprofen: Stereoselective pharmacokinetics, pharmacodynamics and analytical methods

Vashistha,

Kumar,

Yadav

et al. 2024

Chirality

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Ibuprofen (IBP), the 29th most prescribed drug in the United States in 2019, is a widely used nonsteroidal anti‐inflammatory drug (NSAID) comprising two enantiomers, (R)‐IBP and (S)‐IBP, collectively known as (RS)‐IBP. This critical review examines analytical techniques for the enantioselective separation and determination of IBP enantiomers, crucial for pharmaceutical and clinical applications. The review focuses on state‐of‐the‐art methods, including chromatographic techniques including high‐performance liquid chromatography, gas chromatography, liquid chromatography–tandem mass spectrometry, and some other techniques. This review addresses pharmacokinetics, pharmacology, and side effects of each enantiomer, ensuring safe drug usage. By consolidating diverse analytical methods and their applicability in different matrices, this review serves as a valuable resource for researchers, analysts, and practitioners in pharmaceutical analysis, pharmacology, and clinical studies.

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“…The following supporting information can be downloaded at: , Figure S1: Simulated versus observed concentration profiles for plasma and CNS in rats; Figure S2: Simulated versus observed concentration profiles in rats; Figure S3: Goodness-of-fit plots of predicted vs observed pharmacokinetic metrics (AUC & Cmax) in plasma and CSF/ECF in rats; Table S1: Physiological parameters-Rat PBPK model; Table S2: Physiological parameters-Human PBPK model; Table S3: Physicochemical and Drug Specific Parameters for Acetaminophen, Oxycodone, Lacosamide, Ibuprofen & Levetiracetam. References [ 8 , 28 , 34 , 40 , 42 , 44 , 46 , 52 , 53 , 56 , 57 , 59 , 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 , 101 , 102 , 103 , 104 , 105 , 106 , 107 , 108 , 109 ] are cited in the supplementary materials.…”

mentioning

confidence: 99%

Interspecies Brain PBPK Modeling Platform to Predict Passive Transport through the Blood–Brain Barrier and Assess Target Site Disposition

Mehta,

Soliman,

Rodriguez-Vera

et al. 2024

Pharmaceutics

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The high failure rate of central nervous system (CNS) drugs is partly associated with an insufficient understanding of target site exposure. Blood–brain barrier (BBB) permeability evaluation tools are needed to explore drugs’ ability to access the CNS. An outstanding aspect of physiologically based pharmacokinetic (PBPK) models is the integration of knowledge on drug-specific and system-specific characteristics, allowing the identification of the relevant factors involved in target site distribution. We aimed to qualify a PBPK platform model to be used as a tool to predict CNS concentrations when significant transporter activity is absent and human data are sparse or unavailable. Data from the literature on the plasma and CNS of rats and humans regarding acetaminophen, oxycodone, lacosamide, ibuprofen, and levetiracetam were collected. Human BBB permeability values were extrapolated from rats using inter-species differences in BBB surface area. The percentage of predicted AUC and Cmax within the 1.25-fold criterion was 85% and 100% for rats and humans, respectively, with an overall GMFE of <1.25 in all cases. This work demonstrated the successful application of the PBPK platform for predicting human CNS concentrations of drugs passively crossing the BBB. Future applications include the selection of promising CNS drug candidates and the evaluation of new posologies for existing drugs.

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The Pharmacokinetics of Ibuprofen in Humans and Animals

Cited by 8 publications

References 140 publications

Enantioselective determination of representative profens in wastewater by a single-step sample treatment and chiral liquid chromatography–tandem mass spectrometry

Enantioselective determination of representative profens in wastewater by a single-step sample treatment and chiral liquid chromatography–tandem mass spectrometry

Enantioselective separation and determination of ibuprofen: Stereoselective pharmacokinetics, pharmacodynamics and analytical methods

Interspecies Brain PBPK Modeling Platform to Predict Passive Transport through the Blood–Brain Barrier and Assess Target Site Disposition

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