OBJECTIVE: The present study aimed at investigating the effects of concomitant food intake on the bioavailability of a single oral dose of clopidogrel (CAS 113665-84-2). METHODS:Clopidogrel was given under two conditions separated by a 14-day washout period: fasted and fed (after a standardized high fat breakfast). Concentrations of clopidogrel in plasma were quantified by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) with positive ion electro-spray ionization using multiple reaction monitoring (MRM). Pharmacokinetic parameters such as Cmax, Tmax, AUC0-t, AUC0-inf and tl/2z were estimated using a noncompartmental model. RESULTS: The pharmacokinetic parameters were significantly affected by food intake. Specifically, Cm, and AUC0-inf of clopidogrel increased 6.1-fold and 9.2-fold, respectively, in the fed condition compared to the fasted condition. The t1/2 increased from 2.5 h in the fasted state to 5.0 h in the fed state. The limit of quantification was 5 pg/mL for plasma clopidogrel analysis. CONCLUSION: Food substantially enhanced the bioavallability of clopidogrel in healthy subjects.
RCT Entities:
OBJECTIVE: The present study aimed at investigating the effects of concomitant food intake on the bioavailability of a single oral dose of clopidogrel (CAS 113665-84-2). METHODS:Clopidogrel was given under two conditions separated by a 14-day washout period: fasted and fed (after a standardized high fat breakfast). Concentrations of clopidogrel in plasma were quantified by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) with positive ion electro-spray ionization using multiple reaction monitoring (MRM). Pharmacokinetic parameters such as Cmax, Tmax, AUC0-t, AUC0-inf and tl/2z were estimated using a noncompartmental model. RESULTS: The pharmacokinetic parameters were significantly affected by food intake. Specifically, Cm, and AUC0-inf of clopidogrel increased 6.1-fold and 9.2-fold, respectively, in the fed condition compared to the fasted condition. The t1/2 increased from 2.5 h in the fasted state to 5.0 h in the fed state. The limit of quantification was 5 pg/mL for plasma clopidogrel analysis. CONCLUSION: Food substantially enhanced the bioavallability of clopidogrel in healthy subjects.