Effect of food on bioavailability of a single oral dose of clopidogrel in healthy male subjects.
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.


CONCLUSIONS
Food substantially enhanced the bioavallability of clopidogrel in healthy subjects.
Nirogi
Ramakrishna V S
RV
Biopharmaceutical Research, Suven Life Sciences Ltd., Hyderabad, India. ramakrishna_nirogi@yahoo.co.in
Kandikere
Vishwottam N
VN
Mudigonda
Koteshwara
K
D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D002138:Calibration; D000077144:Clopidogrel; D018592:Cross-Over Studies; D004562:Electrocardiography / Q000187:drug effects; D018565:Food-Drug Interactions; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013988:Ticlopidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
D010975:Platelet Aggregation Inhibitors; D000077144:Clopidogrel; D013988:Ticlopidine