Premium
Effect of Food and Antacid on Absorption of Orally Administered Ticlopidine Hydrochloride
Author(s) -
Shah J.,
Fratis A.,
Ellis D.,
Murakami S.,
Teitelbaum P.
Publication year - 1990
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1990.tb03635.x
Subject(s) - ticlopidine , antacid , bioavailability , crossover study , oral administration , pharmacology , absorption (acoustics) , medicine , pharmacokinetics , dosing , postprandial , chemistry , aspirin , placebo , clopidogrel , physics , alternative medicine , pathology , acoustics , insulin
Ticlopidine is a potent inhibitor of platelet aggregation. Absorption of ticlopidine after oral dosing is rapid and complete. Ticlopidine is extensively metabolized with a relative minor component of unchanged ticlopidine in plasma. The randomized crossover study described here was undertaken to examine the effect of food and antacid on the oral bioavailability of a single dose of ticlopidine (250 mg) in normal volunteers. After postprandial treatment the rate and extent of absorption of ticlopidine was earlier and greater relative to fasting treatment [t max = 1.71 ± 0.33 hr (fed) vs 1.92 ± 0.56 hr (fasting) and AUC 0–∝ = 2.164 ± 0.813 μg × hr/mL (fed) vs 1.808 ± 1.052 μg × hr/mL (fasting)]. The oral bioavailability of ticlopidine was increased by 20% when taken after a meal. In contrast, absorption of ticlopidine administered after antacid treatment was approximately 20% lower than under fasting conditions. Administration of ticlopidine with food is recommended to maximize gastrointestinal tolerance.