Effect of food and antacid on absorption of orally administered ticlopidine hydrochloride.
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 [tmax = 1.71 +/- 0.33 hr (fed) vs 1.92 +/- 0.56 hr (fasting) and AUC0-infinity = 2.164 +/- 0.813 micrograms X hr/mL (fed) vs 1.808 +/- 1.052 micrograms X 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.
Bioanalytical and Metabolic Research, Syntex, Palo Alto, CA 94303.
J
J
Shah
A
A
Fratis
D
D
Ellis
S
S
Murakami
P
P
Teitelbaum
D000284:Administration, Oral; D000328:Adult; D000863:Antacids / Q000494:pharmacology*; D001682:Biological Availability; D004334:Drug Administration Schedule; D005215:Fasting / Q000097:blood; D005502:Food; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D011897:Random Allocation; D013988:Ticlopidine / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*
D000863:Antacids; D013988:Ticlopidine