Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Five groups of six healthy subjects received single oral doses of 150, 300, 450, 600 or 750 mg tiacrilast 150 mg capsules, followed 24 h later by the same dose given every 6 h for 7 days, in a study designed to assess the pharmacokinetics of single and multiple doses of tiacrilast. Plasma samples were obtained at specified times after the initial dose, after 4 days of multiple dosing and after the last dose of tiacrilast. Samples were assayed for unchanged drug by a specific HPLC method. Wide variability was seen in the plasma concentration-time data. Plasma concentrations and pharmacokinetic parameters were nearly proportional to dose over the 150 to 750 mg dose range studied. Moreover, there was no evidence of unexpected accumulation of the drug in the plasma during multiple dosing and food did not appear to alter the bioavailability of tiacrilast to any clinically significant extent. The apparent elimination half-life was similar after single and multiple doses and ranged from 1 to 3 h.
D000328:Adult; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D005215:Fasting; D005502:Food; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D011799:Quinazolines / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*
D011799:Quinazolines; C040252:tiacrilast