Effects of food, antacid, and dosage form on the pharmacokinetics and relative bioavailability of sertindole in healthy volunteers.
The pharmacokinetic disposition and relative bioavailability of sertindole administered as a tablet dosage form under fasting conditions, in the presence of food, in the presence of antacid, and as solution was studied in a four-way crossover in young healthy male volunteers. Overall, tablet dosing after a meal or Maalox had no effect on t1/2 or AUC values when compared to fasting conditions, but increased the tmax and decreased the Cmax values slightly. The mean relative bioavailabilities of sertindole administered as tablets after fasting, with food, and with Maalox are 99, 104, and 98%, respectively, compared to sertindole solution. Therefore, sertindole can be administered with and without food and without regard to coadministration of antacids.
Wong
S L
SL
Department of Pharmacokinetics and Biopharmaceutics, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. shekman.wong@abott.com
Linnen
P
P
Mack
R
R
Granneman
G R
GR
D000284:Administration, Oral; D000328:Adult; D000536:Aluminum Hydroxide / Q000494:pharmacology*; D000704:Analysis of Variance; D000863:Antacids / Q000494:pharmacology*; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D004338:Drug Combinations; D005215:Fasting / Q000097:blood; D018565:Food-Drug Interactions; D006801:Humans; D007093:Imidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D007211:Indoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008276:Magnesium Hydroxide / Q000494:pharmacology*; D008297:Male; D012996:Solutions; D013607:Tablets
D000863:Antacids; D014150:Antipsychotic Agents; D004338:Drug Combinations; D007093:Imidazoles; D007211:Indoles; D012996:Solutions; D013607:Tablets; C013591:aluminum hydroxide, magnesium hydroxide, drug combination; D000536:Aluminum Hydroxide; C066304:sertindole; D008276:Magnesium Hydroxide