Comparative oral bioavailability of azimilide dihydrochloride in the fed and fasted states.
OBJECTIVE
This study investigated the relative oral bioavailability of azimilide dihydrochloride following administration in the fed (high-fat meal) and fasted states.


METHODS
This was a single-dose, randomized, two-way crossover study in 30 healthy, Caucasian, male subjects. Following oral administration, blood samples were collected over 27 days and analysed for azimilide using h.p.l.c. with u.v. detection. Pharmacokinetic parameters were determined using 'noncompartmental' analysis and compared using an ANOVA and 90% or 95% confidence intervals.


RESULTS
The extent of absorption was equivalent in the fed and fasted states (ratio = 96.2%; 90% CI=90.5% -102.4%). However, Cmax was decreased 19% following a high-fat meal (ratio=81.4%; 90% CI= 76.2% -87.0%). No difference in tmax or t(1/2),z was observed.


CONCLUSIONS
Azimilide dihydrochloride may be orally administered to patients without regard to the prandial state.
Corey
A E
AE
Procter & Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason, OH 45040-9462, USA.
Agnew
J R
JR
Valentine
S N
SN
Nesbitt
J D
JD
Wagner
D L
DL
Powell
J H
JH
Thompson
G A
GA
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000009:adverse effects / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D004041:Dietary Fats / Q000494:pharmacology; D004435:Eating; D005215:Fasting; D018565:Food-Drug Interactions; D006801:Humans; D006827:Hydantoins; D007093:Imidazoles / Q000009:adverse effects / Q000493:pharmacokinetics*; D048289:Imidazolidines; D008297:Male; D010879:Piperazines / Q000009:adverse effects / Q000493:pharmacokinetics*
D002121:Calcium Channel Blockers; D004041:Dietary Fats; D006827:Hydantoins; D007093:Imidazoles; D048289:Imidazolidines; D010879:Piperazines; C086123:azimilide