The effect of food on the relative bioavailability of deflazacort.
The effect of high- and low-fat meals on the relative bioavailability of deflazacort tablets was investigated in 12 healthy, adult males who were administered 36 mg deflazacort under fasted and fed conditions in a crossover fashion. Serial plasma samples were drawn up to 24 h post-dose and quantified for the active metabolite 21-desacetyl deflazacort (DFZ 21-OH) by a rapid and sensitive HPLC method. Following deflazacort administration with high-fat and low-fat meals and under fasted conditions, DFZ 21-OH area under the curve to infinity averaged 508.39 +/- 131.70, 510.05 +/- 148.30 and 511.90 +/- 188.16 ng.h/ml. DFZ 21-OH Cmax averaged 156.31 +/- 33.31, 156.85 +/- 40.17 and 188.05 +/- 53.35 ng/ml for high-fat, low-fat and fasted treatments, respectively. Differences in Cmax between the fed versus fasted treatments were statistically significant (P < 0.05). The decrease in Cmax under fed conditions was accompanied by an increase in mean Tmax of approximately 17-85% compared to fasted conditions. As expected, terminal half-life was not affected. These data indicate that co-administration of deflazacort tablets with high-fat and low-fat meals leads to a small decrease in rate but does not affect its extent of absorption.
Rao
N
N
Hoechst Marion Roussel, Kansas City, MO 64134, USA.
Eller
M
M
Arumugham
T
T
Weir
S
S
D000284:Administration, Oral; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000493:pharmacokinetics*; D001682:Biological Availability; D018592:Cross-Over Studies; D018752:Diet, Fat-Restricted; D005215:Fasting; D005502:Food; D006801:Humans; D008297:Male; D011282:Pregnenediones / Q000493:pharmacokinetics*; D013607:Tablets
D000893:Anti-Inflammatory Agents; D011282:Pregnenediones; D013607:Tablets; C021988:deflazacort