Drug absorption from nifedipine hydrophilic matrix extended-release (ER) tablet-comparison with an osmotic pump tablet and effect of food.
The aim of the present study was to compare the bioavailability of nifedipine when administered as a hydrophilic matrix tablet (ER) and a push-pull osmotic pump tablet (XL) administrated after fasting, and to evaluate the effect of food for the hydrophilic matrix tablet. For this purpose, three separate studies were performed on healthy volunteers (n = 58) including gammascintigraphic monitoring of tablet erosion and localisation in the gastrointestinal tract for ER in one study. Both ER and XL provided almost constant drug delivery over 24 h, after administration under fasting conditions, and bioequivalence was obtained according to 90% confidence intervals of the difference between formulations within 80-125% for Cmax and AUC. Food significantly increased AUC for ER but no significant difference was obtained between ER and XL with food with respect to extent of bioavailability. The rate of absorption was increased to a higher degree for ER than for XL, as indicated by a Cmax which was almost twice as high for ER compared with XL. This finding was shown to be related to an increased tablet-erosion rate for ER, leading to more rapid drug release.
Abrahamsson
B
B
Astra Hässle AB, Mölndal, Sweden.
Alpsten
M
M
Bake
B
B
Jonsson
U E
UE
Eriksson-Lepkowska
M
M
Larsson
A
A
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D006801:Humans; D008297:Male; D009543:Nifedipine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D009995:Osmosis; D012016:Reference Values; D013607:Tablets
D003692:Delayed-Action Preparations; D013607:Tablets; D009543:Nifedipine