Dissolution testing as a prognostic tool for oral drug absorption: dissolution behavior of glibenclamide.
OBJECTIVE
The dissolution behavior of two commercially available glibenclamide formulations was tested in various media. The aim of the study was to investigate whether the use of biorelevant dissolution media (BDM) would be advantageous over the use of standard media for predicting the in vivo performance of the two formulations.


METHODS
The dissolution tests were performed using USP 23 apparatus 2. Conventional buffers and USP media were compared with two BDM containing different amounts of lecithin and sodium taurocholate.


RESULTS
The dissolution of two drug powders was highly dependent on wetting, particle size, pH, and the composition of the medium used. In addition, the dissolution behavior of the two glibenclamide formulations showed differences in all media tested. The dissolution results of the two formulations were compared with those from an in vivo bioequivalence study undertaken by the central quality control laboratory of the German pharmacists (ZL). The bioequivalence criterion set by the ZL requires more than 80% drug release within 10 minutes. Results in FaSSIF, one of the BDMs, met the ZL criterion and this medium was also able to discriminate between the two formulations. This was not the case for the other media tested.


CONCLUSIONS
The study indicates that BDM are better able to discriminate between glibenclamide formulations than standard dissolution media.
Löbenberg
R
R
Institut für Pharmazeutische Technologie, Johann Wolfgang Goethe-Universität, Frankfurt, Germany.
Krämer
J
J
Shah
V P
VP
Amidon
G L
GL
Dressman
J B
JB
D000284:Administration, Oral; D001646:Bile / Q000378:metabolism; D005905:Glyburide / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012995:Solubility; D012997:Solvents
D007004:Hypoglycemic Agents; D012997:Solvents; D005905:Glyburide