Abstract:
The current study aims to develop orodispersible lyophilisates (ODLs), containing olmesartan medoxomil (OLM),
by applying a quality by design approach to ensure product robustness. A thorough risk assessment study was done,
where the effects of each of the types of matrix former and superdisintegrant were assessed on the drug content,
friability %, cumulative drug released within 15 minutes (Q15%), disintegration time, and wetting time. This was
followed by a D-optimal design, for the optimization of the ODL. The optimization study focused on studying the
effects of the solubilizer concentration (X1
) and solubilizer type (X2
) on the disintegration time (Y1
) and Q15% (Y2
).
A design space was created with an optimized formula, OLM-ODL, which was prepared and tested to indicate the
validity of the design. The optimized formula showed fast drug release with a short disintegration time. Further
characterization tests were done on OLM-ODL, as morphological examination, which showed a highly porous nature.
Infrared spectroscopy showed no incompatibility. The extent of OLM absorption from the optimized ODL compared to
oral OLM suspension from a pharmacokinetic study. The ODL showed an enhancement of the relative bioavailability
of the optimized formula of about 345%. Thus, ODLs were successfully developed using a quality by design approach
with noticeably improved biopharmaceutical performance.
