Background: Solid Dispersions (SDs) have been extensively used to increase the dissolution
of poorly water-soluble drugs. However, there are few studies exploring SDs properties that
must be considered during tablet development, like tabletability. Poorly water-soluble drugs with
poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge
in the production of SDs-based tablets.
Objective: This study evaluates the applicability of SDs to improve both tabletability and dissolution
rate of gemfibrozil. A SD-based tablet formulation was also proposed.
Methods: SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as a
carrier, according to a 23 factorial design. The formulation variables were gemfibrozil:HPMC ratio,
milling speed, and milling time. The response in the factorial analysis was the tensile strength of
the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed.
Results: SDs showed simultaneous drug dissolution enhancement and improved tabletability when
compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug
dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil-
HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release,
while those containing the same SD and sodium starch glycolate exhibited poor drug release
due to their prolonged disintegration time.
Conclusion: SDs proved to be effective for simultaneously improving tabletability and dissolution
profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as
disintegrating agent showed improved drug release and good mechanical strength, demonstrating
the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability
properties of this drug.