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Spherical CocrystallizationAn Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs
journal contribution
posted on 2019-02-28, 00:00 authored by Hongbo Chen, Yiwang Guo, Chenguang Wang, Jiangnan Dun, Changquan Calvin SunSpherical cocrystallization (SCC),
an integrated crystal and particle
engineering approach, was successfully applied to generate spherical
cocrystal agglomerates (SCA) between a poorly soluble drug, griseofulvin
(GSF) and acesulfame (Acs). The SCC process consists of two steps:
(1) GSF-Acs cocrystal formation by reaction crystallization in a slurry;
(2) agglomeration by adding a bridging liquid. The obtained SCA exhibited
superior mechanical and powder properties over GSF. Inclusion of a
small amount (<1%) HPC in the agglomerates improved both the tabletability
and dissolution performance. Using the SCA, a high GSF loading (55.7%)
direct compression tablet formulation was successfully developed,
which exhibited much improved manufacturability and drug release property
over GSF based tablet formulation.