%0 Journal Article %A Chen, Hongbo %A Guo, Yiwang %A Wang, Chenguang %A Dun, Jiangnan %A Sun, Changquan Calvin %D 2019 %T Spherical Cocrystallizationî—¸An Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs %U https://acs.figshare.com/articles/journal_contribution/Spherical_Cocrystallization_An_Enabling_Technology_for_the_Development_of_High_Dose_Direct_Compression_Tablets_of_Poorly_Soluble_Drugs/7836827 %R 10.1021/acs.cgd.9b00219.s001 %2 https://acs.figshare.com/ndownloader/files/14579453 %K High Dose %K drug release property %K dissolution performance %K GSF %K Compression Tablets %K SCA %K cocrystal agglomerates %K particle engineering approach %K powder properties %K compression tablet formulation %K tablet formulation %K HPC %K Poorly Soluble Drugs %K SCC process %K reaction crystallization %X Spherical 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. %I ACS Publications