Spherical CocrystallizationAn Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs
journal contributionposted on 28.02.2019, 00:00 by Hongbo Chen, Yiwang Guo, Chenguang Wang, Jiangnan Dun, Changquan Calvin Sun
Any type of content formally published in an academic journal, usually following a peer-review process.
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.