Spherical CocrystallizationAn Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs
journal contributionposted on 28.02.2019 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.