Spherical CocrystallizationAn Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs
- Hongbo Chen (512850)
- Yiwang Guo (5598620)
- Chenguang Wang (27726)
- Jiangnan Dun (6452351)
- Changquan Calvin Sun (812250)
DOIAbstract
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 manufacturabili...
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