Spherical Cocrystallization - An Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs

Hongbo Chen, Yiwang Guo, Chenguang Wang, Jiangnan Dun, Changquan Calvin Sun

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)2503-2510
Number of pages8
JournalCrystal Growth and Design
Volume19
Issue number4
DOIs
StatePublished - Apr 3 2019

Fingerprint Dive into the research topics of 'Spherical Cocrystallization - An Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs'. Together they form a unique fingerprint.

Cite this